Relugolix: First global approval
Abstract
The orally active nonpeptide gonadotropin-releasing hormone (GnRH)-receptor antagonist relugolix (Relumina) is being developed by Takeda and ASKA Pharmaceutical as a treatment for various sex hormone related disorders. Relugolix was recently approved for marketing in Japan as a treatment for symptoms associated with uterine fibroids, and studies evaluating the efficacy of the drug as treatment for endometriosis-associated pain and prostate cancer are currently underway. This article summarizes the milestones in the development of relugolix leading to this first approval for the treatment of symptoms associated with uterine fibroids.
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Relugolix has a half-life of 37-42 h and is mainly metabolized by the liver.
“Relugolix has a half-life of 37–42 h and is mainly metabolized by the liver [104,117].”
From Endometriosis and Medical Therapy: From Progestogens to Progesterone Resistance to GnRH Antagonists: A Review (2021) · cites this paper as [117]
Cites
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Fluorine-containing pharmaceuticals approved by the FDA in 2020: Synthesis and biological activity
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- Authors
- Markham, A.
- Corresponding author
- Markham, Anthony
- Venue
- Drugs
- Published
- 2019-04
- Volume
- 79
- Issue
- 6
- Pages
- 675-679
- ISSN
- 0012-6667 (ISSN-L)
- 1179-1950
- OpenAlex
- W2925371413
- Cited by
- 60
- References
- 7
- Citations by year
- 2026: 4 · 2025: 6 · 2024: 13 · 2023: 11 · 2022: 12 · 2021: 7 · 2020: 3 · 2019: 3
- FWCI
- 6.80
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- www.springer.com/tdm (tdm)
- Locations
- Drugs (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Obstetrics and Gynecology › Uterine Myomas and Treatments
- Health Sciences › Medicine › Reproductive Medicine › Hypothalamic control of reproductive hormones
- Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Reproductive Health and Contraception
- Keywords
- relugolix, GnRH antagonist, uterine fibroids, endometriosis-associated pain, prostate cancer, drug approval, drug development milestones
- MeSH terms
- Adolescent, Adult, Aged, Dose-Response Relationship, Drug, Endometriosis, Female, Hormone Antagonists, Humans, Japan, Leiomyoma, Male, Middle Aged, Phenylurea Compounds, Prostatic Neoplasms, Pyrimidinones, Receptors, LHRH, Treatment Outcome, Drug Approval
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