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Vemurafenib

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Vemurafenib, plus Obinutuzumab, in patients with previously untreated classical hairy cell leukemia. A separate clinical study treatment with only Vemurafenib (or monotherarpy) demonstrated high response rates in relapsed/refractory (R/R) hairy cell leukemia (HCL), achieving an overall response rate of 86%, including 33% complete response (CR) and 53% partial response. However, after a median follow-up of 40 months, 21 of 31 responders (68%) experienced relapse with a median relapse-free survival (RFS) of 19 months (range, 12.5-53.9 months).
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Foundation supported the discovery of the BRAF mutation in classic HCL. This discovery charted a new path forward for many patients. It improved diagnosis and opened the door for additional therapies to be used in managing HCL. In a phase II clinical trial, Memorial Sloan Kettering is testing
948:). About 60% of melanomas have this mutation. It also has efficacy against the rarer BRAF V600K mutation. Melanoma cells without these mutations are not inhibited by vemurafenib; the drug paradoxically stimulates normal BRAF and may promote tumor growth in such cases. 1012:, vemurafenib (then known as PLX4032) was able to reduce numbers of cancer cells in over half of a group of 16 patients with advanced melanoma. The treated group had a median increased survival time of 6 months over the control group. 999:
in 58% of patients, skin rash in 52%, and photosensitivity in 52%. In order to better manage side effects some form of dose modification was necessary in 45% of patients. The median daily dose was 1750 mg, 91% of the MTD.
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Sala E, Mologni L, Truffa S, Gaetano C, Bollag GE, Gambacorti-Passerini C (May 2008). "BRAF silencing by short hairpin RNA or chemical blockade by PLX4032 leads to different responses in melanoma and thyroid carcinoma cells".
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At the maximum tolerated dose (MTD) of 960 mg twice a day 31% of patients get skin lesions that may need surgical removal. The BRIM-2 trial investigated 132 patients; the most common adverse events were
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InChI=1S/C23H18ClF2N3O3S/c1-2-9-33(31,32)29-19-8-7-18(25)20(21(19)26)22(30)17-12-28-23-16(17)10-14(11-27-23)13-3-5-15(24)6-4-13/h3-8,10-12,29H,2,9H2,1H3,(H,27,28)
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In June 2011, positive results were reported from the phase III BRIM3 BRAF-mutation melanoma study. The BRIM3 trial reported good updated results in 2012.
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A second phase I study, in patients with a V600E mutation in B-Raf, ~80% showed partial to complete regression. The regression lasted from 2 to 18 months.
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Bollag G, Tsai J, Zhang J, Zhang C, Ibrahim P, Nolop K, Hirth P (November 2012). "Vemurafenib: the first drug approved for BRAF-mutant cancer".
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Vemurafenib was approved in the United States for the treatment of late-stage melanoma in August 2011, making it the first drug designed using
795:= red) complexed with vemurafenib (spheres, carbon = white, oxygen = red, nitrogen = blue, chlorine = green, fluorine = cyan, sulfur = yellow). 6786: 6676: 6626: 6597: 6544: 5031: 4898: 6355: 6351: 6347: 6343: 3896: 3880: 2479: 1972:"FDA Approves Zelboraf (Vemurafenib) and Companion Diagnostic for BRAF Mutation-Positive Metastatic Melanoma, a Deadly Form of Skin Cancer" 4624: 4543: 4410: 4327: 2074: 6339: 3457: 6746: 6028: 5147: 4707: 4318: 883: 728: 201: 102: 1861: 3976: 3920: 3911: 2877: 2403: 2043: 6550: 1037:) in patients with previously untreated metastatic melanoma showed an improved rates of overall and progression-free survival. 356: 286: 169: 1957: 6637: 6613: 5753: 5309: 5172: 1932: 1809: 6603: 1080: 6706: 2067:"First Personalized Cancer Medicine Allows Patients with Deadly Form of Metastatic Melanoma to Live Significantly Longer" 6647: 5043: 4925: 4915: 3223: 2102: 1108: 1052: 481: 1112: 5993: 2380: 1009: 569: 6018: 3404: 2252:"Long-term outcomes in patients with relapsed or refractory hairy cell leukemia treated with vemurafenib monotherapy" 1971: 6756: 6751: 6632: 4458: 3529: 3378: 3127: 2629: 6013: 6741: 6540: 2854: 2720: 2433: 183: 6761: 4724: 4640: 4559: 4426: 4343: 2864: 2390: 982: 828: 4158: 1907: 430: 6791: 6324: 4071: 3946: 2360: 1729:"Phase I study of PLX4032: Proof of concept for V600E BRAF mutation as a therapeutic target in human cancer" 242: 6003: 2096: 608: 6796: 6608: 6224: 6128: 5988: 5748: 5167: 4153: 3791: 3232: 2715: 2444: 530: 6776: 6771: 6766: 6682: 4879: 4523: 4163: 3802: 2790: 2730: 2700: 2603: 2439: 2329: 784: 421: 1862:"Plexxikon Announces First Patient Dosed in Phase 3 Trial of PLX4032 (RG7204) for Metastatic Melanoma" 1051:. After good results in 2014, the combination was submitted to the European Medical Agency and the US 6622: 6008: 4940: 4889: 2645: 2540: 2377: 2097:"FDA approves first treatment for certain patients with Erdheim–Chester disease, a rare blood cancer" 1693: 1576: 1519: 1448: 1350: 1208: 1160: 5758: 3833: 585: 37: 5763: 5177: 4874: 4066: 3498: 2765: 2755: 2575: 1337:
Hatzivassiliou G, Song K, Yen I, Brandhuber BJ, Anderson DJ, Alvarado R, et al. (March 2010).
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Vemurafenib only works in melanoma patients whose cancer has a V600E BRAF mutation (that is, at
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Maverakis E, Cornelius LA, Bowen GM, Phan T, Patel FB, Fitzmaurice S, et al. (May 2015).
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Flaherty KT, Puzanov I, Kim KB, Ribas A, McArthur GA, Sosman JA, et al. (August 2010).
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Three mechanisms of resistance to vemurafenib (covering 40% of cases) have been discovered:
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Straussman R, Morikawa T, Shee K, Barzily-Rokni M, Qian ZR, Du J, et al. (July 2012).
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A trial combining vemurafenib and ipilimumab was stopped in April 2013 because of signs of
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Further trials are planned including a trial of vemurafenib co-administered with GDC-0973 (
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Diamond EL, Subbiah V, Lockhart AC, Blay JY, Puzanov I, Chau I, et al. (March 2018).
1565:"Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors" 1386:
Halaban R, Zhang W, Bacchiocchi A, Cheng E, Parisi F, Ariyan S, et al. (April 2010).
1197:"Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma" 1684:
Garber K (December 2009). "Cancer research. Melanoma drug vindicates targeted approach".
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Handa S, Lee JO, Derkach A, Stone RM, Saven A, Altman JK, et al. (December 2022).
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for "A Study of RO5185426 in Previously Treated Patients With Metastatic Melanoma" at
1437:"Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation" 28: 6730: 6366: 6279: 6208: 6178: 6113: 6023: 5977: 5853: 5783: 5728: 5717: 5202: 4910: 4593: 4498: 4390: 3664: 3554: 3516: 3493: 3425: 3420: 3410: 3186: 3182: 3170: 2977: 2760: 2725: 2545: 2525: 1403: 1195:
Bollag G, Hirth P, Tsai J, Zhang J, Ibrahim PN, Cho H, et al. (September 2010).
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Wilson TR, Fridlyand J, Yan Y, Penuel E, Burton L, Chan E, et al. (July 2012).
1339:"RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth" 1282: 6692: 6662: 6401: 6391: 6284: 6183: 6038: 5858: 5793: 5708: 5212: 5015: 4854: 4849: 4769: 4719: 4533: 4287: 4268: 4247: 4218: 3941: 3936: 3704: 3689: 3659: 3639: 3521: 3469: 3430: 3318: 3297: 3204: 3166: 3067: 3042: 3038: 2922: 2887: 2840: 2825: 2780: 2655: 2625: 2550: 2368: 2021: 978: 269: 264: 147: 2233: 1936: 1844: 1826: 1705: 1266: 6652: 6618: 6516: 6506: 6501: 6491: 6441: 6264: 6163: 5924: 5838: 5768: 5663: 5426: 5391: 5341: 5304: 5240: 5122: 5053: 5005: 4995: 4990: 4985: 4869: 4864: 4859: 4237: 4148: 4138: 4106: 4101: 4096: 4091: 4081: 4041: 4006: 3734: 3714: 3709: 3699: 3679: 3654: 3649: 3632: 3580: 3570: 3565: 3560: 3462: 3389: 3359: 3354: 3349: 3333: 3323: 3303: 3178: 3174: 3162: 3158: 3087: 2991: 2937: 2932: 2897: 2835: 2820: 2810: 2805: 2800: 2775: 2740: 2695: 2675: 2665: 2620: 2585: 2565: 2521: 2484: 2472: 2467: 2429: 2413: 2304: 2142: 1733:
2009 ASCO Annual Meeting Abstract, J Clin Oncol 27:15s, 2009 (suppl; abstr 9000)
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Nazarian R, Shi H, Wang Q, Kong X, Koya RC, Lee H, et al. (December 2010).
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approved vemurafenib as a monotherapy for the treatment of adults with BRAF
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In January 2015, trial results compared vemurafenib with the combination of
918: 906: 141: 20: 2322: 2285: 2160: 2013: 1792: 1713: 1606: 1549: 1478: 1421: 1372: 1323: 1274: 1238: 1774: 1314: 1297: 6667: 6386: 6043: 5643: 5633: 5613: 5548: 5517: 5486: 5450: 5356: 5346: 4693: 4173: 4116: 4026: 3986: 3489: 3253: 3057: 2996: 2952: 2912: 2882: 2635: 2499: 2495: 2420: 1097: 968: 922: 895: 804: 441: 1588: 1531: 1460: 1363: 1338: 1298:"Metastatic melanoma - a review of current and future treatment options" 1220: 450: 6642: 6063: 5528: 4930: 3891: 2593: 864: 396: 1189: 6555: 6219: 6108: 6033: 5738: 5733: 5157: 5152: 5106: 5102: 5098: 5094: 5090: 5086: 5082: 4734: 4273: 3951: 961: 941: 902: 521: 2005: 367:-(3-{pyridin-3-yl]carbonyl}-2,4-difluorophenyl)propane-1-sulfonamide 510: 6587: 6583: 6579: 6575: 6571: 6567: 6563: 6559: 6274: 6173: 5848: 5788: 5602: 5325: 5321: 5317: 5313: 4804: 4668: 4587: 4583: 4482: 4478: 4474: 4470: 4379: 4375: 4226: 3473: 3199: 3033: 2982: 2462: 1094: 693: 684: 557: 1958:"MEK/BRAF Inhibitor Combo Reduces Death by One-Third in Melanoma" 1487:"Researchers Uncover Drug-Resistance Mechanisms in BRAF Melanoma" 6058: 4664: 4660: 4656: 4652: 4648: 4644: 4579: 4575: 4571: 4567: 4563: 4466: 4462: 4454: 4450: 4446: 4442: 4438: 4434: 4430: 4371: 4367: 4363: 4359: 4355: 4351: 4347: 4299: 4295: 4291: 4257: 4222: 4203: 3588: 3374: 2872: 2598: 2580: 2570: 2530: 2398: 501: 319: 187: 178: 3764: 2333: 1830:
for "Safety Study of PLX4032 in Patients With Solid Tumors" at
1621:"BRIM-2 Upholds Benefits Emerging with Vemurafenib in Melanoma" 779: 332: 195: 1759:"Inhibition of mutated, activated BRAF in metastatic melanoma" 1086:
Vemurafenib was approved for use in Canada in February 2012.
