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LY3023414 + enzalutamide
- Development stage
- Unknown
- Lead developer
- Eli Lilly
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
LY3023414 + enzalutamide is a combination therapy studied in metastatic castration-resistant prostate cancer. LY3023414 (also known as samotolisib) is an oral, potent, and selective ATP-competitive inhibitor of class I PI3K isoforms, mTOR (mammalian target of rapamycin) complexes 1 and 2, and DNA-dependent protein kinase (DNA-PK). Enzalutamide is an androgen receptor (AR) inhibitor that impairs AR nuclear translocation and DNA binding. This combination targets both the PI3K/mTOR signaling pathway and androgen signaling, which are frequently dysregulated in advanced prostate cancer. The regimen has been studied for safety and efficacy, with modest but significant improvements in progression-free survival observed in certain patient populations, particularly those lacking AR splice variant 7 or with intact PTEN.
- Other names
- samotolisib + enzalutamide
02
Targets
AR (Adrenergic receptors)PI3K (Phosphoinositide-3-kinase regulatory subunit 6)DNA-PK (DNA-dependent protein kinase)Mechanistic target of rapamycin kinase complex 2
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