Tier 2 — strong

Sex-Dependent Effects of CYP2D6 on the Pharmacokinetics of Berberine in Humans

Blöcher JA, Meyer-Tönnies MJ, Morof F, Rönnpagel V, Bethmann J, Vollmer M, Engeli S, Tzvetkov MV
Clinical pharmacology and therapeutics 2025 117(1):250-260

Bibliography

PubMed
PMID 39488825
PubMed Central
PMC11652804
DOI
10.1002/cpt.3454
Trial registry
View on ClinicalTrials.gov Registered trial — results not yet published in a peer-reviewed journal.
Funding
The authors reported receiving no funding for this work.
Competing interests
The authors declared no competing interests in the publication.

Study snapshot

DesignGenotype-stratified human pharmacokinetic study
ModelHuman participants; see population
Sample44 healthy adults: 10 poor OCT1 transporters, 13 poor CYP2D6 metabolizers and 21 controls
InterventionSingle oral berberine 1000 mg; genotype-stratified comparisons
Duration48-hour sampling
EndpointsPlasma exposure and pharmacokinetics; Drug interaction measurements; Short-term tolerability

What the study showed, in plain terms

Exposure differed by sex, and CYP2D6 effects on metabolite ratios appeared predominantly in women. OCT1 deficiency did not explain human exposure variation as predicted from laboratory work.

Key findings

  • Exposure differed by sex, and CYP2D6 effects on metabolite ratios appeared predominantly in women. OCT1 deficiency did not explain human exposure variation as predicted from laboratory work.

What this study can and cannot tell us

Small genotype groups and exploratory sex comparisons; no clinical efficacy endpoint.

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Editorial review

Reviewed by the Biohack Blueprint research team

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Dr. Khaled Mahmoud, MBBChCritical Care Medicine, Longevity Science & Editorial Direction Dr. Amr Yasser, PhDCardiometabolic, Musculoskeletal, Gut & Bioavailability Dr. Abdulla Mostafa, PhDCellular Senescence, Neurological, Mitochondrial & Brain-Ageing Biology