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表观遗传相关抗肿瘤药物(数据来自ClinicalTrials.gov收集截止至2021年8月22日)
Epigenetic drugs against cancer (data collected by ClinicalTrials.gov as of August 22, 2021)
| Target | Regulation | Drugs | NCT number (cancer types) |
| DNMT: DNA methyltransferase; BET: bromodomain and extra-terminal domain; HDAC: histone deacetylase; EZH: enhancer of zeste homolog; LSD1: lysine-specific histone demethylase 1A; NSCLC: non-small cell lung cancer; MDS: myelodysplastic syndrome; AML: acute myeloid leukemia; CML: chronic myeloid leukemia; EC: esophageal carcinoma; MPM: malignant pleural mesothelioma; SCLC: small cell lung cancer; OC: ovarian cancer; BC: bladder cancer; MM: multiple myeloma; NHL: non-hodgkin lymphoma; NMC: NUT midline carcinoma; BRC: breast cancer; ALL: acute lymphocytic leukemia; MF: myelofibrosis; GBM: glioblastoma; GVHD: graft versus host disease; PC: prostate cancer; RCC: renal cell carcinoma; MCC: merkel cell carcinoma; HL: Hodgkin lymphoma; PV: polycythemia vera; ET: essential thrombocythemia; UC: urothelial carcinoma; EBV: Epstein-Barr virus; HNC: head and neck cancer; HCC: hepatocellular carcinoma; CRC: colorectal carcinoma; PTCL: peripheral T-cell lymphoma; BCL: B-cell lymphoma; VS: vestibular schwannoma; DLBCL: diffuse large B-cell lymphoma; FL: follicular lymphoma. | |||
| DNA methylation | |||
| DNMT | Writer | Azacitidine | 02009436 (NSCLC), 01928576 (NSCLC), 01926587 (MDS, AML, CML), etc. |
| Decitabine | 03233724 (NSCLC, EC, MPM), 02996474 (AML), 00744757 (MDS), etc. | ||
| Guadecitabine | 03913455 (SCLC), 01696032 (OC), 02348489 (AML), etc. | ||
| NTX-301 | 04167917 (AML, MDS, CML), 04851834 (OC, BC). | ||
| Histone modification-acetylation | |||
| BET | Reader | Molibresib | 01943851 (MM, AML, NHL, MDS), 01587703 (NMC), 02964507 (BRC), etc. |
| Birabresib | 02259114 (Solid tumors), 02698189 (AML), 01713582 (AML, ALL, MM, NHL), etc. | ||
| AZD5153 | 03205176 (Solid tumors), 03527147 (NHL). | ||
| BMS-986158 | 03936465 (Pediatric cancer), 04817007 (MF), 02419417 (Advanced cancer), etc. | ||
| CC-90010 | 04324840 (GBM), 03220347 (Solid tumors, NHL), etc. | ||
| CPI-0610 | 04603495 (MF), 02157636 (MM), 01949883 (Lymphoma), etc. | ||
| FT-1101 | 02543879 (AML, MDS, NHL). | ||
| INCB057643 | 04279847 (MF), 02959437 (Solid tumors). | ||
| ODM-207 | 03035591 (Solid tumors). | ||
| PLX51107 | 04022785 (AML, MDS), 04910152 (GVHD). | ||
| RO6870810 | 02308761 (AML, MDS), 03068351 (MM), 01987362 (Solid tumors), etc. | ||
| SYHA1801 | 04309968 (Solid tumors). | ||
| ZEN-3694 | 02711956 (PC), 03901469 (BRC), 04840589 (Solid tumors), etc. | ||
| HDAC | Eraser | Abexinostat | 00724984 (Lymphoma), 03592472 (RCC), 01543763 (Solid tumors), etc. |
| Belinostat | 01310244 (NSCLC), 00926640 (SCLC), 00413075 (Solid tumor, lymphoma), etc. | ||
