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. Author manuscript; available in PMC: 2024 Dec 30.
Published in final edited form as: Expert Opin Ther Targets. 2023 Dec 30;27(12):1177–1188. doi: 10.1080/14728222.2023.2288277

Table 2.

List of LSD1 inhibitors in combination with other anticancer drugs.

S.No LSD1 KD/ Inhibitor Combination Drug Class of drug combination Indication Ref

1 GSK-LSD1 Doxorubicin Alkylant agent Breast Cancer 86
anti-PD-1 Immunotherapy HCC 20
AC1Q3QWB HOTAIR-EZH2 Inhibitor Glioblastoma 73

2. Bomedemstat (IMG-7289) anti-PD-1 Immunotherapy Small Cell Lung Cancer 22
Venetoclax BCL-2 Inhibitor HSC-derived leukemias 82

3. SP2509 Panobinostat HDAC inhibitor Acute myeloid leukemia 67
Tazemetostat EZH2 Inhibitor Acute myeloid leukemia 81
Romidepsin HDAC inhibitor Ewing Sarcoma 66
Etoposide Topoisomerase II inhibitor Ewing Sarcoma 66
Verteporfin YAP inhibitor OSCC 19
anti-PD-1 Immunotherapy HNSCC, OSCC, TNBC 18, 19, 36
JQ1 BET bromodomain inhibitor CRPC 83
Sulforaphane HDAC inhibitor Breast Cancer 68
EPZ6438 EZH2 Inhibitor Acute myeloid leukemia 81
Docetaxel Taxans Prostate cancer 84
Regorafenib Multi-kinase inhibitor HCC 91

4. JBI-097 Dual inhibitor LSD1 Inhibitor HDAC6, and Leukemia SCLC Melanoma HCC Multiple Myeloma 62

5. GSK2879552 anti-PD-1 Immunotherapy Colorectal cancer Melanoma 35
Sorafenib Multikinase Inhibitor HCC 92
ATRA Retinoids Acute myeloid leukemia 74

6 ZY0511 DTP3 Vaccine HCC 94
5-fluorouracil Anti-metabolites Colorectal cancer 99

7 GSK690 JNJ-26481585 HDAC inhibitor Rhabdomyosarcoma 69

8 Ex917 Vorinostat HDAC inhibitor Rhabdomyosarcoma 69

9 LSD1 KD Vorinostat HDAC inhibitor Glioblastoma 71
anti-PD-1 Immunotherapy Melanoma, 23
UVA radiation Radiation Skin Cancer 52

10 Tranylcypromine Vorinostat HDAC inhibitor Glioblastoma 71,72
ATRA Retinoids Acute myeloid leukemia 75
Tranylcypromine (Compound 7) Dual inhibitor HDAC1/2, and LSD1 Inhibitor Gastric cancer, Breast cancer, Colorectal cancer, Lung cancer, Prostate cancer 61
OG-86 (Tranylcypromin e -derivatives) RAD001 mTOR Inhibitor Acute myeloid leukemia 79

11 ORY-1001 anti-PD-1 Immunotherapy SCLC 21
anti-CD47/PD-L1 Immunotherapy Cervical Cancer 30
Ruxolitinib JAK inhibitor Acute myeloid leukemia 78
I-BET-762 BET inhibitor CRPC 83

12 NCD38 Temozolomide Alkylant agent Glioblastoma 45
Rapamycin mTOR Inhibitor Endometrial cancer 88

13 Compound 5 Dual inhibitor HDAC/LSD1 Inhibitor Gastric cancer 64

14 Corin Dual inhibitor HDAC/LSD1 Inhibitor DIPG 65

15 Pargyline Vorinostat HDAC inhibitor TNBC 70
Enzalutamide Androgen Receptor Inhibitor Kidney Cancer 97

16 MC_2580 DDP_38003 ATRA Retinoids Acute myeloid leukemia 76

17 INCB059872 OTX-015 BET inhibitor Acute myeloid leukemia 77

18 Clorgyline 5-Aza-CdR DNMT inhibitor Bladder Cancer 98