2307:. In Pratt VM, McLeod HL, Rubinstein WS, et al. (eds.). 1111:(FDA) approved vemurafenib for the treatment of people with 574: 295: 227: 85: 70: 64: 716:
CCCS(=O)(=O)Nc1ccc(F)c(c1F)C(=O)c2cc3c2cc(cn3)c4ccc(Cl)cc4
1161:"Australian Product Information: Zelboraf® (vemurafenib)" 91: 79: 308: 975:
mutates, reactivating the normal BRAF survival pathway.
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Cancer cells begin to overexpress cell surface protein
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Pituitary adenylate cyclase-activating peptide (PACAP)
1864:(Press release). Plexxikon. 2010-01-08. Archived from 6704: 940:
position number 600 on the B-Raf protein, the normal
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Archived from 6638:Macrophage-stimulating protein (MSP; HLP, HGFLP) 2305:"Vemurafenib Therapy and BRAF and NRAS Genotype" 409: 4279:Heparin-binding EGF-like growth factor (HB-EGF) 3962:Heparin-binding EGF-like growth factor (HB-EGF) 384: 2237:for "Hairy Cell Leukemia with Vemurafebib" at 1180: 1178: 1176: 1174: 1030:study (for metastatic melanoma) were ongoing. 933:− if the B-Raf has the common V600E mutation. 200: 6690:Additional growth factor receptor modulators: 3776: 2345: 2315:National Center for Biotechnology Information 1155: 1153: 8: 5044:Insulin-like growth factor-2 (somatomedin A) 4926:Insulin-like growth factor-2 (somatomedin A) 4916:Insulin-like growth factor-1 (somatomedin C) 2207:"Hairy Cell Leukemia: Celebrating Progress?" 1894:Genetic Engineering & Biotechnology News 1491:Genetic Engineering & Biotechnology News 1115:(ECD), a rare type of histiocytic neoplasm. 19: 1896:. Mary Ann Liebert Publishers. 6 June 2011. 1104:, the most aggressive form of skin cancer. 964:, creating an alternative survival pathway. 5713: 5446: 4894: 4323: 3916: 3783: 3769: 3761: 2860: 2386: 2352: 2338: 2330: 1884: 1882: 778: 611: 588: 469: 6737:Antineoplastic and immunomodulating drugs 2275: 2150: 1802:"PLX4032: The Good News and the Bad News" 1782: 1596: 1539: 1468: 1411: 1362: 1313: 1228: 489: 6648:Migration-stimulating factor (MSF; PRG4) 6711: 3977:Transforming growth factor alpha (TGFα) 1149: 925:cell lines. Vemurafenib interrupts the 733: 713: 584: 449: 361: 160: 6551:Connective tissue growth factor (CTGF) 762: 602: 18: 6614:Hepatoma-derived growth factor (HDGF) 894:used for the treatment of late-stage 550: 529: 146: 7: 6782:Drugs developed by Hoffmann-La Roche 1392:Pigment Cell & Melanoma Research 556: 268: 1763:The New England Journal of Medicine 1665:"A Roller Coaster Chase for a Cure" 1022:trial for solid tumors (including 509: 400: 132:PLX4032, RG7204, PLX4720, RO5185426 14: 2036:"Notice of Decision for ZELBORAF" 1643:"Drug hope for advanced melanoma" 6714: 6633:Leukemia inhibitory factor (LIF) 1404:10.1111/j.1755-148X.2010.00685.x 651: 645: 642: 636: 54: 36: 27: 5801:Negative allosteric modulators: 2065:Hofland P (February 20, 2012). 2042:. 11 March 2012. Archived from 741:Key:GPXBXXGIAQBQNI-UHFFFAOYSA-N 6119:Gossypetin (3,5,7,8,3',4'-HHF) 5310:Platelet-derived growth factor 1994:Nature Reviews. Drug Discovery 663: 657: 630: 1: 6325:Placental growth factor (PGF) 1933:"Cobimetinib at exelixis.com" 1706:10.1126/science.326.5960.1619 1267:10.1158/1541-7786.MCR-07-2001 1083:to gain regulatory approval. 1081:fragment-based lead discovery 886:), sold under the brand name 6787:Drugs developed by Genentech 6609:Glia maturation factor (GMF) 5118:Glypromate (GPE, (1-3)IGF-1) 2175:"Getting close and personal" 2103:Food and Drug Administration 1800:Lowe D (September 9, 2010). 1131:Treating Hairy Cell Leukemia 1109:Food and Drug Administration 1053:Food and Drug Administration 898:. It is an inhibitor of the 2143:10.1001/jamaoncol.2017.5029 1625:Oncology & Biotech News 787:of B-Raf (rainbow colored, 6813: 6541:Colony-stimulating factors 6533:Additional growth factors: 2855:Tyrosine kinase inhibitors 2325:. Bookshelf ID: NBK447416. 2310:Medical Genetics Summaries 1974:(Press release). Genentech 1302:Acta Dermato-Venereologica 1165:Roche Products Pty Limited 1135:In 2012, a grant from the 785:Crystallographic structure 620:Chemical and physical data 5889:SNA-120 (pegylated K252a) 5061:(against IGF-1 and IGF-2) 5023:(against IGF-1 and IGF-2) 2721:Mirvetuximab soravtansine 1255:Molecular Cancer Research 1107:In November 2017, the US 1100:positive unresectable or 1066:for metastatic melanoma. 777: 770: 749: 724: 704: 352: 35: 26: 6747:4-Chlorophenyl compounds 4725:Hepatocyte growth factor 4284:Neuregulins (heregulins) 4215:Neuregulins (heregulins) 4159:Trastuzumab duocarmazine 3872:(against angiopoietin 2) 3866:(against angiopoietin 3) 2865:Receptor tyrosine kinase 2391:Receptor tyrosine kinase 2268:10.1182/blood.2022016183 1055:for marketing approval. 983:hepatocyte growth factor 829:protein kinase inhibitor 4072:Depatuxizumab mafodotin 2455:Others for solid tumors 2361:Targeted cancer therapy 1663:Harmon A (2010-02-21). 1113:Erdheim–Chester disease 6695:(neurotrophin mixture) 6683:Wnt signaling proteins 6364:Allosteric modulators: 6084:Norwogonin (5,7,8-THF) 4304:5 (tomoregulin, TMEFF) 4154:Trastuzumab deruxtecan 3792:Growth factor receptor 2716:Loncastuximab tesirine 2445:Trastuzumab deruxtecan 2231:Clinical trial number 1842:Clinical trial number 1824:Clinical trial number 1645:. BBC News. 2009-06-02 1089:In February 2012, the 1033:A phase III trial (vs 1010:phase I clinical study 6623:T-cell growth factors 4880:Telisotuzumab vedotin 4164:Trastuzumab emtansine 2791:Sacituzumab govitecan 2731:Moxetumomab pasudotox 2701:Inotuzumab ozogamicin 2604:Gemtuzumab ozogamicin 2440:Trastuzumab emtansine 2381:monoclonal antibodies 2365:antineoplastic agents 1775:10.1056/NEJMoa1002011 1315:10.2340/00015555-2035 931:B-Raf/MEK/ERK pathway 919:programmed cell death 905:and was developed by 5208:EVT-901 (SAR-127963) 4941:Mecasermin rinfabate 2646:Belantamab mafodotin 1493:. November 25, 2010. 16:Targeted cancer drug 3499:Denileukin diftitox 3161:(ALK, ROS1, NTRK), 2766:Polatuzumab vedotin 2756:Oportuzumab monatox 2181:. January 4, 2014. 1804:. In the Pipeline. 