Ganirelix
JFDA label: ORGALUTRAN PFS
Mechanism of Action
Antagonist of Gonadotropin-releasing hormone receptor — Gonadotropin-releasing hormone receptor antagonist
| Target | Action | Gene / class |
|---|---|---|
| Gonadotropin-releasing hormone receptor efficacy | ANTAGONIST | GNRHR |
Indications
Approved
- Adjunct to controlled ovarian hyperstimulation
Contraindications
Source: Lexicomp
- Hypersensitivity to ganirelix or any component of the formulation Absolute
- hypersensitivity to gonadotropin-releasing hormone (GnRH) or any other GnRH analog Absolute
- known or suspected pregnancy Absolute
Adverse Reactions
Nervous system disorders (1)
Common Headache
Renal and urinary disorders (2)
Common Pelvic pain · vaginal hemorrhage
Metabolism and nutrition disorders (1)
Common Ovarian hyperstimulation syndrome
Gastrointestinal disorders (2)
Common Abdominal pain · nausea
General disorders and administration site conditions (1)
Common Injection site reaction
Dosing
Source: Lexicomp
Warnings & Precautions
Source: Lexicomp
Hypersensitivity
Hypersensitivity reactions, including anaphylactoid reactions, have been reported; may occur with the first dose; use is not recommended in women with severe allergic conditions. Use with caution in women with signs and symptoms of other allergic conditions. Special populations:
Pregnancy
Exclude pregnancy before beginning treatment. Dosage form specific issues:
Latex
The packaging may contain natural rubber latex. Other warnings/precautions:
Experienced specialists
Should only be prescribed by fertility specialists.
Pregnancy & Lactation
Pregnancy
Studies in animals have shown evidence of fetal abnormalities, including fetal resorption, and use is contraindicated in women who are pregnant. Fetal resorption is a result of hormonal alterations and could result in fetal loss in humans. Ganirelix is used to treat infertility; pregnancy should be ruled out prior to therapy.
Lactation
It is not known if ganirelix is excreted in breast milk. Breast-feeding is not recommended by the manufacturer.
Monitoring
| Clinical pearl | Ultrasound to assess follicle size |
|---|
Chemistry & Properties
| Formula | C80H113ClN18O13 |
|---|---|
| Molecular weight | 1570.35 g/mol |
| IUPAC name | (2S)-1-[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-6-[bis(ethylamino)methylideneamino]hexanoyl]amino]-4-methylpentanoyl]amino]-6-[bis(ethylamino)methylideneamino]hexanoyl]-N-[(2R)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamide |
| CAS | 124904-93-4 |
| PubChem CID | 16130957 |
| InChIKey | GJNXBNATEDXMAK-PFLSVRRQSA-N |
SMILES
CC/N=C(\NCC)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCN/C(=N/CC)NCC)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=OBiology & Pharmacokinetics
Pharmacokinetics predicted
| Bioavailability | 70.0% |
|---|---|
| Half-life | 1.55 h |
| Volume of distribution | 0.551 L/kg |
| Protein binding | 87.8% |
| BBB penetrant | No |
Enzyme interactions
| Enzyme | Role | Detail |
|---|---|---|
| CYP2C19 | Substrate | — |
| CYP2D6 | Substrate | — |
| CYP3A4 | Inhibitor | — |
Transporters
BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)
Drug–drug interactions (6, DDInter)
| Interacting drug | Severity | Management |
|---|---|---|
| Chorionic Gonadotropin (Human) | moderate | |
| Follitropin | moderate | |
| Gonadorelin | moderate | |
| Menotropins | moderate | |
| Triptorelin | moderate | |
| Urofollitropin | moderate |
Registered Products (1)
| Brand | Form / strength | Pack | Agent | Citizen (JOD) |
|---|---|---|---|---|
| ORGALUTRAN PFS | Pre-filled Syringe 0.25 mg/0.5 ml | 1 | Sabbagh Drug Store | — |