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gonadorelin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| pituitary hormone-release stimulating peptides | 2958 | 33515-09-2 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A decapeptide that stimulates the synthesis and secretion of both pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE. GnRH is produced by neurons in the septum PREOPTIC AREA of the HYPOTHALAMUS and released into the pituitary portal blood, leading to stimulation of GONADOTROPHS in the ANTERIOR PITUITARY GLAND.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | -1.352 | Moderate | 0.70 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.589 | Moderate | 0.70 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.242 | 10^-6 cm/s | Moderate | 0.70 |
| dh-clint | Dog hepatocyte intrinsic clearance | 0.938 | uL/min/10^6 cells | Moderate | 0.70 |
| dppb | Dog plasma protein binding (% unbound) | 75.680 | % | Moderate | 0.70 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 55.110 | % | Moderate | 0.70 |
| herg | hERG pIC50 | 4.235 | pIC50 | Moderate | 0.70 |
| hh-clint | Human hepatocyte intrinsic clearance | 6.745 | uL/min/10^6 cells | Moderate | 0.70 |
| hlm-clint | Human liver microsomal intrinsic clearance | 4.710 | uL/min/mg protein | Moderate | 0.70 |
| hppb | Human plasma protein binding (% unbound) | 75.470 | % | Moderate | 0.70 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK1,PDK2,PDK4,PRKDC,TEK | 17 | |||
| kinase-selectivity-class | PDK1 | 1 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.318 | Moderate | 0.70 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 8.166 | Moderate | 0.70 | |
| mppb | Mouse plasma protein binding (% unbound) | 64.380 | Moderate | 0.70 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.682 | Moderate | 0.70 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 65.940 | % | Moderate | 0.70 |
| rh-clint | Rat hepatocyte intrinsic clearance | 8.356 | uL/min/10^6 cells | Moderate | 0.70 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 53.680 | % | Moderate | 0.70 |
| rppb | Rat plasma protein binding (% unbound) | 61.090 | % | Moderate | 0.70 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 734.514 | uM | Moderate | 0.70 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 30, 1982 | FDA |
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 |
|---|---|---|---|---|---|---|
| Neutropenia | 223.41 | 53.65 | 89 | 1060 | 224815 | 90402483 |
| Metastases to bone | 139.29 | 53.65 | 37 | 1112 | 25468 | 90601830 |
| Ovarian hyperstimulation syndrome | 126.66 | 53.65 | 26 | 1123 | 5836 | 90621462 |
| Malignant neoplasm progression | 94.01 | 53.65 | 39 | 1110 | 106831 | 90520467 |
| Carcinoembryonic antigen increased | 78.45 | 53.65 | 15 | 1134 | 2335 | 90624963 |
| Alanine aminotransferase increased | 67.83 | 53.65 | 32 | 1117 | 118306 | 90508992 |
| Aspartate aminotransferase increased | 62.57 | 53.65 | 29 | 1120 | 102908 | 90524390 |
| Carbohydrate antigen 15-3 increased | 61.96 | 53.65 | 12 | 1137 | 1995 | 90625303 |
| Bone lesion | 58.19 | 53.65 | 14 | 1135 | 6423 | 90620875 |
| Radiation fibrosis - lung | 56.91 | 53.65 | 7 | 1142 | 53 | 90627245 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Recalled product administered | 61.98 | 36.43 | 10 | 435 | 715 | 42620175 |
| Metastases to bone | 44.96 | 36.43 | 13 | 432 | 14796 | 42606094 |
| Prostatic specific antigen increased | 43.24 | 36.43 | 13 | 432 | 16912 | 42603978 |