1698:2009Sci...326.1619G 1589:10.1038/nature11249 1581:2012Natur.487..505W 1532:10.1038/nature11183 1524:2012Natur.487..500S 1461:10.1038/nature09626 1453:2010Natur.468..973N 1364:10.1038/nature08833 1355:2010Natur.464..431H 1221:10.1038/nature09454 1213:2010Natur.467..596B 1137:Hairy cell leukemia 1102:metastatic melanoma 1091:European Commission 1070:Society and culture 917:Vemurafenib causes 913:Mechanism of action 824:Mechanism of action 328:(Prescription only) 304:(Prescription only) 23: 6374:Kinase inhibitors: 6237:Kinase inhibitors: 6136:Kinase inhibitors: 5811:Kinase inhibitors: 5626:Kinase inhibitors: 5586:Kinase inhibitors: 5567:Kinase inhibitors: 5536:Kinase inhibitors: 5505:Kinase inhibitors: 5474:Kinase inhibitors: 5334:Kinase inhibitors: 4948:Kinase inhibitors: 4742:Kinase inhibitors: 4531:Kinase inhibitors: 4524:Aprutumab ixadotin 4171:Kinase inhibitors: 3984:Kinase inhibitors: 3841:Kinase inhibitors: 3185:(ROS1, TRK, ALK), 2691:Enfortumab vedotin 2239:ClinicalTrials.gov 1850:ClinicalTrials.gov 1832:ClinicalTrials.gov 1670:The New York Times 6757:CYP2D6 inhibitors 6752:CYP1A2 inhibitors 6702: 6701: 6308: 6307: 6069:N-Acetylserotonin 5968:ReN-1820 (TrkAd5) 5597: 5596: 5131: 5130: 5076:Binding proteins: 4735:Dihexa (PNB-0408) 4702: 4701: 4313: 4312: 4227:6 (neuroglycan C) 3947:EGF (urogastrone) 3925: 3758: 3757: 3441: 3440: 2849: 2848: 2831:Tisotumab vedotin 2262:(25): 2663–2671. 2077:on April 11, 2012 1575:(7408): 505–509. 1518:(7408): 500–504. 1447:(7326): 973–977. 1349:(7287): 431–435. 1207:(7315): 596–599. 1024:colorectal cancer 877: 876: 859: 812:Biological target 761: 760: 695:Interactive image 570:CompTox Dashboard 336: 323: 311: 299: 231: 198: 181: 6804: 6742:B-Raf inhibitors 6719: 6718: 6717: 6710: 6514:Decoy receptors: 6487:Alacizumab pegol 5965:Decoy receptors: 5714: 5619:Stem cell factor 5560:Persephin (PSPN) 5498:Neurturin (NRTN) 5447: 5284:LEVI-04 (p75-Fc) 5281:Decoy receptors: 4895: 4324: 3923: 3917: 3785: 3778: 3771: 3762: 3472:peptide against 3045:(AXL, ALK, LTK)) 2861: 2671:Dinutuximab beta 2387: 2354: 2347: 2340: 2331: 2326: 2290: 2289: 2279: 2247: 2241: 2229: 2223: 2222: 2220: 2218: 2203: 2197: 2196: 2194: 2193: 2171: 2165: 2164: 2154: 2122: 2116: 2115: 2113: 2112: 2093: 2087: 2086: 2084: 2082: 2062: 2056: 2055: 2053: 2051: 2032: 2026: 2025: 1989: 1983: 1982: 1980: 1979: 1968: 1962: 1961: 1954: 1948: 1947: 1945: 1944: 1935:. Archived from 1929: 1923: 1922: 1920: 1919: 1910:. Archived from 1904: 1898: 1897: 1886: 1877: 1876: 1874: 1873: 1858: 1852: 1840: 1834: 1822: 1816: 1813: 1808:. Archived from 1796: 1786: 1754: 1748: 1747: 1745: 1744: 1735:. Archived from 1724: 1718: 1717: 1681: 1675: 1674: 1660: 1654: 1653: 1651: 1650: 1639: 1633: 1632: 1617: 1611: 1610: 1600: 1560: 1554: 1553: 1543: 1503: 1497: 1494: 1482: 1472: 1432: 1426: 1425: 1415: 1383: 1377: 1376: 1366: 1334: 1328: 1327: 1317: 1293: 1287: 1286: 1249: 1243: 1242: 1232: 1192: 1182: 1169: 1168: 1167:. 25 March 2020. 1157: 1018:In early 2010 a 873: 858: 852: 847: 782: 763: 757: 756: 697: 677: 665: 659: 653: 647: 644: 638: 632: 615: 604: 593: 592: 578: 576: 560: 554: 533: 513: 493: 473: 453: 433: 413: 403: 402: 388: 334: 331: 321: 318: 310: 307: 297: 294: 272: 229: 226: 208: 197: 194: 191: 180: 177: 164: 150: 110: 106: 101: 100: 97: 96: 93: 90: 87: 84: 81: 78: 75: 72: 69: 66: 63: 60: 40: 31: 24: 22: 6812: 6811: 6807: 6806: 6805: 6803: 6802: 6801: 6762:CYP3A4 inducers 6727: 6726: 6725: 6715: 6713: 6705: 6703: 6698: 6643:Midkine (NEGF2) 6521: 6304: 6203: 5972: 5910:ABT-110 (PG110) 5703: 5683: 5593: 5574: 5543: 5512: 5481: 5436: 5288: 5226:ABT-110 (PG110) 5127: 5064: 5026: 4884: 4698: 4679: 4619: 4616:(against FGF23) 4538: 4405: 4309: 4252: 4198: 4111: 3922: 3906: 3875: 3797: 3789: 3759: 3754: 3608:Pi3K inhibitors 3506:mTOR inhibitors 3437: 3218: 3189:(VEGFR, FGFR), 2845: 2609: 2490: 2450: 2372: 2358: 2303:Dean L (2017). 2302: 2299: 2297:Further reading 2294: 2293: 2249: 2248: 2244: 2230: 2226: 2216: 2214: 2213:. July 29, 2022 2205: 2204: 2200: 2191: 2189: 2173: 2172: 2168: 2124: 2123: 2119: 2110: 2108: 2107:(Press release) 2095: 2094: 2090: 2080: 2078: 2064: 2063: 2059: 2049: 2047: 2034: 2033: 2029: 2006:10.1038/nrd3847 2000:(11): 873–886. 1991: 1990: 1986: 1977: 1975: 1970: 1969: 1965: 1956: 1955: 1951: 1942: 1940: 1931: 1930: 1926: 1917: 1915: 1906: 1905: 1901: 1888: 1887: 1880: 1871: 1869: 1860: 1859: 1855: 1841: 1837: 1823: 1819: 1799: 1756: 1755: 1751: 1742: 1740: 1726: 1725: 1721: 1683: 1682: 1678: 1662: 1661: 1657: 1648: 1646: 1641: 1640: 1636: 1631:(7). July 2011. 1619: 1618: 1614: 1562: 1561: 1557: 1505: 1504: 1500: 1485: 1434: 1433: 1429: 1385: 1384: 1380: 1336: 1335: 1331: 1295: 1294: 1290: 1251: 1250: 1246: 1194: 1184: 1183: 1172: 1159: 1158: 1151: 1146: 1133: 1121: 1077: 1072: 1006: 992: 954: 944:is replaced by 915: 869: 854: 848: 801:Therapeutic use 796: 752: 750: 745: 742: 737: 732: 731: 720: 717: 712: 711: 700: 675: 662: 656: 650: 641: 635: 596: 572: 564: 536: 516: 496: 476: 456: 436: 416: 399: 391: 371: 368: 360: 359: 343: 276: 244: 237: 218: 211: 108: 104: 57: 53: 17: 12: 11: 5: 6810: 6808: 6800: 6799: 6794: 6792:Daiichi Sankyo 6789: 6784: 6779: 6774: 6769: 6764: 6759: 6754: 6749: 6744: 6739: 6729: 6728: 6724: 6723: 6700: 6699: 6697: 6696: 6686: 6685: 6680: 6673:Thrombopoietin 6670: 6665: 6660: 6655: 6650: 6645: 6640: 6635: 6630: 6616: 6611: 6606: 6601: 6594:Erythropoietin 6591: 6553: 6548: 6538: 6536:Adrenomedullin 6529: 6527: 6523: 6522: 6520: 6519: 6510: 6509: 6504: 6499: 6494: 6489: 6480: 6479: 6474: 6469: 6464: 6459: 6454: 6449: 6444: 6439: 6434: 6429: 6424: 6419: 6414: 6409: 6404: 6399: 6394: 6389: 6384: 6379: 6370: 6369: 6360: 6359: 6337: 6332: 6327: 6318: 6316: 6310: 6309: 6306: 6305: 6303: 6302: 6297: 6292: 6287: 6282: 6277: 6272: 6267: 6262: 6257: 6252: 6247: 6242: 6233: 6232: 6227: 6222: 6213: 6211: 6205: 6204: 6202: 6201: 6196: 6191: 6186: 6181: 6176: 6171: 6166: 6161: 6156: 6151: 6146: 6141: 6132: 6131: 6122: 6121: 6116: 6111: 6102: 6101: 6096: 6091: 6086: 6081: 6076: 6071: 6066: 6061: 6056: 6051: 6046: 6041: 6036: 6031: 6026: 6021: 6016: 6011: 6006: 6001: 5999:4'-DMA-7,8-DHF 5996: 5991: 5982: 5980: 5974: 5973: 5971: 5970: 5961: 5960: 5948: 5947: 5942: 5937: 5932: 5927: 5922: 5917: 5912: 5893: 5892: 5886: 5881: 5876: 5871: 5866: 5861: 5856: 5851: 5846: 5841: 5836: 5831: 5826: 5821: 5816: 5807: 5806: 5797: 5796: 5791: 5786: 5781: 5772: 5771: 5766: 5761: 5759:Gambogic amide 5756: 5751: 5746: 5741: 5736: 5731: 5722: 5720: 5711: 5705: 5704: 5702: 5701: 5693: 5691: 5685: 5684: 5682: 5681: 5676: 5671: 5666: 5661: 5656: 5651: 5646: 5641: 5636: 5631: 5622: 5621: 5616: 5607: 5605: 5599: 5598: 5595: 5594: 5592: 5591: 5582: 5580: 5576: 5575: 5573: 5572: 5563: 5562: 5553: 5551: 5545: 5544: 5542: 5541: 5532: 5531: 5529:Artemin (ARTN) 5522: 5520: 5514: 5513: 5511: 5510: 5501: 5500: 5491: 5489: 5483: 5482: 5480: 5479: 5470: 5469: 5464: 5455: 5453: 5444: 5438: 5437: 5435: 5434: 5429: 5424: 5415: 5414: 5409: 5404: 5399: 5394: 5389: 5384: 5379: 5374: 5369: 5364: 5359: 5354: 5349: 5344: 5339: 5330: 5329: 5307: 5298: 5296: 5290: 5289: 5287: 5286: 5277: 5276: 5264: 5263: 5258: 5253: 5248: 5243: 5238: 5233: 5228: 5216: 5215: 5210: 5205: 5200: 5191: 5190: 5185: 5180: 5175: 5170: 5165: 5160: 5155: 5150: 5141: 5139: 5133: 5132: 5129: 5128: 5126: 5125: 5120: 5111: 5110: 5072: 5070: 5066: 5065: 5063: 5062: 5056: 5047: 5046: 5036: 5034: 5028: 5027: 5025: 5024: 5018: 5013: 5008: 5003: 4998: 4993: 4988: 4983: 4974: 4973: 4968: 