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gemcitabine + cisplatin + everolimus
- Development stage
- Phase 2
- Lead developer
- Novartis
- Modality
- Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Gemcitabine + cisplatin + everolimus is a combination chemotherapy regimen investigated primarily for advanced and metastatic solid tumors such as urothelial carcinoma (bladder cancer), triple-negative breast cancer (TNBC), cholangiocarcinoma, and gallbladder carcinoma. - **Gemcitabine** is a nucleoside analog that inhibits DNA synthesis by incorporating into DNA during replication and causing chain termination. - **Cisplatin** is a platinum-based chemotherapeutic agent that forms DNA crosslinks and induces apoptosis in rapidly dividing cells. - **Everolimus** is an mTOR inhibitor that blocks the mammalian target of rapamycin pathway (PI3K/AKT/mTOR), which regulates cell growth and proliferation; this pathway is often dysregulated in various cancers. The combination aims to enhance antitumor efficacy by targeting both cell division (gemcitabine/cisplatin) and cellular signaling pathways involved in tumor growth (everolimus). This regimen has been evaluated in phase I/II clinical trials to determine safety, maximum tolerated dose, dose-limiting toxicities (primarily hematologic), and preliminary efficacy[1][2][5].
- Other names
- GPE regimenGC plus everolimus
02
Targets
RRM1Mechanistic target of rapamycin complex 1Pt-DNA adduct (DNA-oxaliplatin adduct)
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