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bicalutamide + triptorelin
- Development stage
- Phase 4
- Lead developer
- European Organisation for the Research and Treatment of Cancer
- Modality
- Small Molecules, Peptides
- 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
- Pamorelin
- Other names
- bicalutamide and triptorelinbicalutamide/triptorelinADT
02
Targets
AR (Adrenergic receptors)GnRHR (Gonadotropin-releasing hormone receptor)
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