4963: 4958: 4953: 4944: 4943: 4938: 4933: 4928: 4923: 4918: 4913: 4903: 4901: 4892: 4886: 4885: 4883: 4882: 4877: 4872: 4867: 4862: 4857: 4852: 4843: 4842: 4837: 4832: 4827: 4822: 4817: 4812: 4807: 4802: 4797: 4792: 4787: 4782: 4777: 4772: 4767: 4762: 4757: 4752: 4747: 4738: 4737: 4728: 4727: 4722: 4712: 4710: 4704: 4703: 4700: 4699: 4697: 4696: 4687: 4685: 4681: 4680: 4678: 4677: 4672: 4638: 4629: 4627: 4621: 4620: 4618: 4617: 4607: 4606: 4601: 4596: 4591: 4557: 4548: 4546: 4540: 4539: 4537: 4536: 4527: 4526: 4521: 4512: 4511: 4506: 4501: 4496: 4491: 4486: 4424: 4415: 4413: 4407: 4406: 4404: 4403: 4398: 4393: 4388: 4383: 4341: 4332: 4330: 4321: 4315: 4314: 4311: 4310: 4308: 4307: 4281: 4276: 4271: 4262: 4260: 4254: 4253: 4251: 4250: 4245: 4240: 4231: 4230: 4208: 4206: 4200: 4199: 4197: 4196: 4191: 4186: 4181: 4176: 4167: 4166: 4161: 4156: 4151: 4146: 4141: 4132: 4131: 4121: 4119: 4113: 4112: 4110: 4109: 4104: 4099: 4094: 4089: 4084: 4079: 4074: 4069: 4064: 4055: 4054: 4049: 4044: 4039: 4034: 4029: 4024: 4019: 4014: 4009: 4004: 3999: 3994: 3989: 3980: 3979: 3974: 3969: 3964: 3959: 3954: 3949: 3944: 3939: 3929: 3927: 3914: 3908: 3907: 3905: 3904: 3899: 3894: 3885: 3883: 3877: 3876: 3874: 3873: 3867: 3857: 3856: 3851: 3846: 3837: 3836: 3834:Angiopoietin 3 3831: 3829:Angiopoietin 2 3822: 3821: 3819:Angiopoietin 4 3816: 3814:Angiopoietin 1 3807: 3805: 3799: 3798: 3790: 3788: 3787: 3780: 3773: 3765: 3756: 3755: 3753: 3752: 3747: 3742: 3737: 3732: 3727: 3722: 3717: 3712: 3707: 3702: 3697: 3692: 3687: 3682: 3677: 3672: 3667: 3662: 3657: 3652: 3647: 3642: 3637: 3636: 3635: 3630: 3625: 3620: 3615: 3605: 3604: 3603: 3598: 3585: 3584: 3583: 3578: 3573: 3568: 3563: 3555:CDK inhibitors 3551: 3550: 3549: 3544: 3539: 3526: 3525: 3524: 3519: 3514: 3502: 3486: 3466: 3454:fusion protein 3449: 3447: 3443: 3442: 3439: 3438: 3436: 3435: 3434: 3433: 3428: 3423: 3418: 3413: 3400: 3399: 3398: 3397: 3392: 3387: 3370: 3369: 3368: 3367: 3362: 3357: 3352: 3339: 3338: 3337: 3336: 3331: 3326: 3321: 3316: 3311: 3306: 3293: 3292: 3286: 3274: 3273: 3272: 3271: 3266: 3261: 3256: 3251: 3246: 3241: 3228: 3226: 3220: 3219: 3217: 3216: 3195: 3194: 3193:(VEGFR, EGFR). 3149: 3148: 3147: 3146: 3141: 3136: 3123: 3122: 3121: 3120: 3115: 3110: 3105: 3100: 3095: 3090: 3085: 3080: 3075: 3070: 3065: 3060: 3047: 3046: 3030: 3024: 3019: 3014: 3009: 3004: 2999: 2994: 2974: 2973: 2972: 2971: 2966: 2961: 2951:HER1/EGFR and 2947: 2946: 2940: 2935: 2930: 2925: 2920: 2915: 2910: 2905: 2900: 2895: 2890: 2885: 2869: 2867: 2858: 2851: 2850: 2847: 2846: 2844: 2843: 2838: 2833: 2828: 2823: 2818: 2813: 2808: 2803: 2798: 2793: 2788: 2783: 2778: 2773: 2768: 2763: 2758: 2753: 2748: 2743: 2738: 2733: 2728: 2723: 2718: 2713: 2708: 2703: 2698: 2693: 2688: 2683: 2678: 2673: 2668: 2663: 2658: 2653: 2648: 2643: 2638: 2633: 2630:+hyaluronidase 2623: 2617: 2615: 2611: 2610: 2608: 2607: 2590: 2589: 2563: 2558: 2553: 2548: 2543: 2538: 2504: 2502: 2492: 2491: 2489: 2488: 2476: 2470: 2458: 2456: 2452: 2451: 2449: 2448: 2442: 2437: 2434:+hyaluronidase 2417: 2411: 2395: 2393: 2384: 2374: 2373: 2359: 2357: 2356: 2349: 2342: 2334: 2328: 2327: 2298: 2295: 2292: 2291: 2242: 2224: 2198: 2166: 2137:(3): 384–388. 2117: 2088: 2057: 2027: 1984: 1963: 1949: 1924: 1899: 1878: 1853: 1835: 1817: 1815: 1814: 1812:on 2010-09-11. 1769:(9): 809–819. 1749: 1719: 1692:(5960): 1619. 1676: 1655: 1634: 1612: 1555: 1498: 1496: 1495: 1427: 1398:(2): 190–200. 1378: 1329: 1308:(5): 516–524. 1288: 1261:(5): 751–759. 1244: 1170: 1148: 1147: 1145: 1142: 1132: 1129: 1125:liver toxicity 1120: 1117: 1076: 1073: 1071: 1068: 1005: 1002: 991: 988: 987: 986: 976: 965: 953: 950: 927:B-Raf/MEK step 914: 911: 875: 874: 867: 861: 860: 844: 837: 836: 835:External links 832: 831: 826: 820: 819: 814: 808: 807: 802: 798: 797: 783: 775: 774: 772:Drug mechanism 768: 767: 759: 758: 747: 746: 744: 743: 740: 738: 735: 727: 726: 725: 722: 721: 719: 718: 715: 707: 706: 705: 702: 701: 699: 698: 690: 688: 680: 679: 673: 667: 666: 660: 654: 648: 639: 633: 628: 622: 621: 617: 616: 606: 598: 597: 595: 594: 586:DTXSID50238710 581: 579: 566: 565: 563: 562: 546: 544: 538: 537: 535: 534: 526: 524: 518: 517: 515: 514: 506: 504: 498: 497: 495: 494: 486: 484: 478: 477: 475: 474: 466: 464: 458: 457: 455: 454: 446: 444: 438: 437: 435: 434: 426: 424: 418: 417: 415: 414: 406: 404: 393: 392: 390: 389: 381: 379: 373: 372: 370: 369: 363: 355: 354: 353: 350: 349: 345: 344: 342: 341: 329: 316: 305: 291: 289: 283: 282: 278: 277: 275: 274: 261: 259: 253: 252: 247: 245:administration 239: 238: 236: 235: 233: 223: 221: 213: 212: 210: 209: 192: 174: 172: 166: 165: 158: 152: 151: 144: 134: 133: 130: 126: 125: 122: 116: 115: 51: 47: 46: 42: 41: 33: 32: 15: 13: 10: 9: 6: 4: 3: 2: 6809: 6798: 6797:Diarylketones 6795: 6793: 6790: 6788: 6785: 6783: 6780: 6778: 6775: 6773: 6770: 6768: 6765: 6763: 6760: 6758: 6755: 6753: 6750: 6748: 6745: 6743: 6740: 6738: 6735: 6734: 6732: 6722: 6712: 6708: 6694: 6691: 6688: 6687: 6684: 6681: 6678: 6674: 6671: 6669: 6666: 6664: 6661: 6659: 6656: 6654: 6651: 6649: 6646: 6644: 6641: 6639: 6636: 6634: 6631: 6628: 6624: 6620: 6617: 6615: 6612: 6610: 6607: 6605: 6602: 6599: 6595: 6592: 6589: 6585: 6581: 6577: 6573: 6569: 6565: 6561: 6557: 6554: 6552: 6549: 6546: 6542: 6539: 6537: 6534: 6531: 6530: 6528: 6524: 6518: 6515: 6512: 6511: 6508: 6505: 6503: 6500: 6498: 6495: 6493: 6490: 6488: 6485: 6482: 6481: 6478: 6475: 6473: 6470: 6468: 6465: 6463: 6460: 6458: 6455: 6453: 6450: 6448: 6445: 6443: 6440: 6438: 6435: 6433: 6430: 6428: 6425: 6423: 6420: 6418: 6415: 6413: 6410: 6408: 6405: 6403: 6400: 6398: 6395: 6393: 6390: 6388: 6385: 6383: 6380: 6378: 6375: 6372: 6371: 6368: 6367:Cyclotraxin B 6365: 6362: 6361: 6357: 6353: 6349: 6345: 6341: 6338: 6336: 6333: 6331: 6328: 6326: 6323: 6320: 6319: 6317: 6315: 6311: 6301: 6298: 6296: 6293: 6291: 6288: 6286: 6283: 6281: 6280:Larotrectinib 6278: 6276: 6273: 6271: 6268: 6266: 6263: 6261: 6258: 6256: 6253: 6251: 6248: 6246: 6243: 6241: 6238: 6235: 6234: 6231: 6228: 6226: 6223: 6221: 6218: 6215: 6214: 6212: 6210: 6206: 6200: 6197: 6195: 6192: 6190: 6187: 6185: 6182: 6180: 6179:Larotrectinib 6177: 6175: 6172: 6170: 6167: 6165: 6162: 6160: 6157: 6155: 6152: 6150: 6147: 6145: 6142: 6140: 6137: 6134: 6133: 6130: 6127: 6124: 6123: 6120: 6117: 6115: 6114:Cyclotraxin B 6112: 6110: 6107: 6104: 6103: 6100: 6097: 6095: 6092: 6090: 6087: 6085: 6082: 6080: 6077: 6075: 6072: 6070: 6067: 6065: 6062: 6060: 6057: 6055: 6052: 6050: 6047: 6045: 6042: 6040: 6037: 6035: 6032: 6030: 6027: 6025: 6024:Amitriptyline 6022: 6020: 6017: 6015: 6012: 6010: 6007: 6005: 6002: 6000: 5997: 5995: 5992: 5990: 5987: 5984: 5983: 5981: 5979: 5975: 5969: 5966: 5963: 5962: 5959: 5956: 5953: 5950: 5949: 5946: 5943: 5941: 5938: 5936: 5933: 5931: 5928: 5926: 5923: 5921: 5918: 