AO-252

AO-252 is an orally bioavailable small‑molecule inhibitor of transforming acidic coiled-coil containing protein 3 (TACC3) that disrupts TACC3-mediated protein–protein interactions, thereby impairing mitotic spindle function and tumor cell proliferation in TACC3/TP53‑altered cancers.[1][3][6][9] Discovered via phenotypic screening and rational design and originally developed by OncoCube Therapeutics, the program is now led by A2A Pharmaceuticals as a first‑in‑class, first‑in‑human targeted antineoplastic agent for advanced solid tumors, with an emphasis on TP53‑mutated triple‑negative breast cancer, high‑grade serous ovarian/endometrial and related gynecologic malignancies.[1][2][3][4][6] In preclinical xenograft models, AO‑252 has shown robust tumor growth inhibition or regression across multiple tumor types, and it is currently being evaluated in a Phase 1 dose‑escalation and expansion study to define safety, pharmacokinetics, pharmacodynamics, and preliminary efficacy in patients with advanced or metastatic solid tumors.[1][2][3][4][5][6][9]

Other names

TACC3 PPI inhibitor AO-252TACC-3 PPI inhibitor AO-252TACC 3 PPI inhibitor AO-252