Knowledge (XXG)

Phosphoinositide 3-kinase inhibitor

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510:. Kazia reported positive study results for the newly diagnosed, unmethylated population in the concurrent analysis which compares patients treated with paxalisib between January 2021 and March 2022 with those treated with temozolomide during the same time. The results showed a clinically meaningful increase in medium overall survival of 3.8 months, representing an increase of 33% vs. the temozolomide arm which is currently the standard of care. 17: 1632: 184:; codenamed INK1197, IPI-145; PIK3CD and PIK3CG inhibitor): FDA-approved on 24 September 2018 for treatment of relapsed or refractory chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) after at least two prior therapies, and treatment of relapsed or refractory follicular lymphoma after at least two prior systemic therapies. 220:(MZL) after at least one prior anti-CD20-based regimen, and treatment of relapsed or refractory follicular lymphoma after at least three prior lines of systemic therapy. As of May 31, 2022, umbralisib was withdrawn from the US market due to the decrement in overall survival and increased serious adverse events when using umbralisib. 594:(codenamed PF-05212384, PKI-587; PIK3CA, PIK3CG and mTOR inhibitor) has undergone several phase II trials as a potential treatment for different cancers, most of which have been terminated for different reasons. As of March 2022, two phase II trials on breast cancer are still recruiting patients. 71:
regulates cellular functions such as growth and survival. It is strictly regulated in healthy cells, but is always active in many cancer cells, allowing the cancer cells to better survive and multiply. PI3K inhibitors block the PI3K/AKT/mTOR pathway and thus slow down cancer growth. They are examples
610:(codenamed GSK2269557; PIK3CD inhibitor) has undergone several phase II trials as a potential treatment for different respiratory diseases (asthma and COPD) as well as for APDS/PASLI, all of which have been completed or terminated as of March 2022. Results are available for all of these trials. 3292:
Locatelli SL, Stirparo GG, Tartari S, Saba E, Rubino L, Brusamolino E, Castagna L, Santoro A, Carlo-Stella C (2013). "The PI3K/ERK Dual Inhibitor AEZS-136 Induces ROS-Dependent Necroptotic Cell Death and Exerts Potent Antitumor Effects in NOD/SCID Mice with Hodgkin Lymphoma Cell Line Xenografts".
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that lead to approval of idelalisib by FDA and EMA for treatment of patients with CLL. All other phase III trials testing idelalisib-based therapy as an experimental treatment, e.g. in first-line CLL and second-line NHL, had been terminated by end of 2016, mainly due to increased toxicity and
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Di Leo A, Johnston S, Lee KS, Ciruelos E, Lønning PE, Janni W, et al. (January 2018). "Buparlisib plus fulvestrant in postmenopausal women with hormone-receptor-positive, HER2-negative, advanced breast cancer progressing on or after mTOR inhibition (BELLE-3): a randomised, double-blind,
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with placebo + rituximab in patients with relapsed iNHL. Study completion is expected for January 2023. Preliminary results show a strong and significant improvement of progression-free survival under copanlisib treatment, but also considerably more severe and serious side
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Matasar MJ, Capra M, Özcan M, Lv F, Li W, Yañez E, et al. (May 2021). "Copanlisib plus rituximab versus placebo plus rituximab in patients with relapsed indolent non-Hodgkin lymphoma (CHRONOS-3): a double-blind, randomised, placebo-controlled, phase 3 trial".
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for "A Study Evaluating the Efficacy and Safety of Inavolisib + Palbociclib + Fulvestrant vs Placebo + Palbociclib + Fulvestrant in Patients With PIK3CA-Mutant, Hormone Receptor-Positive, Her2-Negative, Locally Advanced or Metastatic Breast Cancer" at
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was planned as a placebo-controlled randomized phase III trial with about 190 patients. However, recruitment was stopped after 25 patients were included and the trial continues as a non-randomized single-arm trial. Results are expected for November
558:(codenamed GDC-0980, GNE 390, RG7422; pan-class I PI3K and mTOR inhibitor) has undergone four phase II trials as a potential treatment for different solid tumours, three of which have been completed or terminated as of March 2022. 2516:
for "A Study of Taselisib + Fulvestrant Versus Placebo + Fulvestrant in Participants With Advanced or Metastatic Breast Cancer Who Have Disease Recurrence or Progression During or After Aromatase Inhibitor Therapy (SANDPIPER)" at
385:(RTB-101-205) was terminated by the sponsor. Dactolisib has also undergone several phase II trials as a potential treatment for solid tumours as well as for respiratory diseases, most of which have been terminated as of 2022. 1833:
for "Phase III Study of BKM120/Placebo With Fulvestrant in Postmenopausal Patients With Hormone Receptor Positive HER2-negative Locally Advanced or Metastatic Breast Cancer Refractory to Aromatase Inhibitor (BELLE-2)" at
1781:"Buparlisib plus fulvestrant versus placebo plus fulvestrant in postmenopausal, hormone receptor-positive, HER2-negative, advanced breast cancer (BELLE-2): a randomised, double-blind, placebo-controlled, phase 3 trial" 736:(codenamed GSK2126458, GSK458) has completed two phase I trials in 2015 and 2016, respectively. No data have been published for these trials and no further trials have been conducted since then as of March 2022. 511: 2245:
for "A Study of Duvelisib in Combination With Rituximab and Bendamustine vs Placebo in Combination With Rituximab and Bendamustine in Subjects With Previously-Treated Indolent Non-Hodgkin Lymphoma (BRAVURA)" at
3491: 622:(codenamed SAR245408 and XL147; inhibitor of PIK3CA, PIK3CD, and PIK3CG) has undergone several phase II trials as a potential treatment for different solid tumours, all of which have been completed as of 2022. 543:). The trial is currently recruiting patients as of March 2022 and will compare inavolisib + palbociclib + fulvestrant with placebo + palbociclib + fulvestrant. Results are expected for September 2025. 672:(codenamed RP6530; dual PIK3CD and PIK3CG inhibitor) is undergoing several phase II trials as a potential treatment for different cancers. Two single-arm trials (in CLL and iNHL) have reported results. 2358:
for "Study of LOXO-305 Versus Investigator's Choice (IdelaR or BR) in Patients With Previously Treated Chronic Lymphocytic Leukemia (CLL)/Small Lymphocytic Lymphoma (SLL) (BRUIN CLL-321)" at
760:(CH5132799, PA799; mainly a PIK3CA inhibitor) will be tested in a phase I/II trial with PIK3CA-mutated colorectal cancer patients that is currently recruiting patients as of March 2022. 648:(codenamed MLN1117 and TAK-117; PIK3CA inhibitor) is undergoing several phase II trials as a potential treatment for different cancers. As of March 2022, results have been reported for 742:(PIK3CA and PIK3CD inhibitor) has completed one phase I trial in 2016. No data have been published for this trial and no further trials have been conducted since then as of March 2022. 730:(codenamed CAL-120, GS-9820) has completed one phase I trial in 2016. No data have been published for this trial and no further trials have been conducted since then as of March 2022. 700:(PIK3CB inhibitor) has undergone several phase II trials as a potential treatment for different cancers, one of which have been completed, with no results published as of March 2022. 568:
dual PI3K/mTOR inhibitor) has undergone several phase II trials as a potential treatment for different solid tumours, all of which have been completed or terminated as of March 2022.
533:. The trial is currently recruiting patients as of March 2022 and will compare zandelisib + rituximab to chemotherapy (CHOP regimen) + rituximab. Results are expected for April 2026. 616:(codenamed GDC-0941; pan-class I PI3K inhibitor) has undergone five phase II trials as a potential treatment for different solid tumours, with no results published as of March 2022. 574:(codenamed IPI-549; PIK3CD inhibitor) is currently undergoing three phase II trials as a potential treatment for different solid tumours, with no published results as of March 2022. 1947:
for "A Study of the Experimental Drug BKM120 With Paclitaxel in Patients With HER2 Negative, Locally Advanced or Metastatic Breast Cancer, With or Without PI3K Activation (BELLE-4)" at
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inhibitor) has undergone several phase II trials as a potential treatment for different cancers, three of which have been completed or terminated and have results as of March 2022.
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Edgar KA, Wallin JJ, Berry M, Lee LB, Prior WW, Sampath D, et al. (February 2010). "Isoform-specific phosphoinositide 3-kinase inhibitors exert distinct effects in solid tumors".
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for "A Phase III Study of BKM120 With Fulvestrant in Patients With HR+,HER2-, AI Treated, Locally Advanced or Metastatic Breast Cancer Who Progressed on or After mTORi (BELLE-3)" at
114:(PIK3CD). All PI3K inhibitors that are currently approved inhibit one or more p110 isoforms of the class I PI3Ks. Inhibiting different p110 isoforms can have different effects, e.g. 2497: 1609: 996:
Sabbah DA, Hajjo R, Bardaweel SK, Zhong HA (October 2021). "Phosphatidylinositol 3-kinase (PI3K) inhibitors: a recent update on inhibitor design and clinical trials (2016-2020)".
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Heffron TP, Berry M, Castanedo G, Chang C, Chuckowree I, Dotson J, et al. (April 2010). "Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor".
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for "To Evaluate Efficacy and Safety of Parsaclisib Plus Either Rituximab or Obinutuzumab in R/R Follicular Lymphoma (FL) and Marginal Zone Lymphoma (MZL) (CITADEL-302)" at
1559:"FDA Approval for duvelisib (COPIKTRA, Verastem, Inc.) for adult patients with relapsed or refractory chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL)" 1903:"A randomized adaptive phase II/III study of buparlisib, a pan-class I PI3K inhibitor, combined with paclitaxel for the treatment of HER2- advanced breast cancer (BELLE-4)" 326:(codenamed BAY 80-6946; predominantly a PIK3CA and PIK3CD inhibitor) ist currently undergoing three phase III trials, all of which are testing it in patients with indolent 76:. While PI3K inhibitors are an effective treatment, they can have very severe side effects and are therefore only used if other treatments have failed or are not suitable. 428:
comparing duvelisib + rituximab with rituximab alone in patients with follicular lymphoma was terminated by the sponsor when it was no longer expected to lead to approval.
198:; codenamed BYL719; PIK3CA inhibitor): FDA-approved in May 2019 for treatment of HR-positive and HER2/neu-negative breast cancer in combination with the endocrine therapy 3518: 2985: 694:(PIK3CB and PIK3CD inhibitor) will be tested as a potential treatment for gastric cancer in a phase II trial that is currently recruiting patients as of March 2022. 2875:
for "A Study of Sapanisertib, Combination of Sapanisertib With MLN1117, Paclitaxel and Combination of Sapanisertib With Paclitaxel in Women With Endometrial Cancer" at
244:). The trial was completed in August 2021 and results have become available in March 2022. Another phase II/III trial for APDS/PASLI that serves as an extension study ( 2412:
for "A Study of Parsaclisib, a PI3Kδ Inhibitor, in Combination With Bendamustine and Rituximab in Patients With Newly Diagnosed Mantle Cell Lymphoma (CITADEL-310)" at
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Garlich JR, Becker MD, Shelton CF, Qi W, Liu X, Cooke L, Mahadevan D (2010). "Phase I Study of Novel Prodrug Dual PI3K/MTOR Inhibitor SF1126 in B-Cell Malignancies".
