All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

elagolix 🐶 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	5293	834153-87-6

Description:

Molecule

Description

Molfile Inchi Smiles Synonyms: elagolix sodium orilissa NBI-56418 BT-620 elagolix

Elagolix is a GnRH receptor antagonist that inhibits endogenous GnRH signaling by binding competitively to GnRH receptors in the pituitary gland. Administration of ORILISSA results in dose-dependent suppression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to decreased blood concentrations of the ovarian sex hormones, estradiol and progesterone. Molecular weight: 631.60 Formula: C32H30F5N3O5 CLOGP: 4.17 LIPINSKI: 1 HAC: 8 HDO: 2 TPSA: 99.18 ALOGS: -5.41 ROTB: 12 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

None

ADMET properties:

Property	Value	Reference
S (Water solubility)	0.89 mg/mL	Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2B,CDK5,EIF2AK3,GRK2,PDK1,PDK2,PDK4,PRKDC	8
kinase-selectivity-class	AXL,BRAF,CDK9,EIF2AK3,EPHB4,GRK2,MAP2K6,MAPK7,MET,PDK4,PIK3CD,SIK2,SIK3,TEK,ZAP70	15
pfas-class	PFAS structural alert (1 = True, 0 = False)	1

Approvals:

Date	Agency	Company	Orphan
July 23, 2018	FDA	ABBVIE 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
Bone density decreased	272	49.22	64	1732	17281	90609370
Suicidal ideation	215.31	49.22	73	1723	73782	90552869
Hot flush	193.93	49.22	64	1732	59424	90567227
Heavy menstrual bleeding	153.65	49.22	42	1754	20488	90606163
Depression	104.62	49.22	68	1728	300533	90326118
Maternal exposure during pregnancy	93.48	49.22	68	1728	359995	90266656
Nausea	58.66	49.22	89	1707	1110227	89516424
Headache	58.54	49.22	78	1718	862668	89763983
Mood swings	54.38	49.22	19	1777	20683	90605968
Hysterectomy	52.21	49.22	16	1780	11568	90615083
Dysmenorrhoea	51.42	49.22	13	1783	4659	90621992
Bone loss	49.98	49.22	12	1784	3480	90623171
Mood altered	49.93	49.22	17	1779	17127	90609524

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
Bone density decreased	308.29	43.80	60	865	15982	110572392
Hot flush	107.24	43.80	34	891	66002	110522372
Heavy menstrual bleeding	90.15	43.80	22	903	16343	110572031
Suicidal ideation	87.94	43.80	32	893	93905	110494469
Maternal exposure during pregnancy	62.85	43.80	34	891	254849	110333525
Depression	61.13	43.80	36	889	317299	110271075
Bone loss	49.78	43.80	10	915	3045	110585329

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	H01CC03	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES HYPOTHALAMIC HORMONES Anti-gonadotropin-releasing hormones
ATC	H01CC53	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES HYPOTHALAMIC HORMONES Anti-gonadotropin-releasing hormones
FDA PE	N0000008638	Decreased GnRH Secretion
FDA MoA	N0000175084	Gonadotropin Releasing Hormone Receptor Antagonists
FDA EPC	N0000175839	Gonadotropin Releasing Hormone Receptor Antagonist
FDA MoA	N0000182140	Cytochrome P450 2C19 Inhibitors
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000190118	Cytochrome P450 3A Inducers

Related Drugs by ATC class:

H01CC Anti-gonadotropin-releasing hormones 6 drugs

cetrorelixestradiolganirelixlinzagolixnorethisteronerelugolix

Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Endometriosis	indication	129103003
Hepatic failure	contraindication	59927004
Osteoporosis	contraindication	64859006	DOID:11476

