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ganirelix 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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.
|
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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 29, 1999 | FDA | ORGANON USA INC | |
| May 16, 2000 | EMA | N.V. ORGANON |
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 | 5008.30 | 62.35 | 695 | 2593 | 5167 | 90619992 |
| Ascites | 849.99 | 62.35 | 219 | 3069 | 47521 | 90577638 |
| Ovarian haemorrhage | 291.90 | 62.35 | 42 | 3246 | 369 | 90624790 |
| Ovarian enlargement | 187.01 | 62.35 | 30 | 3258 | 570 | 90624589 |
| Haemoperitoneum | 156.10 | 62.35 | 34 | 3254 | 3494 | 90621665 |
| Inappropriate schedule of product administration | 144.08 | 62.35 | 81 | 3207 | 149852 | 90475307 |
| Pleural effusion | 139.75 | 62.35 | 72 | 3216 | 111919 | 90513240 |
| Abdominal distension | 132.09 | 62.35 | 73 | 3215 | 130528 | 90494631 |
| Pelvic fluid collection | 130.62 | 62.35 | 24 | 3264 | 1035 | 90624124 |
| Maternal exposure before pregnancy | 121.51 | 62.35 | 35 | 3253 | 11178 | 90613981 |
| Intra-abdominal haemorrhage | 92.18 | 62.35 | 21 | 3267 | 2641 | 90622518 |
| Adnexal torsion | 84.83 | 62.35 | 15 | 3273 | 519 | 90624640 |
| Abdominal pain lower | 77.25 | 62.35 | 32 | 3256 | 30145 | 90595014 |
| Needle issue | 73.12 | 62.35 | 25 | 3263 | 13909 | 90611250 |
| Haemoconcentration | 64.41 | 62.35 | 10 | 3278 | 152 | 90625007 |
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 | 4790.14 | 68.92 | 626 | 1952 | 4734 | 110581987 |
| Ascites | 770.94 | 68.92 | 212 | 2366 | 92596 | 110494125 |
| Ovarian haemorrhage | 307.59 | 68.92 | 41 | 2537 | 319 | 110586402 |
| Ovarian enlargement | 211.59 | 68.92 | 30 | 2548 | 382 | 110586339 |
| Pelvic fluid collection | 141.84 | 68.92 | 24 | 2554 | 1009 | 110585712 |
| Haemoperitoneum | 134.57 | 68.92 | 30 | 2548 | 5358 | 110581363 |
| Pleural effusion | 132.89 | 68.92 | 70 | 2508 | 177639 | 110409082 |
| Maternal exposure before pregnancy | 105.18 | 68.92 | 26 | 2552 | 7239 | 110579482 |
| Adnexal torsion | 94.51 | 68.92 | 15 | 2563 | 421 | 110586300 |
| Abdominal distension | 87.43 | 68.92 | 53 | 2525 | 175050 | 110411671 |
| Abdominal pain lower | 84.45 | 68.92 | 32 | 2546 | 37251 | 110549470 |
| Intra-abdominal haemorrhage | 81.78 | 68.92 | 20 | 2558 | 5322 | 110581399 |
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 |
Related Drugs by ATC class:
H01CC Anti-gonadotropin-releasing hormones 6 drugs
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 |
| 4021229 | VANDF |
| 4021230 | VANDF |
| C0073629 | UMLSCUI |
| CHEMBL1251 | ChEMBL_ID |
| CHEMBL5314377 | ChEMBL_ID |
| DB06785 | DRUGBANK_ID |
| C061018 | MESH_SUPPLEMENTAL_RECORD_UI |
| 3877 | IUPHAR_LIGAND_ID |
| 6830 | INN_ID |
| 129311-55-3 | SECONDARY_CAS_RN |
| IX503L9WN0 | UNII |
| 16130957 | PUBCHEM_CID |
| 259264 | RXNORM |
| 399987 | MMSL |
| 67714 | MMSL |
| 8280 | MMSL |
| d04447 | MMSL |
| 008055 | NDDF |
| 008056 | NDDF |
| 116102008 | SNOMEDCT_US |
| 326088005 | SNOMEDCT_US |
| 395728002 | SNOMEDCT_US |
| CHEBI:135910 | CHEBI |
| IX503L9WN0 | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Ganirelix Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0548-5001 | INJECTION | 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 | 67184-0574 | INJECTION, SOLUTION | 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 | 70700-327 | INJECTION | 250 ug | SUBCUTANEOUS | ANDA | 23 sections |
| Ganirelix Acetate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70748-274 | INJECTION, SOLUTION | 250 ug | SUBCUTANEOUS | ANDA | 19 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 | 83301-0082 | INJECTION, SOLUTION | 250 ug | SUBCUTANEOUS | ANDA | 22 sections |