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for "Efficacy and Safety Study of Tenalisib (RP6530), a Novel PI3K δ/γ Dual Inhibitor in Patients With Relapsed/Refractory Indolent Non-Hodgkin's Lymphoma (iNHL)" at
2727:"First-in-human phase I study of pictilisib (GDC-0941), a potent pan-class I phosphatidylinositol-3-kinase (PI3K) inhibitor, in patients with advanced solid tumors" 2430:
for "To Evaluate Efficacy and Safety of Parsaclisib and Ruxolitinib in Participants With Myelofibrosis Who Have Suboptimal Response to Ruxolitinib (LIMBER-304)" at
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derivative) has undergone several phase II trials as a potential treatment for different solid tumours, all of which have been completed or terminated as of 2022.
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regimen) with placebo + immunochemotherapy in patients with relapsed iNHL who have received 1–3 previous lines of therapy. Results are expected for February 2023.
152:-approved in July 2014 for treatment of three types of blood cancers: treatment of relapsed or refractory chronic lymphocytic leukemia (CLL) in combination with 754:(dual pan-class I PI3K and mTOR inhibitor): The phase I trial of this drug was terminated due to lack of sufficient exposure following single- and repeat-dosing. 519:(codenamed GDC-0032, RG7604; PIK3CA inhibitor): Development was discontinued due to strong side effects and only a minor survival benefit in the phase III trial 5243: 79:
After PI3K inhibitors had been under investigation as anti-cancer drugs for several years, the first one to be approved for treatment in clinical practice was
4218: 1310: 249: 2060:"NVP-BEZ235, a novel dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor, elicits multifaceted antitumor activities in human gliomas" 1039:
Zhong, Lei; Li, Yueshan; Xiong, Liang; Wang, Wenjing; Wu, Ming; Yuan, Ting; Yang, Wei; Tian, Chenyu; Miao, Zhuang; Wang, Tianqi; Yang, Shengyong (2021).
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for "MLN0128 and MLN0128 + MLN1117 Compared With Everolimus in the Treatment of Adults With Advanced or Metastatic Clear-Cell Renal Cell Carcinoma" at
3406:"Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941" 488: 502:(codenamed GDC-0084; pan-class I PI3K and mTOR inhibitor) was tested as a potential treatment for newly diagnosed, unmethylated as well as recurrent 1384:
Ito K, Caramori G, Adcock IM (April 2007). "Therapeutic potential of phosphatidylinositol 3-kinase inhibitors in inflammatory respiratory disease".
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comparing buparlisib + fulvestrant with fulvestrant alone in patients with breast cancer both showed excessive side effects. The phase II/III trial
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mortality. Two trials comparing new experimental treatments to idelalisib as a comparator and a dose optimization study in FL are still ongoing.
792: 450:(codenamed INCB050465, INCB 50465; PIK3CD inhibitor) will be tested as a potential treatment for different diseases in five phase III trials: 5194: 3511: 2890:"The phosphatidylinositol 3-kinase inhibitor, PX-866, is a potent inhibitor of cancer cell motility and growth in three-dimensional cultures" 688:(PIK3CD inhibitor) has undergone a phase II trial as a potential treatment for HNSCC. The trial was terminated in 2018 due to safety reasons. 2264:
for "Study of Duvelisib in Combination With Rituximab vs Rituximab in Subjects With Previously Treated Follicular Lymphoma (DYNAMO + R)" at
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for "Study of Copanlisib in Combination With Standard Immunochemotherapy in Relapsed Indolent Non-Hodgkin's Lymphoma (iNHL) (CHRONOS-4)" at
1181: 588:(DLBCL) was completed in 2019 but its results have not yet been published. Other phase II trials with fimepinostat have been terminated. 539:(codenamed GDC-0077; PIK3CA inhibitor) will be tested as a potential treatment for PIK3CA-mutant breast cancer in a phase II/III trial ( 2297: 5238: 3953: 3909: 3787: 1572: 3712: 3183:
for "Study to Investigate Effects of CAL-263 in Subjects With Allergic Rhinitis Exposed to Allergen in an Environmental Chamber" at
714:, one of the most widely studied dual PI3K/mTOR inhibitors. A phase II trial with SF1126 has been terminated due to slow enrolment. 678:(codenamed SAR245409, XL765; pan-class I PI3K inhibitor and weaker inhibitor of mTOR), in trial for B-cell lymphomas, e.g. CLL and 2632:
for "Study to Evaluate the Efficacy and Safety of CUDC-907 in Patients With RR DLBCL, Including Patients With MYC Alterations" at
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for "A Study of Acalabrutinib vs Investigator's Choice of Idelalisib Plus Rituximab or Bendamustine Plus Rituximab in R/R CLL" at
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Maira SM, Stauffer F, Schnell C, García-Echeverría C (February 2009). "PI3K inhibitors for cancer treatment: where do we stand?".
3504: 2498:"Roche dumps its PhIII PI3K effort on taselisib after researchers track poor survival edge, harsh side effects for breast cancer" 2466:
for "Study of the Efficacy and Safety of Parsaclisib in Participants With Primary Warm Autoimmune Hemolytic Anemia (PATHWAY)" at
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Curigliano G, Shah RR (February 2019). "Safety and Tolerability of Phosphatidylinositol-3-Kinase (PI3K) Inhibitors in Oncology".
122: 2227:
for "A Phase 3 Extension Study of Duvelisib and Ofatumumab in Patients With CLL/SLL Previously Enrolled in Study IPI-145-07" at
170:; codenamed BAY 80-6946; predominantly a PIK3CA and PIK3CD inhibitor): FDA-approved in September 2017 for treatment of relapsed 4434: 4228: 381:
in generally healthy elderly people. However, the trial did not meet this endpoint. Consequently, the related phase III trial
59:) are a class of medical drugs that are mainly used to treat advanced cancers. They function by inhibiting one or more of the 4847: 3849: 3739: 402:
led to its approval for CLL/SLL An extension trial to DUO was completed in 2020, but its results have not yet been published.
2448:
for "To Evaluate the Efficacy and Safety of Parsaclisib and Ruxolitinib in Participants With Myelofibrosis (LIMBER-313)" at
3165:
for "Phase I, Dose Study to Look at the Safety and Pharmacokinetics of AZD8835 in Patients With Advanced Solid Tumours" at
2954:
for "Efficacy and Safety of Tenalisib (RP6530) in Patients With Relapsed/Refractory Chronic Lymphocytic Leukemia (CLL)" at
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Williams R, Berndt A, Miller S, Hon WC, Zhang X (August 2009). "Form and flexibility in phosphoinositide 3-kinases".
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for "A Phase 3 Study to Determine if RTB101 Prevents Clinically Symptomatic Respiratory Illness in the Elderly" at
565: 5248: 5069: 4949: 4939: 311: 156:, treatment of relapsed small lymphocytic lymphoma after at least two prior systemic therapies, and treatment of 91: 60: 3109:
for "SF1126 in Recurrent or Progressive SCCHN and Mutations in PIK3CA Gene and/or PI-3 Kinase Pathway Genes" at
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in several phase II trials that are currently recruiting or scheduled to recruit patients as of March 2022.
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Heavey S, O'Byrne KJ, Gately K (April 2014). "Strategies for co-targeting the PI3K/AKT/mTOR pathway in NSCLC".
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for "Phase 3 Study of Zandelisib (ME-401) in Combination With Rituximab in Patients With iNHL - (COASTAL)" at
2209:
for "A Phase 3 Study of Duvelisib Versus Ofatumumab in Patients With Relapsed or Refractory CLL/SLL (DUO)" at
1592: 529:(codenamed ME-401; PIK3CD inhibitor) will be tested as a potential treatment for iNHL in the phase III trial 5199: 5106: 4924: 4639: 4125: 3973: 3900: 548: 292: 3201:
for "Phase I Open-Label, Dose-Escalation Study of GSK1059615 in Patients With Solid Tumors or Lymphoma" at
1558: 1544: 5004: 4994: 4727: 4569: 457: 217: 2484:
for "A Trial to Evaluate Multiple Regimens in Newly Diagnosed and Recurrent Glioblastoma (GBM AGILE)" at
4276: 4093: 4063: 3923: 2308: 1983:
for "Copanlisib and Rituximab in Relapsed Indolent B-cell Non-Hodgkin's Lymphoma (iNHL) (CHRONOS-3)" at
867: 64: 21: 16: 310:
comparing buparlisib + paclitaxel with paclitaxel alone in patients with breast cancer did not improve
600:(codenamed YY-20394; PIK3CD inhibitor) will be tested as a potential treatment for different types of 4674: 4551: 4072: 3988: 3057: 2705: 2184: 1185: 649: 638:(codenamed UCB-5857; PIK3CD inhibitor) has undergone one phase II trial as a potential treatment for 466: 418: 327: 289: 95: 3252: 2814: 2794: 4959: 4859: 4838: 4559: 4381: 4213: 3944: 3840: 3232: 3140: 2774: 2685: 2645: 2567: 679: 639: 453: 378: 171: 157: 3272: 2665: 2607: 2277: 1610:"FDA grants accelerated approval to umbralisib for marginal zone lymphoma and follicular lymphoma" 577: 41: 4017: 3220: 3202: 3184: 3166: 3128: 3110: 3045: 3027: 3009: 2973: 2955: 2929: 2876: 2858: 2840: 2633: 2587: 2555: 2536: 2518: 2485: 2467: 2449: 2431: 2413: 2395: 2377: 2359: 2341: 2265: 2247: 2228: 2210: 2172: 2171:
for "Effect of RTB101 on Illness Associated With Respiratory Tract Infections in the Elderly" at
2148: 2113: 2046: 2022: 1984: 1966: 1948: 1889: 1835: 1767: 1749: 1682: 1482:
Crabbe T (April 2007). "Exploring the potential of PI3K inhibitors for inflammation and cancer".
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Wu P, Liu T, Hu Y (2009). "PI3K inhibitors for cancer therapy: what has been achieved so far?".
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for "The BURAN Study of Buparlisib in Patients With Recurrent or Metastatic HNSCC (BURAN)" at
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Martín M, Chan A, Dirix L, O'Shaughnessy J, Hegg R, Manikhas A, et al. (February 2017).
