Title : Effect of the CYP2D6*10 allele on the pharmacokinetics of clomiphene and its active metabolites.

Pub. Date : 2018 Mar

PMID : 29516347






7 Functional Relationships(s)
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1 Effect of the CYP2D6*10 allele on the pharmacokinetics of clomiphene and its active metabolites. Clomiphene cytochrome P450 family 2 subfamily D member 6 Homo sapiens
2 Clomiphene citrate, a selective estrogen receptor modulator, is metabolized into its 4-hydroxylated active metabolites, primarily by CYP2D6. Clomiphene cytochrome P450 family 2 subfamily D member 6 Homo sapiens
3 In this study, we investigated the effects of the most common CYP2D6 variant allele in Asians, CYP2D6*10, on the pharmacokinetics of clomiphene and its two active metabolites (4-OH-CLO and 4-OH-DE-CLO) in healthy Korean subjects. Clomiphene cytochrome P450 family 2 subfamily D member 6 Homo sapiens
4 In this study, we investigated the effects of the most common CYP2D6 variant allele in Asians, CYP2D6*10, on the pharmacokinetics of clomiphene and its two active metabolites (4-OH-CLO and 4-OH-DE-CLO) in healthy Korean subjects. Clomiphene cytochrome P450 family 2 subfamily D member 6 Homo sapiens
5 There was a significant difference only in the Cmax of clomiphene between three CYP2D6 genotype groups (p < 0.05). Clomiphene cytochrome P450 family 2 subfamily D member 6 Homo sapiens
6 The AUCinf of corrected clomiphene active moiety in CYP2D6*10/*10 subjects was 2.95- and 2.05-fold higher than that of CYP2D6*wt/*wt and *wt/*10 genotype groups, respectively (both p < 0.001). Clomiphene cytochrome P450 family 2 subfamily D member 6 Homo sapiens
7 Along with the partial impacts on the biotransformation of clomiphene and its metabolites by CYP2D6 genetic polymorphism, further studies on the effects of other CYP enzymes in a multiple-dosing condition can provide more definite evidence for the inter-individual variabilities in clomiphene pharmacokinetics and/or drug response. Clomiphene cytochrome P450 family 2 subfamily D member 6 Homo sapiens