Drug intelligence / Profile preview

LOXO-783 + abemaciclib + imlunestrant

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

Overview

LOXO-783 + abemaciclib + imlunestrant is an investigational oral combination regimen studied primarily in advanced or metastatic breast cancer with PIK3CA mutation[5]. The components target distinct oncogenic pathways: - **LOXO-783** is a small molecule inhibitor designed to selectively inhibit mutant phosphoinositide 3-kinase alpha (PIK3CA), implicated in cancer cell growth and survival[1][3][5][7]. - **Abemaciclib** is a selective cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitor, used to block cell cycle progression, approved for HR-positive, HER2-negative breast cancer[2][4][6][8]. - **Imlunestrant** is an oral selective estrogen receptor degrader (SERD) that antagonizes and degrades the estrogen receptor (ESR1), inhibiting hormone receptor signaling in breast cancers expressing estrogen receptor. This combination aims to provide multi-pathway blockade in PIK3CA-mutant, hormone receptor-positive, HER2-negative breast cancer, and is in early clinical development as part of a multicohort phase 1 trial[5].

Other names
imlunestrant
02

Targets

PIK3CA H1047R (Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha (PIK3CA), H1047R mutant)CDK6 (Cyclin-dependent kinase 6)CDK4 (Cyclin-dependent kinase 4)ER (Estrogen receptor)

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