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 |
|---|---|---|---|---|---|---|
| Metastases to bone | 155.19 | 41.24 | 41 | 1197 | 31331 | 110556730 |
| Ovarian hyperstimulation syndrome | 120.09 | 41.24 | 24 | 1214 | 5336 | 110582725 |
| Neutropenia | 118.87 | 41.24 | 65 | 1173 | 374555 | 110213506 |
| Carcinoembryonic antigen increased | 83.76 | 41.24 | 16 | 1222 | 2808 | 110585253 |
| Malignant neoplasm progression | 80.27 | 41.24 | 39 | 1199 | 174528 | 110413533 |
| Carbohydrate antigen 15-3 increased | 66.26 | 41.24 | 12 | 1226 | 1575 | 110586486 |
| Radiation fibrosis - lung | 54.79 | 41.24 | 7 | 1231 | 85 | 110587976 |
| Metastases to lymph nodes | 52.61 | 41.24 | 15 | 1223 | 15017 | 110573044 |
| Ovarian disorder | 48.83 | 41.24 | 8 | 1230 | 582 | 110587479 |
| Prostatic specific antigen increased | 46.11 | 41.24 | 13 | 1225 | 12498 | 110575563 |
| Uterine enlargement | 44.73 | 41.24 | 8 | 1230 | 977 | 110587084 |
| Bone lesion | 43.38 | 41.24 | 11 | 1227 | 7076 | 110580985 |
| Meningeal disorder | 43.35 | 41.24 | 7 | 1231 | 465 | 110587596 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | H01CA01 | SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES HYPOTHALAMIC HORMONES Gonadotropin-releasing hormones |
| ATC | V04CM01 | VARIOUS DIAGNOSTIC AGENTS OTHER DIAGNOSTIC AGENTS Tests for fertility disturbances |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:50646 | bone density conservation agent |
| CHEBI has role | CHEBI:63533 | gonadotropin releasing hormone agonist |
Related Drugs by ATC class:
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Amenorrhea | indication | 14302001 | DOID:13938 |
| Diagnostic Test for Gonadotropin Deficiency | indication |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Cattle | Reproductive synchrony programs | Indication |
| Cattle | Ovarian cysts | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| CYSTORELIN | Boehringer lngelheim Animal Health USA Inc. | 1 |
| Factrel, Factrel Injection | Zoetis Inc. | 1 |
| Fertelin, OvaCyst | Bimeda Animal Health Limited | 1 |
| FERTAGYL | Intervet Inc. | 1 |
| Gonabreed | Parnell Technologies Pty. Ltd. | 1 |
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 | 12.71 | acidic |
| pKa4 | 12.88 | acidic |
| pKa5 | 13.24 | acidic |
| pKa6 | 13.32 | acidic |
| pKa7 | 13.61 | acidic |
| pKa8 | 13.97 | acidic |
| pKa9 | 10.75 | Basic |
| pKa10 | 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 | IC50 | 8 | CHEMBL | CHEMBL | |||
| Gonadotropin-releasing hormone receptor | GPCR | IC50 | 8.70 | CHEMBL | |||||
| Lutropin-choriogonadotropic hormone receptor | GPCR | Ki | 8.90 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019767 | VUID |
| N0000147858 | NUI |
| D00988 | KEGG_DRUG |
| 51952-41-1 | SECONDARY_CAS_RN |
| 4018487 | VANDF |
| 4018488 | VANDF |
| 4019767 | VANDF |
| C0023610 | UMLSCUI |
| CHEBI:5520 | CHEBI |
| CHEMBL1007 | ChEMBL_ID |
| CHEMBL1200511 | ChEMBL_ID |
| CHEMBL1200516 | ChEMBL_ID |
| DB00644 | DRUGBANK_ID |
| 3627 | INN_ID |
| 52699-48-6 | SECONDARY_CAS_RN |
| 9O7312W37G | UNII |
| 638793 | PUBCHEM_CID |
| 1298838 | RXNORM |
| 4796 | MMSL |
| 4797 | MMSL |
| d00573 | MMSL |
| 002108 | NDDF |
| 002109 | NDDF |
| 004782 | NDDF |
| 008305 | NDDF |
| 008306 | NDDF |
| 325995009 | SNOMEDCT_US |
| 397197007 | SNOMEDCT_US |
| 412193007 | SNOMEDCT_US |
| 49869009 | SNOMEDCT_US |
| 75969007 | SNOMEDCT_US |
| 96365009 | SNOMEDCT_US |
| D007987 | MESH_DESCRIPTOR_UI |
| 9O7312W37G | INXIGHT DRUGS |
Pharmaceutical products:
None