5916: 5913: 5911: 5908: 5904: 5901: 5900:Against TrkA: 5898: 5895: 5894: 5890: 5887: 5885: 5882: 5880: 5877: 5875: 5872: 5870: 5867: 5865: 5862: 5860: 5857: 5855: 5854:Larotrectinib 5852: 5850: 5847: 5845: 5842: 5840: 5837: 5835: 5832: 5830: 5827: 5825: 5822: 5820: 5817: 5815: 5812: 5809: 5808: 5805: 5802: 5799: 5798: 5795: 5792: 5790: 5787: 5785: 5784:Dexamethasone 5782: 5780: 5777: 5774: 5773: 5770: 5767: 5765: 5762: 5760: 5757: 5755: 5752: 5750: 5747: 5745: 5742: 5740: 5737: 5735: 5732: 5730: 5729:Amitriptyline 5727: 5724: 5723: 5721: 5719: 5715: 5712: 5710: 5706: 5699: 5695: 5694: 5692: 5690: 5686: 5680: 5677: 5675: 5672: 5670: 5667: 5665: 5662: 5660: 5657: 5655: 5652: 5650: 5647: 5645: 5642: 5640: 5637: 5635: 5632: 5630: 5627: 5624: 5623: 5620: 5617: 5615: 5612: 5609: 5608: 5606: 5604: 5600: 5590: 5587: 5584: 5583: 5581: 5577: 5571: 5568: 5565: 5564: 5561: 5558: 5555: 5554: 5552: 5550: 5546: 5540: 5537: 5534: 5533: 5530: 5527: 5524: 5523: 5521: 5519: 5515: 5509: 5506: 5503: 5502: 5499: 5496: 5493: 5492: 5490: 5488: 5484: 5478: 5475: 5472: 5471: 5468: 5465: 5463: 5460: 5457: 5456: 5454: 5452: 5448: 5445: 5443: 5439: 5433: 5430: 5428: 5425: 5423: 5420: 5417: 5416: 5413: 5410: 5408: 5405: 5403: 5400: 5398: 5395: 5393: 5390: 5388: 5385: 5383: 5380: 5378: 5375: 5373: 5370: 5368: 5365: 5363: 5360: 5358: 5355: 5353: 5350: 5348: 5345: 5343: 5340: 5338: 5335: 5332: 5331: 5327: 5323: 5319: 5315: 5311: 5308: 5306: 5303: 5300: 5299: 5297: 5295: 5291: 5285: 5282: 5279: 5278: 5275: 5272: 5269: 5266: 5265: 5262: 5259: 5257: 5254: 5252: 5249: 5247: 5244: 5242: 5239: 5237: 5234: 5232: 5229: 5227: 5224: 5221: 5218: 5217: 5214: 5211: 5209: 5206: 5204: 5203:Dexamethasone 5201: 5199: 5196: 5193: 5192: 5189: 5186: 5184: 5181: 5179: 5176: 5174: 5171: 5169: 5166: 5164: 5161: 5159: 5156: 5154: 5151: 5149: 5146: 5143: 5142: 5140: 5138: 5134: 5124: 5121: 5119: 5116: 5113: 5112: 5108: 5104: 5100: 5096: 5092: 5088: 5084: 5080: 5077: 5074: 5073: 5071: 5067: 5060: 5057: 5055: 5052: 5049: 5048: 5045: 5041: 5038: 5037: 5035: 5033: 5029: 5022: 5019: 5017: 5014: 5012: 5009: 5007: 5004: 5002: 4999: 4997: 4994: 4992: 4989: 4987: 4984: 4982: 4979: 4976: 4975: 4972: 4969: 4967: 4964: 4962: 4959: 4957: 4954: 4952: 4949: 4946: 4945: 4942: 4939: 4937: 4934: 4932: 4929: 4927: 4924: 4922: 4919: 4917: 4914: 4912: 4911:des(1-3)IGF-1 4908: 4905: 4904: 4902: 4900: 4896: 4893: 4891: 4887: 4881: 4878: 4876: 4875:Telisotuzumab 4873: 4871: 4868: 4866: 4863: 4861: 4858: 4856: 4853: 4851: 4848: 4845: 4844: 4841: 4838: 4836: 4833: 4831: 4828: 4826: 4823: 4821: 4818: 4816: 4813: 4811: 4808: 4806: 4803: 4801: 4798: 4796: 4793: 4791: 4788: 4786: 4783: 4781: 4778: 4776: 4773: 4771: 4768: 4766: 4763: 4761: 4758: 4756: 4753: 4751: 4748: 4746: 4743: 4740: 4739: 4736: 4733: 4732:Potentiators: 4730: 4729: 4726: 4723: 4721: 4717: 4714: 4713: 4711: 4709: 4705: 4695: 4692: 4689: 4688: 4686: 4682: 4676: 4673: 4670: 4666: 4662: 4658: 4654: 4650: 4646: 4642: 4639: 4637: 4634: 4631: 4630: 4628: 4626: 4622: 4615: 4612: 4609: 4608: 4605: 4602: 4600: 4597: 4595: 4594:Selpercatinib 4592: 4589: 4585: 4581: 4577: 4573: 4569: 4565: 4561: 4558: 4556: 4553: 4550: 4549: 4547: 4545: 4541: 4535: 4532: 4529: 4528: 4525: 4522: 4520: 4517: 4514: 4513: 4510: 4507: 4505: 4502: 4500: 4499:Selpercatinib 4497: 4495: 4492: 4490: 4487: 4484: 4480: 4476: 4472: 4468: 4464: 4460: 4456: 4452: 4448: 4444: 4440: 4436: 4432: 4428: 4425: 4423: 4420: 4417: 4416: 4414: 4412: 4408: 4402: 4399: 4397: 4394: 4392: 4391:Selpercatinib 4389: 4387: 4384: 4381: 4377: 4373: 4369: 4365: 4361: 4357: 4353: 4349: 4345: 4342: 4340: 4337: 4334: 4333: 4331: 4329: 4325: 4322: 4320: 4316: 4305: 4301: 4297: 4293: 4289: 4285: 4282: 4280: 4277: 4275: 4272: 4270: 4267: 4264: 4263: 4261: 4259: 4255: 4249: 4246: 4244: 4241: 4239: 4236: 4233: 4232: 4228: 4224: 4220: 4216: 4213: 4210: 4209: 4207: 4205: 4201: 4195: 4192: 4190: 4187: 4185: 4182: 4180: 4177: 4175: 4172: 4169: 4168: 4165: 4162: 4160: 4157: 4155: 4152: 4150: 4147: 4145: 4142: 4140: 4137: 4134: 4133: 4130: 4126: 4123: 4122: 4120: 4118: 4114: 4108: 4105: 4103: 4100: 4098: 4095: 4093: 4090: 4088: 4085: 4083: 4080: 4078: 4075: 4073: 4070: 4068: 4067:Depatuxizumab 4065: 4063: 4060: 4057: 4056: 4053: 4050: 4048: 4045: 4043: 4040: 4038: 4035: 4033: 4030: 4028: 4025: 4023: 4020: 4018: 4015: 4013: 4010: 4008: 4005: 4003: 4000: 3998: 3995: 3993: 3990: 3988: 3985: 3982: 3981: 3978: 3975: 3973: 3970: 3968: 3965: 3963: 3960: 3958: 3955: 3953: 3950: 3948: 3945: 3943: 3940: 3938: 3934: 3931: 3930: 3928: 3926: 3918: 3915: 3913: 3909: 3903: 3900: 3898: 3895: 3893: 3890: 3887: 3886: 3884: 3882: 3878: 3871: 3868: 3865: 3862: 3859: 3858: 3855: 3852: 3850: 3847: 3845: 3842: 3839: 3838: 3835: 3832: 3830: 3827: 3824: 3823: 3820: 3817: 3815: 3812: 3809: 3808: 3806: 3804: 3800: 3796: 3793: 3786: 3781: 3779: 3774: 3772: 3767: 3766: 3763: 3751: 3748: 3746: 3743: 3741: 3738: 3736: 3733: 3731: 3728: 3726: 3723: 3721: 3718: 3716: 3713: 3711: 3708: 3706: 3703: 3701: 3698: 3696: 3693: 3691: 3688: 3686: 3683: 3681: 3678: 3676: 3673: 3671: 3668: 3666: 3665:Larotrectinib 3663: 3661: 3658: 3656: 3653: 3651: 3648: 3646: 3643: 3641: 3638: 3634: 3631: 3629: 3626: 3624: 3621: 3619: 3616: 3614: 3611: 3610: 3609: 3606: 3602: 3599: 3597: 3594: 3593: 3592: 3590: 3586: 3582: 3579: 3577: 3574: 3572: 3569: 3567: 3564: 3562: 3559: 3558: 3557: 3556: 3552: 3548: 3545: 3543: 3540: 3538: 3535: 3534: 3533: 3531: 3527: 3523: 3520: 3518: 3517:Ridaforolimus 3515: 3513: 3510: 3509: 3508: 3507: 3503: 3500: 3496: 3495: 3491: 3487: 3484: 3480: 3479: 3475: 3471: 3467: 3464: 3460: 3459: 3455: 3451: 3450: 3448: 3444: 3432: 3429: 3427: 3426:Pirtobrutinib 3424: 3422: 3421:Orelabrutinib 3419: 3417: 3414: 3412: 3411:Acalabrutinib 3409: 3408: 3407: 3406: 3402: 3401: 3396: 3393: 3391: 3388: 3386: 3383: 3382: 3381: 3380: 3376: 3372: 3371: 3366: 3363: 3361: 3358: 3356: 3353: 3351: 3348: 3347: 3346: 3345: 3341: 3340: 3335: 3332: 3330: 3327: 3325: 3322: 3320: 3317: 3315: 3312: 3310: 3307: 3305: 3302: 3301: 3300: 3299: 3295: 3294: 3290: 3287: 3285: 3281: 3280: 3276: 3275: 3270: 3267: 3265: 3262: 3260: 3257: 3255: 3252: 3250: 3247: 3245: 3242: 3240: 3237: 3236: 3235: 3234: 3230: 3229: 3227: 3225: 3221: 3214: 3210: 3206: 3203: 3201: 3197: 3196: 3192: 3188: 3187:Selpercatinib 3184: 3183:Repotrectinib 3180: 3176: 3172: 3171:Larotrectinib 3168: 3164: 3160: 3157: 3155: 3151: 3150: 3145: 3142: 3140: 3137: 3135: 3132: 3131: 3130: 3129: 3125: 3124: 3119: 3116: 3114: 3111: 3109: 3106: 3104: 3101: 3099: 3096: 3094: 3091: 3089: 3086: 3084: 3081: 3079: 3076: 3074: 3071: 3069: 3066: 3064: 3061: 3059: 3056: 3055: 3054: 3053: 3049: 3048: 3044: 3040: 3036: 3035: 3031: 3028: 3025: 3023: 3020: 3018: 3015: 3013: 3010: 3008: 3005: 3003: 3000: 2998: 2995: 2993: 2989: 2988: 2984: 2979: 2978:RTK