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 |