buserelin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| pituitary hormone-release stimulating peptides | 436 | 57982-77-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A potent synthetic analog of GONADOTROPIN-RELEASING HORMONE with D-serine substitution at residue 6, glycine10 deletion, and other modifications.
|
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.11 | mg | implant |
| 1.20 | mg | N |
| 1.50 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.02 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 25, 2022 | PMDA | Sanofi K.K. | |
| Jan. 1, 1984 | YEAR INTRODUCED |
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 | 104.13 | 51.45 | 15 | 77 | 3999 | 63484931 |
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 | 95.74 | 63.15 | 15 | 201 | 3556 | 79740616 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L02AE01 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONES AND RELATED AGENTS Gonadotropin releasing hormone analogues |
| 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 |
|---|---|---|---|
| Induction of final follicular maturation | indication | ||
| Prevention of premature ovulation | indication |
🐶 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 | 12.86 | acidic |
| pKa4 | 13.14 | acidic |
| pKa5 | 13.23 | acidic |
| pKa6 | 13.59 | acidic |
| pKa7 | 10.75 | Basic |
| pKa8 | 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 | EC50 | 10.52 | IUPHAR | IUPHAR | |||
| Lutropin-choriogonadotropic hormone receptor | GPCR | Kd | 8.57 | WOMBAT-PK | |||||
| Gonadotropin-releasing hormone receptor | GPCR | AGONIST | EC50 | 10.05 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| N0000170309 | NUI |
| D07259 | KEGG_DRUG |
| 1825 | RXNORM |
| C0006456 | UMLSCUI |
| CHEBI:135907 | CHEBI |
| CHEMBL2110824 | ChEMBL_ID |
| D002064 | MESH_DESCRIPTOR_UI |
| DB06719 | DRUGBANK_ID |
| 3860 | IUPHAR_LIGAND_ID |
| 4045 | INN_ID |
| PXW8U3YXDV | UNII |
| 50225 | PUBCHEM_CID |
| 327301004 | SNOMEDCT_US |
| 395744006 | SNOMEDCT_US |
| 426572004 | SNOMEDCT_US |
| CHEMBL2106198 | ChEMBL_ID |
| 68630-75-1 | SECONDARY_CAS_RN |
| 003708 | NDDF |
| 003709 | NDDF |
| 008310 | NDDF |
| 008311 | NDDF |
Pharmaceutical products:
None