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for "A Study of Investigational SAR245409 in Patients With Certain Lymphoma or Leukemia" at
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Rao VK, Webster S, Dalm VA, Šedivá A, van Hagen PM, Holland S, et al. (November 2017).
1521: 1491: 1451: 1393: 1345: 1337: 1281: 1246: 1208: 1152: 1144: 1097: 1060: 1052: 1005: 965: 957: 916: 906: 840: 745: 703: 73: 1696:"Effective "activated PI3Kδ syndrome"-targeted therapy with the PI3Kδ inhibitor leniolisib" 1041:"Small molecules in targeted cancer therapy: Advances, challenges, and future perspectives" 369:(codenamed BEZ235, NVP-BEZ235; dual pan-class I PI3K and mTOR inhibitor) was tested in the 4585: 4547: 4338: 3760: 3675: 2321: 798: 83:
in 2014. Several others followed, and even more are still under development (see below).
2127:"RTB101 and immune function in the elderly: Interpreting an unsuccessful clinical trial" 1779:
Baselga J, Im SA, Iwata H, Cortés J, De Laurentiis M, Jiang Z, et al. (July 2017).
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has undergone eleven phase III clinical trials as of March 2022. These include the
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Sarker D, Ang JE, Baird R, Kristeleit R, Shah K, Moreno V, et al. (January 2015).
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Overview of phosphoinositide 3-kinase (PI3K) inhibitors and their interaction with the
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Raynaud FI, Eccles SA, Patel S, Alix S, Box G, Chuckowree I, et al. (July 2009).
2010: 1861: 1796: 5232: 5079: 5039: 4409: 4282: 4163: 4106: 3864: 3813: 3322:"B591, a novel specific pan-PI3K inhibitor, preferentially targets cancer stem cells" 2152: 2026: 1636: 1367: 1025: 946:"The PI3K-AKT network at the interface of oncogenic signalling and cancer metabolism" 475: 437: 237: 3306: 3127:
for "A Phase 1b Study Evaluating GS-9820 in Subjects With Lymphoid Malignancies" at
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Howes AL, Chiang GG, Lang ES, Ho CB, Powis G, Vuori K, Abraham RT (September 2007).
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and was stopped for futility at the end of phase II. These results led the sponsor,
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Liu TJ, Koul D, LaFortune T, Tiao N, Shen RJ, Maira SM, et al. (August 2009).
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for "Extension to the Study of Efficacy of CDZ173 in Patients With APDS/PASLI" at
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Study results provide rationale for use of PI3K inhibitors in therapeutic settings
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inhibitor): FDA-approved in February 2021 for treatment of relapsed or refractory
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for "UCB Proof of Concept Study in Patients With Primary Sjögren's Syndrome" at
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was withdrawn by the sponsor when it was no longer expected to lead to approval.
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for "MEN1611 With Cetuximab in Metastatic Colorectal Cancer (C-PRECISE-01)" at
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Blagosklonny MV. Anti-aging: senolytics or gerostatics (unconventional view).
1101: 961: 850: 675: 663: 613: 571: 536: 526: 433: 399: 366: 323: 285: 274: 223: 205: 163: 138: 99: 80: 45: 37: 29: 25: 5176: 5156: 5111: 5101: 5095: 4999: 4944: 4893: 4817: 4807: 4762: 4749: 4690: 4652: 4580: 4518: 4459: 4448: 4404: 4361: 4320: 4314: 4310: 4272: 4199: 4194: 4184: 4156: 4116: 4077: 4052: 4042: 4002: 3648: 3638: 3633: 3628: 3590: 1919: 1902: 1397: 659: 516: 410: 388: 346: 187: 177: 153: 3477: 3439: 3390: 3355: 2915: 2760: 2093: 2018: 1928: 1869: 1814: 1729: 1532: 1503: 1463: 1405: 1359: 1324:
Vanhaesebroeck B, Perry MW, Brown JR, André F, Okkenhaug K (October 2021).
1293: 1258: 1220: 1166: 1109: 1074: 1017: 979: 930: 3058:"Search for phase 2 clinical trials with GSK2636771 on clinicaltrials.gov" 2706:"Search for phase 2 clinical trials with GSK2269557 on clinicaltrials.gov" 2185:"Search for phase 2 clinical trials with Dactolisib on clinicaltrials.gov" 248:) is still ongoing and results are expected for October 2026. The FDA has 5085: 5049: 4989: 4757: 4695: 4475: 4371: 4343: 4022: 3859: 3253:"Search for phase 1 clinical trials with TG100-115 on clinicaltrials.gov" 2815:"Search for phase 2 clinical trials with LY3023414 on clinicaltrials.gov" 2795:"Search for phase 2 clinical trials with SAR245408 on clinicaltrials.gov" 1545:"FDA approves new treatment for adults with relapsed follicular lymphoma" 911: 873: 844: 830: 711: 629: 601: 315: 111: 3233:"Search for phase 1 clinical trials with PWT33597 on clinicaltrials.gov" 2686:"Search for phase 2 clinical trials with YY-20394 on clinicaltrials.gov" 2646:"Search for phase 2 clinical trials with CUDC-907 on clinicaltrials.gov" 2568:"Search for phase 2 clinical trials with GDC-0980 on clinicaltrials.gov" 1133:"Managing toxicities of phosphatidylinositol-3-kinase (PI3K) inhibitors" 3978: 3879: 3693: 3554: 3469: 3273:"Search for phase 1 clinical trials with ZSTK474 on clinicaltrials.gov" 2775:"Search for phase 2 clinical trials with IPI-549 on clinicaltrials.gov" 2666:"Search for phase 2 clinical trials with PKI-587 on clinicaltrials.gov" 2608:"Search for phase 2 clinical trials with IPI-549 on clinicaltrials.gov" 2278:"Search for phase 3 clinical trials with CAL-101 on clinicaltrials.gov" 1965:
for "Phase III Copanlisib in Rituximab-refractory iNHL (CHRONOS-2)" at
1649: 1495: 1250: 685: 87: 2930:"Search for phase 2 clinical trials with PX-866 on clinicaltrials.gov" 2588:"Search for phase 2 clinical trials with PQR309 on clinicaltrials.gov" 2376:
for "Dose Optimization Study of Idelalisib in Follicular Lymphoma" at
895:"PI3K Inhibitors in Cancer: Clinical Implications and Adverse Effects" 3618: 358: 213: 107: 103: 98:
have a catalytic subunit known as p110, with four types (isoforms) –
628:(codenamed GTPL8918, LY3023414; triple pan-class I PI3K, mTOR, and 3141:"Search for clinical trials with GSK2126458 on clinicaltrials.gov" 893:
Mishra R, Patel H, Alanazi S, Kilroy MK, Garrett JT (March 2021).
126: 15: 3320:
Zhou H, Yu C, Kong L, Xu X, Yan J, Li Y, et al. (May 2019).
1681:
for "Study of Efficacy of CDZ173 in Patients With APDS/PASLI" at
1635:
This article incorporates text from this source, which is in the
33: 3500: 121:
PI3K inhibitors are also under investigation as treatments for
318:, to cancel their breast cancer study program with buparlisib. 125:, and are used to investigate the role of the PI3K pathway in 1137:
Hematology. American Society of Hematology. Education Program
118:-negative tumors may be more sensitive to PIK3CB inhibitors. 642:. The trial has been terminated due to enrolment challenges. 277:(codenamed BKM120, NVP-BKM120; pan-class I PI3K inhibitor): 3044:
for "AZD8186 and Paclitaxel in Advanced Gastric Cancer" at
391:(codenamed INK1197, IPI-145; PIK3CD and PIK3CG inhibitor): 1386:
The Journal of Pharmacology and Experimental Therapeutics
212:; codenamed TGR-1202, Rp-5264; PIK3CD and casein kinase 1311:"FDA approves Zydelig for three types of blood cancers" 48:
inhibit the PI3K/AKT/mTOR pathway, but not PI3K itself.