class III 2976: 2975: 2970: 2967: 2965: 2962: 2960: 2957: 2956: 2955: 2954: 2949: 2948: 2944: 2941: 2939: 2936: 2934: 2931: 2929: 2926: 2924: 2921: 2919: 2916: 2914: 2911: 2909: 2906: 2904: 2901: 2899: 2896: 2894: 2891: 2889: 2886: 2884: 2880: 2879: 2874: 2871: 2870: 2868: 2866: 2862: 2859: 2856: 2852: 2842: 2839: 2837: 2834: 2832: 2829: 2827: 2824: 2822: 2819: 2817: 2814: 2812: 2809: 2807: 2804: 2802: 2799: 2797: 2794: 2792: 2789: 2787: 2784: 2782: 2779: 2777: 2774: 2772: 2769: 2767: 2764: 2762: 2761:Pembrolizumab 2759: 2757: 2754: 2752: 2749: 2747: 2744: 2742: 2739: 2737: 2734: 2732: 2729: 2727: 2726:Mogamulizumab 2724: 2722: 2719: 2717: 2714: 2712: 2709: 2707: 2704: 2702: 2699: 2697: 2694: 2692: 2689: 2687: 2684: 2682: 2679: 2677: 2674: 2672: 2669: 2667: 2664: 2662: 2659: 2657: 2654: 2652: 2649: 2647: 2644: 2642: 2639: 2637: 2634: 2631: 2627: 2624: 2622: 2619: 2618: 2616: 2612: 2605: 2601: 2600: 2595: 2592: 2591: 2587: 2583: 2582: 2577: 2573: 2572: 2567: 2564: 2562: 2559: 2557: 2554: 2552: 2549: 2547: 2546:Mosunetuzumab 2544: 2542: 2539: 2537: 2533: 2532: 2527: 2526:Mosunetuzumab 2523: 2519: 2515: 2514: 2509: 2506: 2505: 2503: 2501: 2497: 2493: 2486: 2482: 2481: 2477: 2474: 2471: 2469: 2465: 2464: 2460: 2459: 2457: 2453: 2446: 2443: 2441: 2438: 2435: 2431: 2427: 2423: 2422: 2418: 2415: 2412: 2410: 2406: 2405: 2400: 2397: 2396: 2394: 2392: 2388: 2385: 2382: 2379: 2375: 2370: 2366: 2362: 2355: 2350: 2348: 2343: 2341: 2336: 2335: 2332: 2324: 2320: 2316: 2312: 2311: 2306: 2301: 2300: 2296: 2287: 2283: 2278: 2273: 2269: 2265: 2261: 2257: 2253: 2246: 2243: 2240: 2236: 2235: 2228: 2225: 2212: 2208: 2202: 2199: 2188: 2184: 2180: 2179:The Economist 2176: 2170: 2167: 2162: 2158: 2153: 2148: 2144: 2140: 2136: 2132: 2131:JAMA Oncology 2128: 2121: 2118: 2106: 2104: 2098: 2092: 2089: 2076: 2072: 2068: 2061: 2058: 2046:on 2 May 2012 2045: 2041: 2040:Health Canada 2037: 2031: 2028: 2023: 2019: 2015: 2011: 2007: 2003: 1999: 1995: 1988: 1985: 1973: 1967: 1964: 1959: 1953: 1950: 1939:on 2015-02-04 1938: 1934: 1928: 1925: 1914:on 2022-01-11 1913: 1909: 1903: 1900: 1895: 1891: 1885: 1883: 1879: 1868:on 2020-12-01 1867: 1863: 1857: 1854: 1851: 1847: 1846: 1839: 1836: 1833: 1829: 1828: 1821: 1818: 1811: 1807: 1803: 1798: 1797: 1794: 1790: 1785: 1780: 1776: 1772: 1768: 1764: 1760: 1753: 1750: 1739:on 2013-01-27 1738: 1734: 1730: 1723: 1720: 1715: 1711: 1707: 1703: 1699: 1695: 1691: 1687: 1680: 1677: 1672: 1671: 1666: 1659: 1656: 1644: 1638: 1635: 1630: 1626: 1622: 1616: 1613: 1608: 1604: 1599: 1594: 1590: 1586: 1582: 1578: 1574: 1570: 1566: 1559: 1556: 1551: 1547: 1542: 1537: 1533: 1529: 1525: 1521: 1517: 1513: 1509: 1502: 1499: 1492: 1488: 1484: 1483: 1480: 1476: 1471: 1466: 1462: 1458: 1454: 1450: 1446: 1442: 1438: 1431: 1428: 1423: 1419: 1414: 1409: 1405: 1401: 1397: 1393: 1389: 1382: 1379: 1374: 1370: 1365: 1360: 1356: 1352: 1348: 1344: 1340: 1333: 1330: 1325: 1321: 1316: 1311: 1307: 1303: 1299: 1292: 1289: 1284: 1280: 1276: 1272: 1268: 1264: 1260: 1256: 1248: 1245: 1240: 1236: 1231: 1226: 1222: 1218: 1214: 1210: 1206: 1202: 1198: 1191: 1187: 1181: 1179: 1177: 1175: 1171: 1166: 1162: 1156: 1154: 1150: 1143: 1141: 1138: 1130: 1128: 1126: 1118: 1116: 1114: 1110: 1105: 1103: 1099: 1096: 1092: 1087: 1084: 1082: 1074: 1069: 1067: 1065: 1061: 1056: 1054: 1050: 1049:MEK-inhibitor 1046: 1041: 1038: 1036: 1031: 1029: 1025: 1021: 1016: 1013: 1011: 1003: 1001: 998: 989: 984: 981:secretion of 980: 977: 974: 970: 966: 963: 959: 958: 957: 951: 949: 947: 946:glutamic acid 943: 939: 934: 932: 928: 924: 920: 912: 910: 908: 904: 901: 897: 893: 889: 885: 881: 872: 868: 866: 862: 857: 851: 845: 842: 838: 833: 830: 827: 825: 821: 818: 815: 813: 809: 806: 803: 799: 794: 790: 786: 781: 776: 773: 769: 764: 755: 748: 739: 734: 730: 723: 714: 710: 703: 696: 692: 691: 689: 686: 681: 674: 672: 668: 629: 627: 623: 618: 614: 610: 607: 605: 603:ECHA InfoCard 599: 591: 587: 583: 582: 580: 571: 567: 559: 558:RCSB PDB 553: 548: 547: 545: 543: 539: 532: 531:ChEMBL1229517 528: 527: 525: 523: 519: 512: 508: 507: 505: 503: 499: 492: 488: 487: 485: 483: 479: 472: 468: 467: 465: 463: 459: 452: 448: 447: 445: 443: 439: 432: 428: 427: 425: 423: 419: 412: 408: 407: 405: 398: 394: 387: 383: 382: 380: 378: 374: 366: 362: 358: 351: 346: 340: 330: 327: 317: 315: 306: 303: 293: 292: 290: 288: 284: 279: 271: 266: 263: 262: 260: 258: 254: 251: 248: 246: 240: 234: 225: 224: 222: 220: 214: 207: 203: 193: 190: 185: 176: 175: 173: 171: 167: 163: 159: 157: 153: 149: 145: 143: 139: 135: 131: 127: 123: 121: 117: 113: 112: 99: 52: 50:Pronunciation 48: 45:Clinical data 43: 39: 34: 30: 25: 6777:Chemotherapy 6772:Sulfonamides 6767:Fluoroarenes 6693:Cerebrolysin 6689: 6663:Pleiotrophin 6619:Interleukins 6532: 6513: 6483: 6402:Fruquintinib 6392:Cabozantinib 6373: 6363: 6321: 6285:Lestaurtinib 6236: 6216: 6184:Lestaurtinib 6135: 6125: 6106:Antagonists: 6105: 6039:Deoxygedunin 5994:3,7,8,2'-THF 5985: 5964: 5955:Against NGF: 5954: 5951: 5907:Against NGF: 5906: 5899: 5896: 5859:Lestaurtinib 5810: 5800: 5794:Testosterone 5776:Antagonists: 5775: 5725: 5625: 5610: 5585: 5566: 5556: 5535: 5525: 5504: 5494: 5473: 5458: 5418: 5333: 5301: 5280: 5271:Against NGF: 5270: 5267: 5223:Against NGF: 5222: 5219: 5213:Testosterone 5195:Antagonists: 5194: 5144: 5114: 5075: 5050: 5039: 5016:Teprotumumab 4977: 4947: 4906: 4855:Ficlatuzumab 4850:Emibetuzumab 4846: 4800:JNJ-38877605 4770:Cabozantinib 4741: 4731: 4720:Fosgonimeton 4715: 4690: 4632: 4610: 4551: 4534:Infigratinib 4530: 4515: 4418: 4335: 4269:Betacellulin 4265: 4248:Seribantumab 4234: 4211: 4170: 4135: 4129:Unknown/none 4128: 4124: 4058: 3983: 3942:Betacellulin 3937:Amphiregulin 3932: 3924:(ErbB1/HER1) 3888: 3860: 3840: 3826:Antagonists: 3825: 3810: 3803:Angiopoietin 3705:Pexidartinib 3690:Odronextamab 3660:Gilteritinib 3640:Cabozantinib 3587: 3553: 3528: 3522:Temsirolimus 3504: 3488: 3470:proapoptotic 3468: 3452: 3431:Zanubrutinib 3403: 3373: 3342: 3319:Lestaurtinib 3298:Janus kinase 3296: 3277: 3231: 3224:Non-receptor 3205:Cabozantinib 3198: 3167:Infigratinib 3152: 3126: 3068:Fruquintinib 3050: 3043:Gilteritinib 3039:Lestaurtinib 3032: 2981: 2950: 2923:Mobocertinib 2888:Aumolertinib 2876: 2841:Tremelimumab 2826:Tislelizumab 2781:Retifanlimab 2656:Blinatumomab 2626:Atezolizumab 2597: 2579: 2569: 2551:Obinutuzumab 2529: 2511: 2478: 2461: 2419: 2402: 2309: 2259: 2255: 2245: 2232: 2227: 2215:. Retrieved 2210: 2201: 2190:. Retrieved 2178: 2169: 2134: 2130: 2120: 2109:. Retrieved 2100: 2091: 2081:February 18, 2079:. Retrieved 2075:the original 2070: 2060: 2048:. Retrieved 2044:the original 2039: 2030: 1997: 1993: 1987: 1976:. Retrieved 1966: 1952: 1941:. Retrieved 1937:the original 1927: 1916:. Retrieved 1912:the original 1902: 1893: 1870:. Retrieved 1866:the original 1856: 1843: 1838: 