Drug intelligence / Profile preview

PF-04691502

Development stage
Phase 2
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral
01

Overview

PF-04691502 is a potent, orally bioavailable small molecule that acts as an ATP‐competitive dual inhibitor of phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR), key kinases in the PI3K/mTOR signaling pathway. By inhibiting both PI3K and mTOR, it disrupts downstream signaling involved in cell growth, survival, and resistance to therapy. This results in apoptosis and growth inhibition of cancer cells with aberrant activation of this pathway. The drug was developed by Pfizer for potential antineoplastic activity and has been investigated primarily for various cancers including breast cancer and endometrial cancer[1][2][3][4].

Other names
2-amino-8-((1r,4r)-4-(2-hydroxyethoxy)cyclohexyl)-6-(6-methoxypyridin-3-yl)-4-methylpyrido[2,3-d]pyrimidin-7(8H)-one
02

Targets

mTOR (Mammalian target of rapamycin kinase)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CD (Phosphatidylinositol 3-kinase delta)

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