Drug intelligence / Profile preview

GDC-0980 + capecitabine

Development stage
Phase 1
Lead developer
Genentech
Modality
Small Molecules
Administration
Oral
01

Overview

GDC-0980 + capecitabine is a combination therapy under clinical investigation for advanced solid tumors, including colorectal cancer. GDC-0980 (apitolisib) is a small molecule dual inhibitor targeting class I phosphatidylinositol-3-kinase (PI3K) and mammalian target of rapamycin (mTOR), which are key components in the PI3K/AKT/mTOR pathway, a signaling axis frequently dysregulated in cancer. Capecitabine is an oral prodrug of 5-fluorouracil (5-FU), a widely used chemotherapeutic agent that inhibits thymidylate synthase, interfering with DNA synthesis and repair. The rationale for this combination is to simultaneously disrupt cancer cell survival signaling and impair DNA synthesis, thereby synergistically inhibiting tumor growth. This combination has been investigated in phase I clinical trials for advanced solid tumors and colorectal cancer[3].

Other names
apitolisib + capecitabine
02

Targets

PI3K (Phosphoinositide-3-kinase regulatory subunit 6)TS (Thymidylate synthase)mTOR (Mammalian target of rapamycin kinase)

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