Drug intelligence / Profile preview

PF-05212384 + irinotecan

Development stage
Discontinued
Lead developer
Pfizer
Modality
Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

PF-05212384 (gedatolisib, also known as PKI-587) is an investigational, intravenous, dual inhibitor of phosphoinositide 3‑kinase (PI3K) and mammalian target of rapamycin (mTOR), developed for the treatment of advanced solid tumors. When combined with irinotecan—a topoisomerase I inhibitor chemotherapy—the regimen aims to enhance antitumor activity by targeting both cell signaling pathways involved in tumor growth and DNA replication. This combination has been studied primarily in patients with advanced or metastatic colorectal cancer, particularly those with KRAS and NRAS wild-type tumors. Clinical trials have shown a modest response rate (~5%) and some clinical benefit in this population[1][2][3]. The combination is administered intravenously on a repeating cycle schedule.

Other names
PKI-587 + irinotecangedatolisib + irinotecan
02

Targets

TOP1 (DNA Topoisomerase I)mTOR (Mammalian target of rapamycin kinase)PIK3CA (Phosphoinositide 3-kinase alpha)

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