587:(FDA) approved tazemetostat in January 2020, based on the results of a clinical trial (NCT02601950) enrolling 62 subjects with metastatic or locally advanced epithelioid sarcoma. During the clinical trial, subjects received 800 milligrams (mg) of tazemetostat twice a day until the disease progressed or the subject reached an unacceptable level of toxicity. Tumor response assessments were performed every eight weeks during the clinical trial. The trial measured how many subjects experienced complete or partial shrinkage (by a certain amount) of their tumors during treatment (overall response rate). The overall response rate was 15%, with 1.6% of subjects having a complete response and 13% having a partial response. Of the nine subjects that had a response, six (67%) subjects had a response lasting six months or longer.
551:. Tazemetostat blocks activity of the EZH2 methyltransferase, which may help keep the cancer cells from growing. Most cases of epithelioid sarcoma begin in the soft tissue under the skin of an extremity, though it can start in other areas of the body. Surgical removal is considered the main treatment when the cancer is localized to one area of the body. Chemotherapy or radiation may also be given. However, there is a high likelihood for local and regional spread of the disease even with treatment and approximately 50% of patients have metastatic disease at the time of diagnosis. Metastatic disease is considered life-threatening to the patient.
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The most common side effects are pain, fatigue, nausea, decreased appetite, vomiting and constipation. People taking tazemetostat are at increased risk of developing secondary malignancies including: T-cell lymphoblastic lymphoma (a type of blood cancer that affects the lymphatic system usually found
559:
27 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways and results in decreased tumor cell proliferation in EZH2 mutated cancer cells. EZH2, which belongs to the class of histone methyltransferases (HMTs), is overexpressed or mutated in a
554:
According to the NCI Drug
Dictionary, "tazemetostat is an orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyl transferase EZH2, with potential antineoplastic activity. Upon oral administration, tazemetostat selectively inhibits the
533:, is a medication used for the treatment of adults and adolescents aged 16 years and older with metastatic (when cancer cells spread to other parts of the body) or locally advanced (when cancer has grown outside the organ it started in, but has not yet spread to distant parts of the body)
511:
InChI=1S/C34H44N4O4/c1-5-38(29-10-14-41-15-11-29)32-20-28(27-8-6-26(7-9-27)22-37-12-16-42-17-13-37)19-30(25(32)4)33(39)35-21-31-23(2)18-24(3)36-34(31)40/h6-9,18-20,29H,5,10-17,21-22H2,1-4H3,(H,35,39)(H,36,40)
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in the lymph nodes), myelodysplastic syndrome (a disorder resulting from poorly formed or dysfunctional blood cells) and acute myeloid leukemia (a cancer of the blood and bone marrow).
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activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3
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The trial was conducted at 22 sites in France, United
Kingdom, Taiwan, Italy, Canada, Belgium, and the United States.
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654:"FDA approves first treatment option specifically for patients with epithelioid sarcoma, a rare soft tissue cancer"
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Lue JK, Amengual JE (October 2018). "Emerging EZH2 Inhibitors and Their
Application in Lymphoma".
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not eligible for complete resection (surgically removing all of a tissue, structure, or organ).
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CCN(C1CCOCC1)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C4=CC=C(C=C4)CN5CCOCC5
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designation. The FDA granted the approval of
Tazverik to Epizyme Inc.
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This article incorporates text from this source, which is in the
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This article incorporates text from this source, which is in the
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This article incorporates text from this source, which is in the
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Tazemetostat is a cancer drug that acts as a potent selective
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593:The FDA granted the application for tazemetostat
560:variety of cancer cells and plays a key role in
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850:. U.S. National Library of Medicine.
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1146:ribonucleotide reductase inhibitors
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247:
1312:Ribonucleotide reductase inhibitor
1268:Ribonucleotide reductase inhibitor
14:
1071:Dihydrofolate reductase inhibitor
800:"Drug Trials Snapshots: Tazverik"
755:"New Drug Therapy Approvals 2020"
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664:(Press release). 23 January 2020
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516:Key:NSQSAUGJQHDYNO-UHFFFAOYSA-N
1208:Thymidylate synthase inhibitor
1098:Thymidylate synthase inhibitor
435:
417:
1:
2924:Clonally transmissible cancer
1128:Adenosine deaminase inhibitor
969:Block microtubule disassembly
806:Food and Drug Administration
761:Food and Drug Administration
743:. National Cancer Institute.
