Relugolix is an oral GnRH receptor antagonist for androgen deprivation therapy in the treatment of advanced prostate cancer. Relugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist used in the treatment of several hormone-responsive conditions.
- Mechanism
- Curator reviewed · 3 references
The pathogenesis and progression of prostate cancer appear driven, at least in part, by the effects of testosterone. Androgen deprivation has been demonstrated to result in cell death and tumor regression in many well-differentiated prostate cancer cell lines - for this reason, androgen deprivation therapy (ADT) has become a standard in the treatment of prostate cancer, particularly in advanced disease.
Testosterone production in males is carried out in the Leydig cells of testes and is stimulated by luteinizing hormone (LH), which itself is produced in the pituitary gland following the binding of gonadotropin-releasing hormone (GnRH) to corresponding GnRH receptors. Relugolix is a competitive antagonist of these GnRH receptors, thereby decreasing the release of LH and, ultimately, testosterone.
- Primary indication
- Relugolix is indicated for the treatment of adult patients with advanced prostate cancer.Curator reviewed · 5 structured indications
- Formula / weight
- C29H27F2N7O5S · 623.64 g/mol (avg)
- First approval
- Canada, 2025 · United States, 2020 · European Union, 2021
- Code names
- RVT-601 · TAK-385
- Brand names
Resolves to
AOMXMOCNKJTRQP-UHFFFAOYSA-NSMILESCONC(=O)NC1=CC=C(C=C1)C1=C(CN(C)C)C2=C(S1)N(CC1=C(F)C=CC=C1F)C(=O)N(C2=O)C1=CC=C(OC)N=N1What you can answer from here — as of June 15, 2026
Which drugs share a target with Relugolix, and which of those have an active Phase 3 trial?
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