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relugolix

Structure via PubChem · Public domain (PubChem)

EntityQ21099000· pop 8· linked from 68 articles

Also known as TAK 385

Relugolix, sold under the brand names Orgovyx and Relumina among others, is a gonadotropin-releasing hormone antagonist (GnRH receptor antagonist) medication which is used in the treatment of prostate cancer, uterine fibroids and endometriosis. It is taken by mouth.

Chemical data

Formula
C29H27F2N7O5S
Molecular weight
623.6 g/mol
IUPAC name
1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
SMILES
CN(C)CC1=C(SC2=C1C(=O)N(C(=O)N2CC3=C(C=CC=C3F)F)C4=NN=C(C=C4)OC)C5=CC=C(C=C5)NC(=O)NOC
InChIKey
AOMXMOCNKJTRQP-UHFFFAOYSA-N
XLogP
3.2
Polar surface area
157 Ų
H-bond donors
2
H-bond acceptors
11
Formal charge
0

via PubChem

Drug data · ChEMBL

Max clinical phase
Approved
Molecule type
Small molecule
Admin. routes
oral
Indications
endometriosis, uterine fibroid, pain, prostate cancer

via ChEMBL · EBI

Wikidata facts

Mass
623.176244
Show 3 more facts
canonical SMILES
CN(C)CC1=C(SC2=C1C(=O)N(C(=O)N2CC3=C(C=CC=C3F)F)C4=NN=C(C=C4)OC)C5=CC=C(C=C5)NC(=O)NOC
chemical formula
C₂₉H₂₇F₂N₇O₅S
Commons category
Relugolix
Sources (3)

via Wikidata · CC0

~8 min read

Encyclopedic overview

15 sections
Contents
  • Medical uses
  • Available forms
  • Side effects
  • Pharmacology
  • Pharmacodynamics
  • Pharmacokinetics
  • Chemistry
  • Synthesis
  • History
  • Society and culture
  • Names
  • Legal status
  • References
  • Further reading
  • External links

Relugolix, sold under the brand names Orgovyx and Relumina among others, is a gonadotropin-releasing hormone antagonist (GnRH receptor antagonist) medication which is used in the treatment of prostate cancer, uterine fibroids and endometriosis. It is taken by mouth.

Side effects of relugolix include menstrual abnormalities, hot flashes, excessive sweating, headache, and decreased bone mineral density. Relugolix is a GnRH antagonist, or an antagonist of the gonadotropin-releasing hormone receptor. Unlike most other GnRH modulators, but similarly to elagolix (brand name Orilissa), relugolix is a non-peptide, small-molecule compound and is orally active. It suppresses sex hormone levels to the postmenopausal or castrate range in both women and men.

Excerpted from Wikipedia’s “relugolix” article, available under the CC BY-SA 4.0 licence.

Available in 7 languages

via Wikidata sitelinks · CC0