linzagolix 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
gonadotropin releasing hormone (GnRH) antagonists	5701	935283-04-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: linzagolix linzagolix choline yselty OBE2109 KLH-2109	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. Molecular weight: 508.42 Formula: C22H15F3N2O7S CLOGP: 5.31 LIPINSKI: 1 HAC: 9 HDO: 2 TPSA: 114.40 ALOGS: -5.41 ROTB: 6

Molecule

Description

Molfile Inchi Smiles

Synonyms:

linzagolix
linzagolix choline
yselty
OBE2109
KLH-2109

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.

Molecular weight: 508.42
Formula: C22H15F3N2O7S
CLOGP: 5.31
LIPINSKI: 1
HAC: 9
HDO: 2
TPSA: 114.40
ALOGS: -5.41
ROTB: 6

Drug dosage:

None

ADMET properties:

None

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

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	P30968	GNRHR_HUMAN	ANTAGONIST	Ki	7.56		DRUG LABEL	DRUG LABEL

External reference:

ID	Source
CHEMBL3668014	ChEMBL_ID
C000716911	MESH_SUPPLEMENTAL_RECORD_UI
12283	IUPHAR_LIGAND_ID
DB17083	DRUGBANK_ID
C5235403	UMLSCUI
CHEMBL4298171	ChEMBL_ID
10711	INN_ID
1321816-57-2	SECONDARY_CAS_RN
D11608	KEGG_DRUG
16656889	PUBCHEM_CID
2621019	RXNORM
7CDW97HUEX	UNII

Pharmaceutical products:

None