General
Preferred name
Relugolix
Synonyms
RVT-601 ()
TAK-385 ()
RVT-601, TAK-385 ()
Relugolix component of myfembree ()
Orgovyx ()
P&D ID
PD051359
CAS
737789-87-6
Tags
available
drug
Approved by
EMA
PMDA
FDA
First approval
2019
Drug indication
Endometriosis
Prostate cancer
Drug Status
approved
investigational
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209)[1]. Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al[2].
PRICE 133
DESCRIPTION Relugolix (TAK-385) is a non-peptide, orally active GnRH receptor antagonist . Administration suppresses the hypothalamic-pituitary-gonadal axis. In males this causes chemical castration. (GtoPdb)
DESCRIPTION Relugolix (RVT-601) is an orally available, non-peptide gonadotropin-releasing hormone (GnRH or luteinizing hormone-releasing hormone (LHRH)) antagonist, with potential antineoplastic activity. Relugolix competitively binds to and blocks the GnRH receptor in the anterior pituitary gland, which both prevents GnRH binding to the GnRH receptor and inhibits the secretion and release of both luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone from Leydig cells in the testes. Since testosterone is required to sustain prostate growth, reducing testosterone levels may inhibit hormone-dependent prostate cancer cell proliferation. (TargetMol Bioactive Compound Library)
Compound Sets
19
Cayman Chemical Bioactives
29512
ChEMBL Approved Drugs
CHEMBL1800159
ChEMBL Drugs
CHEMBL1800159
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB11853
DrugBank Approved Drugs
DB11853
DrugCentral
5432
DrugCentral Approved Drugs
5432
DrugMAP
DMK7IWL
DrugMAP Approved Drugs
DMK7IWL
EU-OPENSCREEN Bioactive Compound Library
EOS100587
Guide to Pharmacology
5586
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1800159
MedChem Express Bioactive Compound Library
HY-16474
NCATS Inxight Approved Drugs
P76B05O5V6
ReFrame library
Selleckchem Bioactive Compound Library
relugolix
TargetMol Bioactive Compound Library
T3630
External IDs
24
Properties
(calculated by RDKit )
Molecular Weight
623.18
Hydrogen Bond Acceptors
11
Hydrogen Bond Donors
2
Rotatable Bonds
9
Ring Count
5
Aromatic Ring Count
5
cLogP
3.75
TPSA
132.61
Fraction CSP3
0.21
Chiral centers
0.0
Largest ring
6.0
QED
0.24
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
GNRHR
GNRH Receptor
MOA
gonadotropin releasing factor hormone receptor antagonist
Pathway
GPCR/G protein
Source data