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. 2021 Oct 20;24(10):705–713. [Article in Chinese] doi: 10.3779/j.issn.1009-3419.2021.102.34

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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).