Vardenafil is a phosphodiesterase 5 inhibitor used to treat 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...
- Mechanism
- Curator reviewed · 1 reference
Vardenafil inhibits cyclic guanosine monophosphate (GMP) specific phosphodiesterase type 5 (PDE5), which is responsible for the degradation of cyclic GMP in the corpus cavernosum located around the penis. Penile erection during sexual stimulation is caused by increased penile blood flow resulting from the relaxation of penile arteries and corpus cavernosal smooth muscle. This response is mediated by the release of nitric oxide (NO) from nerve terminals and endothelial cells, which stimulates the synthesis of cyclic GMP in smooth muscle cells. Cyclic GMP causes smooth muscle relaxation and increased blood flow into the corpus cavernosum. The tissue concentration of cyclic GMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs), and the most abundant PDE in the human corpus cavernosum is PDE5. Therefore, the inhibition of PDE5 by vardenafil enhances erectile function by increasing the amount of cyclic GMP.
- Primary indication
- Vardenafil is indicated for the treatment of erectile dysfunction.Curator reviewed · 1 structured indication
- Formula / weight
- C23H32N6O4S · 488.603 g/mol (avg)
- First approval
- Canada, 2004 · United States, 2003 · European Union, 2016
- Code names
- BAY-389456 · DE 19750085 1997 · WO 99/24433 1999
- Brand names
Resolves to
SECKRCOLJRRGGV-UHFFFAOYSA-NSMILESCCCC1=NC(C)=C2N1NC(=NC2=O)C1=C(OCC)C=CC(=C1)S(=O)(=O)N1CCN(CC)CC1What you can answer from here — as of September 23, 2026
Which drugs share a target with Vardenafil, and which of those have an active Phase 3 trial?
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