1561:. US Food and Drug Administration. September 24, 2018. 1547:. US Food and Drug Administration. September 14, 2017. 228: 1573:"FDA approves first PI3K inhibitor for breast cancer" 394:
The results of the completed pivotal phase III trial
3026:
for "AMG 319 in HPV Positive and Negative HNSCC" at
4886: 4837: 4617: 4610: 4546: 4500: 4433: 4390: 4227: 4212: 4092: 4062: 3987: 3972: 3943: 3839: 3759: 3702: 3685: 3674: 3610: 3563: 3544: 2986:"In Focus: Voxtalisib for CLL and B-Cell Lymphomas" 870:
for inhibitors of AKT and mTOR downstream from PI3K
1313:. US Food and Drug Administration. July 23, 2014. 160:(FL) after at least two prior systemic therapies. 148:; codenamed CAL-101, GS-1101; PIK3CD inhibitor): 377:(RTB-101-204) to prevent clinically symptomatic 295:(HNSCC). Results are expected for December 2022. 226:(codenamed CDZ173; PIK3CD inhibitor, trade name 24:. There are pan-class I PI3K inhibitors such as 857:PI3K inhibitor), mainly used as a research tool 837:PI3K inhibitor), mainly used as a research tool 417:with rituximab + bendamustine in patients with 2298:"Zydelig : EPAR - Scientific conclusions" 1671: 1669: 3512: 3492:Novartis on BEZ235 and BKM120 PI3K inhibitors 8: 3371:Bioorganic & Medicinal Chemistry Letters 1437: 1435: 1429:. News-medical.net. Retrieved on 2010-11-05. 1305: 1303: 991: 989: 240:in a placebo-controlled phase II/III trial ( 174:after at least two prior systemic therapies. 1593:"Ukoniq (umbralisib) tablets, for oral use" 1326:"PI3K inhibitors are finally coming of age" 1232: 1230: 899:International Journal of Molecular Sciences 28:, isoform-specific PI3K inhibitors such as 4614: 4224: 3984: 3699: 3682: 3560: 3519: 3505: 3497: 357:compares copanlisib + immunochemotherapy ( 232:) was tested as a potential treatment for 3429: 3345: 2905: 2750: 2142: 2083: 1918: 1804: 1719: 1650:"Federal Register :: Request Access" 1477: 1475: 1473: 1349: 1156: 1064: 969: 920: 910: 489:Warm antibody autoimmune hemolytic anemia 1045:Signal Transduction and Targeted Therapy 885: 807:(dual PIK3CA and mTOR inhibitor with IC 2317: 2306: 1379: 1377: 1131:Hanlon A, Brander DM (December 2020). 944:Hoxhaj G, Manning BD (February 2020). 772:(mainly a PIK3CD and PIK3CG inhibitor) 63:(PI3K) enzymes, which are part of the 998:Expert Opinion on Therapeutic Patents 876:, P110δ (PI3K-delta) as a drug target 584:): A phase II trial in patients with 398:comparing duvelisib monotherapy with 288:to paclitaxel alone in patients with 7: 5244:Phosphoinositide 3-kinase inhibitors 1848:placebo-controlled, phase 3 trial". 843:(triple pan-class I PI3K, mTOR, and 53:Phosphoinositide 3-kinase inhibitors 3788:ribonucleotide reductase inhibitors 811:values of 4 nM and 21 nM) 580:(codenamed CUDC-907; PI3K p110 and 3954:Ribonucleotide reductase inhibitor 3910:Ribonucleotide reductase inhibitor 14: 3713:Dihydrofolate reductase inhibitor 3458:Biochemical Society Transactions 1630: 1520:. 2021 Aug 31;12(18):1821-1835. 1484:Biochemical Society Transactions 1239:Biochemical Society Transactions 766:(dual PIK3CA and mTOR inhibitor) 706:is a peptidic prodrug targeting 123:inflammatory respiratory disease 86:There are different classes and 3307:10.1182/blood.V122.21.3067.3067 3091:10.1182/blood.V116.21.1783.1783 2131:Translational Medicine of Aging 723:In early stage clinical trials 523:in patients with breast cancer. 491:(WAIHA) in the phase III trial 424:Similarly, the phase III trial 3850:Thymidylate synthase inhibitor 3740:Thymidylate synthase inhibitor 1330:Nature Reviews. Drug Discovery 1: 3770:Adenosine deaminase inhibitor 3611:Block microtubule disassembly 3422:10.1158/1535-7163.MCT-08-1200 3410:Molecular Cancer Therapeutics 2907:10.1158/1535-7163.MCT-06-0698 2894:Molecular Cancer Therapeutics 2743:10.1158/1078-0432.CCR-14-0947 2076:10.1158/1535-7163.MCT-09-0160 2064:Molecular Cancer Therapeutics 2011:10.1016/S1470-2045(21)00145-5 1862:10.1016/S1470-2045(17)30688-5 1797:10.1016/S1470-2045(17)30376-5 1456:10.1158/0008-5472.CAN-09-2525 1149:10.1182/hematology.2020000119 1010:10.1080/13543776.2021.1924150 586:diffuse large B-cell lymphoma 469:(MCL) in the phase III trial 460:(MZL) in the phase III trial 252:leniolisib on March 24, 2023. 234:activated PI3K delta syndrome 1712:10.1182/blood-2017-08-801191 1616:Food and Drug Administration 1578:Food and Drug Administration 1182:"Zeroing in on PI3K Pathway" 801:(pan-class I PI3K inhibitor) 1654:unblock.federalregister.gov 1201:Current Medicinal Chemistry 827:(mainly a PIK3CD inhibitor) 778:(mainly a PIK3CD inhibitor) 5265: 3383:10.1016/j.bmcl.2010.03.046 1342:10.1038/s41573-021-00209-1 1286:10.1016/j.ctrv.2013.08.006 1213:10.2174/092986709787581905 1057:10.1038/s41392-021-00572-w 506:in the phase II/III trial 257:Under clinical development 5239:Experimental cancer drugs 5189: 5070:Omacetaxine mepesuccinate 4950:Ciltacabtagene autoleucel 4940:Brexucabtagene autoleucel 3338:10.1038/s41388-018-0674-5 2144:10.1016/j.tma.2020.01.002 1526:10.18632/oncotarget.28049 1102:10.1007/s40264-018-0778-4 962:10.1038/s41568-019-0216-7 312:progression-free survival 268:phase III clinical trials 61:phosphoinositide 3-kinase 5122:Talimogene laherparepvec 5055:Nadofaragene firadenovec 5025:Lisocabtagene maraleucel 3974:Topoisomerase inhibitors 3893:DNA polymerase inhibitor 2731:Clinical Cancer Research 1274:Cancer Treatment Reviews 549:phase II clinical trials 478:in the phase III trials 4925:Axicabtagene ciloleucel 3529:chemotherapeutic agents 1398:10.1124/jpet.106.111674 293:squamous cell carcinoma 5107:Sitimagene ceradenovec 5005:Idecabtagene vicleucel 4570:Methyl aminolevulinate 3213:Clinical trial number 3195:Clinical trial number 3177:Clinical trial number 3159:Clinical trial number 3121:Clinical trial number 3103:Clinical trial number 3038:Clinical trial number 3020:Clinical trial number 3002:Clinical trial number 2990:Cancer Therapy Advisor 2966:Clinical trial number 2948:Clinical trial number 2869:Clinical trial number 2851:Clinical trial number 2833:Clinical trial number 2626:Clinical trial number 2547:Clinical trial number 2529:Clinical trial number 2510:Clinical trial number 2478:Clinical trial number 2460:Clinical trial number 2442:Clinical trial number 2424:Clinical trial number 2406:Clinical trial number 2388:Clinical trial number 2370:Clinical trial number 2352:Clinical trial number 2334:Clinical trial number 2316:Cite journal requires 2258:Clinical trial number 2239:Clinical trial number 2221:Clinical trial number 2203:Clinical trial number 2165:Clinical trial number 2106:Clinical trial number 2039:Clinical trial number 1977:Clinical trial number 1959:Clinical trial number 1941:Clinical trial number 1882:Clinical trial number 1827:Clinical trial number 1760:Clinical trial number 1742:Clinical trial number 1675:Clinical trial number 950:Nature Reviews. Cancer 783:Not in clinical trials 458:marginal zone lymphoma 409:comparing duvelisib + 345:compares copanlisib + 284:compares buparlisib + 218:marginal zone lymphoma 133:Approved for treatment 49: 4581:Porphyrin derivatives 4277:Melphalan flufenamide 3924:Hypomethylating agent 3533:antineoplastic agents 2125:Kaeberlein M (2020). 1920:10.1093/annonc/mdw562 1180:Flanagan (Dec 2008). 