Drug intelligence / Profile preview

letrozole + taselisib

Development stage
Phase 2
Lead developer
Genentech
Modality
Small Molecules
Administration
Oral
01

Overview

Letrozole + taselisib is a combination of two small molecule drugs used in the neoadjuvant treatment of hormone receptor-positive, HER2-negative early breast cancer. Letrozole is an aromatase inhibitor that reduces estrogen production, thereby inhibiting the growth of estrogen-dependent breast cancer cells. Taselisib is an oral, potent, and selective phosphoinositide 3-kinase (PI3K) inhibitor with enhanced activity against PIK3CA-mutant cancer cells. The combination was evaluated in the phase II LORELEI trial, which demonstrated that adding taselisib to letrozole increased objective response rates compared to letrozole alone in postmenopausal women with ER-positive/HER2-negative early breast cancer[1][3][5]. The most common adverse events were gastrointestinal disorders, infections, and skin-subcutaneous tissue disorders[1].

Other names
letrozoleGDC-0032 + letrozole
02

Targets

CYP19A1 (Aromatase)PIK3CA (Phosphoinositide 3-kinase alpha)

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