2018
DOI: 10.1007/s12272-018-1005-7
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Effect of the CYP2D6*10 allele on the pharmacokinetics of clomiphene and its active metabolites

Abstract: Clomiphene citrate, a selective estrogen receptor modulator, is metabolized into its 4-hydroxylated active metabolites, primarily by CYP2D6. 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. A single 50-mg oral dose of clomiphene citrate was given to 22 Korean subjects divided into three genotype groups according to CYP2D6 genotypes,… Show more

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Cited by 23 publications
(9 citation statements)
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“…Similarly, in a recent study, Kim et al (39) found higher concentrations of active metabolites in women with CYP2D6 mutations causing decreased CYP2D6 activity. Their results disagreed with those of Mürdter et al (37), who reported a correlation between genotype and plasma concentrations.…”
Section: Discussionmentioning
confidence: 64%
See 1 more Smart Citation
“…Similarly, in a recent study, Kim et al (39) found higher concentrations of active metabolites in women with CYP2D6 mutations causing decreased CYP2D6 activity. Their results disagreed with those of Mürdter et al (37), who reported a correlation between genotype and plasma concentrations.…”
Section: Discussionmentioning
confidence: 64%
“…Until now, only four teams have studied the link between the response to CC and the CYP2D6 genotype, and their results have been contradictory (35,(37)(38)(39).…”
Section: Introductionmentioning
confidence: 99%
“…The chromatogram of an AAF sample (Figure 5C) exhibits characteristics highly comparable with the excretion pattern of the urine specimen sampled 4 weeks after the last drug intake. To draw conclusions on when and how much clomiphene was taken by the athlete, more extensive studies that also consider polymorphisms of the enzyme CYP 2D6 are needed, because this enzyme significantly influences HC metabolism 4,9 . The study presented here suggests that ( Z )‐3′‐HC has the potential to be a long‐term marker metabolite for ingestion of larger amounts of clomiphene and over a longer time period, respectively.…”
Section: Resultsmentioning
confidence: 90%
“…Furthermore, gefitinib undergoes extensive hepatic metabolism in humans, predominantly by CYP3A4, which metabolizes the N -propoxymorpholino group. At the same time, the generation of O -desmethyl gefitinib is the major active component produced by CYP2D6, which accounts for 14% of the dose (Li et al, 2006 ; Arafa and Atteia, 2018 ; Kim et al, 2018 ) 1 .…”
Section: Discussionmentioning
confidence: 99%