868:PI3K/AKT/mTOR pathway 662:(codenamed PX-866; a 298:The phase III trials 65:PI3K/AKT/mTOR pathway 22:PI3K/AKT/mTOR pathway 19: 4910:Asparagine depleters 4839:Receptor antagonists 4753:+abiraterone acetate 1999:The Lancet. Oncology 1850:The Lancet. Oncology 1785:The Lancet. Oncology 912:10.3390/ijms22073464 650:renal cell carcinoma 467:Mantle cell lymphoma 419:non-Hodgkin lymphoma 405:The phase III trial 353:The phase III trial 341:The phase III trial 328:non-Hodgkin lymphoma 280:The phase III trial 4960:Denileukin diftitox 4860:Retinoid X receptor 4560:Aminolevulinic acid 4382:Triethylenemelamine 4214:Crosslinking of DNA 3945:Deoxyribonucleotide 3884:+gimeracil/oteracil 680:follicular lymphoma 564:(codenamed PQR309; 454:Follicular lymphoma 379:respiratory illness 172:follicular lymphoma 158:follicular lymphoma 36:inhibitors such as 5216:Never to phase III 4018:Etirinotecan pegol 3470:10.1042/BST0370615 3221:ClinicalTrials.gov 3203:ClinicalTrials.gov 3185:ClinicalTrials.gov 3167:ClinicalTrials.gov 3129:ClinicalTrials.gov 3111:ClinicalTrials.gov 3046:ClinicalTrials.gov 3028:ClinicalTrials.gov 3010:ClinicalTrials.gov 2974:ClinicalTrials.gov 2956:ClinicalTrials.gov 2877:ClinicalTrials.gov 2859:ClinicalTrials.gov 2841:ClinicalTrials.gov 2634:ClinicalTrials.gov 2556:ClinicalTrials.gov 2537:ClinicalTrials.gov 2519:ClinicalTrials.gov 2486:ClinicalTrials.gov 2468:ClinicalTrials.gov 2450:ClinicalTrials.gov 2432:ClinicalTrials.gov 2414:ClinicalTrials.gov 2396:ClinicalTrials.gov 2378:ClinicalTrials.gov 2360:ClinicalTrials.gov 2342:ClinicalTrials.gov 2266:ClinicalTrials.gov 2248:ClinicalTrials.gov 2229:ClinicalTrials.gov 2211:ClinicalTrials.gov 2173:ClinicalTrials.gov 2114:ClinicalTrials.gov 2047:ClinicalTrials.gov 1985:ClinicalTrials.gov 1967:ClinicalTrials.gov 1949:ClinicalTrials.gov 1907:Annals of Oncology 1890:ClinicalTrials.gov 1836:ClinicalTrials.gov 1768:ClinicalTrials.gov 1750:ClinicalTrials.gov 1683:ClinicalTrials.gov 1598:. TG Therapeutics. 1496:10.1042/BST0350253 1251:10.1042/BST0370265 874:P110δ#Pharmacology 748:(PIK3CD inhibitor) 708:integrin receptors 654:endometrial cancer 512:Kazia PR July 2024 371:placebo-controlled 50: 5226: 5225: 5185: 5184: 5142:Tigilanol tiglate 4619:Enzyme inhibitors 4542: 4541: 4538: 4537: 4238:Nitrogen mustards 4208: 4207: 3968: 3967: 3670: 3669: 3464:(Pt 4): 615–626. 3332:(18): 3371–3386. 2992:. March 27, 2018. 1706:(21): 2307–2316. 1620:. 5 February 2021 1490:(Pt 2): 253–256. 1245:(Pt 1): 265–272. 710:that converts to 5256: 5249:Targeted therapy 5147:Tisagenlecleucel 4904:Arsenic trioxide 4615: 4548:Photosensitizers 4339:Alkyl sulfonates 4253:Cyclophosphamide 4225: 4164:Anthracenediones 3985: 3959:Hydroxycarbamide 3700: 3683: 3561: 3521: 3514: 3507: 3498: 3481: 3444: 3443: 3433: 3416:(7): 1725–1738. 3401: 3395: 3394: 3377:(8): 2408–2411. 3366: 3360: 3359: 3349: 3317: 3311: 3310: 3289: 3283: 3282: 3280: 3279: 3269: 3263: 3262: 3260: 3259: 3249: 3243: 3242: 3240: 3239: 3229: 3223: 3211: 3205: 3193: 3187: 3175: 3169: 3157: 3151: 3150: 3148: 3147: 3137: 3131: 3119: 3113: 3101: 3095: 3094: 3074: 3068: 3067: 3065: 3064: 3054: 3048: 3036: 3030: 3018: 3012: 3000: 2994: 2993: 2982: 2976: 2964: 2958: 2946: 2940: 2939: 2937: 2936: 2926: 2920: 2919: 2909: 2900:(9): 2505–2514. 2885: 2879: 2867: 2861: 2849: 2843: 2831: 2825: 2824: 2822: 2821: 2811: 2805: 2804: 2802: 2801: 2791: 2785: 2784: 2782: 2781: 2771: 2765: 2764: 2754: 2722: 2716: 2715: 2713: 2712: 2702: 2696: 2695: 2693: 2692: 2682: 2676: 2675: 2673: 2672: 2662: 2656: 2655: 2653: 2652: 2642: 2636: 2624: 2618: 2617: 2615: 2614: 2604: 2598: 2597: 2595: 2594: 2584: 2578: 2577: 2575: 2574: 2564: 2558: 2545: 2539: 2527: 2521: 2508: 2502: 2501: 2494: 2488: 2476: 2470: 2458: 2452: 2440: 2434: 2422: 2416: 2404: 2398: 2386: 2380: 2368: 2362: 2350: 2344: 2332: 2326: 2325: 2319: 2314: 2312: 2304: 2302: 2294: 2288: 2287: 2285: 2284: 2274: 2268: 2256: 2250: 2237: 2231: 2219: 2213: 2201: 2195: 2194: 2192: 2191: 2181: 2175: 2163: 2157: 2156: 2146: 2122: 2116: 2104: 2098: 2097: 2087: 2070:(8): 2204–2210. 2055: 2049: 2037: 2031: 2030: 1993: 1987: 1975: 1969: 1957: 1951: 1939: 1933: 1932: 1922: 1898: 1892: 1880: 1874: 1873: 1844: 1838: 1825: 1819: 1818: 1808: 1776: 1770: 1758: 1752: 1740: 1734: 1733: 1723: 1691: 1685: 1673: 1664: 1663: 1661: 1660: 1646: 1640: 1634: 1633: 1629: 1627: 1625: 1606: 1600: 1599: 1597: 1589: 1583: 1582: 1569: 1563: 1562: 1555: 1549: 1548: 1541: 1535: 1514: 1508: 1507: 1479: 1468: 1467: 1450:(3): 1164–1172. 1439: 1430: 1424: 1418: 1417: 1381: 1372: 1371: 1353: 1321: 1315: 1314: 1307: 1298: 1297: 1269: 1263: 1262: 1234: 1225: 1224: 1196: 1190: 1189: 1184:. Archived from 1177: 1171: 1170: 1160: 1128: 1122: 1121: 1085: 1079: 1078: 1068: 1036: 1030: 1029: 993: 984: 983: 973: 941: 935: 934: 924: 914: 890: 640:Sjögren syndrome 373:phase III trial 74:targeted therapy 32:, and dual PI3K/ 5264: 5263: 5259: 5258: 5257: 5255: 5254: 5253: 5229: 5228: 5227: 5222: 5221: 5206:Clinical trials 5181: 4887:Other/ungrouped 4882: 4833: 4606: 4586:Porfimer sodium 4534: 4496: 4429: 4386: 4216: 4204: 4088: 4058: 3976: 3964: 3939: 3835: 3755: 3691: 3689:antimetabolites 3687: 3686:DNA precursors/ 3678: 3676:DNA replication 3666: 3606: 3576:Vinca alkaloids 3552: 3540: 3525: 3488: 3455: 3452: 3450:Further reading 3447: 3403: 3402: 3398: 3368: 3367: 3363: 3319: 3318: 3314: 3291: 3290: 3286: 3277: 3275: 3271: 3270: 3266: 3257: 3255: 3251: 3250: 3246: 3237: 3235: 3231: 3230: 3226: 3212: 3208: 3194: 3190: 3176: 3172: 3158: 3154: 3145: 3143: 3139: 3138: 3134: 3120: 3116: 3102: 3098: 3076: 3075: 3071: 3062: 3060: 3056: 3055: 3051: 3037: 3033: 3019: 3015: 3001: 2997: 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4977: 4972: 4967: 4962: 4957: 4952: 4947: 4942: 4937: 4932: 4927: 4922: 4906: 4901: 4896: 4890: 4888: 4884: 4883: 4881: 4880: 4868: 4856: 4843: 4841: 4835: 4834: 4832: 4831: 4825: 4820: 4815: 4810: 4798: 4792: 4787: 4782: 4777: 4766: 4760: 4755: 4747: 4740:PARP inhibitor 4736: 4724: 4712: 4700: 4699: 4698: 4693: 4688: 4683: 4671: 4665: 4660: 4655: 4650: 4636: 4623: 4621: 4612: 4608: 4607: 4605: 4604: 4598: 4593: 4588: 4577: 4572: 4567: 4562: 4556: 4554: 4544: 4543: 4540: 4539: 4536: 4535: 4533: 4532: 4526: 4521: 4516: 4506: 4504: 4498: 4497: 4495: 4494: 4488: 4483: 4472: 4467: 4462: 4457: 4445: 4439: 4437: 4431: 4430: 4428: 4427: 4422: 4417: 4412: 4407: 4402: 4396: 4394: 4392:Platinum-based 4388: 4387: 4385: 4384: 4379: 4374: 4369: 4357: 4356: 4350: 4334: 4333: 4328: 4323: 4318: 4308: 4303: 4291: 4290: 4285: 4280: 4270: 4265: 4259: 4250: 4245: 4233: 4231: 4222: 4210: 4209: 4206: 4205: 4203: 4202: 4197: 4192: 4187: 4182: 4176: 4171: 4160: 4154: 4149: 4144: 4139: 4134: 4129: 4119: 4114: 4107:Anthracyclines 4102: 4100: 4090: 4089: 4087: 4086: 4080: 4068: 4066: 4060: 4059: 4057: 4056: 4050: 4045: 4040: 4035: 4030: 4025: 4020: 4015: 4010: 4005: 3993: 3991: 3982: 3970: 3969: 3966: 3965: 3963: 3962: 3949: 3947: 3941: 3940: 3938: 3937: 3931: 3919: 3918: 3905: 3904: 3888: 3887: 3877: 3872: 3867: 3862: 3857: 3845: 3843: 3837: 3836: 3834: 3833: 3827: 3825:Mercaptopurine 3816: 3811: 3806: 3800: 3795: 3779: 3778: 3765: 3763: 3757: 3756: 3754: 3753: 3747: 3736: 3730: 3725: 3720: 3708: 3706: 3697: 3680: 3672: 3671: 3668: 3667: 3665: 3664: 3652: 3646: 3641: 3636: 3631: 3626: 3614: 3612: 3608: 3607: 3605: 3604: 3598: 3593: 3588: 3583: 3571: 3569: 3558: 3542: 3541: 3527:Intracellular 3526: 3524: 3523: 3516: 3509: 3501: 3495: 3494: 3487: 3486:External links 3484: 3483: 3482: 3451: 3448: 3446: 3445: 3396: 3361: 3312: 3284: 3264: 3244: 3224: 3206: 3188: 3170: 3152: 3132: 3114: 3096: 3069: 3049: 3031: 3013: 2995: 2977: 2959: 2941: 2921: 2880: 2862: 2844: 2826: 2806: 2786: 2766: 2717: 2697: 2677: 2657: 2637: 2619: 2599: 2579: 2559: 2540: 2522: 2503: 2489: 2471: 2453: 2435: 2417: 2399: 2381: 2363: 2345: 2327: 2318:|journal= 2289: 2269: 2251: 2232: 2214: 2196: 2176: 2158: 2117: 2099: 2050: 2032: 2005:(5): 678–689. 1988: 1970: 1952: 1934: 1913:(2): 313–320. 