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High Biochemical Selectivity of Tadalafil, Sildenafil and Vardenafil for Human Phosphodiesterase 5A1 (PDE5) Over PDE11A4 Suggests the Absence of PDE11A4 Cross-Reaction in Patients

High Biochemical Selectivity of Tadalafil, Sildenafil and Vardenafil for Human Phosphodiesterase 5A1 (PDE5) Over PDE11A4 Suggests the Absence of PDE11A4 Cross-Reaction in Patients

J L Weeks, R Zoraghi, A Beasley, K R Sekhar, S H Francis, J D Corbin

Int J Impot Res. Jan-Feb 2005;17(1):5-9.

PMID: 15538396

Abstract:

The physiological role of phosphodiesterase (PDE)11 is unknown and its biochemical characteristics are poorly understood. We have expressed human His-tagged PDE11A4 and purified the enzyme to apparent homogeneity. PDE11A4 displays K(m) values of 0.97 microM for cGMP and 2.4 microM for cAMP, and maximal velocities were 4- to 10-fold higher for cAMP than for cGMP. Given the homology between PDE11 and PDE5, we have compared the biochemical potencies of tadalafil (Cialis, Lilly-ICOS), vardenafil (Levitra, Bayer-GSK), and sildenafil (Viagra, Pfizer Inc.) for PDE11A4 and PDE5A1. PDE5A1/PDE11A4 selectivities are 40-, 9300-, and 1000-fold for tadalafil, vardenafil, and sildenafil, respectively. This suggests that none of these three compounds is likely to crossreact with PDE11A4 in patients.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
IAR42415175	Phosphodiesterase 5A1 human			Price

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