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buparlisib + MK2206

Development stage: Preclinical
Lead developer: Adlai Nortye
Modality: Small Molecules
Administration: Oral

Overview

A combination therapy consisting of buparlisib (BKM120), an oral pan-class I phosphoinositide 3-kinase (PI3K) inhibitor, and MK2206, an AKT inhibitor. This combination targets two key components of the PI3K/AKT/mTOR signaling pathway, which is frequently dysregulated in various cancers. The dual inhibition approach aims to achieve more complete pathway blockade and potentially overcome resistance mechanisms that may develop with single-agent therapy.

Targets

PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)AKT2 (Rac-beta serine/threonine-protein kinase)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)PIK3CD (Phosphatidylinositol 3-kinase delta)mTOR (Mammalian target of rapamycin kinase)TUBB (Tubulin (alpha and beta subunits))

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