venetoclax

Ligand id: 8318

Name: venetoclax

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 10
Hydrogen bond donors 3
Rotatable bonds 14
Topological polar surface area 180.41
Molecular weight 867.32
XLogP 8.56
No. Lipinski's rules broken 2

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Venetoclax (in combination with and in comparison with currently approved anti-neoplastics) was assessed in Phase III clinical trials as a potential treatment for chronic lymphocytic leukemia (CLL). See NCT02005471 and NCT02242942 for full details.
In January 2016, the US FDA granted venetoclax (in combination with hypomethylating agents) breakthrough designation as a first-line treatment for patients with acute myeloid leukemia (AML) who are ineligible to receive high-dose chemotherapy.

Full marketing authorisation: In April 2016, the US FDA granted full approval for venetoclax as an oral treatment regimen for patients with chronic lymphocytic leukemia (CLL) with 17p deletion (detected by an FDA-approved test), who have received at least one prior therapy.
Mechanism Of Action and Pharmacodynamic Effects
Venetoclax selectively inhibits the ability of the Bcl-2 protein to sequester its pro-apoptotic family members, thereby restoring the apoptotic balance in cells with aberrant Bcl-2 activity. Venetoclax does not inhibit Bcl-xL, so does not exhibit the anti-platelet side-effect of previously investigated non-selective Bcl-2 inhibitors (eg navitoclax; research code ABT-263).