1893: 1875: 1839: 1820: 1791:(7): 904–916. 1771: 1753: 1735: 1686: 1665: 1641: 1601: 1584: 1564: 1550: 1536: 1509: 1469: 1431: 1419: 1373: 1316: 1299: 1280:(3): 445–456. 1264: 1226: 1207:(8): 916–930. 1191: 1188:on 2013-01-24. 1172: 1143:(1): 346–356. 1123: 1096:(2): 247–262. 1080: 1031: 985: 936: 884: 882: 879: 878: 877: 871: 863: 860: 859: 858: 848: 838: 828: 822: 812: 808: 802: 796: 784: 781: 780: 779: 773: 767: 761: 755: 749: 743: 737: 731: 720: 717: 716: 715: 701: 695: 689: 683: 673: 667: 657: 643: 633: 623: 617: 611: 605: 595: 589: 582:HDAC inhibitor 575: 569: 566:brain-permeant 559: 545: 544: 534: 524: 514: 497: 496: 495: 486: 473: 464: 445: 441:GS-US-312-0116 431: 430: 429: 422: 403: 386: 364: 363: 362: 351: 339: 321: 320: 319: 296: 263: 260: 258: 255: 254: 253: 221: 203: 185: 175: 161: 134: 131: 69:signal pathway 13: 10: 9: 6: 4: 3: 2: 5261: 5250: 5247: 5245: 5242: 5240: 5237: 5236: 5234: 5215: 5213: 5210: 5209: 5207: 5204: 5201: 5198: 5196: 5193: 5192: 5188: 5178: 5175: 5173: 5170: 5168: 5165: 5163: 5160: 5158: 5155: 5153: 5150: 5148: 5145: 5143: 5140: 5138: 5135: 5133: 5130: 5128: 5125: 5123: 5120: 5118: 5115: 5113: 5110: 5108: 5105: 5103: 5100: 5097: 5094: 5092: 5088: 5087: 5083: 5081: 5080:Tabelecleucel 5078: 5076: 5073: 5071: 5068: 5066: 5063: 5061: 5058: 5056: 5053: 5051: 5048: 5046: 5043: 5041: 5040:Lurbinectedin 5038: 5036: 5033: 5031: 5028: 5026: 5023: 5021: 5018: 5016: 5013: 5011: 5008: 5006: 5003: 5001: 4998: 4996: 4993: 4991: 4988: 4986: 4983: 4981: 4978: 4976: 4973: 4971: 4968: 4966: 4963: 4961: 4958: 4956: 4953: 4951: 4948: 4946: 4943: 4941: 4938: 4936: 4933: 4931: 4928: 4926: 4923: 4920: 4916: 4912: 4911: 4907: 4905: 4902: 4900: 4897: 4895: 4892: 4891: 4889: 4885: 4878: 4874: 4873: 4869: 4866: 4862: 4861: 4857: 4854: 4850: 4849: 4845: 4844: 4842: 4840: 4836: 4829: 4826: 4824: 4821: 4819: 4816: 4814: 4811: 4809: 4805: 4803: 4799: 4796: 4793: 4791: 4788: 4786: 4783: 4781: 4778: 4776: 4772: 4771: 4767: 4764: 4761: 4759: 4756: 4754: 4751: 4748: 4746: 4742: 4741: 4737: 4734: 4730: 4729: 4725: 4722: 4718: 4717: 4713: 4710: 4706: 4705: 4701: 4697: 4694: 4692: 4689: 4687: 4684: 4682: 4679: 4678: 4677: 4676: 4672: 4669: 4666: 4664: 4661: 4659: 4656: 4654: 4651: 4649: 4645: 4644: 4641: 4637: 4634: 4630: 4629: 4625: 4624: 4622: 4620: 4616: 4613: 4609: 4602: 4599: 4597: 4594: 4592: 4589: 4587: 4583: 4582: 4578: 4576: 4573: 4571: 4568: 4566: 4563: 4561: 4558: 4557: 4555: 4553: 4549: 4545: 4530: 4527: 4525: 4522: 4520: 4517: 4515: 4511: 4508: 4507: 4505: 4503: 4502:Intercalation 4499: 4492: 4489: 4487: 4484: 4482: 4478: 4477: 4473: 4471: 4468: 4466: 4463: 4461: 4458: 4455: 4451: 4450: 4446: 4444: 4441: 4440: 4438: 4436: 4432: 4426: 4423: 4421: 4418: 4416: 4413: 4411: 4410:Dicycloplatin 4408: 4406: 4403: 4401: 4398: 4397: 4395: 4393: 4389: 4383: 4380: 4378: 4375: 4373: 4370: 4368: 4365: 4363: 4359: 4358: 4354: 4351: 4349: 4345: 4342: 4340: 4336: 4335: 4332: 4329: 4327: 4324: 4322: 4319: 4316: 4312: 4309: 4307: 4304: 4302: 4299: 4297: 4293: 4292: 4289: 4286: 4284: 4283:Prednimustine 4281: 4278: 4274: 4271: 4269: 4266: 4263: 4260: 4258: 4254: 4251: 4249: 4246: 4244: 4241: 4239: 4235: 4234: 4232: 4230: 4226: 4223: 4220: 4215: 4211: 4201: 4198: 4196: 4193: 4191: 4188: 4186: 4183: 4180: 4177: 4175: 4172: 4170: 4166: 4165: 4161: 4158: 4155: 4153: 4150: 4148: 4145: 4143: 4140: 4138: 4135: 4133: 4130: 4127: 4123: 4120: 4118: 4115: 4113: 4109: 4108: 4104: 4103: 4101: 4099: 4098:Intercalation 4095: 4091: 4084: 4081: 4079: 4075: 4074: 4070: 4069: 4067: 4065: 4061: 4054: 4051: 4049: 4046: 4044: 4041: 4039: 4036: 4034: 4031: 4029: 4026: 4024: 4021: 4019: 4016: 4014: 4011: 4009: 4006: 4004: 4000: 3999: 3995: 3994: 3992: 3990: 3986: 3983: 3980: 3975: 3971: 3960: 3956: 3955: 3951: 3950: 3948: 3946: 3942: 3935: 3932: 3930: 3926: 3925: 3921: 3920: 3916: 3912: 3911: 3907: 3906: 3902: 3901:+daunorubicin 3899: 3895: 3894: 3890: 3889: 3885: 3881: 3878: 3876: 3873: 3871: 3868: 3866: 3865:Doxifluridine 3863: 3861: 3858: 3856: 3852: 3851: 3847: 3846: 3844: 3842: 3838: 3831: 3828: 3826: 3822: 3821: 3817: 3815: 3814:Rabacfosadine 3812: 3810: 3807: 3804: 3801: 3799: 3796: 3794: 3790: 3789: 3785: 3781: 3780: 3776: 3772: 3771: 3767: 3766: 3764: 3762: 3758: 3751: 3748: 3746: 3742: 3741: 3737: 3734: 3731: 3729: 3726: 3724: 3721: 3719: 3715: 3714: 3710: 3709: 3707: 3705: 3701: 3698: 3695: 3690: 3684: 3681: 3677: 3673: 3662: 3658: 3657: 3653: 3650: 3647: 3645: 3642: 3640: 3637: 3635: 3632: 3630: 3627: 3625: 3621: 3620: 3616: 3615: 3613: 3609: 3602: 3599: 3597: 3594: 3592: 3589: 3587: 3584: 3582: 3578: 3577: 3573: 3572: 3570: 3567: 3562: 3559: 3556: 3551: 3547: 3543: 3538: 3534: 3530: 3522: 3517: 3515: 3510: 3508: 3503: 3502: 3499: 3493: 3490: 3489: 3485: 3479: 3475: 3471: 3467: 3463: 3459: 3454: 3453: 3449: 3441: 3437: 3432: 3427: 3423: 3419: 3415: 3411: 3407: 3400: 3397: 3392: 3388: 3384: 3380: 3376: 3372: 3365: 3362: 3357: 3353: 3348: 3343: 3339: 3335: 3331: 3327: 3323: 3316: 3313: 3308: 3304: 3300: 3296: 3288: 3285: 3274: 3268: 3265: 3254: 3248: 3245: 3234: 3228: 3225: 3222: 3218: 3217: 3210: 3207: 3204: 3200: 3199: 3192: 3189: 3186: 3182: 3181: 3174: 3171: 3168: 3164: 3163: 3156: 3153: 3142: 3136: 3133: 3130: 3126: 3125: 3118: 3115: 3112: 3108: 3107: 3100: 3097: 3092: 3088: 3084: 3080: 3073: 3070: 3059: 3053: 3050: 3047: 3043: 3042: 3035: 3032: 3029: 3025: 3024: 3017: 3014: 3011: 3007: 3006: 2999: 2996: 2991: 2987: 2981: 2978: 2975: 2971: 2970: 2963: 2960: 2957: 2953: 2952: 2945: 2942: 2931: 2925: 2922: 2917: 2913: 2908: 2903: 2899: 2895: 2891: 2884: 2881: 2878: 2874: 2873: 2866: 2863: 2860: 2856: 2855: 2848: 2845: 2842: 2838: 2837: 2830: 2827: 2816: 2810: 2807: 2796: 2790: 2787: 2776: 2770: 2767: 2762: 2758: 2753: 2748: 2744: 2740: 2736: 2732: 2728: 2721: 2718: 2707: 2701: 2698: 2687: 2681: 2678: 2667: 2661: 2658: 2647: 2641: 2638: 2635: 2631: 2630: 2623: 2620: 2609: 2603: 2600: 2589: 2583: 2580: 2569: 2563: 2560: 2557: 2552: 2551: 2544: 2541: 2538: 2534: 2533: 2526: 2523: 2520: 2515: 2514: 2507: 2504: 2499: 2493: 2490: 2487: 2483: 2482: 2475: 2472: 2469: 2465: 2464: 2457: 2454: 2451: 2447: 2446: 2439: 2436: 2433: 2429: 2428: 2421: 2418: 2415: 2411: 2410: 2403: 2400: 2397: 2393: 2392: 2385: 2382: 2379: 2375: 2374: 2367: 2364: 2361: 2357: 2356: 2349: 2346: 2343: 2339: 2338: 2331: 2328: 2323: 2310: 2303:. 2016-11-21. 2299: 2293: 2290: 2279: 2273: 2270: 2267: 2263: 2262: 2255: 2252: 2249: 2244: 2243: 2236: 2233: 2230: 2226: 2225: 2218: 2215: 2212: 2208: 2207: 2200: 2197: 2186: 2180: 2177: 2174: 2170: 2169: 2162: 2159: 2154: 2150: 2145: 2140: 2136: 2132: 2128: 2121: 2118: 2115: 2111: 2110: 2103: 2100: 2095: 2091: 2086: 2081: 2077: 2073: 2069: 2065: 2061: 2054: 2051: 2048: 2044: 2043: 2036: 2033: 2028: 2024: 2020: 2016: 2012: 2008: 2004: 2000: 1992: 1989: 1986: 1982: 1981: 1974: 1971: 1968: 1964: 1963: 1956: 1953: 1950: 1946: 1945: 1938: 1935: 1930: 1926: 1921: 1916: 1912: 1908: 1904: 1897: 1894: 1891: 1887: 1886: 1879: 1876: 1871: 1867: 1863: 1859: 1856:(1): 87–100. 1855: 1851: 1843: 1840: 1837: 1832: 1831: 1824: 1821: 1816: 1812: 1807: 1802: 1798: 1794: 1790: 1786: 1782: 1775: 1772: 1769: 1765: 1764: 1757: 1754: 1751: 1747: 1746: 1739: 1736: 1731: 1727: 1722: 1717: 1713: 1709: 1705: 1701: 1697: 1690: 1687: 1684: 1680: 1679: 1672: 1670: 1666: 1655: 1651: 1645: 1642: 1638: 1637:public domain 1619: 1617: 1611: 1605: 1602: 1594: 1588: 1585: 1581:. 2019-05-24. 