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

Stem definitionDrug idCAS RN
gonadotropin releasing hormone (GnRH) antagonists 5293 834153-87-6

Description:

MoleculeDescription

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:

PropertyValueReference
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

Approvals:

DateAgencyCompanyOrphan
July 23, 2018 FDA ABBVIE INC

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
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

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

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (acidic/basic)
pKa1 3.43 acidic
pKa2 6.88 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent 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 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 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 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 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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
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 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 July 23, 2023 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Gonadotropin-releasing hormone receptor GPCR ANTAGONIST IC50 8.82 SCIENTIFIC LITERATURE DRUG LABEL
Gonadotropin-releasing hormone receptor GPCR Ki 5.36 CHEMBL
Gonadotropin-releasing hormone receptor GPCR Ki 8.48 CHEMBL

External reference:

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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