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

Stem definitionDrug idCAS RN
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:

None

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
Suicidal ideation 191.80 57.92 68 1451 57674 56232874
Bone density decreased 155.86 57.92 41 1478 12719 56277829
Endometriosis 151.00 57.92 33 1486 4669 56285879
Hot flush 147.29 57.92 53 1466 46673 56243875
Heavy menstrual bleeding 141.59 57.92 40 1479 16169 56274379
Depression 104.40 57.92 63 1456 180054 56110494
Maternal exposure during pregnancy 84.00 57.92 56 1463 189497 56101051

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 186.50 59.63 39 726 11435 70916244
Suicidal ideation 89.48 59.63 32 733 69564 70858115
Endometriosis 82.25 59.63 16 749 3220 70924459
Heavy menstrual bleeding 80.13 59.63 20 745 12645 70915034
Hot flush 79.89 59.63 27 738 49557 70878122
Maternal exposure during pregnancy 64.07 59.63 29 736 115316 70812363

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
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 INC 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 INC 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 INC 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 INC 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 INC 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 INC 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 INC 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 INC 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 INC 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 INC 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

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 INC N213388 May 29, 2020 RX CAPSULE ORAL May 29, 2023 NEW PRODUCT
EQ 150MG BASE ORILISSA ABBVIE INC N210450 July 23, 2018 RX TABLET ORAL July 23, 2023 NEW CHEMICAL ENTITY
EQ 200MG BASE ORILISSA ABBVIE INC 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 INC 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
C539351 MESH_SUPPLEMENTAL_RECORD_UI
2049846 RXNORM

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 0074-0039 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