Drug intelligence / Profile preview

gedatolisib + FOLFIRI

Development stage
Unknown
Lead developer
Celcuity
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

**Gedatolisib + FOLFIRI** is a combination therapy consisting of gedatolisib, a dual pan-class I PI3K/mTOR inhibitor, and the FOLFIRI chemotherapy regimen (folinic acid [leucovorin], fluorouracil, and irinotecan)[1][3][5]. Gedatolisib inhibits the phosphatidylinositol-4,5-bisphosphate 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) pathways, disrupting key cellular signaling processes related to cell survival, proliferation, and metabolic regulation[5]. FOLFIRI contains irinotecan (a topoisomerase I inhibitor causing DNA strand breaks), fluorouracil (a thymidylate synthase inhibitor blocking DNA synthesis), and folinic acid (enhancer of fluorouracil activity; not cytotoxic itself)[1][2][4][6]. This combination is under early-phase clinical investigation for advanced/metastatic colorectal cancer and other solid malignancies for cases that are refractory to standard irinotecan-based therapies, aiming to overcome chemoresistance[3][5]. Gedatolisib is administered intravenously and is being studied in combination with FOLFIRI to provide synergistic anticancer effects by dual PI3K/mTOR pathway blockade and cytotoxic therapy[3][5].

Brand names
Camptosar (for irinotecan)none for the combination as a whole or for PF-05212384
Other names
irinotecan with fluorouracil and folinic acid plus gedatolisibirinotecan de Gramont plus gedatolisib
02

Targets

PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)TS (Thymidylate synthase)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)TOP1 (DNA Topoisomerase I)PIK3CA (Phosphoinositide 3-kinase alpha)mTOR (Mammalian target of rapamycin kinase)PIK3CD (Phosphatidylinositol 3-kinase delta)

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