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Relugolix information


Relugolix
Clinical data
Pronunciation/ˌrɛlʊˈɡlɪks/
RE-luu-GOH-liks
Trade namesOrgovyx, Relumina
Other namesRGX; RVT-601; TAK-385
AHFS/Drugs.comMonograph
MedlinePlusa621006
License data
  • US DailyMed: Relugolix
Routes of
administration
By mouth[1]
Drug classGnRH antagonist
ATC code
  • L02BX04 (WHO)
    H01CC54 (WHO) (combination with estradiol and norethisterone)
Legal status
Legal status
  • CA: ℞-only[2][3]
  • US: ℞-only[4]
  • EU: Rx-only[5]
Pharmacokinetic data
Protein binding68–71%[1]
Elimination half-life36 to 65 hours[1]
ExcretionFeces: 82%[1]
Urine: 4%[1]
Identifiers
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
CAS Number
  • 737789-87-6
PubChem CID
  • 10348973
IUPHAR/BPS
  • 5586
DrugBank
  • DB11853
ChemSpider
  • 8524431
UNII
  • P76B05O5V6
KEGG
  • D10888
ChEMBL
  • ChEMBL1800159
CompTox Dashboard (EPA)
  • DTXSID40224167 Edit this at Wikidata
Chemical and physical data
FormulaC29H27F2N7O5S
Molar mass623.64 g·mol−1
3D model (JSmol)
  • Interactive image
SMILES
  • CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nn2)c(=O)n3Cc2c(F)cccc2F)cc1
InChI
  • 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.[4][1][6] It is taken by mouth.[1][6]

Side effects of relugolix include menstrual abnormalities, hot flashes, excessive sweating, headache, and decreased bone mineral density.[6][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.[7][8][9] It suppresses sex hormone levels to the postmenopausal or castrate range in both women and men.[1][10][4]

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.[11][12]

  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. ^ "Notice: Multiple additions to the Prescription Drug List (PDL) [2023-12-22]". Health Canada. 22 December 2023. Retrieved 3 January 2024.
  3. ^ "Summary Basis of Decision (SBD) for Orgovyx". Health Canada. 16 February 2024. Retrieved 24 February 2024.
  4. ^ a b c "Orgovyx- relugolix tablet, film coated". DailyMed. Retrieved 25 May 2021.
  5. ^ Cite error: The named reference Orgovyx EPAR was invoked but never defined (see the help page).
  6. ^ 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.
  7. ^ Cite error: The named reference pmid21657270 was invoked but never defined (see the help page).
  8. ^ Cite error: The named reference pmid24333551 was invoked but never defined (see the help page).
  9. ^ Cite error: The named reference pmid29232843 was invoked but never defined (see the help page).
  10. ^ Cite error: The named reference pmid26502357 was invoked but never defined (see the help page).
  11. ^ "Relugolix - Myovant/Takeda". AdisInsight. Springer Nature Switzerland AG.
  12. ^ Cite error: The named reference PRNewswire2019 was invoked but never defined (see the help page).

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Relugolix

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Relugolix, sold under the brand names Orgovyx and Relumina among others, is a gonadotropin-releasing hormone antagonist (GnRH receptor antagonist) medication...

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Prostate cancer

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symptoms of metastases. In these people, GnRH antagonists like degarelix or relugolix are given instead, and can also rapidly reduce testosterone levels. Reducing...

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Luteinizing hormone

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Triptorelin Antagonists Peptide: Abarelix Cetrorelix Degarelix Ganirelix Non-peptide: Elagolix Linzagolix† Relugolix (+estradiol/norethisterone acetate)...

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Menotropin

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Triptorelin Antagonists Peptide: Abarelix Cetrorelix Degarelix Ganirelix Non-peptide: Elagolix Linzagolix† Relugolix (+estradiol/norethisterone acetate)...

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Human chorionic gonadotropin

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Triptorelin Antagonists Peptide: Abarelix Cetrorelix Degarelix Ganirelix Non-peptide: Elagolix Linzagolix† Relugolix (+estradiol/norethisterone acetate)...

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Gonadotropin

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ATC code L02

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Exemestane L02BX01 Abarelix L02BX02 Degarelix L02BX03 Abiraterone L02BX04 Relugolix L02BX53 Abiraterone and prednisolone "ATC (Anatomical Therapeutic Chemical...

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Elagolix

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introduction of elagolix in the United States and Canada was followed by that of relugolix (brand name Relumina), the next second-generation GnRH antagonist, in...

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Triptorelin

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Gonadotropin preparations

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Antigonadotropin

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Puberty blocker

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Transgender hormone therapy

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Triptorelin Antagonists Peptide: Abarelix Cetrorelix Degarelix Ganirelix Non-peptide: Elagolix Linzagolix† Relugolix (+estradiol/norethisterone acetate)...

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Degarelix

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Triptorelin Antagonists Peptide: Abarelix Cetrorelix Degarelix Ganirelix Non-peptide: Elagolix Linzagolix† Relugolix (+estradiol/norethisterone acetate)...

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Buserelin

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Androgen deprivation therapy

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Ganirelix

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List of antiandrogens

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Cetrorelix

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Leuprorelin

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ATC code H01

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Masculinizing hormone therapy

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Goserelin

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Gonadorelin

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