Overview

Generic Name(s):
venetoclax
Trade Name(s):
Venclexta
NCI Definition [1]:
An orally bioavailable, selective small molecule inhibitor of the anti-apoptotic protein Bcl-2, with potential antineoplastic activity. Venetoclax mimics BH3-only proteins, the native ligands of Bcl-2 and apoptosis activators, by binding to the hydrophobic groove of Bcl-2 proteins thereby repressing Bcl-2 activity and restoring apoptotic processes in tumor cells. Bcl-2 protein is overexpressed in some cancers and plays an important role in the regulation of apoptosis; its expression is associated with increased drug resistance and tumor cell survival. Compared to the Bcl-2 inhibitor navitoclax, this agent does not inhibit bcl-XL and does not cause bcl-XL-mediated thrombocytopenia.

Venetoclax has been investigated in 212 clinical trials, of which 192 are open and 20 are closed. Of the trials investigating venetoclax, 1 is early phase 1 (1 open), 66 are phase 1 (58 open), 56 are phase 1/phase 2 (49 open), 66 are phase 2 (63 open), 2 are phase 2/phase 3 (1 open), and 21 are phase 3 (20 open).

PML-RARA Fusion, t(15;17)(q22;q12), and t(15;17)(q24;q21) are the most frequent biomarker inclusion criteria for venetoclax clinical trials.

Acute myeloid leukemia, chronic lymphocytic leukemia, and myelodysplastic syndromes are the most common diseases being investigated in venetoclax clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Venetoclax
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Venetoclax
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating venetoclax and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
gdc-0199, abt-0199, abt199, rg7601, venetoclax, 4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl)methyl)piperazin-1-yl)-n-((3-nitro-4-((tetrahydro-2h-pyran-4-ylmethyl)amino)phenyl)sulfonyl)-2-(1h-pyrrolo(2,3-b)pyridin-5-yloxy)benzamide, venetoclax, venetoclax (substance), 4-(4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl)methyl)piperazin-1-yl)-n-((3-nitro-4-((tetrahydro-2h-pyran-4-ylmethyl)amino)phenyl)sulfonyl)-2-(1h-pyrrolo(2,3-b)pyridin-5-yloxy)benzamide, bcl-2 inhibitor gdc-0199, abt-199, Venclexta
Drug Categories [2]:
BCL inhibitors/BCL-2 inhibitors
Drug Target(s) [2]:
BCL2
NCIT ID [1]:
C103147
SNOMED ID [1]:
R0-006C7

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.