660:Food and Drug Administration
585:Food and Drug Administration
569:Food and Drug Administration
529:, sold under the brand name
571:(FDA) considers it to be a
3049:
2955:Index of oncology articles
407:Chemical and physical data
2547:
2428:Omacetaxine mepesuccinate
2308:Ciltacabtagene autoleucel
2298:Brexucabtagene autoleucel
707:10.1007/s11899-018-0466-6
573:first-in-class medication
499:
479:
214:--3--2-methyl-5-benzamide
199:
28:
2480:Talimogene laherparepvec
2413:Nadofaragene firadenovec
2383:Lisocabtagene maraleucel
1332:Topoisomerase inhibitors
1251:DNA polymerase inhibitor
2877:Prostate cancer staging
2841:Paraneoplastic syndrome
2283:Axicabtagene ciloleucel
887:chemotherapeutic agents
848:Drug Information Portal
2915:Tumor suppressor genes
2882:Gleason grading system
2836:Precancerous condition
2465:Sitimagene ceradenovec
2363:Idecabtagene vicleucel
1928:Methyl aminolevulinate
695:Curr Hematol Malig Rep
2934:Carcinogenic bacteria
2674:Malignant progression
1939:Porphyrin derivatives
1635:Melphalan flufenamide
1282:Hypomethylating agent
891:antineoplastic agents
564:cell proliferation."
3018:Antineoplastic drugs
2887:Dukes classification
2268:Asparagine depleters
2197:Receptor antagonists
2111:+abiraterone acetate
595:accelerated approval
2706:Sentinel lymph node
2318:Denileukin diftitox
2218:Retinoid X receptor
1918:Aminolevulinic acid
1740:Triethylenemelamine
1572:Crosslinking of DNA
1303:Deoxyribonucleotide
1242:+gimeracil/oteracil
741:NCI Drug Dictionary
535:epithelioid sarcoma
25:
2754:Respiratory system
2574:Never to phase III
1376:Etirinotecan pegol
765:. 31 December 2020
3023:Cancer treatments
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2970:Cancer and nausea
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2686:Carcinoma in situ
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2500:Tigilanol tiglate
1977:Enzyme inhibitors
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810:. 23 January 2020
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470:Interactive image
376:CompTox Dashboard
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2098:PARP inhibitor
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885:Intracellular
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844:"Tazemetostat"
838:
837:External links
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832:
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786:
746:
737:"Tazemetostat"
728:
701:(5): 369โ382.
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474:
473:
465:
463:
455:
454:
448:
442:
441:
438:
432:
426:
420:
415:
409:
408:
404:
403:
401:
400:
387:
385:
372:
371:
369:
368:
360:
358:
352:
351:
349:
348:
341:
333:
331:
325:
324:
322:
321:
313:
311:
305:
304:
302:
301:
293:
291:
285:
284:
282:
281:
273:
271:
265:
264:
262:
261:
253:
251:
240:
239:
237:
236:
228:
226:
220:
219:
217:
216:
210:
202:
201:
200:
197:
196:
192:
191:
189:
188:
175:
173:
167:
166:
162:
161:
159:
158:
145:
143:
137:
136:
134:
133:
116:
98:
96:
90:
89:
82:
76:
75:
68:
58:
57:
54:
50:
49:
46:
40:
39:
35:
34:
15:
13:
10:
9:
6:
4:
3:
2:
3045:
3034:
3031:
3029:
3026:
3024:
3021:
3019:
3016:
3015:
3013:
3003:
2993:
2989:
2976:
2973:
2971:
2968:
2966:
2963:
2961:
2958:
2956:
2953:
2951:
2948:
2947:
2945:
2941:
2935:
2932:
2930:
2927:
2925:
2922:
2920:
2916:
2913:
2911:
2908:
2906:
2903:
2902:
2900:
2898:
2894:
2888:
2885:
2883:
2880:
2878:
2875:
2873:
2870:
2868:
2865:
2864:
2862:
2860:
2856:
2852:
2842:
2839:
2837:
2834:
2833:
2831:
2827:
2821:
2818:
2816:
2813:
2811:
2808:
2806:
2803:
2801:
2798:
2797:
2795:
2791:
2785:
2782:
2780:
2777:
2775:
2772:
2770:
2767:
2765:
2762:
2760:
2757:
2755:
2752:
2750:
2747:
2743:
2740:
2738:
2735:
2733:
2732:oropharyngeal
2730:
2728:
2725:
2724:
2723:
2722:Head and neck
2720:
2719:
2717:
2713:
2707:
2704:
2702:
2701:Primary tumor
2699:
2697:
2694:
2692:
2689:
2687:
2684:
2682:
2679:
2678:
2676:
2672:
2666:
2663:
2661:
2658:
2656:
2653:
2651:
2648:
2647:
2645:
2643:
2642:Benign tumors
2639:
2636:
2632:
2628:
2624:
2620:
2612:
2607:
2605:
2600:
2598:
2593:
2592:
2589:
2573:
2571:
2568:
2567:
2565:
2562:
2559:
2556:
2554:
2551:
2550:
2546:
2536:
2533:
2531:
2528:
2526:
2523:
2521:
2518:
2516:
2513:
2511:
2508:
2506:
2503:
2501:
2498:
2496:
2493:
2491:
2488:
2486:
2483:
2481:
2478:
2476:
2473:
2471:
2468:
2466:
2463:
2461:
2458:
2455:
2452:
2450:
2446:
2445:
2441:
2439:
2438:Tabelecleucel
2436:
2434:
2431:
2429:
2426:
2424:
2421:
2419:
2416:
2414:
2411:
2409:
2406:
2404:
2401:
2399:
2398:Lurbinectedin
2396:
2394:
2391:
2389:
2386:
2384:
2381:
2379:
2376:
2374:
2371:
2369:
2366:
2364:
2361:
2359:
2356:
2354:
2351:
2349:
2346:
2344:
2341:
2339:
2336:
2334:
2331:
2329:
2326:
2324:
2321:
2319:
2316:
2314:
2311:
2309:
2306:
2304:
2301:
2299:
2296:
2294:
2291:
2289:
2286:
2284:
2281:
2278:
2274:
2270:
2269:
2265:
2263:
2260:
2258:
2255:
2253:
2250:
2249:
2247:
2243:
2236:
2232:
2231:
2227:
2224:
2220:
2219:
2215:
2212:
2208:
2207:
2203:
2202:
2200:
2198:
2194:
2187:
2184:
2182:
2179:
2177:
2174:
2172:
2169:
2167:
2163:
2161:
2157:
2154:
2151:
2149:
2146:
2144:
2141:
2139:
2136:
2134:
2130:
2129:
2125:
2122:
2119:
2117:
2114:
2112:
2109:
2106:
2104:
2100:
2099:
2095:
2092:
2088:
2087:
2083:
2080:
2076:
2075:
2071:
2068:
2064:
2063:
2059:
2055:
2052:
2050:
2047:
2045:
2042:
2040:
2037:
2036:
2035:
2034:
2030:
2027:
2024:
2022:
2019:
2017:
2014:
2012:
2009:
2007:
2003:
2002:
1999:
1995:
1992:
1988:
1987:
1983:
1982:
1980:
1978:
1974:
1971:
1967:
1960:
1957:
1955:
1952:
1950:
1947:
1945:
1941:
1940:
1936:
1934:
1931:
1929:
1926:
1924:
1921:
1919:
1916:
1915:
1913:
1911:
1907:
1903:
1888:
1885:
1883:
1880:
1878:
1875:
1873:
1869:
1866:
1865:
1863:
1861:
1860:Intercalation
1857:
1850:
1847:
