ganirelix
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
Earliest trial started Jul 1, 2001 (NCT00702806)
Timeline
1990s
2000s
2010s
- Nov 30, 2018
Sun Pharmaceuticals — Marketing Organization
2020s
- Apr 7, 2022
Amphastar Pharmaceuticals — Marketing Organization
- Jun 6, 2022
Eu Yan Sang — Marketing Organization
- Jun 6, 2022
Meitheal — Marketing Organization
- Feb 28, 2023
Gland Pharma Ltd — Marketing Organization
- Feb 28, 2023
Fosun — Marketing Organization
- Nov 16, 2023
Lupin — Marketing Organization
- Apr 23, 2025
Qilu Pharmaceutical Co., Ltd. — Marketing Organization
- Jun 27, 2025
Tris Pharma, Inc. — Marketing Organization
Indications
Approved for
Studied for
- Blastocyst · Phase 4
- Cerebral Arterial Diseases · Early Phase 1
- Embryonic Structures · Phase 4
- Estrogens · Phase 4
- Fertility Preservation · Phase 4
- Fertilization in Vitro · Phase 4
- Genetic Diseases, Inborn · Phase 4
- Infertility · Phase 4
- Oocyte Retrieval · Phase 4
- Oocytes · Phase 4
- Orthostatic Intolerance · Phase 2
- Ovarian Cysts · Phase 4
- Ovarian Diseases · Phase 4
- Ovarian Hyperstimulation Syndrome · Phase 4
- Ovarian Neoplasms · Phase 3
- Ovulation Induction · Phase 4
- Ovum · Phase 4
- Polycystic Ovary Syndrome · Phase 4
- Premenopause · Phase 4
- Primary Ovarian Insufficiency · Phase 4
- Prostheses and Implants · Phase 4
- Puberty, Delayed · Early Phase 1
- Puberty, Precocious · Early Phase 1
- Quality of Life · Phase 4
- Reproductive Health · Phase 4
- Sleep Disorders, Intrinsic · Early Phase 1
Mechanism of action
- Gonadotropin-releasing hormone receptorANTAGONIST
GNRHR antagonist
- Progonadoliberin-1ANTAGONIST
GNRH1 antagonist
Approval history
- approvedPriority reviewJul 29, 1999
Chemistry & pharmacology
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
- WikipediaGanirelix ↗
- NCATSIX503L9WN0 ↗
- ChEMBLCHEMBL5314377 ↗
- ChEMBLCHEMBL1251 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06745466 | Phase 4 | Nov 15, 2024 | National Institute on Aging (NIA), University of Delaware |
| NCT06637189 | Phase 4 | Oct 15, 2024 | Ginefiv, Theramex |
| NCT06481696 | N/A | Jun 1, 2024 | Andros Day Surgery Clinic |
| NCT06175832 | Phase 4 | Jan 1, 2024 | Ghent University |
| NCT05954962 | Phase 4 | Oct 23, 2023 | Instituto Bernabeu |
| NCT05994378 | Phase 3 | Aug 29, 2023 | Hengrui Therapeutics, Inc. |
| NCT05751252 | Early Phase 1 (Phase 1) | Jul 31, 2023 | University of Lille |
| NCT06091436 | Phase 3 | Mar 24, 2023 | GeneScience Pharmaceuticals Co., Ltd., Sun Yat-Sen University |
| NCT04993924 | Phase 4 | May 1, 2021 | Hebrew University |
| NCT05071339 | Phase 4 | Apr 1, 2021 | Hebrew University |
| NCT04728659 | Phase 4 | Oct 1, 2020 | Casa di Cura Privata del Policlinico SpA |
| NCT04654741 | Phase 4 | Sep 1, 2020 | Casa di Cura Privata del Policlinico SpA |
| NCT04265053 | Early Phase 1 (Phase 1) | May 31, 2020 | University of Wisconsin |
| NCT04037605 | Early Phase 1 (Phase 1) | Jul 24, 2019 | Los Angeles Biomedical Research Institute |
| NCT03746535 | N/A | Jan 31, 2019 | Yale University |
| NCT03477929 | Phase 4 | Nov 15, 2017 | D'Annunzio University of Chieti–Pescara |
| NCT03300518 | N/A | Nov 15, 2017 | Central South University, Merck |
| NCT03300960 | Phase 3 | Oct 20, 2017 | University of Valencia |
| NCT03051087 | Phase 4 | Oct 1, 2016 | LG |
| NCT02796105 | Phase 4 | Jun 1, 2016 | Clinica Eugin, Fundació Privada Eugin |
Organizations
Research & Development (57)
Marketing (14)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Amphastar Pharmaceuticals | For profit | MKTG | Apr 7, 2022 |
| Eu Yan Sang | For profit | MKTG | Jun 6, 2022 |
| Fosun | For profit | MKTG | Feb 28, 2023 |
| Gland Pharma Ltd | For profit | MKTG | Feb 28, 2023 |
| Gland Pharma Ltd | For profit | SYN | Feb 28, 2023 |
| Lupin | For profit | MKTG | Nov 16, 2023 |
| Lupin | For profit | SYN | Nov 16, 2023 |
| Meitheal | For profit | MKTG | Jun 6, 2022 |
| Organon | For profit | NDA | Jul 29, 1999 |
| Organon | For profit | MKTG | Jul 29, 1999 |
| Qilu Pharmaceutical Co., Ltd. | For profit | MKTG | Apr 23, 2025 |
| Sun Pharmaceuticals | For profit | MKTG | Nov 30, 2018 |
| Sun Pharmaceuticals | For profit | SYN | Nov 30, 2018 |
| Tris Pharma, Inc. | For profit | MKTG | Jun 27, 2025 |