Cilostazol

Phosphodiesterase 3 Inhibitor — BLOOD AND BLOOD FORMING ORGANS

Key facts

Cilostazol is an ofp drug in the Phosphodiesterase 3 Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 1999. Its mechanism of action is classified as Phosphodiesterase 3 Inhibitors. DrugCentral lists 3 molecular targets, including PDE3A, PDE3B and CYP2C9. Recorded indications include Intermittent claudication.

• Approval status: ofp (first approved 1999 by the FDA).
• Drug class: Phosphodiesterase 3 Inhibitor.
• Mechanism of action: Phosphodiesterase 3 Inhibitors.
• Molecular targets: PDE3A, PDE3B and CYP2C9 (3 listed in DrugCentral).
• Indications: Intermittent claudication.
• ATC code: B01AC23 (Platelet aggregation inhibitors excl. heparin).
• Molecular formula: C20H27N5O2; molecular weight 369.47 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Intermittent claudication

Contraindications (3)

• Chronic heart failure
• Disease of liver
• Kidney disease

Mechanism & targets

• Mechanism of action (MoA): Phosphodiesterase 3 Inhibitors
• Established pharmacologic class: Phosphodiesterase 3 Inhibitor

Molecular targets (3)

Target	Gene	Action	Activity
cGMP-inhibited 3',5'-cyclic phosphodiesterase A	PDE3A	inhibitor	IC50 6.70
cGMP-inhibited 3',5'-cyclic phosphodiesterase B	PDE3B	inhibitor	IC50 6.42
Cytochrome P450 2C9	CYP2C9	unknown	IC50 5.00

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1999-01-15	FDA	—	OTSUKA

ATC classification

ATC code	Therapeutic hierarchy
B01AC23	BLOOD AND BLOOD FORMING ORGANS › ANTITHROMBOTIC AGENTS › ANTITHROMBOTIC AGENTS › Platelet aggregation inhibitors excl. heparin

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Cerebral infarction	198.4
Interstitial lung disease	90.4
Gastrointestinal haemorrhage	73.1
Hepatic function abnormal	71.1
Cardiac failure	65.6
Cerebral haemorrhage	60.4
Lacunar infarction	58.2
Peripheral arterial occlusive disease	58.1
Renal impairment	57.6
Ventricular fibrillation	55.3
Pemphigoid	53.6
Cardiac failure congestive	51.8

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Cilostazol is on its molecule page.

• Molecular formula: C₂₀H₂₇N₅O₂
• Molecular weight: 369.47 g/mol
• CAS number: 73963-72-1
• InChIKey: RRGUKTPIGVIEKM-UHFFFAOYSA-N
• PubChem CID: 2754

O=C1CCC2=CC(OCCCCC3=NN=NN3C3CCCCC3)=CC=C2N1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Cilostazol used for?

DrugCentral lists the following indications for Cilostazol: Intermittent claudication.

How does Cilostazol work?

Cilostazol is classified as Phosphodiesterase 3 Inhibitors; its molecular targets in DrugCentral include PDE3A (inhibitor), PDE3B (inhibitor) and CYP2C9.

When was Cilostazol first approved?

Cilostazol was first approved by the FDA in 1999.

What drug class does Cilostazol belong to?

Cilostazol is in the Phosphodiesterase 3 Inhibitor class.

What is the chemical formula of Cilostazol?

Cilostazol has the molecular formula C20H27N5O2 and a molecular weight of 369.47 g/mol.

Sources

• DrugCentral drug card 644 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL799 — compound record and bioactivity
• PubChem CID 2754 — chemical identifiers
• DrugBank DB01166 — drug record
• FDA UNII N7Z035406B — substance identity
• DailyMed: FDA labels for Cilostazol — current prescribing information (label search)
• UniProt Q14432 (PDE3A) — target protein
• UniProt Q13370 (PDE3B) — target protein
• UniProt P11712 (CYP2C9) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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