Relugolix

Relugolix
Clinical data
Pronunciation/ˌrɛlʊˈɡoʊlɪks/
RE-luu-GOH-liks
Trade namesOrgovyx, Relumina
Other namesRGX; RVT-601; TAK-385
AHFS/Drugs.comMonograph
MedlinePlusa621006
License data
Routes of
administration		By mouth[1]
Drug classGnRH antagonist
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding68–71%[1]
Elimination half-life36 to 65 hours[1]
ExcretionFeces: 82%[1]
Urine: 4%[1]
Identifiers
  • 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
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC29H27F2N7O5S
Molar mass623.64 g·mol−1
3D model (JSmol)
  • CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nn2)c(=O)n3Cc2c(F)cccc2F)cc1
  • InChI=1S/C29H27F2N7O5S/c1-36(2)14-19-24-26(39)38(22-12-13-23(42-3)34-33-22)29(41)37(15-18-20(30)6-5-7-21(18)31)27(24)44-25(19)16-8-10-17(11-9-16)32-28(40)35-43-4/h5-13H,14-15H2,1-4H3,(H2,32,35,40)
  • Key:AOMXMOCNKJTRQP-UHFFFAOYSA-N

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 in men and uterine fibroids in women.[5][1][7] It is taken by mouth.[1][7]

Side effects of relugolix include menstrual abnormalities, hot flashes, excessive sweating, headache, and decreased bone mineral density.[7][1] Relugolix is a GnRH antagonist, or an antagonist of the gonadotropin-releasing hormone receptor.[1] Unlike most other GnRH modulators, but similarly to elagolix (brand name Orilissa), relugolix is a non-peptide, small-molecule compound and is orally active.[8][9][10] It suppresses sex hormone levels to the postmenopausal or castrate range in both women and men.[1][11][5]

Relugolix was approved for use for the treatment of uterine fibroids in Japan in January 2019, and for the treatment of prostate cancer in the United States in December 2020.[12][13]

  1. ^ a b c d e f g h i j Barra F, Seca M, Della Corte L, Giampaolino P, Ferrero S (August 2019). "Relugolix for the treatment of uterine fibroids". Drugs of Today. 55 (8): 503–512. doi:10.1358/dot.2019.55.8.3020179. PMID 31461087. S2CID 201654739.
  2. ^ "Therapeutic Goods (Poisons Standard—June 2024) Instrument 2024". Federal Register of Legislation. 30 May 2024. Retrieved 10 June 2024.
  3. ^ "Notice: Multiple additions to the Prescription Drug List (PDL) [2023-12-22]". Health Canada. 22 December 2023. Retrieved 3 January 2024.
  4. ^ "Summary Basis of Decision (SBD) for Orgovyx". Health Canada. 16 February 2024. Retrieved 24 February 2024.
  5. ^ a b c "Orgovyx- relugolix tablet, film coated". DailyMed. Retrieved 25 May 2021.
  6. ^ Cite error: The named reference Orgovyx EPAR was invoked but never defined (see the help page).
  7. ^ a b c "Relumina (relugolix) Information" (PDF). ASKA Pharmaceutical (in Japanese). January 2019. Archived from the original (PDF) on 16 February 2019. Retrieved 16 February 2019.
  8. ^ Cite error: The named reference pmid21657270 was invoked but never defined (see the help page).
  9. ^ Cite error: The named reference pmid24333551 was invoked but never defined (see the help page).
  10. ^ Cite error: The named reference pmid29232843 was invoked but never defined (see the help page).
  11. ^ Cite error: The named reference pmid26502357 was invoked but never defined (see the help page).
  12. ^ "Relugolix - Myovant/Takeda". AdisInsight. Springer Nature Switzerland AG.
  13. ^ Cite error: The named reference PRNewswire2019 was invoked but never defined (see the help page).