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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 1.

LSD1 inhibitors in clinical/preclinical trials.

S. No LSD1 Inhibitor Mode of Action Single/Dual Inhibitor Indications Phase Trial Number/Ref Status
1 Bomedemstat
(IMG-7289)
Irreversible Single Inhibitor AML
SCLC
AML
Phase I
Phase I
Phase I
NCT05597306
NCT05191797
NCT02842827
Recruiting
Recruiting
Completed
2. SP2509/SP2577 Reversible Single Inhibitor ES
Advanced Solid Tumors
Gynecologic Cancers
ES, CCS, LGFMS, SEF, EMC, AFH
Phase I
Phase I
Phase I
Phase I/II
NCT03600649
NCT03895684
NCT04611139
NCT05266196
Recruiting
Completed
Withdrawn
Enrolling
3. GSK2879552 Irreversible Single Inhibitor SCLC
MDS
Leukemia
Phase I
Phase I
Phase I
NCT02034123
NCT02929498
NCT02177812
Terminated
Terminated
Terminated
4. Tranylcypromine Irreversible Single inhibitor AML
AML

AML
Phase I
Phase I
Phase I
NCT02273102
NCT02261779
NCT02717884
Completed
Unknown
Unknown
5. ORY-1001 Irreversible Single Inhibitor AML
AML
SCLC
AML
Phase I
Phase II
Phase II
Phase I
NCT05546580
2018–000482-36
2018–000469-35
2013–002447-29
Recruiting
Completed
Completed
Completed
6 Corin Irreversible Dual Inhibitor
LSD1/HDACs
NSCLC Phase II NCT02264210 Recruiting
7 INCB059872 Irreversible Single Inhibitor Solid Tumors
Solid Tumors,
Hematologic Malignancy
Relapsed ES
Phase II
Phase I
Phase I
NCT02959437
NCT02712905
NCT03514407
Terminated
Terminated
Terminated
8 GSK-LSD1 Irreversible Single Inhibitor BC
HCC
Pre-Clinical
Pre-Clinical
86
20
-
9 JBI-097 Irreversible Dual Inhibitor
LSD1/HDAC6
MM, Leukaemia Pre-Clinical 62 -
10 ZY0511 Reversible Single Inhibitor HCC, CC Pre-Clinical 94, 99 -
11 GSK690 Reversible Single Inhibitor NA NA 69 -
12 NCD38 Irreversible Single Inhibitor GBM, EC Pre-Clinical 45,88 -
13 Compound 5 Reversible NA NA NA 64 -
14 Pargyline Irreversible Single
inhibitor
KC Pre-Clinical 97 -
15 MC_2580 DDP_38003 Irreversible Single inhibitor AML Pre-Clinical 76 -
16 Clorgyline Irreversible Single
inhibitor
PC Pre-Clinical 98 -