BH3-mimetics in clinical trials for various tumour types. The chemical structures are shown in Figure 3. Note that only the completed clinical trials in which the compounds were used as single agents are reported. For ongoing clinical trials visit https://clinicaltrials.gov/. The bibliographic references refer to the discovery, the synthesis, and/or the patenting of the compounds
Compound | Type of cancer | Clinical trials | References |
---|---|---|---|
ABT-199 (venetoclax) | Chronic lymphocytic leukaemia (CLL); acute myeloid leukaemia (AML); non-Hodgkin lymphoma (NHL); Waldenstrom macroglobulinemia |
| [59] |
APG-2575 (lisaftoclax) | Waldenstrom macroglobulinemia |
| [60] |
S55746 | CLL; B-Cell NHL; multiple myeloma (MM) |
| [61] |
A-1155463 | Preclinical | - | [62] |
A-1331852 | Preclinical | - | [63] |
WEHI-539 | Preclinical | - | [64] |
ABT-263 (navitoclax) | Ovarian cancer; small cell lung carcinoma; CLL; leukaemias; lymphomas; solid tumours; lymphoid malignancies; NHL |
| [65, 66] |
ABT-737 | Ovarian cancer |
| [67] |
S63845 | Preclinical | - | [51] |
S64315 | MM; diffuse large B-cell lymphoma (DLBCL); AML; myelodysplastic syndrome (MDS) |
| [68, 69] |
VU661013 | Preclinical | - | [70, 71] |
AZD-5991 | Relapsed or refractory AML |
| [72] |
AMG-176 | Higher risk MDS; Chronic myelomonocytic leukaemia; relapsed or refractory MM or AML |
| [52, 73] |
AM-8621 | Preclinical | - | [52, 73] |
TW-37 | Preclinical | - | [74] |
*: clinical trials in which the compound was used exclusively in combination regimen with other chemotherapeutic drugs; -: no data
AV and RDM: Conceptualization, Validation, Writing—original draft, Writing—review & editing, Supervision. DL: Validation, Writing—review & editing. All authors read and approved the submitted version.
The authors declare that they have no conflicts of interest.
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© The Author(s) 2024.