1825: 1820: 1810:the original 1805: 1766: 1762: 1752: 1741:. Retrieved 1737:the original 1732: 1727:Flaherty K. 1722: 1689: 1685: 1679: 1668: 1658: 1647:. Retrieved 1637: 1628: 1624: 1615: 1572: 1568: 1558: 1515: 1511: 1501: 1490: 1444: 1440: 1430: 1395: 1391: 1381: 1346: 1342: 1332: 1305: 1301: 1291: 1258: 1254: 1247: 1204: 1200: 1164: 1134: 1122: 1106: 1088: 1085: 1078: 1075:Legal status 1057: 1042: 1039: 1032: 1017: 1014: 1007: 993: 990:Side effects 979:Stromal cell 955: 935: 916: 887: 879: 878: 771: 751:   364: 287:Legal status 281:Legal status 170:License data 6653:Oncomodulin 6517:Aflibercept 6507:Ranibizumab 6502:Ramucirumab 6492:Bevacizumab 6484:Antibodies: 6442:Regorafenib 6382:Altiratinib 6295:ONO-5390556 6265:Entrectinib 6240:Altiratinib 6194:ONO-5390556 6164:Entrectinib 6139:Altiratinib 5925:Frunevetmab 5897:Antibodies: 5874:ONO-5390556 5839:Entrectinib 5814:Altiratinib 5769:Tavilermide 5664:Quizartinib 5603:SCF (c-Kit) 5427:Ramucirumab 5419:Antibodies: 5392:Quizartinib 5342:Avapritinib 5305:Becaplermin 5241:Frunevetmab 5220:Antibodies: 5123:Trofinetide 5054:Dusigitumab 5051:Antibodies: 5006:Robatumumab 4996:Figitumumab 4991:Dalotuzumab 4986:Cixutumumab 4978:Antibodies: 4870:Rilotumumab 4865:Onartuzumab 4860:Flanvotumab 4847:Antibodies: 4815:PF-04217903 4745:Altiratinib 4708:HGF (c-Met) 4611:Antibodies: 4516:Antibodies: 4238:Duligotumab 4235:Antibodies: 4149:Trastuzumab 4139:Ertumaxomab 4136:Antibodies: 4107:Zalutumumab 4102:Panitumumab 4097:Nimotuzumab 4092:Necitumumab 4082:Imgatuzumab 4059:Antibodies: 4042:Osimertinib 4007:Dacomitinib 3902:Dapiclermin 3861:Antibodies: 3844:Altiratinib 3735:Tebentafusp 3715:Regorafenib 3710:Quizartinib 3700:Pemigatinib 3680:Midostaurin 3655:Erdafitinib 3650:Entrectinib 3633:Parsaclisib 3581:Trilaciclib 3571:Palbociclib 3566:Dalpiciclib 3561:Abemaciclib 3463:Aflibercept 3390:Entrectinib 3360:Selumetinib 3355:Cobimetinib 3350:Binimetinib 3334:Ruxolitinib 3324:Momelotinib 3304:Baricitinib 3202:inhibitors: 3179:Pralsetinib 3175:Pemigatinib 3163:Futibatinib 3159:Entrectinib 3156:inhibitors: 3088:Regorafenib 2992:Avapritinib 2938:Rociletinib 2933:Osimertinib 2898:Dacomitinib 2836:Toripalimab 2821:Teclistamab 2811:Talquetamab 2806:Tafasitamab 2801:Sugemalimab 2796:Serplulimab 2786:Sabatolimab 2776:Ramucirumab 2771:Prolgolimab 2741:Necitumumab 2696:Epcoritamab 2676:Dostarlimab 2666:Daratumumab 2621:Amivantamab 2586:Alemtuzumab 2576:Brentuximab 2566:Tositumomab 2541:Ibritumomab 2522:Elranatamab 2485:Bevacizumab 2473:Edrecolomab 2468:Catumaxomab 2430:Trastuzumab 2414:Panitumumab 2234:NCT03410875 1845:NCT00949702 1827:NCT00405587 1045:cobimetinib 1035:dacarbazine 880:Vemurafenib 766:vemurafenib 678: g·mol 609:100.287.801 386:918504-65-1 348:Identifiers 206:Vemurafenib 156:MedlinePlus 129:Other names 120:Trade names 21:Vemurafenib 6731:Categories 6472:Vandetanib 6437:Rebastinib 6432:Pegaptanib 6422:Nintedanib 6412:Lenvatinib 6377:Agerafenib 6330:Ripretinib 6255:CH-7057288 6154:CH-7057288 6019:7,8,3'-THF 6014:7,8,2'-THF 5940:Ranevetmab 5930:Fulranumab 5884:Rebastinib 5829:CH-7057288 5744:Cenegermin 5629:Agerafenib 5589:Agerafenib 5570:Vandetanib 5539:Vandetanib 5508:Vandetanib 5477:Vandetanib 5422:Olaratumab 5397:Ripretinib 5377:Nintedanib 5362:Lenvatinib 5352:Crenolanib 5337:Agerafenib 5256:Ranevetmab 5246:Fulranumab 5163:Cenegermin 5137:LNGF (p75) 5059:Xentuzumab 5021:Xentuzumab 4966:NVP-AEW541 4961:NVP-ADW742 4956:Linsitinib 4951:BMS-754807 4936:Mecasermin 4835:Tivantinib 4825:PHA-665752 4820:PF-2341066 4790:Golvatinib 4780:Crizotinib 4775:Capmatinib 4765:BMS-777607 4760:Amuvatinib 4636:Ersofermin 4599:Sprifermin 4555:Ersofermin 4504:Sprifermin 4494:Repifermin 4489:Palifermin 4422:Ersofermin 4401:Velafermin 4386:Repifermin 4339:Ersofermin 4258:ErbB4/HER4 4243:Patritumab 4204:ErbB3/HER3 4184:Mubritinib 4144:Pertuzumab 4117:ErbB2/HER2 4047:Vandetanib 4002:Canertinib 3997:Brigatinib 3992:Agerafenib 3972:Nepidermin 3967:Murodermin 3957:Epiregulin 3912:EGF (ErbB) 3870:Nesvacumab 3864:Evinacumab 3854:Rebastinib 3795:modulators 3750:Venetoclax 3745:Vandetanib 3720:Ripretinib 3685:Nintedanib 3670:Lenvatinib 3645:Capmatinib 3628:Idelalisib 3618:Copanlisib 3591:inhibitors 3576:Ribociclib 3547:Vismodegib 3532:inhibitors 3512:Everolimus 3478:prohibitin 3395:Lorlatinib 3385:Crizotinib 3365:Trametinib 3329:Pacritinib 3314:Filgotinib 3309:Fedratinib 3213:Crizotinib 3209:Capmatinib 3191:Vandetanib 3139:Brigatinib 3118:Vandetanib 3078:Nintedanib 3073:Lenvatinib 3012:Ripretinib 2943:Vandetanib 2918:Lazertinib 2893:Brigatinib 2816:Tarlatamab 2751:Olaratumab 2711:Isatuximab 2706:Ipilimumab 2686:Elotuzumab 2681:Durvalumab 2661:Cemiplimab 2651:Bermekimab 2641:Axatilimab 2556:Ofatumumab 2536:Glofitamab 2518:Glofitamab 2426:Pertuzumab 2192:2016-04-15 2111:2018-05-20 1978:2011-08-17 1943:2015-02-04 1918:2012-12-17 1872:2011-02-03 1743:2010-09-10 1649:2009-06-07 1144:References 1064:trametinib 1060:dabrafenib 997:arthralgia 952:Resistance 938:amino acid 892:medication 793:C-terminus 789:N-terminus 683:3D model ( 671:Molar mass 542:PDB ligand 491:207SMY3FQT 462:ChemSpider 422:IUPHAR/BPS 377:CAS Number 357:IUPAC name 6497:Icrucumab 6477:WHI-P 154 6467:Tivozanib 6462:Toceranib 6457:Sunitinib 6452:Sorafenib 6447:Semaxanib 6427:Pazopanib 6417:Motesanib 6407:Lapatinib 6397:Cediranib 6335:Telbermin 6322:Agonists: 6270:GZ-389988 6250:CE-245677 6217:Agonists: 6169:GZ-389988 6149:CE-245677 6049:Diosmetin 5986:Agonists: 5952:Aptamers: 5945:Tanezumab 5920:Fasinumab 5864:Milciclib 5844:GZ-389988 5824:CE-245677 5726:Agonists: 5679:Toceranib 5674:Sunitinib 5669:Sorafenib 5659:Pazopanib 5654:Nilotinib 5649:Masitinib 5639:Dasatinib 5611:Agonists: 5557:Agonists: 5526:Agonists: 5495:Agonists: 5467:Liatermin 5459:Agonists: 5442:RET (GFL) 5432:Tovetumab 5412:Toceranib 5407:Sorafenib 5402:Sunitinib 5387:Radotinib 5382:Pazopanib 5372:Motesanib 5367:Masitinib 5302:Agonists: 5268:Aptamers: 5261:Tanezumab 5236:Fasinumab 5145:Agonists: 5001:Ganitumab 4921:IGF-1 LR3 4840:Volitinib 4795:INCB28060 4785:Foretinib 4691:Agonists: 4675:Trafermin 4633:Agonists: 4614:Burosumab 4604:Trafermin 4552:Agonists: 4519:Aprutumab 4509:Trafermin 4471:10 (KGF2) 4419:Agonists: 4396:Trafermin 4376:10 (KGF2) 4336:Agonists: 4266:Agonists: 4212:Agonists: 4194:Tucatinib 4189:Neratinib 4179:Lapatinib 4087:Matuzumab 4077:Futuximab 4062:Cetuximab 4052:WHI-P 154 4037:Neratinib 4032:Lapatinib 4022:Grandinin 4017:Gefitinib 4012:Erlotinib 3889:Agonists: 3849:CE-245677 3811:Agonists: 3740:Tepotinib 3730:Sunitinib 3725:Sorafenib 3695:Pazopanib 3675:Masitinib 3623:Duvelisib 3613:Alpelisib 3601:Sotorasib 3596:Adagrasib 3542:Sonidegib 3537:Glasdegib 3483:Adipotide 3416:Ibrutinib 3289:Dasatinib 3284:Bosutinib 3269:Radotinib 3264:Ponatinib 3259:Nilotinib 3249:Dasatinib 3244:Bosutinib 3239:Asciminib 3207:(VEGFR), 3165:(FGFR2), 3144:Ceritinib 3134:Alectinib 3113:Toceranib 3108:Tivozanib 3103:Sunitinib 3098:Sorafenib 3093:Semaxanib 3083:Pazopanib 3063:Cediranib 3027:Toceranib 3022:Sunitinib 3017:Sorafenib 3007:Pazopanib 3002:Masitinib 2969:Tucatinib 2964:Neratinib 2959:Lapatinib 2928:Olmutinib 2908:Gefitinib 2903:Erlotinib 2878:HER1/EGFR 2746:Nivolumab 2736:Naxitamab 2561:Rituximab 2409:Cetuximab 2404:HER1/EGFR 2211:HCLF Blog 2187:0013-0613 2071:Onco'Zine 1193:​; 1026:), and a 967:A second 907:Plexxikon 843:ligand id 243:Routes of 217:Pregnancy 148:Monograph 142:Drugs.com 6721:Medicine 6679:instead) 6668:Renalase 6629:instead) 6600:instead) 6547:instead) 6387:Axitinib 6356:D (FIGF) 6300:PLX-7486 6290:ONO-4474 6245:AZD-6918 6199:PLX-7486 6189:ONO-4474 6144:AZD-6918 6126:Ligands: 6044:Deprenyl 6004:7,3'-DHF 5935:MEDI-578 5915:ASP-6294 5879:PLX-7486 5869:ONO-4474 5819:AZD-6918 5779:ALE-0540 5700:instead. 