PKI-179

PKI-179 is a second-generation, orally efficacious small molecule that acts as a dual inhibitor of phosphatidylinositol 3-kinase (PI3K), particularly the alpha isoform, and mammalian target of rapamycin (mTOR). By selectively inhibiting both mTOR and PI3Kα, PKI-179 disrupts the PI3K/AKT/mTOR signaling pathway, which is critical for tumor cell proliferation and survival. This mechanism confers potential antineoplastic activity. Preclinical studies have demonstrated pronounced tumor growth arrest in models such as MDA-361 human breast cancer xenografts. The drug was developed by Wyeth (later acquired by Pfizer) for oncology indications but its development was discontinued after early-phase clinical trials in cancer[1][2][3][4][5][8].

Other names

PI3Ka/mTOR inhibitor PKI-179PI 3-K/mTOR Inhibitor III