ganirelix

Peptideapproved

Approved

Jul 29, 1999

Ganirelix (N-acetyl-3-(2-naphthyl)-D-alanyl-4-chloro-D-phenylalanyl-3-(3-pyridyl)-D-alanyl-L-seryl-L-tyrosyl-N9 ,N10-diethyl-D-homoarginyl-L-leucylN9 ,N10-diethyl-L-homoarginyl-L-prolyl-D-acrylamide) is a synthetic decapeptide with high antagonistic activity against naturally occurring gonadotropin-releasing hormone (GnRH). Ganirelix Acetate Injection is indicated for the inhibition of premature luteinizing hormone (LH) surges in women undergoing controlled ovarian hyperstimulation. Ganirelix is administered by a subcutaneous injection of 250 µg once per day during the mid to late follicular phase of a woman’s menstrual cycle. Treatment should start on the 5th or 6th day after the start of ovarian stimulation, and the mean duration of its use is five days. Clinical studies have shown that the most common side effect is a slight reaction at the site of injection in the form of redness, and sometimes swelling. Clinical studies have shown that, one hour after injection, the incidence of at least one moderate or severe local skin reaction per treatment cycle was 12% in 4 patients treated with Ganirelix and 25% in patients treated subcutaneously with a GnRH agonist. The local reactions generally disappear within 4 hours after administration. Other reported side effects are some that are known to be associated with ovarian hyperstimulation, including gynecological abdominal pain, headache, vaginal bleeding, nausea, and gastrointestinal abdominal pain. — NCATS

Clinical trial activity

52 trials · 57 clinical orgs · 10 marketing orgs

Phase 1
6
Phase 2
16
Phase 3
12
Phase 4
21

Earliest trial started Jul 1, 2001 (NCT00702806)

Timeline

1990s

  1. Jul 29, 1999

    Organon — Earliest FDA Approval

  2. Jul 29, 1999

    Organon — NDA Organization

  3. Jul 29, 1999

    Organon — Marketing Organization

2000s

  1. Jan 1, 2001

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2001

    Earliest Phase 3 Sponsor(trial)

  3. Jan 1, 2006

    Earliest Phase 1 Sponsor(trial)

2010s

  1. Nov 30, 2018

    Sun Pharmaceuticals — Marketing Organization

2020s

  1. Apr 7, 2022

    Amphastar Pharmaceuticals — Marketing Organization

  2. Jun 6, 2022

    Eu Yan Sang — Marketing Organization

  3. Jun 6, 2022

    Meitheal — Marketing Organization

  4. Feb 28, 2023

    Gland Pharma Ltd — Marketing Organization

  5. Feb 28, 2023

    Fosun — Marketing Organization

  6. Nov 16, 2023

    Lupin — Marketing Organization

  7. Apr 23, 2025

    Qilu Pharmaceutical Co., Ltd. — Marketing Organization

  8. Jun 27, 2025

    Tris Pharma, Inc. — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedPriority reviewJul 29, 1999

Chemistry & pharmacology

Loading structure…

SMILES

CCNC(NCC)=NCCCC[C@@H](NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CO)NC(=O)[C@@H](CC2=CC=CN=C2)NC(=O)[C@@H](CC3=CC=C(Cl)C=C3)NC(=O)[C@@H](CC4=CC5=C(C=CC=C5)C=C4)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN=C(NCC)NCC)C(=O)N6CCC[C@H]6C(=O)N[C@H](C)C(N)=O
Mol. weight
1570.319 g/mol
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Parenteral
Availability
Prescription Only
Multi-specific
No

Oral

No

Parenteral

Yes

Topical

No

Sources

Also known as

  • antagon
  • antagon
  • antagon
  • d-alaninamide, n-acetyl-3-(1-naphthalenyl)-d-alanyl-4-chloro-d-phenylalanyl-3-(3-pyridinyl)-d-alanyl-l-seryl-l-tyrosyl-n6-(bis(ethylamino)methylene)-d-lysyl-l-leucyl-n6-(bis(ethylamino)methylene)-l-lysyl-l-prolyl-
  • ganirelix
  • ganirelix
  • ganirelix
  • ganirelix
  • ganirelix
  • ganirelix
  • ganirelix
  • ganirelix
  • ganirelix
  • ganirelix
  • ganirelix
  • ganirelix acetate
  • ganirelix acetate
  • ganirelix acetate
  • ganirelix acetate
  • ganirelix acetate
  • ganirelix acetate
  • ganirelix acetate injection
  • ganirelix acetate injection
  • ganirelix diacetate
  • gnrh, n-ac-2-nal(1)-4-cl-phe(2)-3-pal(3)-et2-harg(6,8)-alanh2(10)-
  • lhrh,n-ac-2-nal(1)-4-cl-phe(2)-3-pal(3)-et2-harg(6,8)-alanh2(10)-
  • lhrh, n-acetyl-2-naphthylalanyl(1)-(4-chlorophenylalanyl)(2)-3-pyrdinylalanyl(3)-diethylhomoarginyl(6,8)-alaninamide(10)-
  • n-ac-(2-naphthyl)ala-2-(4-cl-phe)-3-(3-pyridinyl-ala)-6,8-et2-harg-10-alanh2-lhrh
  • n-acetyl-3-(2-naphthyl)-d-alanyl-p-chloro-d-phenylalanyl-3-(3-pyridyl)-d-alanyl-l-seryl-l-tyrosyl-n(sup 6)-(n,n'-diethylamidino)-d-lysyl-l-leucyl-n(sup 6)-(n,n'-diethylamidino)-l-lysyl-l-prolyl-d-alaninamide diacetate (salt)
  • orgalutran
  • orgalutran
  • orgalutran
  • orgalutran
  • orgalutran
  • rs 26306
  • rs-26306
  • rs-26306
  • rs-26306
  • rs-26306-298

