^
Association details:
| Biomarker: | BCL2 G101V |
|---|---|
| Cancer: | Chronic Lymphocytic Leukemia |
| Drug: | sonrotoclax (BGB-11417) (Bcl2 inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Abstract 3077: Preclinical characterization of BGB-11417, a potent and selective Bcl-2 inhibitor with superior antitumor activities in haematological tumor models
Published date:
05/15/2020
Excerpt:
With longer term treatment, recurrent mutation G101V in Bcl-2 has been reported to mediate resistance to venetoclax in patients with CLL. Herein, we report the pharmacological properties of BGB-11417, a highly potent and selective BCL-2 inhibitor, in preclinical models. BGB-11417 potently inhibited both wildtype and G101V-mutated Bcl-2 in SPR binding assay with IC50 of 0.035 and 0.28 nM, respectively.
DOI:
10.1158/1538-7445.AM2020-3077
