Vardenafil

Phosphodiesterase 5 Inhibitor — GENITO URINARY SYSTEM AND SEX HORMONES

Key facts

Vardenafil is an ofp drug in the Phosphodiesterase 5 Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2003. Its mechanism of action is classified as Phosphodiesterase 5 Inhibitors. DrugCentral lists 10 molecular targets, including PDE5A, PDE6A and PDE1A. Recorded indications include Impotence.

• Approval status: ofp (first approved 2003 by the FDA).
• Drug class: Phosphodiesterase 5 Inhibitor.
• Mechanism of action: Phosphodiesterase 5 Inhibitors.
• Molecular targets: PDE5A, PDE6A, PDE1A and PDE11A (10 listed in DrugCentral).
• Indications: Impotence.
• ATC code: G04BE09 (Drugs used in erectile dysfunction).
• Molecular formula: C23H32N6O4S; molecular weight 488.61 g/mol.

Indications & contraindications

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

Indications (1)

• Impotence

Contraindications (24)

• Acute coronary syndrome
• Acute nephropathy
• Acute peptic ulcer
• Anterior ischemic optic neuropathy
• Aortic valve stenosis
• Blood coagulation disorder
• Cerebrovascular accident
• Chronic heart failure
• Congenital long QT syndrome
• Fibrosis of corpus cavernosum
• Hb SS disease
• Hearing loss
• Hepatic failure
• Hypertensive urgency
• Idiopathic hypertrophic subaortic stenosis
• Induratio penis plastica
• Leukemia, disease
• Life-Threatening Cardiac Arrhythmias
• Low blood pressure
• Multiple myeloma
• Myocardial infarction
• Penis bent
• Pigmentary Retinopathy
• Priapism

Mechanism & targets

• Mechanism of action (MoA): Phosphodiesterase 5 Inhibitors
• Established pharmacologic class: Phosphodiesterase 5 Inhibitor

Molecular targets (10)

Target	Gene	Action	Activity
cGMP-specific 3',5'-cyclic phosphodiesterase	PDE5A	inhibitor	IC50 9.15
Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha	PDE6A	unknown	IC50 7.46
Calcium/calmodulin-dependent 3',5'-cyclic nucleotide phosphodiesterase 1A	PDE1A	unknown	IC50 7.04
Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A	PDE11A	unknown	IC50 6.89
Phosphodiesterase 1	PDE1A|PDE1B	unknown	IC50 6.74
High affinity cGMP-specific 3',5'-cyclic phosphodiesterase 9A	PDE9A	unknown	IC50 6.34
cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A	PDE10A	unknown	IC50 6.10
Phosphodiesterase 3	PDE3B|PDE3A	unknown	IC50 5.68
cGMP-dependent 3',5'-cyclic phosphodiesterase	PDE2A	unknown	IC50 5.51
Phosphodiesterase 4	PDE4A|PDE4B|PDE4C|PDE4D	unknown	IC50 5.35

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2003-08-19	FDA	—	BAYER HLTHCARE

ATC classification

ATC code	Therapeutic hierarchy
G04BE09	GENITO URINARY SYSTEM AND SEX HORMONES › UROLOGICALS › UROLOGICALS › Drugs used in erectile dysfunction

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label

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
Enterocolitis infectious	112.8
Accessory spleen	66.1
Optic ischaemic neuropathy	54.9
Food interaction	52.0
Retinal deposits	39.1
Hepatic cyst	32.8
Biliary tract infection	31.6
Macular thickening	30.1
Drug ineffective	28.4
Dyschromatopsia	27.8
Immune-mediated myositis	27.7

Chemical structure

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

• Molecular formula: C₂₃H₃₂N₆O₄S
• Molecular weight: 488.61 g/mol
• CAS number: 224785-90-4
• InChIKey: SECKRCOLJRRGGV-UHFFFAOYSA-N
• PubChem CID: 135400189

CCCC1=NC(C)=C2N1N=C(NC2=O)C1=CC(=CC=C1OCC)S(=O)(=O)N1CCN(CC)CC1

Frequently asked questions

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

What is Vardenafil used for?

DrugCentral lists the following indications for Vardenafil: Impotence.

How does Vardenafil work?

Vardenafil is classified as Phosphodiesterase 5 Inhibitors; its molecular targets in DrugCentral include PDE5A (inhibitor), PDE6A, PDE1A and PDE11A.

When was Vardenafil first approved?

Vardenafil was first approved by the FDA in 2003.

What drug class does Vardenafil belong to?

Vardenafil is in the Phosphodiesterase 5 Inhibitor class.

What is the chemical formula of Vardenafil?

Vardenafil has the molecular formula C23H32N6O4S and a molecular weight of 488.61 g/mol.

Sources

• DrugCentral drug card 2809 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1339 — compound record and bioactivity
• PubChem CID 135400189 — chemical identifiers
• DrugBank DB00862 — drug record
• FDA UNII UCE6F4125H — substance identity
• DailyMed: FDA labels for Vardenafil — current prescribing information (label search)
• UniProt O76074 (PDE5A) — target protein
• UniProt P16499 (PDE6A) — target protein
• UniProt P54750 (PDE1A) — target protein
• UniProt Q9HCR9 (PDE11A) — target protein
• UniProt O76083 (PDE9A) — target protein
• UniProt Q9Y233 (PDE10A) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.