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Original Research

Effects of 22 novel CYP2D6 variants found in Chinese population on the metabolism of dapoxetine

, , , , , & show all
Pages 687-696 | Published online: 15 Feb 2016

Figures & data

Figure 1 Structures of the analytes and Phase I metabolic pathway of dapoxetine by CYP2D6 enzyme.

Notes: (A) Dapoxetine hydrochloride. (B) Desmethyldapoxetine. (C) Dapoxetine-N-oxide.
Figure 1 Structures of the analytes and Phase I metabolic pathway of dapoxetine by CYP2D6 enzyme.

Table 1 Kinetic parameters from demethylation by recombinant wild-type and 24 CYP2D6 allelic variants on dapoxetine

Table 2 Kinetic parameters from oxidational activities of recombinant wild-type and 24 CYP2D6 allelic variants toward dapoxetine

Figure 2 Michaelis–Menten curves of the enzymatic activity of the wild-type and 24 variants toward dapoxetine demethylation (each point represents the mean ± standard deviation of three parallel experiments).

Note: The allelic variants with designated allele names have been properly arranged into six groups.
Figure 2 Michaelis–Menten curves of the enzymatic activity of the wild-type and 24 variants toward dapoxetine demethylation (each point represents the mean ± standard deviation of three parallel experiments).

Figure 3 Michaelis–Menten curves of the enzymatic activity of the wild-type and 24 variants toward dapoxetine oxidation (each point represents the mean ± standard deviation of three parallel experiments).

Note: The allelic variants with designated allele names have been properly arranged into six groups.
Figure 3 Michaelis–Menten curves of the enzymatic activity of the wild-type and 24 variants toward dapoxetine oxidation (each point represents the mean ± standard deviation of three parallel experiments).

Figure 4 The catalytic activity of expressed CYP2D6 variants toward the two metabolites of dapoxetine, when compared with the counterpart values of the wild-type 2D6*1.

Note: #P<0.05.
Figure 4 The catalytic activity of expressed CYP2D6 variants toward the two metabolites of dapoxetine, when compared with the counterpart values of the wild-type 2D6*1.