Drug intelligence / Profile preview

TP197

Development stage
Preclinical
Lead developer
University of Southern California
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

TP197 is a novel small molecule triphenylphosphonium (TPP) salt analogue developed as a mitochondria-targeted anticancer agent. Identified through high-throughput cytotoxicity screening of a drug-like small molecule library, TP197 exhibits potent anti-proliferative activity in the low micromolar range across various cancer cell lines, including breast and pancreatic cancers. Its mechanism of action involves selective accumulation in the mitochondria of cancer cells, driven by the negative mitochondrial membrane potential. This localization leads to disrupted mitochondrial respiration, decreased oxygen consumption, and increased production of mitochondrial superoxide (reactive oxygen species), ultimately inducing cell cycle arrest and apoptosis. In preclinical studies, TP197 demonstrated significant in vivo tumor growth inhibition as a single agent in mouse xenograft models of human breast cancer (such as MDA-MB-435) with no observed systemic toxicities.

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