Drug intelligence / Profile preview

tersolisib (Eli Lilly and Company)

Development stage
Discontinued
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

Tersolisib (LY3023414) is an orally bioavailable, small-molecule dual inhibitor of phosphoinositide 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR), developed by Eli Lilly. It targets all four isoforms of Class I PI3K (alpha, beta, delta, and gamma) as well as mTORC1 and mTORC2. By inhibiting these key components of the PI3K/AKT/mTOR signaling pathway, tersolisib aims to suppress tumor cell proliferation and induce apoptosis in various malignancies, including breast cancer and other solid tumors. Clinical development has primarily focused on its use in combination with other therapies, such as endocrine therapy for hormone receptor-positive, HER2-negative breast cancer, although several trials have been discontinued.

Other names
tersolisib hemihydrate
02

Targets

PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CD (Phosphatidylinositol 3-kinase delta)mTOR (Mammalian target of rapamycin kinase)

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