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

CompoundType of cancerClinical trialsReferences
ABT-199 (venetoclax)Chronic lymphocytic leukaemia (CLL); acute myeloid leukaemia (AML); non-Hodgkin lymphoma (NHL); Waldenstrom macroglobulinemia
  • NCT05909553

  • NCT04810598

  • NCT04171791

  • NCT03873857

  • NCT03552692

  • NCT02980731

  • NCT02756611

  • NCT02677324

  • NCT02141282

  • NCT01994837

  • NCT01969695

  • NCT01889186

  • NCT01328626

[59]
APG-2575 (lisaftoclax)Waldenstrom macroglobulinemia
  • NCT04260217

[60]
S55746CLL; B-Cell NHL; multiple myeloma (MM)
  • NCT02920697

[61]
A-1155463Preclinical-[62]
A-1331852Preclinical-[63]
WEHI-539Preclinical-[64]
ABT-263 (navitoclax)Ovarian cancer; small cell lung carcinoma; CLL; leukaemias; lymphomas; solid tumours; lymphoid malignancies; NHL
  • NCT02591095

  • NCT01557777

  • NCT00982566

  • NCT00743028

  • NCT00481091

  • NCT00445198

  • NCT00406809

[65, 66]
ABT-737Ovarian cancer
  • NCT01440504

[67]
S63845Preclinical-[51]
S64315MM; diffuse large B-cell lymphoma (DLBCL); AML; myelodysplastic syndrome (MDS)
  • NCT02992483

  • NCT02979366

[68, 69]
VU661013Preclinical-[70, 71]
AZD-5991Relapsed or refractory AML
  • NCT03218683

[72]
AMG-176Higher risk MDS; Chronic myelomonocytic leukaemia; relapsed or refractory MM or AML
  • NCT05209152*

  • NCT02675452*

  • NCT03797261*

[52, 73]
AM-8621Preclinical-[52, 73]
TW-37Preclinical-[74]

*: clinical trials in which the compound was used exclusively in combination regimen with other chemotherapeutic drugs; -: no data