1845:
1842:
1840:
1836:
1835:
1831:
1829:
1826:
1824:
1821:
1819:
1816:
1813:
1809:
1808:
1804:
1802:
1799:
1798:
1796:
1794:
1790:
1784:
1781:
1779:
1776:
1774:
1771:
1769:
1768:Dicycloplatin
1766:
1764:
1761:
1759:
1756:
1755:
1753:
1751:
1747:
1741:
1738:
1736:
1733:
1731:
1728:
1726:
1723:
1721:
1717:
1716:
1712:
1709:
1707:
1703:
1700:
1698:
1694:
1693:
1690:
1687:
1685:
1682:
1680:
1677:
1674:
1670:
1667:
1665:
1662:
1660:
1657:
1655:
1651:
1650:
1647:
1644:
1642:
1641:Prednimustine
1639:
1636:
1632:
1629:
1627:
1624:
1621:
1618:
1616:
1612:
1609:
1607:
1604:
1602:
1599:
1597:
1593:
1592:
1590:
1588:
1584:
1581:
1578:
1573:
1569:
1559:
1556:
1554:
1551:
1549:
1546:
1544:
1541:
1538:
1535:
1533:
1530:
1528:
1524:
1523:
1519:
1516:
1513:
1511:
1508:
1506:
1503:
1501:
1498:
1496:
1493:
1491:
1488:
1485:
1481:
1478:
1476:
1473:
1471:
1467:
1466:
1462:
1461:
1459:
1457:
1456:Intercalation
1453:
1449:
1442:
1439:
1437:
1433:
1432:
1428:
1427:
1425:
1423:
1419:
1412:
1409:
1407:
1404:
1402:
1399:
1397:
1394:
1392:
1389:
1387:
1384:
1382:
1379:
1377:
1374:
1372:
1369:
1367:
1364:
1362:
1358:
1357:
1353:
1352:
1350:
1348:
1344:
1341:
1338:
1333:
1329:
1318:
1314:
1313:
1309:
1308:
1306:
1304:
1300:
1293:
1290:
1288:
1284:
1283:
1279:
1278:
1274:
1270:
1269:
1265:
1264:
1260:
1259:+daunorubicin
1257:
1253:
1252:
1248:
1247:
1243:
1239:
1236:
1234:
1231:
1229:
1226:
1224:
1223:Doxifluridine
1221:
1219:
1216:
1214:
1210:
1209:
1205:
1204:
1202:
1200:
1196:
1189:
1186:
1184:
1180:
1179:
1175:
1173:
1172:Rabacfosadine
1170:
1168:
1165:
1162:
1159:
1157:
1154:
1152:
1148:
1147:
1143:
1139:
1138:
1134:
1130:
1129:
1125:
1124:
1122:
1120:
1116:
1109:
1106:
1104:
1100:
1099:
1095:
1092:
1089:
1087:
1084:
1082:
1079:
1077:
1073:
1072:
1068:
1067:
1065:
1063:
1059:
1056:
1053:
1048:
1042:
1039:
1035:
1031:
1020:
1016:
1015:
1011:
1008:
1005:
1003:
1000:
998:
995:
993:
990:
988:
985:
983:
979:
978:
974:
973:
971:
967:
960:
957:
955:
952:
950:
947:
945:
942:
940:
936:
935:
931:
930:
928:
925:
920:
917:
914:
909:
905:
901:
896:
892:
888:
880:
875:
873:
868:
866:
861:
860:
857:
849:
845:
841:
840:
836:
828:
827:public domain
809:
807:
801:
795:
793:
791:
787:
783:
782:public domain
764:
762:
756:
750:
747:
742:
738:
732:
729:
724:
720:
716:
712:
708:
704:
700:
696:
689:
686:
682:
681:public domain
663:
661:
655:
649:
647:
645:
643:
641:
639:
637:
635:
633:
631:
629:
627:
625:
623:
621:
619:
617:
615:
611:
604:
602:
600:
596:
591:
588:
586:
578:
576:
574:
570:
565:
563:
558:
552:
550:
547:
542:
538:
536:
532:
528:
514:
509:
505:
498:
489:
485:
478:
471:
467:
466:
464:
461:
456:
449:
447:
443:
416:
414:
410:
405:
397:
393:
389:
388:
386:
377:
373:
366:
365:ChEMBL3414621
362:
361:
359:
357:
353:
346:
342:
339:
335:
334:
332:
330:
326:
319:
315:
314:
312:
310:
306:
299:
295:
294:
292:
290:
286:
279:
275:
274:
272:
270:
