Patient

Clinical Evidence

Clinical Evidence: Registration Study¹

Single-dose, randomized, open-label, 2-treatment, 2-period crossover (n=18 healthy adult males)

Pivotal Pharmacokinetic Study
Parameter Roxus® Nasal Spray (5mg) Vardenafil Oral Tablet (10mg) Difference
Tmax (mean) 12 minutes 56 minutes 78% faster (p<0.0001)
Cmax/D (ng/mL/mg) 1.9864 1.2769 155.6% (dose-normalized)
AUC0-t/D (h*ng/mL/mg) 3.8921 3.4815 111.8% (dose-normalized)
Half-life (t½) 4.15 hours 4.23 hours Comparable

Tmax (mean)

Roxus® 5mg 12 minutes
Vardenafil 10mg 56 minutes
78% faster (p<0.0001)

Cmax/D (ng/mL/mg)

Roxus® 5mg 1.9864
Vardenafil 10mg 1.2769
155.6% (dose-normalized)

AUC0-t/D (h*ng/mL/mg)

Roxus® 5mg 3.8921
Vardenafil 10mg 3.4815
111.8% (dose-normalized)

Half-life (t½)

Roxus® 5mg 4.15 hours
Vardenafil 10mg 4.23 hours
Comparable

Clinical Evidence: Pharmacokinetic Studies

Wang et al. 2023¹

The Journal of Sexual Medicine

Comparison study:

5mg intranasal vs 10mg oral vardenafil

  • Median Tmax: 10 min vs 58 min (p<0.001)
  • Relative bioavailability: 1.67× oral
  • Similar Cmax and half-life
  • 50% had transient nasal discomfort (tolerable, resolved quickly)
  • Similar systemic adverse events
Chung et al. 2025²

European Journal of Pharmaceutical Sciences

Phase 1 crossover:

intranasal vs oral vardenafil

  • Intranasal associated with more rapid onset
  • Similar plasma concentrations achieved
  • Some local irritation but well-tolerated
  • Important implications for spontaneity

References:

  1. Wang, J et al. “Pharmacokinetics Comparison of Vardenafil as Administered by an Intranasal Spray Formulation vs a 10-mg Oral Tablet.” The Journal of Sexual Medicine 00, no. 00 (2023) 1–6. https://doi.org/10.1093/jsxmed/qdad056.
  2. E. Chung et. al. 2025, Pharmacokinetics of an oral versus intranasal delivered formulation of the phosphodiesterase type 5 inhibitor vardenafil in healthy men – a phase 1, randomized open label, single dose, two period, two treatment, cross-over study. European Journal of Pharmaceutical Sciences 213 (2025) 107226.

The Roxus Difference

Onset Time

Route of Administration

Delivery Route

Dosage

Onset Time

Under 10 minutes

Route of Administration

Intranasal

Delivery Route

Efficient absorption through nasal tissue

Dosage

Lower systemic dose required

Onset Time

30-120 minutes

Route of Administration

Oral

Delivery Route

Digestive system and liver metabolism

Dosage

Higher dose needed for same effect

Indication:

ROXUS® (vardenafil HCL nasal spray) is indicated for the treatment of erectile dysfunction (ED).

Contraindications

Use of vardenafil, including ROXUS, is contraindicated in patients taking organic nitrates or nitric oxide donors.

Warnings and Precautions

The warnings and precautions for vardenafil tablets apply equally to ROXUS nasal spray:

  • Priapism: Erections lasting over 4 hours require immediate medical intervention.
  • Sudden Hearing Loss: Discontinue use and seek immediate medical attention if sudden hearing loss occurs.
  • Effects on the Eye: Discontinue use and seek immediate medical attention if sudden vision loss occurs, potentially indicating NAION.
  • QT Prolongation: Avoid use in patients with QT prolongation or those taking class IA or III antiarrhythmics.
  • Hepatic Impairment: Not recommended for patients with severe hepatic impairment. Reduced dose advised for moderate impairment.
  • Renal Impairment: Not recommended for patients on dialysis; no data available for renal impairment use.
  • Pregnancy and Lactation: Classified as Pregnancy Category B. Not indicated for use in women. No data on excretion in breast milk.
  • Paediatric Use: Not indicated for use in patients under 18 years.
  • Management of Overdose: There is no specific antidote for vardenafil overdose. Management should involve standard supportive care. Renal dialysis is unlikely to be effective due to high plasma protein binding.

Drug Interactions:

  • Nitrates: Concurrent use with organic nitrates is contraindicated due to severe hypotension risk.
  • Alpha-Blockers: Use with caution due to potential for significant hypotension.
  • Antihypertensives: May enhance blood pressure-lowering effects.
  • CYP3A4 Inhibitors: Potent inhibitors (e.g., ketoconazole, indinavir, ritonavir) and moderate inhibitors (e.g., erythromycin, azithromycin) increase vardenafil levels and prolong its half-life. Dosage adjustments or avoidance are recommended.
  • Antiarrhythmics: Patients on class IA or III antiarrhythmics should avoid vardenafil.

Adverse Effects:

Common side effects include headache, flushing, rhinitis, dyspepsia, sinusitis, flu syndrome, dizziness, increased creatine kinase, and nausea. Rare cases of vision loss (NAION), sudden hearing loss, and prolonged erections (priapism) have been reported.

Dosage:

ROXUS is administered via a nasal spray device, delivering 2.5 mg of vardenafil hydrochloride per spray. The recommended dosage is 2 sprays (one per nostril). ROXUS is a prescription medicine.

IFU date: 22 May 2024. Edition 1.1 Roxus® is a registered trade mark of LTR Pharma Ltd.