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Tazemetostat

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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. 396: 31: 2997: 822: 777: 676: 540:
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
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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
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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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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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U.S. National Library of Medicine. 152: 1146:ribonucleotide reductase inhibitors 343: 336: 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" 2995: 820: 775: 674: 664:(Press release). 23 January 2020 429: 423: 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 2983: 2982: 2970:Cancer and nausea 2849: 2848: 2686:Carcinoma in situ 2584: 2583: 2543: 2542: 2500:Tigilanol tiglate 1977:Enzyme inhibitors 1900: 1899: 1896: 1895: 1596:Nitrogen mustards 1566: 1565: 1326: 1325: 1028: 1027: 810:. 23 January 2020 524: 523: 470:Interactive image 376:CompTox Dashboard 183: 122: 105: 16:Chemical compound 3040: 3000: 2999: 2998: 2991: 2784:Endocrine system 2749:Digestive system 2638: 2611: 2604: 2597: 2588: 2505:Tisagenlecleucel 2262:Arsenic trioxide 1973: 1906:Photosensitizers 1697:Alkyl sulfonates 1611:Cyclophosphamide 1583: 1522:Anthracenediones 1343: 1317:Hydroxycarbamide 1058: 1041: 919: 879: 872: 865: 856: 851: 830: 824: 823: 819: 817: 815: 796: 785: 779: 778: 774: 772: 770: 751: 745: 744: 733: 727: 726: 690: 684: 678: 677: 673: 671: 669: 650: 472: 452: 437: 431: 425: 419: 399: 398: 384: 382: 367: 347: 340: 320: 300: 280: 260: 250: 249: 235: 181: 178: 156: 132: 121: 118: 115: 104: 101: 88: 74: 33: 26: 24: 3048: 3047: 3043: 3042: 3041: 3039: 3038: 3037: 3008: 3007: 3006: 2996: 2994: 2986: 2984: 2979: 2938: 2891: 2845: 2824: 2788: 2710: 2669: 2629: 2615: 2585: 2580: 2579: 2564:Clinical trials 2539: 2245:Other/ungrouped 2240: 2191: 1964: 1944:Porfimer sodium 1892: 1854: 1787: 1744: 1574: 1562: 1446: 1416: 1334: 1322: 1297: 1193: 1113: 1049: 1047:antimetabolites 1045: 1044:DNA precursors/ 1036: 1034:DNA replication 1024: 964: 934:Vinca alkaloids 910: 898: 883: 842: 839: 834: 833: 821: 813: 811: 798: 797: 788: 776: 768: 766: 753: 752: 748: 735: 734: 730: 692: 691: 687: 675: 667: 665: 652: 651: 612: 607: 581: 520: 517: 512: 507: 506: 495: 492: 487: 486: 475: 450: 440: 434: 428: 422: 402: 392:DTXSID201025831 378: 370: 350: 323: 303: 283: 263: 246: 238: 218: 215: 207: 206: 190: 160: 135: 17: 12: 11: 5: 3046: 3044: 3036: 3035: 3030: 3025: 3020: 3010: 3009: 3005: 3004: 2981: 2980: 2978: 2977: 2972: 2967: 2962: 2957: 2952: 2946: 2944: 2940: 2939: 2937: 2936: 2931: 2926: 2921: 2912: 2907: 2901: 2899: 2897:Carcinogenesis 2893: 2892: 2890: 2889: 2884: 2879: 2874: 2869: 2863: 2861: 2851: 2850: 2847: 2846: 2844: 2843: 2838: 2832: 2830: 2826: 2825: 2823: 2822: 2817: 2812: 2807: 2802: 2796: 2794: 2790: 2789: 2787: 2786: 2781: 2779:Nervous system 2776: 2771: 2766: 2761: 2756: 2751: 2746: 2745: 2744: 2742:nasopharyngeal 2739: 2734: 2729: 2718: 2716: 2712: 2711: 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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„ž-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 703:doi 381:EPA 248:CID 154:WHO 126:FDA 3014:: 2621:, 2566:: 2086:LI 1986:FI 1452:II 1422:II 1244:)) 846:. 802:. 789:^ 757:. 739:. 717:. 709:. 699:13 697:. 656:. 613:^ 575:. 427:44 421:34 180:US 120:US 103:US 2990:: 2917:/ 2857:/ 2610:e 2603:t 2596:v 2456:) 2447:( 2279:) 2275:/ 2271:( 2237:) 2233:( 2225:) 2221:( 2213:) 2209:( 2188:) 2164:( 2155:) 2131:( 2123:) 2101:( 2093:) 2089:( 2081:) 2077:( 2069:) 2065:( 2028:) 2004:( 1993:) 1989:( 1961:) 1942:( 1908:/ 1889:) 1870:( 1851:) 1837:( 1814:) 1810:( 1722:: 1713:) 1704:( 1699:: 1675:) 1671:( 1656:: 1637:) 1633:( 1622:) 1613:( 1598:: 1579:) 1575:( 1539:) 1525:( 1517:) 1486:) 1482:( 1468:( 1454:+ 1443:) 1434:( 1413:) 1359:( 1347:I 1339:) 1335:( 1319:) 1315:( 1294:) 1285:( 1275:) 1271:( 1261:) 1254:( 1240:( 1211:( 1190:) 1181:( 1163:) 1149:( 1144:/ 1135:) 1131:( 1110:) 1101:( 1093:) 1074:( 1054:) 1050:( 1021:) 1017:( 1009:) 980:( 961:) 937:( 915:) 911:( 906:/ 897:) 893:( 878:e 871:t 864:v 829:. 818:. 784:. 773:. 725:. 705:: 683:. 672:. 462:) 439:4 436:O 433:4 430:N 424:H 418:C 383:) 379:( 212:N 182:: 64:/

Index


Trade names
AHFS
Drugs.com
Monograph
MedlinePlus
a620018
License data
DailyMed
Tazemetostat
FDA
Tazverik
ATC code
L01XX72
WHO
Legal status
โ„ž-only
IUPAC name
CAS Number
1403254-99-8
PubChem
66558664
DrugBank
DB12887
ChemSpider
30208713
UNII
Q40W93WPE1
KEGG
D11485

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