| Bisthianostat | 03618602 (MM). | ||
| Chidamide | 01836679 (NSCLC), 04582955 (BRC), 02697552 (NHL), etc. | ||
| Citarinostat | 02886065 (MM). | ||
| Domatinostat | 04874831 (MCC), 04871594 (UC), 04133948 (Melanoma), etc. | ||
| Entinostat | 00602030 (NSCLC), 02833155 (BRC), 03179930 (Lymphoma), etc. | ||
| Givinostat | 00792467 (HL), 01901432 (PV), 00606307 (PV, ET, MF), etc. | ||
| Mocetinostat | 03220477 (NSCLC), 00359086 (Lymphoma), 02236195 (UC), etc. | ||
| Nanatinostat | 05011058 (EBV+lymphoma). | ||
| Panobinostat | 04326764 (AML, MDS), 00738751 (NSCLC, HNC), 01242774 (AML), etc. | ||
| Pracinostat | 03151304 (MDS), 01912274 (AML), 01112384 (Sarcoma), etc. | ||
| Quisinostat | 02728492 (NSCLC, OC), 02948075 (OC), 00677105 (Solid tumors, lymphoma), etc. | ||
| Resminostat | 01037478 (HL), 02400788 (HCC), 01277406 (CRC), etc. | ||
| Ricolinostat | 02632071 (BRC), 02091063 (Lymphoma), 02189343 (MM), etc. | ||
| Romidepsin | 01302808 (NSCLC), 00086827 (SCLC), 01822886 (PTCL), etc. | ||
| Tacedinaline | 00005093 (NSCLC), 00005624 (MM), 00004861 (Pancreatic cancer). | ||
| Tefinostat | 00820508 (Hematological disease, Lymphoid malignancies), 02759601 (HCC). | ||
| Tinostamustine | 03903458 (Melanoma), 02576496 (Hematological malignancies), 03345485 (Solid tumors), etc. | ||
| Trichostatin A | 03838926 (Hematologic malignancies), etc. | ||
| Valproic acid | 00084981 (NSCLC), 02124174 (AML, MDS), 02068586 (Melanoma), etc. | ||
| Vorinostat | 02151721 (NSCLC), 03263936 (AML), 03742245 (BRC), etc. | ||
| AR-42 | 02569320 (MM), 02282917 (VS, meningiomas), 01798901 (AML), etc. | ||
| CXD101 | 01977638 (Solid tumors, lymphoma, MM). | ||
| HG146 | 03710915 (MM), 04977167 (Solid tumors, lymphoma). | ||
| KA2507 | 03008018 (Solid tumors). | ||
| OKI-179 | 03931681 (Solid tumors). | ||
| Histone modification-methylation | |||
| EZH | Writer | Lirametostat | 02395601 (BCL), 03525795 (Solid tumors), 03480646 (PC). |
| Tazemetostat | 02860286 (MPM), 04624113 (HNC), 04846478 (PC), etc. | ||
| Valemetostat | 04703192 (PTCL), 04842877 (BCL), 04388852 (PC, RCC, UC). | ||
| CPI-0209 | 04104776 (Solid tumors, lymphoma). | ||
| HH2853 | 04390737 (Solid tumors, NHL). | ||
| MAK683 | 02900651 (DLBCL). | ||
| PF-06821497 | 03460977 (SCLC, PC, FL, DLBCL). | ||
| SHR2554 | 04407741 (Solid tumors, lymphoma), 03603951 (Mature lymphoid neoplasms), 04355858 (BRC). | ||
| LSD1 | Eraser | Seclidemstat | 03600649 (Ewing or Ewing-related Sarcomas), 04734990 (CML, MDS), 03895684 (Solid tumors). |
| Tranylcypromine | 02261779 (AML), 02717884 (AML, MDS), etc. | ||
| CC-90011 | 03850067 (SCLC), 04628988 (PC), 02875223 (Solid tumors, NHL), etc. | ||
| IMG-7289 | 04262141 (ET, PV), 02842827 (AML, MDS), etc. | ||
| INCB059872 | 02712905 (Solid tumors and Hematologic malignancies). | ||