Drug intelligence / Profile preview

cisplatin + docetaxel + gossypol

Development stage
Unknown
Lead developer
Third Military Medical University
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen consisting of three agents—cisplatin, docetaxel, and gossypol—investigated primarily for the treatment of advanced non-small cell lung cancer (NSCLC) with high expression of apurinic/apyrimidinic endonuclease 1 (APE1). - **Cisplatin** is a platinum-based chemotherapeutic that forms DNA crosslinks, leading to apoptosis in rapidly dividing cells. - **Docetaxel** is a taxane-class antineoplastic agent that stabilizes microtubules and inhibits their depolymerization, disrupting mitosis. - **Gossypol** is a natural polyphenolic compound known to inhibit APE1 and Bcl-2 family proteins; it acts as an inhibitor of DNA repair mechanisms and induces apoptosis. The rationale for this combination is that gossypol may sensitize tumor cells to chemotherapy by inhibiting APE1-mediated DNA repair pathways, potentially improving efficacy in patients with high APE1 expression[1][2][3][4].

02

Targets

APEX1 (DNA-apurinic apyrimidinic site lyase)BCL2L1 (B-cell lymphoma-extra large protein)DNATUBB (Tubulin (alpha and beta subunits))

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