Drug intelligence / Profile preview

bicalutamide + triptorelin

Development stage
Unknown
Lead developer
European Organisation for the Research and Treatment of Cancer
Modality
Peptides, Small Molecules
Administration
Oral, Intramuscular
01

Overview

Bicalutamide + triptorelin is a combination therapy consisting of two active ingredients: bicalutamide, a nonsteroidal antiandrogen that blocks androgen receptors, and triptorelin, a gonadotropin-releasing hormone (GnRH) agonist. This combination is primarily used for androgen deprivation therapy (ADT) in the treatment of hormone-sensitive cancers. Triptorelin acts by initially stimulating and then downregulating GnRH receptors in the pituitary gland, leading to a profound suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion, which subsequently reduces testosterone production to castrate levels. Bicalutamide is added to competitively inhibit the binding of residual androgens to the androgen receptor, thereby preventing the 'testosterone flare' often associated with GnRH agonist initiation and providing a more complete blockade of the androgen signaling pathway. This combination is currently being evaluated in clinical trials for androgen receptor-positive (AR+) recurrent or metastatic salivary gland cancer and is a standard approach in metastatic prostate cancer management.

Brand names
CasodexTrelstarDecapeptylGonapeptyl
Other names
bicalutamide and triptorelinbicalutamide/triptorelinADT
02

Targets

GnRHR (Gonadotropin-releasing hormone receptor)AR (Adrenergic receptors)

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