Table 1.
Information on BH3 Mimetics
| Compound | Inhibitory Profile | Approval/Clinical Trial Status in Adults | Example Clinical Trial | Achievable Nontoxic Cmax (nM) | Reference (PMID) | |||
|---|---|---|---|---|---|---|---|---|
| (Ki Cell Free Assays; nM) | ||||||||
| BCL-2 | BCL-XL | BCL-W | MCL-1 | |||||
| venetoclax | <0.01 | 48 | 245 | >440 | FDA approved (CLL; SLL) | n.a. | 2533 ± 1612 | 23291630; 32171069 |
| navitoclax | <1 | <0.05 | <1 | 550 | Phase 3 | NCT02591095 | 6607 ± 3262 | 18451170; 21094089 |
| (±40) | (ovarian cancer) | |||||||
| AZD4320 | 3.9 | 4.5 | n.a. | n.a. | Phase 1 (dendrimer conjugate; AZD0466) | NCT04214093 | n.a. | 32988967 |
| (Hematologic or Solid Tumors) | ||||||||
| APG-1252 (pelcitoclax) | 0.7 | <1 | n.a. | n.a. | Phase 1/2 | NCT03080311 | n.a. | 24901320 |
| NCT04210037 | ||||||||
| (SCLC, other solid tumors) | ||||||||
| AZD5991 | n.a. | n.a. | n.a. | 0.7 | Phase 1/2 | NCT03013998 | n.a. | 30559424 |
| (AML) | ||||||||
| A-1331852 | 6 | <0.01 | 4 | 142 | Preclinical | n.a. | n.a. | 25787766 |
| A-1155463 | 74 | <0.01 | 8 | >444 | Preclinical | n.a. | n.a. | 25787766 |
| A-1210477 | 132 | >660 | 2280 | <0.5 | Preclinical | n.a. | n.a. | 25590800 |
| S63845 | >10000 | >10000 | n.a. | <1.2 | Preclinical | n.a. | n.a. | 27760111 |
n.a.: not available.
Ki values below 1.5 nM indicating strong target inhibition are marked in bold.