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Vardenafil

Generic Name
Vardenafil
Brand Names
Levitra, Staxyn
Drug Type
Small Molecule
Chemical Formula
C23H32N6O4S
CAS Number
224785-90-4
Unique Ingredient Identifier
UCE6F4125H
Background

Vardenafil is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5) and an oral therapy for the treatment of erectile dysfunction. During sexual stimulation, nitric oxide (NO) is released from nerve endings and endothelial cells in the corpus cavernosum, activating the enzyme guanylate cyclase and increasing the synthesis of cGMP in the smooth muscle cells of the corpus cavernosum. PDE5 inhibitors, such as vardenafil, inhibit the degradation of cGMP and allow increased blood flow into the penis, resulting in an erection.. Compared to sildenafil and tadalafil, vardenafil is a more potent inhibitor of PDE5; however, its selectivity for other PDE isoforms is lower than the one detected for tadalafil.

The FDA approved the use of vardenafil for the treatment of erectile dysfunction in 2003. Although other PDE5 inhibitors such as sildenafil and tadalafil have been associated with rare cases of acute liver injury, the use of vardenafil has not been linked to hepatotoxic effects. The use of vardenafil as a monotherapy for the treatment of pulmonary arterial hypertension has also been evaluated.

Indication

Vardenafil is indicated for the treatment of erectile dysfunction.

Associated Conditions
Erectile Dysfunction
Clinical Trials
Related News

Respira Therapeutics to Present Phase 2b Results of RT234 Inhalation Therapy for PAH at ATS 2025

• Respira Therapeutics will present late-breaking results from its Phase 2b trial of RT234, an inhaled vardenafil powder for pulmonary arterial hypertension, at the ATS 2025 International Conference on May 20. • RT234 is being developed as the first as-needed (PRN) therapy for PAH patients to acutely improve exercise tolerance and reduce exertional symptoms, potentially enhancing daily activities and quality of life. • The innovative treatment utilizes Respira's proprietary Axial Oscillating Sphere Dry Powder Inhaler technology to maximize drug delivery to the distal lung for optimal therapeutic effect.

Karma Biosciences Files Patents for Rapid-Acting Nasal PDE-5 Inhibitors with 5-Minute Onset

• Karma Biosciences has applied for patents on nasally-administered formulations of sildenafil and vardenafil using their proprietary Zenergy™ excipient technology, showing onset within 5 minutes of administration. • In-vivo testing demonstrated the nasal formulations achieve significantly higher peak blood levels compared to conventional oral versions of these erectile dysfunction medications. • The company's Zenergy™ technology forms a carrier vehicle around drug particles, enabling rapid penetration of nasal membranes and potentially expanding applications beyond the $3 billion global erectile dysfunction market.

First Patient Dosed in Phase 2b Trial of RT234, a Novel Inhaled Therapy for Pulmonary Arterial Hypertension

• Respira Therapeutics has dosed the first patient in its Phase 2b VIPAH-PRN trial evaluating RT234, an innovative dry powder inhaled formulation of vardenafil for on-demand symptom relief in PAH patients. • RT234 represents a first-in-class approach for PAH, designed for "as needed" use to acutely improve exercise capacity and reduce breathlessness, unlike current maintenance therapies that don't address episodic symptoms. • The multicenter dose-escalation study will assess RT234's ability to provide rapid symptom relief for patients with NYHA Functional Class II-III PAH symptoms, potentially addressing a significant unmet need in disease management.
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