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PF-05212384 + irinotecan
- Development stage
- Unknown
- Lead developer
- Pfizer
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding 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
PIK3CA (Phosphoinositide 3-kinase alpha)mTOR (Mammalian target of rapamycin kinase)TOP1 (DNA Topoisomerase I)
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