DS-7423

DS-7423 is a novel, orally administered small-molecule dual inhibitor of phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin (mTOR). It potently inhibits PI3Kα (IC50 = 15.6 nM) and mTOR (IC50 = 34.9 nM), with less activity against other class I PI3K isoforms. The drug was developed as an antineoplastic agent targeting the frequently activated PI3K/mTOR pathway in various solid tumors, including ovarian clear cell adenocarcinoma, prostate cancer, colorectal cancer, endometrial carcinoma, and other advanced solid malignancies. Preclinical studies demonstrated anti-tumor activity through inhibition of cell proliferation and induction of TP53-dependent apoptosis in TP53 wild-type cells. Clinical development reached phase I trials but was discontinued after evaluation[1][2][5][6][7].