Drug intelligence / Profile preview

retaspimycin + everolimus

Development stage
Phase 2
Lead developer
Infinity Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Retaspimycin + everolimus is an investigational combination therapy consisting of **retaspimycin HCl (IPI-504)**, a potent small molecule inhibitor of **Heat Shock Protein 90 (Hsp90)**, and **everolimus**, a small molecule inhibitor of **mechanistic target of rapamycin (mTOR)**. This combination is being evaluated primarily for the treatment of solid tumors, specifically KRAS-mutant non-small cell lung cancer (NSCLC). Retaspimycin targets the chaperone protein Hsp90, leading to degradation of client oncoproteins, while everolimus allosterically inhibits mTORC1, suppressing cellular growth and proliferation pathways. This dual targeting approach aims to overcome resistance mechanisms linked to KRAS mutations and PI3K/mTOR pathway activation[1][4].

Other names
retaspimycin HCl + everolimus
02

Targets

HSP90AA1 (Heat shock protein HSP90-alpha)Mechanistic target of rapamycin complex 1

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