General
Preferred name
DEGARELIX
Synonyms
DEGARELIX ACETATE ()
FE 200486 (free base) ()
Degarelix (acetate) ()
FE200486 (FREE BASE) ()
Degarelix accord ()
FE200486 ()
Degarelix (as acetate) ()
FIRMAGON ()
FE-200486 ()
Degarelix acetate hydrate ()
FE200486 (AS ACETATE SALT) ()
P&D ID
PD016212
CAS
934016-19-0
214766-78-6
Tags
available
drug
Approved by
PMDA
FDA
First approval
2008
Drug indication
prostate adenocarcinoma
Prostate cancer
Neoplasm
Drug Status
approved
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)
ABSORPTION Degarelix forms a depot at the site of injection after subcutaneous administration from which the drug slowly released into circulation. After a single bolus dose of 2mg/kg, peak plasma concentrations of degarelix occured within 6 hours at a concentration of 330 ng/mL. ; Ki = 0.082 ng/mL and 93% of receptors were fully suppressed; ; MRT = 4.5 days.
MOA Degarelix competitively inhibits GnRH receptors in the pituitary gland, preventing the release of luteinizing hormone (LH) and follicle stimulating hormone. Reduced LH suppresses testosterone release, which slows the growth and reduces the size of prostate cancers.
HALF-LIFE Terminal half-life: 41.5 - 70.2 days; ; Absorption half-life: 32.9 hours; ; Half-life from injection site: 1.17 days.
DESCRIPTION Synthetic analogue of the GnRH decapeptide, with antagonistic action. (GtoPdb)
Cell lines
0
Organisms
1
Compound Sets
17
AdooQ Bioactive Compound Library
A12840
Cayman Chemical Bioactives
24069
ChEMBL Approved Drugs
CHEMBL415606
CHEMBL2028987
ChEMBL Drugs
CHEMBL415606
CHEMBL2028987
Drug Repurposing Hub
DrugBank
DB06699
DrugBank Approved Drugs
DB06699
DrugCentral
4379
DrugCentral Approved Drugs
4379
DrugMAP
DM3O8QY
DrugMAP Approved Drugs
DM3O8QY
EUbOPEN Chemogenomics Library
EUB0000760
Guide to Pharmacology
5585
MedChem Express Bioactive Compound Library
HY-16168A
NCATS Inxight Approved Drugs
SX0XJI3A11
ReFrame library
Selleckchem Bioactive Compound Library
degarelix-acetate
External IDs
45
Properties
(calculated by RDKit )
Molecular Weight
1630.75
Hydrogen Bond Acceptors
18
Hydrogen Bond Donors
17
Rotatable Bonds
41
Ring Count
8
Aromatic Ring Count
6
cLogP
1.51
TPSA
512.87
Fraction CSP3
0.41
Chiral centers
11.0
Largest ring
6.0
QED
0.02
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Indication
prostate cancer
Target
GNRHR
Apoptosis
GNRH Receptor
MOA
gonadotropin releasing factor hormone receptor antagonist
Pathway
GPCR/G protein
Recommended Cell Concentration
10 nM
Source data