nafarelin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| pituitary hormone-release stimulating peptides | 1868 | 76932-56-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A potent synthetic agonist of GONADOTROPIN-RELEASING HORMONE with 3-(2-naphthyl)-D-alanine substitution at residue 6. Nafarelin has been used in the treatments of central PRECOCIOUS PUBERTY and ENDOMETRIOSIS.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.40 | mg | N |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 1 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 3 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.02 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| Vd (Volume of distribution) | 0.14 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.72 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.19 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 3.50 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 13, 1990 | FDA | GD SEARLE LLC | |
| Aug. 24, 2022 | PMDA | Pfizer Japan 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 | 300.08 | 61.35 | 43 | 212 | 3971 | 63484796 |
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 | 312.28 | 83.17 | 42 | 183 | 3529 | 79740634 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | H01CA02 | SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES HYPOTHALAMIC HORMONES Gonadotropin-releasing hormones |
| CHEBI has role | CHEBI:50751 | anti-estrogenic drug |
| CHEBI has role | CHEBI:63533 | gonadotropin releasing hormone agonists |
| FDA MoA | N0000175654 | Gonadotropin Releasing Hormone Receptor Agonists |
| FDA EPC | N0000175655 | Gonadotropin Releasing Hormone Receptor Agonist |
| MeSH PA | D005300 | Fertility Agents, Female |
| MeSH PA | D012102 | Reproductive Control Agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Endometriosis | indication | 129103003 | |
| Precocious puberty | indication | 400179000 | |
| Prevention of premature ovulation | indication | ||
| Alcoholism | contraindication | 7200002 | |
| Hypercholesterolemia | contraindication | 13644009 | |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Osteoporosis | contraindication | 64859006 | DOID:11476 |
| Intermenstrual bleeding - irregular | contraindication | 64996003 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Hyperglycemia | contraindication | 80394007 | DOID:4195 |
| Pregnancy, function | contraindication | 289908002 | |
| Osteopenia | contraindication | 312894000 | |
| Cardiovascular event risk | contraindication | 395112001 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Obesity | contraindication | 414916001 | DOID:9970 |
| Smokes tobacco daily | contraindication | 449868002 |
🐶 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 | 11.9 | acidic |
| pKa3 | 12.8 | acidic |
| pKa4 | 12.93 | acidic |
| pKa5 | 13.31 | acidic |
| pKa6 | 13.4 | acidic |
| pKa7 | 13.73 | acidic |
| pKa8 | 10.75 | Basic |
| pKa9 | 6.69 | 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 | AGONIST | Kd | 9.70 | WOMBAT-PK | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019848 | VUID |
| N0000147934 | NUI |
| D00990 | KEGG_DRUG |
| 86220-42-0 | SECONDARY_CAS_RN |
| 4019489 | VANDF |
| 4019848 | VANDF |
| C0064906 | UMLSCUI |
| CHEBI:7445 | CHEBI |
| CHEMBL1201309 | ChEMBL_ID |
| CHEMBL1200671 | ChEMBL_ID |
| D017274 | MESH_DESCRIPTOR_UI |
| DB00666 | DRUGBANK_ID |
| 3902 | IUPHAR_LIGAND_ID |
| 5402 | INN_ID |
| 1X0094V6JV | UNII |
| 25077405 | PUBCHEM_CID |
| 203147 | RXNORM |
| 5144 | MMSL |
| d00574 | MMSL |
| 003536 | NDDF |
| 004783 | NDDF |
| 008316 | NDDF |
| 008317 | NDDF |
| 109046009 | SNOMEDCT_US |
| 109047000 | SNOMEDCT_US |
| 126196000 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Synarel | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0025-0166 | SPRAY, METERED | 2 mg | NASAL | NDA | 25 sections |
| Synarel | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0025-0166 | SPRAY, METERED | 2 mg | NASAL | NDA | 25 sections |
| Synarel | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0025-0166 | SPRAY, METERED | 2 mg | NASAL | NDA | 25 sections |