Drug intelligence / Profile preview

ABT-737

Development stage
Preclinical
Lead developer
Abbott
Modality
Small Molecules
Administration
Intraperitoneal (preclinical/animal Studies)
01

Overview

ABT-737 is a small molecule experimental drug that functions as a BH3 mimetic and potent inhibitor of anti-apoptotic Bcl-2 family proteins, specifically Bcl-2, Bcl-xL (BCL2L1), and Bcl-w. It was developed to induce apoptosis in cancer cells by binding to the hydrophobic groove of these proteins and disrupting their function in preventing programmed cell death. ABT-737 has demonstrated high affinity for its targets and significant preclinical efficacy against various hematologic malignancies (such as lymphoma, multiple myeloma, acute myeloid leukemia) and solid tumors in animal models. However, it is not orally bioavailable; this limitation led to the development of navitoclax (ABT-263), an orally available derivative. In addition to its antitumor activity, ABT-737 has been identified as a senolytic agent capable of selectively inducing apoptosis in senescent cells[1][2][5].

Other names
Benzamide, 4-(4-((4'-chloro(1,1'-biphenyl)-2-yl)methyl)-1-piperazinyl)-n-((4-(((1r)-3-(dimethylamino)-1-((phenylthio)methyl)propyl)amino)-3-nitrophenyl)sulfonyl)
02

Targets

Bcl-w (B-cell lymphoma 2-like 2)BCL2L1 (B-cell lymphoma-extra large protein)

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