Drug intelligence / Profile preview

letrozole + pictilisib

Development stage
Unknown
Lead developer
Genentech
Modality
Small Molecules
Administration
Oral
01

Overview

Letrozole + pictilisib is an investigational combination therapy consisting of two small molecule drugs used in the treatment of breast cancer. Letrozole is a nonsteroidal aromatase inhibitor that suppresses estrogen synthesis by inhibiting the aromatase enzyme, thereby reducing estrogen-driven tumor growth in hormone receptor-positive breast cancer. Pictilisib (GDC-0941) is a pan-phosphatidylinositol 3-kinase (PI3K) inhibitor that blocks PI3K signaling, a pathway frequently activated in cancers and associated with resistance to endocrine therapies. The combination aims to enhance antitumor activity by simultaneously targeting estrogen production and PI3K-mediated survival pathways. This regimen has been evaluated primarily for patients with locally recurrent or metastatic breast cancer[1][3].

02

Targets

PI3K (Phosphoinositide-3-kinase regulatory subunit 6)CYP19A1 (Aromatase)

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