Elagolix

Gonadotropin Releasing Hormone Receptor Antagonist — SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS

Key facts

Elagolix is an onp drug in the Gonadotropin Releasing Hormone Receptor Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 2018. Its mechanism of action is classified as Cytochrome P450 2C19 Inhibitors, Cytochrome P450 3A Inducers and Gonadotropin Releasing Hormone Receptor Antagonists. DrugCentral lists 4 molecular targets, including GNRHR, GNRHR and OPRK1. Recorded indications include Endometriosis.

• Approval status: onp (first approved 2018 by the FDA).
• Drug class: Gonadotropin Releasing Hormone Receptor Antagonist.
• Mechanism of action: Cytochrome P450 2C19 Inhibitors; Cytochrome P450 3A Inducers; Gonadotropin Releasing Hormone Receptor Antagonists.
• Molecular targets: GNRHR, GNRHR, OPRK1 and Gnrhr (4 listed in DrugCentral).
• Indications: Endometriosis.
• ATC code: H01CC03 (Anti-gonadotropin-releasing hormones).
• Molecular formula: C32H30F5N3O5; molecular weight 631.60 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Endometriosis

Contraindications (2)

• Hepatic failure
• Osteoporosis

Mechanism & targets

• Mechanism of action (MoA): Cytochrome P450 2C19 Inhibitors; Cytochrome P450 3A Inducers; Gonadotropin Releasing Hormone Receptor Antagonists; P-Glycoprotein Inhibitors
• Established pharmacologic class: Gonadotropin Releasing Hormone Receptor Antagonist

Molecular targets (4)

Target	Gene	Action	Activity
Gonadotropin-releasing hormone receptor	GNRHR	antagonist	IC50 8.82
Gonadotropin-releasing hormone receptor	GNRHR	unknown	Ki 8.48
Kappa-type opioid receptor	OPRK1	unknown	Ki 5.62
Gonadotropin-releasing hormone receptor	Gnrhr	unknown	Ki 5.36

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2018-07-23	FDA	—	ABBVIE INC

ATC classification

ATC code	Therapeutic hierarchy
H01CC03	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS › PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES › HYPOTHALAMIC HORMONES › Anti-gonadotropin-releasing hormones
H01CC53	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS › PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES › HYPOTHALAMIC HORMONES › Anti-gonadotropin-releasing hormones

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• FDA label: SLCO1B1 · Informative PGx
• HCSC label: SLCO1B1 · No Clinical PGx

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Bone density decreased	282.9
Suicidal ideation	209.3
Hot flush	204.1
Heavy menstrual bleeding	169.8
Depression	111.6
Maternal exposure during pregnancy	109.8
Headache	72.4
Nausea	65.5
Hysterectomy	58.6
Dysmenorrhoea	55.8
Mood swings	54.7
Anxiety	52.1

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Elagolix is on its molecule page.

• Molecular formula: C₃₂H₃₀F₅N₃O₅
• Molecular weight: 631.60 g/mol
• CAS number: 834153-87-6
• InChIKey: HEAUOKZIVMZVQL-VWLOTQADSA-N
• PubChem CID: 11250647

COC1=CC=CC(=C1F)C1=C(C)N(CC2=C(F)C=CC=C2C(F)(F)F)C(=O)N(C[C@H](NCCCC(O)=O)C2=CC=CC=C2)C1=O

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Elagolix used for?

DrugCentral lists the following indications for Elagolix: Endometriosis.

How does Elagolix work?

Elagolix is classified as Cytochrome P450 2C19 Inhibitors, Cytochrome P450 3A Inducers and Gonadotropin Releasing Hormone Receptor Antagonists; its molecular targets in DrugCentral include GNRHR (antagonist), GNRHR, OPRK1 and Gnrhr.

When was Elagolix first approved?

Elagolix was first approved by the FDA in 2018.

What drug class does Elagolix belong to?

Elagolix is in the Gonadotropin Releasing Hormone Receptor Antagonist class.

What is the chemical formula of Elagolix?

Elagolix has the molecular formula C32H30F5N3O5 and a molecular weight of 631.60 g/mol.

Sources

• DrugCentral drug card 5293 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1208155 — compound record and bioactivity
• PubChem CID 11250647 — chemical identifiers
• DrugBank DB11979 — drug record
• FDA UNII 5B2546MB5Z — substance identity
• DailyMed: FDA labels for Elagolix — current prescribing information (label search)
• UniProt P30968 (GNRHR) — target protein
• UniProt P41145 (OPRK1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.