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

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:

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

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Approvals:

Date	Agency	Company	Orphan
July 23, 2018	FDA	ABBVIE INC

FDA Adverse Event Reporting System (Female)

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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	221.77	59.35	55	1542	14557	63472868
Suicidal ideation	206.58	59.35	72	1525	62349	63425076
Hot flush	169.04	59.35	59	1538	51100	63436325
Heavy menstrual bleeding	145.23	59.35	41	1556	17732	63469693
Depression	113.82	59.35	67	1530	196425	63291000
Maternal exposure during pregnancy	87.06	59.35	59	1538	220003	63267422

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FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

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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	259.74	60.14	52	750	13295	79730291
Hot flush	95.02	60.14	31	771	54846	79688740
Suicidal ideation	88.75	60.14	32	770	76308	79667278
Heavy menstrual bleeding	84.50	60.14	21	781	13990	79729596
Depression	65.02	60.14	35	767	216755	79526831
Maternal exposure during pregnancy	64.41	60.14	30	772	136508	79607078

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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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 EPC	N0000175839	Gonadotropin Releasing Hormone Receptor Antagonist
FDA MoA	N0000175084	Gonadotropin Releasing Hormone Receptor Antagonists
FDA MoA	N0000182140	Cytochrome P450 2C19 Inhibitors
FDA MoA	N0000185503	P-Glycoprotein Inhibitors
FDA MoA	N0000190118	Cytochrome P450 3A Inducers
FDA PE	N0000008638	Decreased GnRH Secretion

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

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

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🐶 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)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 150MG BASE	ORILISSA	ABBVIE	N210450	July 23, 2018	RX	TABLET	ORAL	7176211	July 6, 2024	MANAGEMENT OF MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS
EQ 150MG BASE	ORILISSA	ABBVIE	N210450	July 23, 2018	RX	TABLET	ORAL	7419983	July 6, 2024	MANAGEMENT OF MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS
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 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	7176211	July 6, 2024	MANAGEMENT OF MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS
EQ 200MG BASE	ORILISSA	ABBVIE	N210450	July 23, 2018	RX	TABLET	ORAL	7419983	July 6, 2024	MANAGEMENT OF MODERATE TO SEVERE PAIN 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 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

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
EQ 150MG BASE	ORILISSA	ABBVIE	N210450	July 23, 2018	RX	TABLET	ORAL	July 23, 2023	NEW CHEMICAL ENTITY
EQ 200MG BASE	ORILISSA	ABBVIE	N210450	July 23, 2018	RX	TABLET	ORAL	July 23, 2023	NEW CHEMICAL ENTITY
EQ 300MG BASE,1MG,0.5MG; EQ 300MG BASE	ORIAHNN (COPACKAGED)	ABBVIE	N213388	May 29, 2020	RX	CAPSULE	ORAL	May 29, 2023	NEW PRODUCT
EQ 300MG BASE,1MG,0.5MG; EQ 300MG BASE	ORIAHNN (COPACKAGED)	ABBVIE	N213388	May 29, 2020	RX	CAPSULE	ORAL	July 23, 2023	NEW CHEMICAL ENTITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Gonadotropin-releasing hormone receptor	GPCR	P30968	GNRHR_HUMAN	ANTAGONIST	IC50	8.82	SCIENTIFIC LITERATURE	DRUG LABEL
Gonadotropin-releasing hormone receptor	GPCR		GNRHR_RAT		Ki	5.36	CHEMBL
Gonadotropin-releasing hormone receptor	GPCR		GNRHR_MACMU		Ki	8.48	CHEMBL

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External reference:

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ID	Source
017652	NDDF
017653	NDDF
11250647	PUBCHEM_CID
2049846	RXNORM
286383	MMSL
34698	MMSL
4037713	VANDF
5B2546MB5Z	UNII
773185009	SNOMEDCT_US
773234007	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Orilissa	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0038	TABLET, FILM COATED	150 mg	ORAL	NDA	32 sections
Orilissa	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0038	TABLET, FILM COATED	150 mg	ORAL	NDA	32 sections
Orilissa	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0038	TABLET, FILM COATED	150 mg	ORAL	NDA	32 sections
Orilissa	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0039	TABLET, FILM COATED	200 mg	ORAL	NDA	32 sections
Orilissa	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0039	TABLET, FILM COATED	200 mg	ORAL	NDA	32 sections
Orilissa	HUMAN PRESCRIPTION DRUG LABEL	1	0074-0039	TABLET, FILM COATED	200 mg	ORAL	NDA	32 sections

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