A Phase 1B Study to Evaluate the Safety and Pharmacology of the Dual PI3K-MTOR Inhibitor GDC-0980 in Combination with a Fluoropyrimidine, Oxaliplatin, and Bevacizumab (BEV) in Patients with Advanced Solid Tumors

Rosen, Lee S.; Goldman, Jonathan H.; Stewart, S.; Hubbard, Joleen M.; Roos, Michelle; Lin, WT; Shankar, Geetha; Capdevila, Jaume; Freas, Elizabeth; Leong, Stephen

doi:10.1016/s0923-7534(20)33010-6

Cited by 3 publications

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“…This phase I study concluded that GDC-0980 has a narrow therapeutic window, and dose of 40 mg 28/28 days was reasonably tolerated. More recently, a single arm, open-label trial phase II study in recurrent or persistent endometrial carcinoma patients reported that anti-tumor activity of 40 mg GDC-0980 daily was limited by tolerability, especially in diabetic patients, and patients with mutations of PI3K pathway may benefit more from GDC-0980 [91].…”

Section: Gdc-0980 (Apitolisib Rg7422)mentioning

confidence: 99%

Targeting PI3K in cancer: mechanisms and advances in clinical trials

et al. 2019

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Phosphatidylinositol-3-kinase (PI3K)/AKT/mammalian target of rapamycin (mTOR) signaling is one of the most important intracellular pathways, which can be considered as a master regulator for cancer. Enormous efforts have been dedicated to the development of drugs targeting PI3K signaling, many of which are currently employed in clinical trials evaluation, and it is becoming increasingly clear that PI3K inhibitors are effective in inhibiting tumor progression. PI3K inhibitors are subdivided into dual PI3K/mTOR inhibitors, pan-PI3K inhibitors and isoform-specific inhibitors. In this review, we performed a critical review to summarize the role of the PI3K pathway in tumor development, recent PI3K inhibitors development based on clinical trials, and the mechanisms of resistance to PI3K inhibition.

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Section: Gdc-0980 (Apitolisib Rg7422)mentioning

confidence: 99%