General
Preferred name
ENZALUTAMIDE
Synonyms
MDV3100 ()
Xtandi ()
MDV 3100 ()
HC-1119 ()
HC-1119,?MDV3100 ()
Enzalutamide (MDV3100) ()
DEUTENZALUTAMIDE ()
EnzalutamideMDV-3100F2175N-Methyl-4-[3-(4-cyano-3-trifluoromethylphenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl]-2-fluorobenzamide ()
Enzalutamide d3 ()
MDV-3100 ()
Enzalutamida ()
HC 1119 ()
Deutenzalutamida ()
Hc1119 ()
P&D ID
PD004101
CAS
915087-33-1
1443331-82-5
Tags
available
drug
drug candidate
Approved by
PMDA
FDA
First approval
2012
Drug indication
prostate adenocarcinoma
Prostate cancer
Drug Status
approved
investigational
Max Phase
3.0
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 Enzalutamide is an androgen receptor antagonist
ABSORPTION The pharmacokinetic profile of enzalutamide and N-desmethyl enzalutamide (its major active metabolite) is described by a linear two-compartment model with first-order absorption. Enzalutamide also accumulates. Food does not affect its absorption. ; Tmax, prostate cancer patients = 1 hour (range of 0.5-3 hours);; Cmax, steady state, enzalutamide = 16.6 μg/mL;; Cmax, steady state, N-desmethyl enzalutamide = 12.7 μg/mL;; Time to steady state, daily dosing = 28 days;
DESCRIPTION Enzalutamide is an androgen receptor antagonist. (GtoPdb)
DESCRIPTION Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator[1][2].
PRICE 49
DESCRIPTION Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP) that activates autophagy, exhibits antitumor activity, and is commonly used in treating desmoplasia-resistant prostate cancer. (TargetMol Bioactive Compound Library)
Cell lines
8
Organisms
0
Compound Sets
28
AdooQ Bioactive Compound Library
A10562
Axon Medchem Screening Library
1613
Cayman Chemical Bioactives
11596
ChEMBL Approved Drugs
CHEMBL1082407
ChEMBL Drugs
CHEMBL1082407
CHEMBL4594421
Concise Guide to Pharmacology 2017/18
6812
Concise Guide to Pharmacology 2019/20
6812
Concise Guide to Pharmacology 2021/22
6812
Concise Guide to Pharmacology 2023/24
6812
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB08899
DB19123
DrugBank Approved Drugs
DB08899
DrugCentral
4628
DrugCentral Approved Drugs
4628
DrugMAP
DMGL19D
DMB06MU
DrugMAP Approved Drugs
DMGL19D
Guide to Pharmacology
6812
LINCS compound set
10353-101
Mcule NIBR MoA Box Subset
MCULE-4665809964
MedChem Express Bioactive Compound Library
HY-70002
Natural product-based probes and drugs
NCATS Inxight Approved Drugs
93T0T9GKNU
NIH Approved Oncology Drugs
440803814
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
MDV3100
deutenzalutamide
TargetMol Bioactive Compound Library
T6002
External IDs
42
Properties
(calculated by RDKit )
Molecular Weight
464.09
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
3
Ring Count
3
Aromatic Ring Count
2
cLogP
3.99
TPSA
76.44
Fraction CSP3
0.24
Chiral centers
0.0
Largest ring
6.0
QED
0.55
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
MOA
androgen receptor
Androgen Receptor Antagonists
Androgen Receptor antagonist
Member status
member
Indication
prostate cancer
Target
AR
AR antagonist
Androgen Receptor
Androgen Receptor,Autophagy
Pathway
Autophagy
Endocrinology/Hormones
Vitamin D Related/Nuclear Receptor
Therapeutic Indication
Anticancer
Source data