Table 2.
Histone methyltransferase/demethylase inhibitors.
| Chemical class | Compound | Clinical stage | Cancer specificity | Reference/NCT number |
|---|---|---|---|---|
| G9a substrate competitive inhibitor | BIX01294 | Preclinical | Breast cancer, myeloid leukemia | 197, 198 |
| UNC0638 | Preclinical | Breast cancer | 199 | |
| A-366 | Preclinical | Leukemia | 200 | |
| G9a inhibitor | BRD4770 | Preclinical | Pancreatic cancer | 201 |
| SMYD2 inhibitor | AZ505 | Preclinical | Polycystic kidney | 202 |
| LLY-507 | Preclinical | Esophageal, liver | 179 | |
| DOT1L inhibitor | EPZ-5676 | Phase I | Leukemia | NCT02141828 |
| SYC-552 | Preclinical | Leukemia | 181 | |
| EZH2 inhibitor | EPZ005687 | Preclinical | Lymphoma | 203 |
| UNC1999 | Preclinical | Lymphoma | 204 | |
| GSK343 | Preclinical | Breast cancer, prostate cancer | 205 | |
| CPI-1205 | Phase I and II | B cell lymphoma, solid tumor | NCT02395601 | |
| GSK2816126 | Phase I | Cancer, neoplasm | NCT02082977 | |
| EI1 | Preclinical | Lymphoma | 206 | |
| Tazemetostat | FDA approved (2020) | Epithelioid sarcoma | NCT02875548 | |
| EPZ6438 | Phase I and II | Solid and hematological tumors | NCT01897571 | |
| DZNeo | Preclinical | Solid tumor, glioblastoma | 207 | |
| DS-3201 | Phase I and II | Leukemia, small cell lung carcinoma, lymphoma | NCT04388852 | |
| PF-06821497 | Phase I | small cell lung carcinoma | NCT03460977 | |
| MAK683 | Phase I and II | Lymphoma, advanced solid tumor | NCT02900651 | |
| SHR2554 | Phase I | Prostate cancer, lymphoid neoplasm | NCT04407741 | |
| PRMT1 inhibitor | DB75 | Phase I and II | Leukemia | NCT00408369 |
| PRMT4 inhibitor | TP-064 | Preclinical | Multiple myeloma | 208 |
| PRMT5 inhibitor | GSK3326595 | Phase I and II | Solid tumor, lymphoma | NCT03614728 |
| JNJ-64619178 | Phase I | Solid and hematological tumors | NCT03573310 | |
| PF-06939999 | Phase I | Advanced or metastatic solid tumor | NCT03854227 | |
| LSD1 inhibitor | Tranylcypromine | Phase I and II | Solid and hematological tumors | NCT02273102 |
| Bizine | Preclinical | Lung cancer, prostate cancer | 209 | |
| PG11144 | Preclinical | Breast cancer | 210 | |
| Namoline | Preclinical | Prostate cancer | 211 | |
| ORY-1001 | Preclinical | Acute leukemia | 212 | |
| GSK2879552 | Phase I and II | Small cell lung cancer, acute myeloid leukemia | NCT02177812 | |
| CC-90011 | Phase I and II | Solid tumor and lymphoma | NCT04748848 | |
| INCB059872 | Phase I and II | Solid and hematological tumors | NCT02712905 | |
| IMG-7289 | Phase I and II | Acute myeloid leukemia | NCT02842827 | |
| KDM inhibitor | JIB-04 | Preclinical | Breast cancer | 213 |
| IOX1 | Preclinical | Esophageal squamous cell carcinoma | 214 |