266:
259:
255:
254:
252:
245:
241:
234:
230:
229:
227:
225:
221:
213:
209:
205:
198:
193:
187:
177:
176:
174:
172:
168:
163:
155:
150:
147:
146:
144:
142:
138:
131:
127:
117:
114:
109:
100:
99:
97:
95:
91:
87:
83:
81:
77:
73:
69:
67:
63:
59:
55:
51:
47:
45:
41:
38:Clinical data
36:
32:
27:
19:
3033:Orphan drugs
3028:Chemotherapy
2617:Overview of
2485:Tazemetostat
2484:
2449:Alitretinoin
2442:
2353:Estramustine
2333:Elsamitrucin
2323:Eflornithine
2277:Pegaspargase
2273:Asparaginase
2266:
2235:Testolactone
2228:
2216:
2204:
2158:
2143:Panobinostat
2126:
2096:
2084:
2072:
2060:
2031:
1996:
1984:
1937:
1933:Padeliporfin
1872:Dactinomycin
1868:Streptomyces
1849:Temozolomide
1844:Mitozolomide
1832:
1823:Mitobronitol
1812:Procarbazine
1805:
1793:Nonclassical
1718:
1695:
1689:Streptozocin
1654:Nitrosoureas
1652:
1626:Chlorambucil
1620:Trofosfamide
1606:Chlormethine
1601:Bendamustine
1594:
1532:Mitoxantrone
1527:Losoxantrone
1520:
1480:Daunorubicin
1463:
1429:
1366:Camptothecin
1354:
1310:
1280:
1266:
1249:
1233:Fluorouracil
1213:Capecitabine
1206:
1176:
1140:
1126:
1096:
1091:Pralatrexate
1081:Methotrexate
1069:
1012:
975:
932:
847:
812:. Retrieved
803:
767:. Retrieved
758:
749:
740:
731:
698:
694:
688:
666:. Retrieved
657:
592:
589:
582:
566:
553:
543:
539:
530:
527:Tazemetostat
526:
525:
233:1403254-99-8
211:
171:Legal status
165:Legal status
113:Tazemetostat
94:License data
23:Tazemetostat
18:
2965:Cancer pain
2905:Cancer cell
2650:Hyperplasia
2560:from market
2530:Vorasidenib
2510:Trabectedin
2495:Tiazofurine
2490:Tebentafusp
2475:Tagraxofusp
2433:Plitidepsin
2403:Mitoguazone
2343:Epacadostat
2313:Demecolcine
2257:Aflibercept
2230:Sex steroid
2103:Fuzuloparib
2044:Carfilzomib
2016:Palbociclib
2006:Abemaciclib
1959:Verteporfin
1923:Efaproxiral
1839:Dacarbazine
1801:Altretamine
1783:Satraplatin
1778:Oxaliplatin
1758:Carboplatin
1735:Triaziquone
1706:Mannosulfan
1684:Ranimustine
1664:Fotemustine
1505:Pirarubicin
1490:Doxorubicin
1484:+cytarabine
1470:Aclarubicin
1431:Podophyllum
1356:Camptotheca
1287:Azacitidine
1273:Gemcitabine
1228:Floxuridine
1161:Fludarabine
1156:Clofarabine
1142:Halogenated
1133:Pentostatin
1108:Raltitrexed
1076:Aminopterin
1019:Ixabepilone
1014:Epothilones
982:Cabazitaxel
959:Vinorelbine
944:Vincristine
939:Vinblastine
924:microtubule
814:22 February
599:orphan drug
453: gยทmol
195:Identifiers
80:MedlinePlus
53:Other names
44:Trade names
3012:Categories
2910:Carcinogen
2774:Urogenital
2715:Topography
2696:Metastasis
2660:Pseudocyst
2634:Conditions
2525:Verdinexor
2520:Venetoclax
2423:Oblimersen
2418:Navitoclax
2393:Lucanthone
2388:Lonidamine
2378:Lifileucel
2373:Ivosidenib
2368:Imetelstat
2338:Enasidenib
2328:Elesclomol
2293:Bexarotene
2288:Belzutifan
2223:Bexarotene
2211:Atrasentan
2186:Umbralisib
2181:Idelalisib
2171:Copanlisib
2153:Vorinostat
2148:Romidepsin
2138:Entinostat
2133:Belinostat
