Drug intelligence / Profile preview

dasatinib + venetoclax

Development stage
Phase 2
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

Dasatinib + venetoclax is an investigational oral combination regimen of dasatinib, a second-generation BCR-ABL1 tyrosine kinase inhibitor (TKI), and venetoclax, a selective BCL-2 inhibitor. The combination is being studied primarily for the treatment of Philadelphia chromosome-positive leukemias including chronic myeloid leukemia in chronic phase (CML-CP) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL). Dasatinib inhibits BCR-ABL1 kinase activity, directly targeting the leukemic driver, while venetoclax blocks the anti-apoptotic BCL-2 protein, promoting apoptosis of malignant cells. Preclinical and early clinical evidence indicates that dual inhibition may lead to deeper molecular responses than TKIs alone, and may help reduce the population of immature leukemic stem cells. The combination is being explored in phase 1 and phase 2 clinical trials and shows a manageable safety profile, with neutropenia as a notable adverse effect that can be mitigated by dose adjustments[1][2][3][6][7][8].

02

Targets

BCL-2 (BCL-2 family)ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)

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