1580: 1579: 1574: 1568: 1565: 1560: 1554: 1551: 1546: 1540: 1537: 1534: 1530: 1527: 1523: 1519: 1513: 1510: 1505: 1501: 1497: 1493: 1489: 1485: 1478: 1476: 1474: 1470: 1465: 1461: 1457: 1453: 1449: 1445: 1438: 1436: 1432: 1428: 1423: 1420: 1415: 1411: 1407: 1403: 1399: 1395: 1391: 1387: 1380: 1378: 1374: 1369: 1365: 1361: 1357: 1352: 1347: 1343: 1339: 1335: 1331: 1327: 1320: 1317: 1312: 1306: 1304: 1300: 1295: 1291: 1287: 1283: 1279: 1275: 1268: 1265: 1260: 1256: 1252: 1248: 1244: 1240: 1233: 1231: 1227: 1222: 1218: 1214: 1210: 1206: 1202: 1195: 1192: 1187: 1183: 1176: 1173: 1168: 1164: 1159: 1154: 1150: 1146: 1142: 1138: 1134: 1127: 1124: 1119: 1115: 1111: 1107: 1103: 1099: 1095: 1091: 1084: 1081: 1076: 1072: 1067: 1062: 1058: 1054: 1050: 1046: 1042: 1035: 1032: 1027: 1023: 1019: 1015: 1011: 1007: 1003: 999: 992: 990: 986: 981: 977: 972: 967: 963: 959: 955: 951: 947: 940: 937: 932: 928: 923: 918: 913: 908: 904: 900: 896: 889: 886: 880: 875: 872: 869: 866: 865: 861: 856: 852: 849: 846: 842: 839: 836: 832: 829: 826: 823: 820: 816: 813: 806: 803: 800: 797: 794: 790: 787: 786: 782: 777: 774: 771: 768: 765: 762: 759: 756: 753: 750: 747: 744: 741: 738: 735: 732: 729: 726: 725: 724: 718: 713: 709: 705: 702: 699: 696: 693: 690: 687: 684: 681: 677: 674: 671: 668: 665: 661: 658: 655: 651: 647: 644: 641: 637: 634: 631: 627: 624: 621: 618: 615: 612: 609: 606: 603: 599: 596: 593: 590: 587: 583: 579: 576: 573: 570: 567: 563: 560: 557: 554: 553: 552: 550: 542: 538: 535: 532: 528: 525: 522: 518: 515: 513: 509: 505: 501: 498: 494: 490: 487: 485: 481: 477: 476:Myelofibrosis 474: 472: 468: 465: 463: 459: 455: 452: 451: 449: 446: 442: 439: 438:pivotal trial 435: 432: 427: 423: 420: 416: 412: 408: 404: 401: 397: 393: 392: 390: 387: 384: 380: 376: 372: 368: 365: 360: 356: 352: 348: 344: 340: 336: 332: 331: 329: 325: 322: 317: 313: 309: 305: 301: 297: 294: 291: 290:head and neck 287: 283: 279: 278: 276: 273: 272: 271: 269: 261: 256: 251: 247: 243: 239: 238:PASLI disease 235: 231: 230: 225: 222: 219: 215: 211: 207: 204: 201: 197: 193: 190:(trade names 189: 186: 183: 179: 176: 173: 169: 165: 162: 159: 155: 151: 147: 144: 140: 137: 136: 132: 130: 128: 124: 119: 117: 113: 110:(PIK3CG) and 109: 105: 101: 97: 96:Class 1 PI3Ks 93: 89: 84: 82: 77: 75: 70: 66: 62: 58: 54: 47: 43: 39: 35: 31: 27: 23: 18: 5127:Tazemetostat 5091:Alitretinoin 5084: 4995:Estramustine 4975:Elsamitrucin 4965:Eflornithine 4919:Pegaspargase 4915:Asparaginase 4908: 4877:Testolactone 4870: 4858: 4846: 4801: 4800: 4785:Panobinostat 4768: 4738: 4726: 4714: 4702: 4673: 4638: 4626: 4579: 4575:Padeliporfin 4514:Dactinomycin 4510:Streptomyces 4491:Temozolomide 4486:Mitozolomide 4474: 4465:Mitobronitol 4454:Procarbazine 4447: 4435:Nonclassical 4360: 4337: 4331:Streptozocin 4296:Nitrosoureas 4294: 4268:Chlorambucil 4262:Trofosfamide 4248:Chlormethine 4243:Bendamustine 4236: 4174:Mitoxantrone 4169:Losoxantrone 4162: 4122:Daunorubicin 4105: 4071: 4008:Camptothecin 3996: 3952: 3922: 3908: 3891: 3875:Fluorouracil 3855:Capecitabine 3848: 3818: 3782: 3768: 3738: 3733:Pralatrexate 3723:Methotrexate 3711: 3654: 3617: 3574: 3461: 3457: 3413: 3409: 3399: 3374: 3370: 3364: 3329: 3325: 3315: 3301:(21): 3067. 3298: 3294: 3287: 3276:. Retrieved 3267: 3256:. Retrieved 3247: 3236:. Retrieved 3227: 3214: 3209: 3196: 3191: 3178: 3173: 3160: 3155: 3144:. Retrieved 3135: 3122: 3117: 3104: 3099: 3085:(21): 1783. 3082: 3078: 3072: 3061:. Retrieved 3052: 3039: 3034: 3021: 3016: 3003: 2998: 2989: 2980: 2967: 2962: 2949: 2944: 2933:. Retrieved 2924: 2897: 2893: 2883: 2870: 2865: 2852: 2847: 2834: 2829: 2818:. Retrieved 2809: 2798:. Retrieved 2789: 2778:. Retrieved 2769: 2737:(1): 77–86. 2734: 2730: 2720: 2709:. Retrieved 2700: 2689:. Retrieved 2680: 2669:. Retrieved 2660: 2649:. Retrieved 2640: 2627: 2622: 2611:. Retrieved 2602: 2591:. Retrieved 2582: 2571:. Retrieved 2562: 2548: 2543: 2530: 2525: 2511: 2506: 2492: 2479: 2474: 2461: 2456: 2443: 2438: 2425: 2420: 2407: 2402: 2389: 2384: 2371: 2366: 2353: 2348: 2335: 2330: 2309:cite journal 2292: 2281:. Retrieved 2272: 2259: 2254: 2240: 2235: 2222: 2217: 2204: 2199: 2188:. Retrieved 2179: 2166: 2161: 2134: 2130: 2120: 2107: 2102: 2067: 2063: 2053: 2040: 2035: 2002: 1998: 1991: 1978: 1973: 1960: 1955: 1942: 1937: 1910: 1906: 1896: 1883: 1878: 1853: 1849: 1842: 1828: 1823: 1788: 1784: 1774: 1761: 1756: 1743: 1738: 1703: 1699: 1689: 1676: 1657:. Retrieved 1653: 1644: 1622:. Retrieved 1613: 1604: 1587: 1576: 1567: 1553: 1539: 1517: 1512: 1487: 1483: 1447: 1443: 1422: 1389: 1385: 1333: 1329: 1319: 1277: 1273: 1267: 1242: 1238: 1204: 1200: 1194: 1186:the original 1175: 1140: 1136: 1126: 1093: 1089: 1083: 1048: 1044: 1034: 1001: 997: 956:(2): 74–88. 953: 949: 939: 902: 898: 888: 855:irreversible 854: 834: 819:irreversible 818: 722: 578:Fimepinostat 546: 540: 530: 520: 507: 504:glioblastoma 492: 483: 479: 470: 461: 440: 425: 415:bendamustine 406: 395: 382: 374: 354: 342: 334: 307: 303: 299: 281: 265: 245: 241: 227: 209: 208:(trade name 195: 191: 181: 180:(trade name 167: 166:(trade name 145: 120: 85: 78: 56: 52: 51: 42:fimepinostat 40:. Note that 5202:from market 5172:Vorasidenib 5152:Trabectedin 5137:Tiazofurine 5132:Tebentafusp 5117:Tagraxofusp 5075:Plitidepsin 5045:Mitoguazone 4985:Epacadostat 4955:Demecolcine 4899:Aflibercept 4872:Sex steroid 4745:Fuzuloparib 4686:Carfilzomib 4658:Palbociclib 4648:Abemaciclib 4601:Verteporfin 4565:Efaproxiral 4481:Dacarbazine 4443:Altretamine 4425:Satraplatin 4420:Oxaliplatin 4400:Carboplatin 4377:Triaziquone 4348:Mannosulfan 4326:Ranimustine 4306:Fotemustine 4147:Pirarubicin 4132:Doxorubicin 4126:+cytarabine 4112:Aclarubicin 4073:Podophyllum 3998:Camptotheca 3929:Azacitidine 3915:Gemcitabine 3870:Floxuridine 3803:Fludarabine 3798:Clofarabine 3784:Halogenated 3775:Pentostatin 3750:Raltitrexed 3718:Aminopterin 3661:Ixabepilone 3656:Epothilones 3624:Cabazitaxel 3601:Vinorelbine 3586:Vincristine 3581:Vinblastine 3566:microtubule 3216:NCT04495621 3198:NCT00695448 3180:NCT01066611 3162:NCT02260661 3124:NCT01705847 3106:NCT02644122 3041:NCT04001569 3023:NCT02540928 3005:NCT01403636 2969:NCT03711578 2951:NCT04204057 2872:NCT02725268 2854:NCT02724020 2836:NCT02610543 2629:NCT02674750 2550:NCT04191499 2532:NCT04745832 2513:NCT02340221 2481:NCT03970447 2463:NCT05073458 2445:NCT04551066 2427:NCT04551053 2409:NCT04849715 2391:NCT04796922 2373:NCT02536300 2355:NCT04666038 2337:NCT02970318 2261:NCT02204982 2242:NCT02576275 2224:NCT02049515 2206:NCT02004522 2168:NCT04139915 2109:NCT04668352 2042:NCT02626455 1980:NCT02367040 1962:NCT02369016 1944:NCT01572727 1885:NCT01633060 1830:NCT01610284 1763:NCT04338399 1745:NCT02859727 1678:NCT02435173 1090:Drug Safety 905:(7): 3464. 815:Hibiscone C 719:Early stage 646:Serabelisib 636:Seletalisib 626:Samotolisib 620:Pilaralisib 608:Nemiralisib 598:Linperlisib 592:Gedatolisib 562:Bimiralisib 541:NCT04191499 471:CITADEL-310 462:CITADEL-302 448:Parsaclisib 383:PROTECTOR 2 375:PROTECTOR 1 246:NCT02859727 242:NCT02435173 200:fulvestrant 5233:Categories 5167:Verdinexor 5162:Venetoclax 5065:Oblimersen 5060:Navitoclax 5035:Lucanthone 5030:Lonidamine 5020:Lifileucel 5015:Ivosidenib 5010:Imetelstat 4980:Enasidenib 4970:Elesclomol 4935:Bexarotene 4930:Belzutifan 4865:Bexarotene 4853:Atrasentan 4828:Umbralisib 4823:Idelalisib 4813:Copanlisib 4795:Vorinostat 4790:Romidepsin 4780:Entinostat 4775:Belinostat 4733:Masoprocol 4721:Tiazofurin 4709:Anagrelide 4681:Bortezomib 4668:Seliciclib 4663:Ribociclib 4643:inhibitors 4633:Tipifarnib 4596:Temoporfin 4591:Talaporfin 4529:Plicamycin 4524:Mitomycins 4470:Pipobroman 4449:Hydrazines 4415:Nedaplatin 4367:Carboquone 4362:Aziridines 4353:Treosulfan 4301:Carmustine 4288:Uramustine 4257:Ifosfamide 4229:Alkylating 4190:Bisantrene 4179:Pixantrone 4152:Valrubicin 4142:Idarubicin 4137:Epirubicin 4083:Teniposide 4038:Lurtotecan 4033:Irinotecan 3934:Decitabine 3898:Cytarabine 3841:Pyrimidine 3830:Tioguanine 3820:Thiopurine 3809:Nelarabine 3793:Cladribine 3745:Pemetrexed 3728:Pemetrexed 3704:Folic acid 3644:Paclitaxel 3596:Vinflunine 3278:2022-03-09 3258:2022-03-09 3238:2022-03-09 3146:2022-03-17 3063:2022-03-17 2935:2022-03-04 2820:2022-03-17 2800:2022-03-09 2780:2022-03-07 2711:2022-03-17 2691:2022-03-18 2671:2022-03-17 2651:2022-03-04 2613:2022-03-07 2593:2022-03-17 2573:2022-03-17 2283:2022-03-21 2190:2022-03-04 1659:2022-10-06 1624:5 February 1518:Oncotarget 1392:(1): 1–8. 