Drug intelligence / Profile preview

giredestrant + lhrh agonist

Development stage
Unknown
Lead developer
Roche
Modality
Small Molecules
Administration
Oral, Subcutaneous, Intramuscular
01

Overview

Giredestrant + LHRH agonist is a combination investigational therapy for estrogen receptor-positive (ER+), HER2-negative breast cancer, particularly in premenopausal women. Giredestrant is an oral, nonsteroidal selective estrogen receptor degrader (SERD) that acts as a potent antagonist and induces proteasome-mediated degradation of the estrogen receptor, even in wild-type and mutant forms such as ESR1. In this combination, giredestrant is administered with a luteinizing hormone-releasing hormone (LHRH) agonist, such as leuprolide, goserelin, or triptorelin, to suppress ovarian estrogen production, achieving effective endocrine therapy in premenopausal patients. This combination has been studied in phase I/Ib clinical trials for safety and efficacy, demonstrating robust ER antagonism and favorable tolerability. Giredestrant is under development primarily for breast cancer and has shown clinical benefit in patients who progressed on prior endocrine therapies[1][2][3].

02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)ESR1 (ERα)

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