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retaspimycin

Development stage: Phase 3
Lead developer: Infinity Pharmaceuticals
Modality: Small Molecules
Administration: Intravenous

Overview

Retaspimycin is a small molecule inhibitor of heat shock protein 90 (Hsp90), developed primarily as an anticancer agent by Infinity Pharmaceuticals. It is a hydroquinone hydrochloride salt derivative of 17-AAG (tanespimycin), designed to improve solubility and pharmacokinetics compared to earlier Hsp90 inhibitors. Retaspimycin binds to the ATP-binding domain of Hsp90, inhibiting its chaperone function and leading to the degradation of multiple oncogenic client proteins involved in cancer cell growth and survival. The drug was investigated for use in various cancers, including non-small cell lung cancer and gastrointestinal stromal tumors.

Other names: retaspimycin hydrochlorideIPI-504IPI504IPI 504

Targets

HSP90 (Heat shock protein 90 chaperone complex)GRP94 (Endoplasmin)

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