Drug intelligence / Profile preview

GDC-0980 + pemetrexed + cisplatin

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

Overview

GDC-0980 + pemetrexed + cisplatin is a combination investigational cancer therapy regimen. **GDC-0980 (apitolisib)** is a small molecule dual inhibitor targeting both class I phosphatidylinositol-3-kinase (PI3K) and mammalian target of rapamycin (mTOR) kinases, designed to block key pathways involved in tumor cell growth and survival[7][4]. **Pemetrexed** is a folate antimetabolite that inhibits several folate-dependent enzymes essential for DNA and RNA synthesis, approved for non-small cell lung cancer and malignant pleural mesothelioma[3][6]. **Cisplatin** is a platinum-based chemotherapeutic agent that forms DNA crosslinks, leading to apoptosis of rapidly dividing cells and commonly used in various solid tumors[3][6]. The combination has been considered to potentiate antitumor activity by synergistically inhibiting tumor growth, particularly in research and early-phase clinical development settings for solid tumors. GDC-0980 is being developed by Genentech/Roche[7]; pemetrexed is developed and manufactured by Eli Lilly, and cisplatin is generic, with numerous manufacturers. GDC-0980 has been studied alone in solid tumors and endometrial carcinoma, but combination studies with pemetrexed and cisplatin (for example, in NSCLC or mesothelioma) are preclinical or early clinical and not standard of care.

Other names
apitolisib + pemetrexed + cisplatin
02

Targets

mTOR (Mammalian target of rapamycin kinase)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)GART (GAR transformylase)DHFR (Dihydrofolate reductase)DNATS (Thymidylate synthase)

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