General
Preferred name
ELAGOLIX
Synonyms
ELAGOLIX SODIUM ()
NBI-56418 ()
(R)-Elagolix ()
NBI-56418 sodium ()
NBI-56418, ABT-620 ()
ORILISSA ()
NBI-56418 NA ()
ELAGOLIX SODIUM SALT ()
NBI-56418-NA ()
ORLISSA ()
Elagolix (sodium salt) ()
P&D ID
PD046271
CAS
834153-87-6
832720-36-2
Tags
available
drug
Approved by
FDA
First approval
2018
Drug indication
Uterine fibroids
Endometriosis
Drug Status
approved
investigational
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Elagolix is a non-peptide gonadotrophin receptor (GnRHR) antagonist . Note that some bioactivity data may be generated using the elagolix sodium salt.
PHARMACODYNAMICS
During a three menstrual cycle study in healthy women, an elagolix 150 mg once daily regimen and a 200 mg twice daily regimen resulted in an ovulation rate of about 50% and 32%, respectively [FDA Label]. In Phase 3 trials in women with endometriosis, elagolix caused a dose-dependent reduction in median estradiol concentrations to approximately 42 pg/mL for the 150 mg once daily regimen and 12 pg/mL for the 200 mg twice daily regimen [FDA Label].; ; Furthermore, the effect of elagolix on the QTc interval was investigated in a randomized, placebo- and positive-controlled, open-label, single-dose, crossover thorough QTc study in 48 healthy adult premenopausal women [FDA Label]. Elagolix concentrations in subjects administered a single dose of 1200 mg was seventeen times higher than the concentration in subjects given elagolix 200 mg twice daily. Nevertheless, there was no clinically relevant prolongation of the QTc interval [FDA Label].
MOA
Endometriosis develops when tissue that is similar to the kind that is normally located in the uterus starts to grow outside of the uterus [A35868, F801]. Such growth leads to various symptoms like pain during periods, pelvic pain between periods, and pain during sexual intercourse [A35868, F801]. The growths themselves are referred to as lesions and frequently develop on the ovaries, fallopian tubes, and other areas around the uterus, including the bowel or bladder [A35868, F801]. The growth of these lesions is dependent upon the estrogen hormone [A35868].; ; Elagolix is an orally-administered, nonpeptide small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist that inhibits endogenous GnRH signaling by binding competitively to GnRH receptors in the pituitary gland [FDA Label, A35855, A35856, A35857]. Administration of elagolix 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.
TOXICITY
In case of overdose, monitor the patient for any signs or symptoms of adverse reactions and initiate appropriate symptomatic treatment, as needed [FDA Label]. Common adverse reactions of elagolix include hot flush, headache, nausea, insomnia, mood alterations, amenorrhea, depression, anxiety, arthralgia, bone loss, changes in menstrual bleeding patterns, suicidal ideation and behavior, exacerbation of existing mood disorders, and/or hepatic transaminase elevations [FDA Label].; ; The recommended duration of use for elagolix is up to 24 months for the 150 mg once daily dose and up to six months for the 200 mg twice daily dose, as it causes a dose-dependent decrease in bone mineral density (BMD) [FDA Label]. BMD loss is greater with increasing duration of use and may not be completely reversible after stopping treatment [FDA Label]. For women with moderate hepatic impairment, the recommended dosage is 150 mg once daily for up to six months [FDA Label].
DESCRIPTION
Elagolix is a non-peptide gonadotrophin receptor (GnRHR) antagonist . As of July 2018, it is the first and only FDA-approved oral GnRH antagonist available for the treatment of moderate to severe endometriosis pain.
(GtoPdb)
DESCRIPTION
Elagolix is a Gonadotropin-Releasing Hormone (GnRH) Antagonist. Elagolix inhibits gonadatropin releasing hormone (GnRH) receptors in the pituitary gland and ultimately reduces circulating sex hormone levels. To date, elagolix has been studied in over 20 clinical trials totaling more than 1,000 subjects. A Phase 2a trial of elagolix for the treatment of uterine fibroids is also ongoing. Endometriosis can be a debilitating disease that affects millions of women around the world and the exploration of new treatments could offer other options for women with this disease
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
23
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP Approved Drugs
EUbOPEN Chemogenomics Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
Mcule NIBR MoA Box Subset
NCATS Inxight Approved Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
46
Molecular Weight
631.21
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
12
Ring Count
4
Aromatic Ring Count
4
cLogP
5.54
TPSA
102.56
Fraction CSP3
0.28
Chiral centers
1.0
Largest ring
6.0
QED
0.16
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
GPCR/G protein
Immunology/Inflammation
Target
GNRHR
GNRH Receptor
Nuclear Factor of activated T Cells (NFAT)
Member status
member
MOA
Antagonist of GNRHR
gonadotropin releasing factor hormone receptor antagonist
Recommended Cell Concentration
None
Source data
