Drug intelligence / Profile preview

DEBIO 0932 + cisplatin + pemetrexed

Development stage
Unknown
Lead developer
Debiopharm
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination regimen consisting of **DEBIO 0932**, a second-generation oral small molecule inhibitor of heat shock protein 90 (Hsp90), with the standard chemotherapeutic agents **cisplatin** and **pemetrexed**. DEBIO 0932 selectively binds to the N-terminal ATP-binding pocket of Hsp90, inhibiting its chaperone function, leading to the degradation of multiple oncogenic client proteins and resulting in tumor growth inhibition. Hsp90 inhibition targets numerous pro-survival signaling pathways commonly overactive in cancer. The combination with cisplatin and pemetrexed, both DNA-damaging chemotherapeutics commonly used in non-small cell lung cancer (NSCLC), is intended to improve anti-tumor efficacy by simultaneously targeting multiple mechanisms crucial to tumor cell survival and proliferation. Preclinical studies and early-phase clinical trials indicate synergistic anti-tumor effects of DEBIO 0932 with such standard of care regimens[5][4][9]. The combination is being evaluated in Phase I/II clinical trials for NSCLC and other advanced solid tumors[4][5].

Other names
debio 0932 + cisplatin + pemetrexed
02

Targets

GART (GAR transformylase)HSP90 (Heat shock protein 90 chaperone complex)DNADHFR (Dihydrofolate reductase)TS (Thymidylate synthase)

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