1051:(1): 201. 881:References 851:Wortmannin 847:inhibitor) 835:reversible 795:inhibitor) 752:GSK1059615 734:Omipalisib 698:GSK2636771 676:Voxtalisib 664:wortmannin 614:Pictilisib 572:Eganelisib 556:Apitolisib 537:Inavolisib 527:Zandelisib 484:LIMBER-313 480:LIMBER-304 434:Idelalisib 426:DYNAMO + R 400:ofatumumab 367:Dactolisib 333:The trial 324:Copanlisib 286:paclitaxel 275:Buparlisib 262:Late stage 224:Leniolisib 206:Umbralisib 164:Copanlisib 143:trade name 139:Idelalisib 112:p110 delta 108:p110 gamma 106:(PIK3CB), 102:(PIK3CA), 100:p110 alpha 81:idelalisib 46:rigosertib 38:dactolisib 30:idelalisib 26:copanlisib 5212:Phase III 5200:Withdrawn 5177:Vosaroxin 5157:Veliparib 5112:Sotorasib 5102:Selinexor 5096:Tretinoin 5086:Retinoids 5000:Glasdegib 4945:Celecoxib 4894:Adagrasib 4818:Duvelisib 4808:Alpelisib 4763:Rucaparib 4750:Niraparib 4691:Oprozomib 4653:Alvocidib 4519:Bleomycin 4476:Triazenes 4460:Etoglucid 4405:Cisplatin 4321:Nimustine 4315:Semustine 4311:Lomustine 4273:Melphalan 4200:Menogaril 4195:Crisnatol 4185:Amsacrine 4157:Zorubicin 4117:Amrubicin 4078:Etoposide 4053:Topotecan 4048:Silatecan 4043:Rubitecan 4028:Gimatecan 4013:Cositecan 4003:Belotecan 3679:inhibitor 3649:Tesetaxel 3639:Ortataxel 3634:Larotaxel 3629:Docetaxel 3591:Vindesine 2153:213379077 2137:: 32–34. 2027:233234876 1368:235437841 1026:234360275 770:TG100-115 670:Tenalisib 660:Sonolisib 521:SANDPIPER 517:Taselisib 508:GBM AGILE 500:Paxalisib 456:(FL) and 411:rituximab 389:Duvelisib 355:CHRONOS-4 347:rituximab 343:CHRONOS-3 335:CHRONOS-2 236:(APDS) / 188:Alpelisib 178:Duvelisib 154:rituximab 104:p110 beta 5050:Mitotane 4990:Eribulin 4758:Olaparib 4696:Ixazomib 4372:Thiotepa 4344:Busulfan 4023:Exatecan 3860:Carmofur 3568:assembly 3531: / 3478:19614567 3440:19584227 3391:20346656 3356:30635656 3326:Oncogene 2916:17766839 2761:25370471 2094:19671762 2019:33848462 1929:27803006 1870:29223745 1815:28576675 1730:28972011 1533:34504654 1504:17371252 1464:20103642 1406:17021257 1360:34127844 1294:24055012 1259:19143644 1221:19275602 1167:33275709 1118:58657824 1110:30649751 1075:34054126 1018:33970742 980:31686003 931:33801659 862:See also 831:LY294002 789:AEZS-136 764:PWT33597 728:Acalisib 712:LY294002 602:lymphoma 350:effects. 330:(iNHL): 316:Novartis 250:approved 182:Copiktra 88:isoforms 3979:S phase 3880:Tegafur 3694:S phase 3619:Taxanes 3555:M phase 3431:2718129 3347:6756013 2752:4287394 2085:2752877 1806:5549667 1721:5701526 1414:1906947 1351:9297732 1158:7727518 1066:8165101 971:7314312 922:8037248 825:IC87114 805:GNE-477 776:ZSTK474 758:MEN1611 740:AZD8835 692:AZD8186 686:AMG 319 531:COASTAL 493:PATHWAY 407:BRAVURA 308:BELLE-4 304:BELLE-3 300:BELLE-2 196:Pivikto 168:Aliqopa 146:Zydelig 67:. This 5195:WHO-EM 4804:(Pi3K) 3761:Purine 3564:Block 3476:  3438:  3428:  3389:  3354:  3344:  2914:  2759:  2749:  2151:  2092:  2082:  2025:  2017:  1927:  1868:  1813:  1803:  1728:  1718:  1531:  1502:  1462:  1412:  1404:  1366:  1358:  1348:  1292:  1257:  1219:  1165:  1155:  1116:  1108:  1073:  1063:  1024:  1016:  978:  968:  929:  919:  845:DNA-PK 841:PI-103 746:CAL263 704:SF1126 630:DNA-PK 359:R-CHOP 229:Joenja 214:CSNK1E 210:Ukoniq 192:Piqray 4716:IMPDI 4611:Other 3295:Blood 3079:Blood 2301:(PDF) 2149:S2CID 2023:S2CID 1700:Blood 1618:(FDA) 1614:U.S. 1596:(PDF) 1410:S2CID 1364:S2CID 1114:S2CID 1022:S2CID 338:2022. 282:BURAN 127:aging 92:PI3Ks 72:of a 4802:PIKI 4770:HDAC 4219:CCNS 3474:PMID 3436:PMID 3387:PMID 3352:PMID 2912:PMID 2757:PMID 2322:help 2090:PMID 2015:PMID 1925:PMID 1866:PMID 1811:PMID 1726:PMID 1626:2021 1529:PMID 1500:PMID 1460:PMID 1402:PMID 1356:PMID 1290:PMID 1255:PMID 1217:PMID 1163:PMID 1141:2020 1106:PMID 1071:PMID 1014:PMID 976:PMID 927:PMID 799:B591 652:and 482:and 302:and 194:and 116:PTEN 44:and 34:mTOR 4848:ERA 4704:PhI 4675:PrI 4640:CDK 4552:PDT 3550:MIs 3546:SPs 3537:L01 3466:doi 3426:PMC 3418:doi 3379:doi 3342:PMC 3334:doi 3303:doi 3299:122 3087:doi 3083:116 2902:doi 2747:PMC 2739:doi 2139:doi 2080:PMC 2072:doi 2007:doi 1915:doi 1858:doi 1801:PMC 1793:doi 1716:PMC 1708:doi 1704:130 1522:doi 1492:doi 1452:doi 1394:doi 1390:321 1346:PMC 1338:doi 1282:doi 1247:doi 1209:doi 1153:PMC 1145:doi 1098:doi 1061:PMC 1053:doi 1006:doi 966:PMC 958:doi 917:PMC 907:doi 793:ERK 547:In 396:DUO 266:In 150:FDA 90:of 5235:: 5208:: 4728:LI 4628:FI 4094:II 4064:II 3886:)) 3472:. 3462:37 3460:. 3434:. 3424:. 3412:. 3408:. 3385:. 3375:20 3373:. 3350:. 3340:. 3330:38 3328:. 3324:. 3297:. 3081:. 2988:. 2910:. 2896:. 2892:. 2755:. 2745:. 2735:21 2733:. 2729:. 2313:: 2311:}} 2307:{{ 2147:. 2133:. 2129:. 2088:. 2078:. 2066:. 2062:. 2021:. 2013:. 2003:22 2001:. 1923:. 1911:28 1909:. 1905:. 1864:. 1854:19 1852:. 1809:. 1799:. 1789:18 1787:. 1783:. 1724:. 1714:. 1702:. 1698:. 1668:^ 1652:. 1612:. 1575:. 1498:. 1488:35 1486:. 1472:^ 1458:. 1448:70 1446:. 1434:^ 1408:. 1400:. 1388:. 1376:^ 1362:. 1354:. 1344:. 1334:20 1332:. 1328:. 1302:^ 1288:. 1278:40 1276:. 1253:. 1243:37 1241:. 1229:^ 1215:. 1205:16 1203:. 1161:. 1151:. 1139:. 1135:. 1112:. 1104:. 1094:42 1092:. 1069:. 1059:. 1047:. 1043:. 1020:. 1012:. 1002:31 1000:. 988:^ 974:. 964:. 954:20 952:. 948:. 925:. 915:. 903:22 901:. 897:. 809:50 551:: 413:+ 270:: 129:. 94:. 5098:) 5089:( 4921:) 4917:/ 4913:( 4879:) 4875:( 4867:) 4863:( 4855:) 4851:( 4830:) 4806:( 4797:) 4773:( 4765:) 4743:( 4735:) 4731:( 4723:) 4719:( 4711:) 4707:( 4670:) 4646:( 4635:) 4631:( 4603:) 4584:( 4550:/ 4531:) 4512:( 4493:) 4479:( 4456:) 4452:( 4364:: 4355:) 4346:( 4341:: 4317:) 4313:( 4298:: 4279:) 4275:( 4264:) 4255:( 4240:: 4221:) 4217:( 4181:) 4167:( 4159:) 4128:) 4124:( 4110:( 4096:+ 4085:) 4076:( 4055:) 4001:( 3989:I 3981:) 3977:( 3961:) 3957:( 3936:) 3927:( 3917:) 3913:( 3903:) 3896:( 3882:( 3853:( 3832:) 3823:( 3805:) 3791:( 3786:/ 3777:) 3773:( 3752:) 3743:( 3735:) 3716:( 3696:) 3692:( 3663:) 3659:( 3651:) 3622:( 3603:) 3579:( 3557:) 3553:( 3548:/ 3539:) 3535:( 3520:e 3513:t 3506:v 3480:. 3468:: 3442:. 3420:: 3414:8 3393:. 3381:: 3358:. 3336:: 3309:. 3305:: 3281:. 3261:. 3241:. 3149:. 3093:. 3089:: 3066:. 2938:. 2918:. 2904:: 2898:6 2823:. 2803:. 2783:. 2763:. 2741:: 2714:. 2694:. 2674:. 2654:. 2616:. 2596:. 2576:. 2500:. 2324:) 2320:( 2286:. 2193:. 2155:. 2141:: 2135:4 2096:. 2074:: 2068:8 2029:. 2009:: 1931:. 1917:: 1872:. 1860:: 1817:. 1795:: 1732:. 1710:: 1662:. 1639:. 1628:. 1524:: 1506:. 1494:: 1466:. 1454:: 1416:. 1396:: 1370:. 1340:: 1296:. 1284:: 1261:. 1249:: 1223:. 1211:: 1169:. 1147:: 1120:. 1100:: 1077:. 1055:: 1049:6 1028:. 1008:: 982:. 960:: 933:. 909:: 853:( 833:( 817:( 682:. 656:. 202:. 141:( 55:(

Index


PI3K/AKT/mTOR pathway
copanlisib
idelalisib
mTOR
dactolisib
fimepinostat
rigosertib
phosphoinositide 3-kinase
PI3K/AKT/mTOR pathway
signal pathway
targeted therapy
idelalisib
isoforms
PI3Ks
Class 1 PI3Ks
p110 alpha
p110 beta
p110 gamma
p110 delta
PTEN
inflammatory respiratory disease
aging
Idelalisib
trade name
FDA
rituximab
follicular lymphoma
Copanlisib
follicular lymphoma

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