5644:Imatinib 5634:Axitinib 5614:Ancestim 5579:Unsorted 5357:Imatinib 5347:Axitinib 5251:MEDI-578 5231:ASP-6294 5198:ALE-0540 5040:Agonists 4981:AVE-1642 4907:Agonists 4830:SU-11274 4716:Agonists 4694:FGF15/19 4684:Unsorted 4649:2 (bFGF) 4568:2 (bFGF) 4435:2 (bFGF) 4352:2 (bFGF) 4174:Afatinib 4125:Agonists 4027:Icotinib 3987:Afatinib 3933:Agonists 3530:hedgehog 3492:against 3490:exotoxin 3456:against 3405:Bruton's 3254:Imatinib 3177:(FGFR), 3173:(NTRK), 3058:Axitinib 2997:Axitinib 2953:HER2/neu 2913:Icotinib 2883:Afatinib 2857:("-nib") 2636:Avelumab 2508:lymphoid 2500:lymphoma 2496:Leukemia 2421:HER2/neu 2383:("-mab") 2323:28809522 2317:(NCBI). 2286:35930750 2217:July 25, 2161:29188284 2050:21 April 2014:23060265 1793:20818844 1714:20019269 1607:22763448 1550:22763439 1479:21107323 1422:20149136 1373:20130576 1324:25520039 1283:16031942 1275:18458053 1239:20823850 1119:Research 1098:mutation 1028:phase II 969:oncogene 923:melanoma 896:melanoma 888:Zelboraf 856:RCSB PDB 805:melanoma 791:= blue, 754:(verify) 471:24747352 442:DrugBank 411:42611257 257:ATC code 250:By mouth 219:category 124:Zelboraf 6556:Ephrins 6260:DS-6051 6159:DS-6051 6064:LM22A-4 6054:DMAQ-B1 6009:7,8-DHF 5989:3,7-DHF 5958:RBM-004 5903:GBR-900 5834:DS-6051 5804:VM-902A 5274:RBM-004 4971:OSl-906 4931:Insulin 4810:MK-2461 4755:AMG-458 3892:Axokine 3233:bcr-abl 2594:myeloid 2277:9935554 2152:5844839 2022:9337155 1960:. 2015. 1806:Corante 1784:3724529 1694:Bibcode 1686:Science 1598:3724525 1577:Bibcode 1541:3711467 1520:Bibcode 1470:3143360 1449:Bibcode 1413:2848976 1351:Bibcode 1230:2948082 1209:Bibcode 1020:Phase I 1004:History 971:called 929:on the 890:, is a 865:LIGPLOT 626:Formula 451:DB08881 397:PubChem 312:: 273:) 267: ( 265:L01XE15 232: D 204::  186::  162:a612009 6707:Portal 6526:Others 6220:BNN-20 6109:ANA-12 6034:BNN-20 5754:DHEA-S 5739:BNN-27 5734:BNN-20 5173:DHEA-S 5158:BNN-27 5153:BNN-20 5069:Others 4274:Epigen 3952:Epigen 2480:VEGF-A 2321:  2284:  2274:  2185:  2159:  2149:  2020:  2012:  1791:  1781:  1712:  1605:  1595:  1569:Nature 1548:  1538:  1512:Nature 1477:  1467:  1441:Nature 1420:  1410:  1371:  1343:Nature 1322:  1281:  1273:  1237:  1227:  1201:Nature 985:(HGF). 962:PDGFRB 942:valine 903:enzyme 709:SMILES 676:489.92 522:ChEMBL 511:D09996 339:℞-only 337: 324: 314:℞-only 300: 199:  189:by INN 182:  114: 111:-ə-nib 6675:(see 6625:(see 6596:(see 6543:(see 6275:K252a 6174:K252a 5849:K252a 5789:FX007 5549:GFRα4 5518:GFRα3 5487:GFRα2 5451:GFRα1 5079:IGFBP 5032:IGF-2 5011:R1507 4899:IGF-1 4805:K252a 4625:FGFR4 4544:FGFR3 4411:FGFR2 4328:FGFR1 3474:ANXA2 3446:Other 3344:MAP2K 3215:(ALK) 3200:c-MET 3052:VEGFR 2987:PDGFR 2983:C-kit 2614:Other 2463:EpCAM 2256:Blood 2105:(FDA) 2101:U.S. 2018:S2CID 1279:S2CID 1095:V600E 1047:), a 1008:In a 900:B-Raf 846:032: 729:InChI 685:JSmol 549:032 ( 6677:here 6627:here 6598:here 6545:here 6340:VEGF 6314:VEGF 6230:NT-3 6225:DHEA 6209:TrkC 6129:DHEA 6099:TDP6 6079:NT-4 6074:NT-3 6059:HIOC 6029:BDNF 5978:TrkB 5749:DHEA 5718:TrkA 5698:here 5696:See 5689:TGFβ 5294:PDGF 5188:NT-4 5183:NT-3 5168:DHEA 5148:BDNF 3897:CNTF 3881:CNTF 3589:KRAS 3494:IL-2 3476:and 3458:VEGF 3375:EML4 3034:FLT3 2985:and 2873:ErbB 2599:CD33 2581:CD52 2571:CD30 2531:CD20 2399:ErbB 2319:PMID 2282:PMID 2219:2022 2183:ISSN 2157:PMID 2083:2013 2052:2012 2010:PMID 1789:PMID 1710:PMID 1603:PMID 1546:PMID 1475:PMID 1418:PMID 1369:PMID 1320:PMID 1271:PMID 1235:PMID 1190:3OG7 1062:and 973:NRAS 871:3og7 850:PDBe 817:BRAF 552:PDBe 502:KEGG 482:UNII 431:5893 138:AHFS 6094:R13 5764:NGF 5709:Trk 5178:NGF 4890:IGF 4750:AM7 4641:FGF 4560:FGF 4461:), 4459:KGF 4427:FGF 4344:FGF 4319:FGF 3921:EGF 3379:ALK 3279:Src 3154:RET 3128:ALK 2578:), 2568:), 2528:), 2513:CD3 2369:L01 2272:PMC 2264:doi 2260:140 2147:PMC 2139:doi 2002:doi 1779:PMC 1771:doi 1767:363 1702:doi 1690:326 1593:PMC 1585:doi 1573:487 1536:PMC 1528:doi 1516:487 1465:PMC 1457:doi 1445:468 1408:PMC 1400:doi 1359:doi 1347:464 1310:doi 1263:doi 1225:PMC 1217:doi 1205:467 1186:PDB 921:in 884:INN 841:PDB 575:EPA 401:CID 326:POM 270:WHO 202:FDA 184:EMA 109:RAF 107:-ə- 105:VEM 6733:: 6588:B3 6586:, 6584:B2 6582:, 6580:B1 6578:, 6576:A5 6574:, 6572:A4 6570:, 6568:A3 6566:, 6564:A2 6562:, 6560:A1 6354:, 6350:, 6346:, 6089:R7 5905:; 5324:, 5320:, 5316:, 5105:, 5101:, 5097:, 5093:, 5089:, 5085:, 5042:: 4909:: 4718:: 4669:19 4667:, 4663:, 4659:, 4655:, 4651:, 4647:, 4588:23 4586:, 4584:18 4582:, 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6348:B 6344:A 6342:( 5891:) 5328:) 5326:D 5322:C 5318:B 5314:A 5312:( 5109:) 5107:7 5103:6 5099:5 5095:4 5091:3 5087:2 5083:1 5081:( 4671:) 4665:9 4661:8 4657:6 4653:4 4645:1 4643:( 4590:) 4580:9 4576:8 4572:4 4564:1 4562:( 4485:) 4467:9 4463:8 4457:( 4455:7 4451:6 4447:5 4443:4 4439:3 4431:1 4429:( 4382:) 4372:8 4368:6 4364:5 4360:4 4356:3 4348:1 4346:( 4306:) 4300:4 4296:3 4292:2 4288:1 4286:( 4229:) 4223:2 4219:1 4217:( 3784:e 3777:t 3770:v 3501:) 3497:( 3485:) 3481:( 3465:) 3461:( 3377:- 3291:) 3282:( 3037:( 3029:) 2990:( 2945:) 2881:( 2632:) 2628:( 2606:) 2602:( 2588:) 2584:( 2574:( 2534:( 2516:( 2498:/ 2487:) 2483:( 2475:) 2466:( 2447:) 2436:) 2432:( 2424:( 2416:) 2407:( 2371:) 2367:( 2353:e 2346:t 2339:v 2288:. 2266:: 2221:. 2195:. 2163:. 2141:: 2135:4 2114:. 2085:. 2054:. 2024:. 2004:: 1981:. 1946:. 1921:. 1875:. 1795:. 1773:: 1746:. 1716:. 1704:: 1696:: 1673:. 1652:. 1629:5 1609:. 1587:: 1579:: 1552:. 1530:: 1522:: 1481:. 1459:: 1451:: 1424:. 1402:: 1375:. 1361:: 1353:: 1326:. 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Index



/ˌvɛməˈræfənɪb/
VEM-ə-RAF-ə-nib
Trade names
AHFS
Drugs.com
Monograph
MedlinePlus
a612009
License data
EMA
by INN
FDA
Vemurafenib
Pregnancy
category

Routes of
administration

By mouth
ATC code
L01XE15
WHO
Legal status
S4
℞-only
POM
℞-only
IUPAC name
CAS Number
918504-65-1
PubChem

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