Drug intelligence / Profile preview

birelentinib + venetoclax

Development stage
Preclinical
Lead developer
Equillium
Modality
Small Molecules
Administration
Oral
01

Overview

birelentinib + venetoclax is a combination therapy consisting of birelentinib (a small molecule inhibitor, also known as EQS-110, that selectively targets neurotrophic tyrosine kinase receptors) and venetoclax (a potent oral BCL-2 inhibitor). Venetoclax induces apoptosis in cancer cells by inhibiting the anti-apoptotic protein BCL-2, leading to cell death. Birelentinib, though not as widely established as venetoclax, is characterized as a targeted kinase inhibitor against Trk family neurotrophic receptors. This combination is being evaluated for synergistic antitumor effects, particularly in hematologic malignancies where BCL-2 dependence is prominent and Trk signaling has been implicated. Combination regimens like these are designed to block multiple pathways critical for cancer cell survival, potentially overcoming resistance to monotherapy and enhancing the induction of apoptosis. Venetoclax is developed and manufactured by AbbVie, and birelentinib's developer is Equillium.

Other names
birelentinibvenetoclax
02

Targets

BCL-2 (BCL-2 family)BTK (Bruton tyrosine kinase)LYN (LYN proto-oncogene, Src family tyrosine kinase)

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