Overview

Generic Name(s):
navitoclax
NCI Definition [1]:
An orally active, synthetic small molecule and an antagonist of a subset of the B-cell leukemia 2 (Bcl-2) family of proteins with potential antineoplastic activity. Navitoclax selectively binds to apoptosis suppressor proteins Bcl-2, Bcl-XL, and Bcl-w, which are frequently overexpressed in a wide variety of cancers, including those of the lymph, breast, lung, prostate, and colon, and are linked to tumor drug resistance. Inhibition of these apoptosis suppressors prevents their binding to the apoptotic effectors Bax and Bak proteins, thereby triggering apoptotic processes in cells overexpressing Bcl-2, Bcl-XL, and Bcl-w. This eventually reduces tumor cell proliferation.

Navitoclax has been investigated in 11 clinical trials, of which 11 are open and 0 are closed. Of the trials investigating navitoclax, 5 are phase 1 (5 open), 3 are phase 1/phase 2 (3 open), 1 is phase 2 (1 open), and 2 are phase 3 (2 open).

KMT2A Fusion, KMT2A-AFF1 Fusion, and KMT2A-ELL Fusion are the most frequent biomarker inclusion criteria for navitoclax clinical trials.

Myelofibrosis transformation in essential thrombocythemia, polycythemia vera, post-polycythemic myelofibrosis phase, and primary myelofibrosis are the most common diseases being investigated in navitoclax clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Navitoclax
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating navitoclax 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]:
abt263, bci-2 family protein inhibitor abt-263, a-855071.0, abt 263, bci-2 family protein inhibitor abt-263, navitoclax, abt-263
Drug Categories [2]:
BCL inhibitors/BCL-2 inhibitors
Drug Target(s) [2]:
BCL2, BCL2L1, BCL2L2
NCIT ID [1]:
C64776

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.