Tadalafil and vardenafil

Abstract

In 2003, two inhibitors of phosphodiesterase 5 (PDE5) — tadalafil (Cialis; Lilly ICOS) and vardenafil hydrochloride (Levitra; Bayer/ GlaxoSmithKline) — were approved by the US FDA for the treatment of erectile dysfunction. Can they challenge the dominance of the first PDE5 inhibitor, sildenafil citrate (Viagra; Pfizer), which rapidly became a blockbuster following its market entry in the late 1990s?

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Figure 1: PDE5 inhibition.
Figure 2: Market for drugs to treat erectile dysfunction in US $ million.

References

  1. 1

    Lue, T. F. Erectile dysfunction. N. Engl. J. Med. 342, 1802–1813 (2000).

  2. 2

    NIH Consensus Conference. Impotence. NIH Consensus Development Panel on Impotence. JAMA 270, 83–90 (1993).

  3. 3

    Rotella, D. P. Phosphodiesterase 5 inhibitors: current status and potential applications. Nature Rev. Drug Disc. 1, 674–682 (2002).

  4. 4

    Terrett, N. K. et al. Sildenafil (Viagra), a potent and selective inhibitor of type 5 cGMP phosphodiesterase with utility for the treatment of male erectile dysfunction. Bioorg. Med. Chem. Lett. 6, 1819–1824 (1996).

  5. 5

    Daugan, A. et al. The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 1:5,6,11,11a-tetrahydro-1H-imidazo[1′,5′:1,6]pyrido[3,4-b]indole-1,3(2H)-dione analogues. J. Med. Chem. 46, 4525–4532 (2003).

  6. 6

    Daugan, A. et al. The discovery of tadalafil: a novel and highly selective PDE5 inhibitor. 2: 2,3,6,7,12,12a-hexahydropyrazino[1′,2′:1,6]pyrido[3,4-b]indole-1,4-dione analogues. J. Med. Chem. 46, 4533–4542 (2003).

  7. 7

    Haning, H. et al. Imidazo[5,1-f][1,2,4]triazin-4(3H)-ones, a new class of potent PDE 5 inhibitors. Bioorg. Med. Chem. Lett. 12, 865–868 (2002).

  8. 8

    FDA Drug Approvals List [online], (cited 10 Feb 2004), <http://www.fda.gov/cder/foi/label/2003/021368lbl.pdf> (2003).

  9. 9

    FDA Drug Approvals List [online], (cited 10 Feb 2004), <http://www.fda.gov/cder/foi/label/2003/021400lbl.pdf> (2003).

  10. 10

    Rajfer, J. et al. Nitric oxide as a mediator of relaxation of the corpus cavernosum in response to nonadrenergic, noncholinergic neurotransmission. N. Engl. J. Med. 326, 90–94 (1992).

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Correspondence to Katherine Neumeyer.

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Neumeyer, K., Kirkpatrick, P. Tadalafil and vardenafil. Nat Rev Drug Discov 3, 295–296 (2004). https://doi.org/10.1038/nrd1362

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