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.43	acidic
pKa2	6.88	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 300MG BASE,1MG,0.5MG; EQ 300MG BASE	ORIAHNN (COPACKAGED)	ABBVIE	N213388	May 29, 2020	RX	CAPSULE	ORAL	11459305	Nov. 7, 2028	MANAGEMENT OF HEAVY MENSTRUAL BLEEDING ASSOCIATED WITH UTERINE LEIOMYOMAS (FIBROIDS)
EQ 150MG BASE	ORILISSA	ABBVIE	N210450	July 23, 2018	RX	TABLET	ORAL	7419983	July 6, 2029	MANAGEMENT OF MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS
EQ 200MG BASE	ORILISSA	ABBVIE	N210450	July 23, 2018	RX	TABLET	ORAL	7419983	July 6, 2029	MANAGEMENT OF MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS
EQ 150MG BASE	ORILISSA	ABBVIE	N210450	July 23, 2018	RX	TABLET	ORAL	11707464	March 14, 2034	MANAGEMENT OF MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS USING 150 MG ELAGOLIX FOR UP TO 24 MONTHS
EQ 200MG BASE	ORILISSA	ABBVIE	N210450	July 23, 2018	RX	TABLET	ORAL	11344551	March 14, 2034	USE OF ELAGOLIX 200 MG BID FOR 6 MONTHS TO MANAGE MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS IN PREMENOPAUSAL WOMEN HAVING DYSPAREUNIA ASSOCIATED WITH ENDOMETRIOSIS
EQ 200MG BASE	ORILISSA	ABBVIE	N210450	July 23, 2018	RX	TABLET	ORAL	11344551	March 14, 2034	USE OF ELAGOLIX 200 MG BID FOR 6 MONTHS TO MANAGE MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS IN PREMENOPAUSAL WOMEN TO REDUCE DYSMENORRHEA AND NON-MENSTRUAL PELVIC PAIN
EQ 300MG BASE,1MG,0.5MG; EQ 300MG BASE	ORIAHNN (COPACKAGED)	ABBVIE	N213388	May 29, 2020	RX	CAPSULE	ORAL	10881659	March 14, 2034	MANAGEMENT OF HEAVY MENSTRUAL BLEEDING ASSOCIATED WITH UTERINE LEIOMYOMAS (FIBROIDS)
EQ 300MG BASE,1MG,0.5MG; EQ 300MG BASE	ORIAHNN (COPACKAGED)	ABBVIE	N213388	May 29, 2020	RX	CAPSULE	ORAL	11045470	March 14, 2034	MANAGEMENT OF HEAVY MENSTRUAL BLEEDING ASSOCIATED WITH UTERINE LEIOMYOMAS (FIBROIDS)
EQ 150MG BASE	ORILISSA	ABBVIE	N210450	July 23, 2018	RX	TABLET	ORAL	10537572	Sept. 1, 2036	MANAGEMENT OF MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS USING 150MG ELAGOLIX WHILE CO-ADMINISTERING RIFAMPIN
EQ 150MG BASE	ORILISSA	ABBVIE	N210450	July 23, 2018	RX	TABLET	ORAL	10682351	Sept. 1, 2036	MANAGEMENT OF MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS USING 150 MG ELAGOLIX WHILE CO-ADMINISTERING KETOCONAZOLE
EQ 150MG BASE	ORILISSA	ABBVIE	N210450	July 23, 2018	RX	TABLET	ORAL	11690854	April 19, 2038	MANAGEMENT OF MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS IN A PATIENT WITH MODERATE HEPATIC IMPAIRMENT
EQ 300MG BASE,1MG,0.5MG; EQ 300MG BASE	ORIAHNN (COPACKAGED)	ABBVIE	N213388	May 29, 2020	RX	CAPSULE	ORAL	12083227	Aug. 20, 2038	MANAGEMENT OF HEAVY MENSTRUAL BLEEDING ASSOCIATED WITH UTERINE LEIOMYOMAS (FIBROIDS)
EQ 150MG BASE	ORILISSA	ABBVIE	N210450	July 23, 2018	RX	TABLET	ORAL	11690845	Aug. 27, 2040	MANAGEMENT OF MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS USING 150 MG OR 200 MG ELAGOLIX WHILE CO-ADMINISTERING OMEPRAZOLE
EQ 200MG BASE	ORILISSA	ABBVIE	N210450	July 23, 2018	RX	TABLET	ORAL	11690845	Aug. 27, 2040	MANAGEMENT OF MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS USING 150 MG OR 200 MG ELAGOLIX WHILE CO-ADMINISTERING OMEPRAZOLE
EQ 300MG BASE,1MG,0.5MG; EQ 300MG BASE	ORIAHNN (COPACKAGED)	ABBVIE	N213388	May 29, 2020	RX	CAPSULE	ORAL	11690845	Aug. 27, 2040	MANAGEMENT OF HEAVY MENSTRUAL BLEEDING ASSOCIATED WITH UTERINE LEIOMYOMAS (FIBROIDS) USING 300 MG ELAGOLIX WHILE CO-ADMINISTERING OMEPRAZOLE

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	IC50	8.82		SCIENTIFIC LITERATURE	DRUG LABEL
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN		Ki	5.62		CHEMBL
Gonadotropin-releasing hormone receptor	GPCR		GNRHR_RAT		Ki	5.36		CHEMBL
Gonadotropin-releasing hormone receptor	GPCR		GNRHR_MACMU		Ki	8.48		CHEMBL

External reference:

ID	Source
5B2546MB5Z	UNII
832720-36-2	SECONDARY_CAS_RN
4037713	VANDF
C2714632	UMLSCUI
CHEBI:177453	CHEBI
F5O	PDB_CHEM_ID
CHEMBL1208155	ChEMBL_ID
11250647	PUBCHEM_CID
DB11979	DRUGBANK_ID
CHEMBL502182	ChEMBL_ID
D09335	KEGG_DRUG
8983	INN_ID
C539351	MESH_SUPPLEMENTAL_RECORD_UI
8362	IUPHAR_LIGAND_ID
773185009	SNOMEDCT_US
773234007	SNOMEDCT_US
773235008	SNOMEDCT_US
286383	MMSL
34698	MMSL
d08851	MMSL
017652	NDDF
017653	NDDF
2049846	RXNORM
5B2546MB5Z	INXIGHT DRUGS

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Orilissa	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0038	TABLET, FILM COATED	150 mg	ORAL	NDA	31 sections
Orilissa	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0039	TABLET, FILM COATED	200 mg	ORAL	NDA	31 sections