ganirelix 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| gonadotropin-releasing-hormone (GnRH) inhibitors, peptides | 1279 | 124904-93-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Ganirelix is a GnRH antagonist, which modulates the hypothalamic-pituitary-gonadal axis by competitive binding to the GnRH receptors in the pituitary gland. As result a rapid, profound,reversible suppression of endogenous gonadotropins occurs, without initial stimulation as induced by GnRH agonists.
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Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.25 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 0.21 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.63 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.18 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 9.09 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| May 16, 2000 | EMA | N.V. ORGANON | |
| July 29, 1999 | FDA | ORGANON USA INC |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Ovarian hyperstimulation syndrome | 3442.42 | 64.13 | 482 | 1983 | 3532 | 63483025 |
| Ascites | 675.65 | 64.13 | 179 | 2286 | 40549 | 63446008 |
| Inappropriate schedule of product administration | 167.18 | 64.13 | 81 | 2384 | 103884 | 63382673 |
| Ovarian haemorrhage | 163.95 | 64.13 | 25 | 2440 | 313 | 63486244 |
| Ovarian enlargement | 140.18 | 64.13 | 23 | 2442 | 471 | 63486086 |
| Haemoperitoneum | 139.54 | 64.13 | 30 | 2435 | 2711 | 63483846 |
| Pleural effusion | 90.68 | 64.13 | 52 | 2413 | 93158 | 63393399 |
| Abdominal distension | 88.77 | 64.13 | 50 | 2415 | 86565 | 63399992 |
| Maternal exposure before pregnancy | 86.40 | 64.13 | 25 | 2440 | 7578 | 63478979 |
| Adnexal torsion | 79.54 | 64.13 | 14 | 2451 | 440 | 63486117 |
| Needle issue | 74.61 | 64.13 | 24 | 2441 | 10352 | 63476205 |
| Haemoconcentration | 72.77 | 64.13 | 11 | 2454 | 129 | 63486428 |
| No adverse event | 71.58 | 64.13 | 34 | 2431 | 41371 | 63445186 |
| Pelvic fluid collection | 70.36 | 64.13 | 14 | 2451 | 862 | 63485695 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Ovarian hyperstimulation syndrome | 3239.17 | 73.74 | 421 | 1370 | 3150 | 79739447 |
| Ascites | 641.92 | 73.74 | 174 | 1617 | 75388 | 79667209 |
| Ovarian haemorrhage | 171.20 | 73.74 | 24 | 1767 | 292 | 79742305 |
| Ovarian enlargement | 159.58 | 73.74 | 23 | 1768 | 345 | 79742252 |
| Haemoperitoneum | 119.51 | 73.74 | 26 | 1765 | 4317 | 79738280 |
| Pleural effusion | 95.91 | 73.74 | 52 | 1739 | 145210 | 79597387 |
| Adnexal torsion | 89.59 | 73.74 | 14 | 1777 | 369 | 79742228 |
| Pelvic fluid collection | 78.96 | 73.74 | 14 | 1777 | 805 | 79741792 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | H01CC01 | SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES HYPOTHALAMIC HORMONES Anti-gonadotropin-releasing hormones |
| FDA PE | N0000008638 | Decreased GnRH Secretion |
| FDA MoA | N0000175084 | Gonadotropin Releasing Hormone Receptor Antagonists |
| MeSH PA | D006727 | Hormone Antagonists |
| FDA EPC | N0000175839 | Gonadotropin Releasing Hormone Receptor Antagonist |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Ovulation induction | indication | 61285001 | |
| Prevention of Luteinizing Hormone Surge when undergoing Controlled Ovarian Hyperstimulation | indication | ||
| Pregnancy, function | contraindication | 289908002 | |
| Breastfeeding (mother) | contraindication | 413712001 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.65 | acidic |
| pKa2 | 12.09 | acidic |
| pKa3 | 12.73 | acidic |
| pKa4 | 13.33 | acidic |
| pKa5 | 13.33 | acidic |
| pKa6 | 13.78 | acidic |
| pKa7 | 8.8 | Basic |
| pKa8 | 8.2 | Basic |
| pKa9 | 5.35 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Gonadotropin-releasing hormone receptor | GPCR | ANTAGONIST | CHEMBL | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4021229 | VUID |
| N0000148673 | NUI |
| D04302 | KEGG_DRUG |
| 129311-55-3 | SECONDARY_CAS_RN |
| 4021229 | VANDF |
| 4021230 | VANDF |
| C0073629 | UMLSCUI |
| CHEBI:135910 | CHEBI |
| CHEMBL1251 | ChEMBL_ID |
| DB06785 | DRUGBANK_ID |
| C061018 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3877 | IUPHAR_LIGAND_ID |
| 6830 | INN_ID |
| IX503L9WN0 | UNII |
| 16130957 | PUBCHEM_CID |
| 259264 | RXNORM |
| 67714 | MMSL |
| 8280 | MMSL |
| d04447 | MMSL |
| 008055 | NDDF |
| 008056 | NDDF |
| 116102008 | SNOMEDCT_US |
| 326088005 | SNOMEDCT_US |
| 395728002 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Ganirelix Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0052-0301 | INJECTION, SOLUTION | 250 ug | SUBCUTANEOUS | NDA | 23 sections |
| Ganirelix Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0548-5001 | INJECTION | 250 ug | SUBCUTANEOUS | ANDA | 23 sections |
| Ganirelix Acetate | Human Prescription Drug Label | 1 | 55566-1000 | INJECTION, SOLUTION | 250 ug | SUBCUTANEOUS | ANDA | 19 sections |
| Fyremadel | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55566-1010 | INJECTION, SOLUTION | 250 ug | SUBCUTANEOUS | ANDA | 23 sections |
| Fyremadel | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55566-1010 | INJECTION, SOLUTION | 250 ug | SUBCUTANEOUS | ANDA | 23 sections |
| Ganirelix Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65219-028 | INJECTION | 250 ug | SUBCUTANEOUS | ANDA | 23 sections |
| GANIRELIX ACETATE | Human Prescription Drug Label | 1 | 68083-472 | INJECTION, SOLUTION | 250 ug | SUBCUTANEOUS | ANDA | 11 sections |
| Ganirelix Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71288-554 | INJECTION, SOLUTION | 250 ug | SUBCUTANEOUS | ANDA | 23 sections |
| Ganirelix Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 78206-138 | INJECTION, SOLUTION | 250 ug | SUBCUTANEOUS | NDA | 23 sections |
| Ganirelix Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 78206-138 | INJECTION, SOLUTION | 250 ug | SUBCUTANEOUS | NDA | 23 sections |
| Ganirelix Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 78206-138 | INJECTION, SOLUTION | 250 ug | SUBCUTANEOUS | NDA | 23 sections |