2091:Masoprocol
2079:Tiazofurin
2067:Anagrelide
2039:Bortezomib
2026:Seliciclib
2021:Ribociclib
2001:inhibitors
1991:Tipifarnib
1954:Temoporfin
1949:Talaporfin
1887:Plicamycin
1882:Mitomycins
1828:Pipobroman
1807:Hydrazines
1773:Nedaplatin
1725:Carboquone
1720:Aziridines
1711:Treosulfan
1659:Carmustine
1646:Uramustine
1615:Ifosfamide
1587:Alkylating
1548:Bisantrene
1537:Pixantrone
1510:Valrubicin
1500:Idarubicin
1495:Epirubicin
1441:Teniposide
1396:Lurtotecan
1391:Irinotecan
1292:Decitabine
1256:Cytarabine
1199:Pyrimidine
1188:Tioguanine
1178:Thiopurine
1167:Nelarabine
1151:Cladribine
1103:Pemetrexed
1086:Pemetrexed
1062:Folic acid
1002:Paclitaxel
954:Vinflunine
769:17 January
668:23 January
605:References
458:3D model (
446:Molar mass
318:Q40W93WPE1
289:ChemSpider
224:CAS Number
204:IUPAC name
2929:Oncovirus
2919:oncogenes
2872:Ann Arbor
2815:Papilloma
2800:Carcinoma
2793:Histology
2737:laryngeal
2681:Dysplasia
2665:Hamartoma
2570:Phase III
2558:Withdrawn
2535:Vosaroxin
2515:Veliparib
2470:Sotorasib
2460:Selinexor
2454:Tretinoin
2444:Retinoids
2358:Glasdegib
2303:Celecoxib
2252:Adagrasib
2176:Duvelisib
2166:Alpelisib
2121:Rucaparib
2108:Niraparib
2049:Oprozomib
2011:Alvocidib
1877:Bleomycin
1834:Triazenes
1818:Etoglucid
1763:Cisplatin
1679:Nimustine
1673:Semustine
1669:Lomustine
1631:Melphalan
1558:Menogaril
1553:Crisnatol
1543:Amsacrine
1515:Zorubicin
1475:Amrubicin
1436:Etoposide
1411:Topotecan
1406:Silatecan
1401:Rubitecan
1386:Gimatecan
1371:Cositecan
1361:Belotecan
1037:inhibitor
1007:Tesetaxel
997:Ortataxel
992:Larotaxel
987:Docetaxel
949:Vindesine
583:The U.S.
567:The U.S.
549:inhibitor
72:Monograph
66:Drugs.com
3002:Medicine
2950:Research
2810:Blastoma
2627:oncology
2408:Mitotane
2348:Eribulin
2116:Olaparib
2054:Ixazomib
1730:Thiotepa
1702:Busulfan
1381:Exatecan
1218:Carmofur
926:assembly
889: /
723:52010283
715:30112706
531:Tazverik
298:30208713
269:DrugBank
258:66558664
141:ATC code
130:Tazverik
108:DailyMed
56:EPZ-6438
48:Tazverik
2960:History
2859:grading
2855:Staging
2820:Adenoma
2805:Sarcoma
1337:S phase
1238:Tegafur
1052:S phase
977:Taxanes
913:M phase
579:History
451:572.750
413:Formula
278:DB12887
244:PubChem
157:)
151: (
149:L01XX72
128::
110::
86:a620018
2988:Portal
2691:Cancer
2623:cancer
2619:tumors
2553:WHO-EM
2162:(Pi3K)
1119:Purine
922:Block
721:
713:
557:lysine
484:SMILES
356:ChEMBL
345:D11444
338:D11485
186:โ-only
184:
123:
106:
2943:Misc.
2829:Other
2769:Blood
2074:IMPDI
1969:Other
808:(FDA)
804:U.S.
763:(FDA)
759:U.S.
719:S2CID
662:(FDA)
658:U.S.
562:tumor
504:InChI
460:JSmol
2975:Diet
2764:Skin
2759:Bone
2727:oral
2655:Cyst
2625:and
2160:PIKI
2128:HDAC
1577:CCNS
816:2020
771:2021
711:PMID
670:2020
597:and
546:EZH2
329:KEGG
309:UNII
62:AHFS
2867:TNM
2206:ERA
2062:PhI
2033:PrI
1998:CDK
1910:PDT
908:MIs
904:SPs
895:L01
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