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linzagolix 🐶 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) antagonists | 5701 | 935283-04-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Linzagolix is a selective, non-peptide gonadotropin-releasing hormone (GnRH) receptor antagonist that inhibits endogenous GnRH signalling by binding competitively to GnRH receptors in the pituitary gland, thereby modulating the hypothalamic-pituitary-gonadal axis.
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,FLT3,GRK2,GSK3B,IKBKB,ITK,JAK1,KIT,MAP2K6,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK7,MAPKAPK2,MTOR,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK | 46 | |||
| kinase-selectivity-class | ACVR2A,ACVR2B,AXL,BRAF,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,MAP2K3,MAP2K6,MAPK7,MARK4,PDK4,PRKDC,SIK2,STK10,STK33,TEK,TTK | 22 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 14, 2022 | EMA | OBSEVA IRELAND LTD |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | H01CC04 | SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES HYPOTHALAMIC HORMONES Anti-gonadotropin-releasing hormones |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:231911 | renoprotective agent |
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 |
|---|---|---|---|
| Uterine fibroids | indication | 95315005 | DOID:13223 |
| Osteoporosis | contraindication | 64859006 | DOID:11476 |
| Pregnancy, function | contraindication | 289908002 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Genital bleeding | contraindication | 890094005 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
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 | Ki | 7.56 | DRUG LABEL | DRUG LABEL |
External reference:
| ID | Source |
|---|---|
| CHEBI:755689 | CHEBI |
| CHEMBL3668014 | ChEMBL_ID |
| C000716911 | MESH_SUPPLEMENTAL_RECORD_UI |
| 12283 | IUPHAR_LIGAND_ID |
| DB17083 | DRUGBANK_ID |
| 1351549009 | SNOMEDCT_US |
| 42992811000001103 | SNOMEDCT_US |
| C5235403 | UMLSCUI |
| CHEMBL4298171 | ChEMBL_ID |
| 10711 | INN_ID |
| 1321816-57-2 | SECONDARY_CAS_RN |
| D11608 | KEGG_DRUG |
| 16656889 | PUBCHEM_CID |
| 7CDW97HUEX | UNII |
| 2621019 | RXNORM |
Pharmaceutical products:
None