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06745466Phase 4Nov 15, 2024National Institute on Aging (NIA), University of Delaware
NCT06637189Phase 4Oct 15, 2024Ginefiv, Theramex
NCT06481696N/AJun 1, 2024Andros Day Surgery Clinic
NCT06175832Phase 4Jan 1, 2024Ghent University
NCT05954962Phase 4Oct 23, 2023Instituto Bernabeu
NCT05994378Phase 3Aug 29, 2023Hengrui Therapeutics, Inc.
NCT05751252Early Phase 1 (Phase 1)Jul 31, 2023University of Lille
NCT06091436Phase 3Mar 24, 2023GeneScience Pharmaceuticals Co., Ltd., Sun Yat-Sen University
NCT04993924Phase 4May 1, 2021Hebrew University
NCT05071339Phase 4Apr 1, 2021Hebrew University
NCT04728659Phase 4Oct 1, 2020Casa di Cura Privata del Policlinico SpA
NCT04654741Phase 4Sep 1, 2020Casa di Cura Privata del Policlinico SpA
NCT04265053Early Phase 1 (Phase 1)May 31, 2020University of Wisconsin
NCT04037605Early Phase 1 (Phase 1)Jul 24, 2019Los Angeles Biomedical Research Institute
NCT03746535N/AJan 31, 2019Yale University
NCT03477929Phase 4Nov 15, 2017D'Annunzio University of Chieti–Pescara
NCT03300518N/ANov 15, 2017Central South University, Merck
NCT03300960Phase 3Oct 20, 2017University of Valencia
NCT03051087Phase 4Oct 1, 2016LG
NCT02796105Phase 4Jun 1, 2016Clinica Eugin, Fundació Privada Eugin
Showing 20 of 52 trials
Page 1 / 3

Organizations

Research & Development (57)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
MerckFor profit10642001
Yale UniversityAcademic/Hospital4432006
EugoniaAcademic/Hospital3312003
Casa di Cura Privata del Policlinico SpAAcademic/Hospital2212020
FerringFor profit2122008
Hebrew UniversityAcademic/Hospital2212021
John B. Pierce LaboratoryAcademic/Hospital2022006
Merck SeronoFor profit2122003
National Heart, Lung, and Blood Institute (NHLBI)Government2022006
National Institute on Aging (NIA)Government2022007
Shahid Sadoughi University of Medical ScienceAcademic/Hospital2222008
University of ValenciaAcademic/Hospital2212013
Yazd Research & Clinical Center for InfertilityAcademic/Hospital2022008
Andros Day Surgery ClinicAcademic/Hospital1112024
Central South UniversityAcademic/Hospital1112017
Chongqing Medical UniversityAcademic/Hospital1012016
Chong Qing Reproducive and Genetic InstituteAcademic/Hospital1112016
Clinica EuginAcademic/Hospital1012016
D'Annunzio University of Chieti–PescaraAcademic/Hospital1112017
European HospitalAcademic/Hospital1112012
57 organizations
Page 1 / 3

Marketing (14)

OrganizationOrg typeRelationshipDate
Amphastar PharmaceuticalsFor profitMKTGApr 7, 2022
Eu Yan SangFor profitMKTGJun 6, 2022
FosunFor profitMKTGFeb 28, 2023
Gland Pharma LtdFor profitMKTGFeb 28, 2023
Gland Pharma LtdFor profitSYNFeb 28, 2023
LupinFor profitMKTGNov 16, 2023
LupinFor profitSYNNov 16, 2023
MeithealFor profitMKTGJun 6, 2022
OrganonFor profitNDAJul 29, 1999
OrganonFor profitMKTGJul 29, 1999
Qilu Pharmaceutical Co., Ltd.For profitMKTGApr 23, 2025
Sun PharmaceuticalsFor profitMKTGNov 30, 2018
Sun PharmaceuticalsFor profitSYNNov 30, 2018
Tris Pharma, Inc.For profitMKTGJun 27, 2025