General
Preferred name
CILOSTAZOL
Synonyms
Opc-13013 ()
OPC 21 ()
OPC 13013 ()
cilostazol SR ()
Cilostazol (OPC-13013) ()
Pletal,OPC-13013 ()
NSC-758936 ()
Pletal ()
OPC-21 ()
Cilostazol-d4 ()
P&D ID
PD000554
CAS
1073608-02-2
73963-72-1
1215541-47-1
Tags
natural product
drug
available
Approved by
FDA
First approval
1999
Drug Status
investigational
approved
Drug indication
Vasodilator
Inhibitor (platelet)
Antithrombotic
Intermittent claudication
Max Phase
Phase 4
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PHARMACODYNAMICS Cilostazol reduces the symptoms of intermittent claudication, as indicated by an increased walking distance. Intermittent claudication is pain in the legs that occurs with walking and disappears with rest. The pain occurs due to reduced blood flow to the legs.
INDICATION Indicated for the alleviation of symptoms of intermittent claudication (pain in the legs that occurs with walking and disappears with rest).
ROE Cilostazol is extensively metabolized by hepatic cytochrome P-450 enzymes, mainly 3A4, and, to a lesser extent, 2C19, with metabolites largely excreted in urine. Cilostazol is eliminated predominately by metabolism and subsequent urinary excretion of metabolites. The primary route of elimination was via the urine (74%), with the remainder excreted in feces (20%). No measurable amount of unchanged cilostazol was excreted in the urine, and less than 2% of the dose was excreted as 3,4-dehydro-cilostazol.; About 30% of the dose was excreted in urine as 4'-trans-hydroxy-cilostazol.
DESCRIPTION Cilostazol is a quinolinone-derivative phosphodiesterase (PDE) inhibitor. (GtoPdb)
DESCRIPTION PDE3 inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION PDE3A inhibitor. Also adenosine uptake inhibitor (Tocriscreen Plus)
DESCRIPTION Specific type III phosphodiesterase (PDE) inhibitor (LOPAC library)
DESCRIPTION PDE3A inhibitor. Also adenosine uptake inhibitor (Tocriscreen Total)
Cell lines
0
Organisms
3
Compound Sets
35
AdooQ Bioactive Compound Library
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
DrugMatrix
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
JUMP-Target 1 Compound Set
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
NCATS Inxight Approved Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
The Spectrum Collection
Tocris Bioactive Compound Library
Tocriscreen Plus
Tocriscreen Total
External IDs
39
Properties
(calculated by RDKit )
Molecular Weight
369.22
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
1
Rotatable Bonds
7
Ring Count
4
Aromatic Ring Count
2
cLogP
3.46
TPSA
81.93
Fraction CSP3
0.6
Chiral centers
0.0
Largest ring
6.0
QED
0.76
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target Type
Enzymes
Selectivity
PDE III
Pathway
Metabolism
Autophagy
Metabolic Enzyme/Protease
Target
PDE3
PDE3A, PDE3B
PDE3A
Phosphodiesterase (PDE)
PDE
Primary Target
Phosphodiesterases
MOA
Inhibitor
Phosphodiesterase III Inhibitors
phosphodiesterase inhibitor
Member status
member
Indication
claudication
Therapeutic Class
Vasodilator Agents
Source data