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DRUG:

Bcl-2 Family Inhibitors

i
Other names: Bcl-2 Family Inhibitors
Associations
Trials
Company:
Infinity Pharma, Novartis
Drug class:
Bcl2 inhibitor
Related drugs:
Associations
Trials
over3years
[VIRTUAL] Identification of S65487/VOB560 as a potent and selective intravenous 2nd-generation BCL-2 inhibitor active in wild-type and clinical mutants resistant to Venetoclax (AACR 2021)
Strong and persistent tumor regression in xenograft models of lymphoid malignancies in mouse and rat were observed at well tolerated doses following weekly IV administration of S65487 in combination with the MCL-1-specific inhibitor, S64315/MIK665. Altogether, these data demonstrate that S65487/VOB560 has significant therapeutic potential against human lymphoid and myeloid malignancies as well as in patients with Venetoclax resistant leukemias. Clinical studies are currently ongoing with S65487/VOB560 (NCT03755154).
Clinical • IO biomarker
|
BCL2L1 (BCL2-like 1)
|
BCL2 mutation • BCL2 G101V
|
Venclexta (venetoclax) • Bcl-2 Family Inhibitors • MIK665 • S65487
4years
[VIRTUAL] Acquired Mutations in BAX Confer Resistance to BH3 Mimetics in Acute Myeloid Leukemia (ASH 2020)
Background: Recent randomized trials have demonstrated improvements in overall survival (OS) for the BCL-2 inhibitor venetoclax (VEN) in combination with azacitidine and low dose cytarabine in older unfit patients with AML...S63845 and S55746 were obtained from Servier/Novartis, A1155463 from G. Lessene (WEHI), venetoclax and cytarabine from Selleckchem... We identified the presence of BAX mutations in AML samples from patients progressing on VEN-containing regimens. We show that BAX, but not BAK loss in an AML cell line is associated with resistance to BH3-mimetic drug combinations resulting in reduced survival in AML xenograft models. In contrast, BAX deficiency does not impede the cytotoxic actions of conventional chemotherapy.
IO biomarker
|
BCL2L1 (BCL2-like 1)
|
BAX expression
|
Venclexta (venetoclax) • cytarabine • azacitidine • S63845 • S55746 • Bcl-2 Family Inhibitors