LOXO-783 + abemaciclib + anastrozole + exemestane + letrozole

This drug is a **combination regimen** comprised of LOXO-783, abemaciclib, anastrozole, exemestane, and letrozole, under investigation for the treatment of advanced or metastatic breast cancer and other solid tumors harboring the PIK3CA H1047R mutation. - **LOXO-783** is an investigational, oral, allosteric, brain-penetrant inhibitor highly selective for the PI3Kα H1047R mutant, developed to improve tolerability and efficacy versus nonselective PI3K inhibitors by sparing wild-type PI3Kα and the associated toxicities such as hyperglycemia and rash[1][3][5]. - **Abemaciclib** is a small-molecule inhibitor of cyclin-dependent kinases 4 and 6 (CDK4/6), used mainly in hormone receptor-positive, HER2-negative breast cancer, and blocks cell cycle progression by preventing retinoblastoma protein phosphorylation[4][6]. - **Anastrozole, exemestane, and letrozole** are nonsteroidal and steroidal aromatase inhibitors that reduce estrogen synthesis, thereby inhibiting growth of hormone receptor-positive breast cancers. The regimen targets **multiple pathways driving tumor growth and survival**, including PI3Kα signaling and estrogen-dependent proliferation. Clinical trials are investigating the safety, tolerability, and efficacy of this multi-agent approach, particularly for patients with breast cancer carrying the PIK3CA H1047R mutation[1][3][5][7].

Other names

LOXO-783LOXO783LOXO 783abemaciclibanastrozoleexemestaneletrozole