Steady-State Pharmacokinetics of Metformin Is Independent of the OCT1 Genotype in Healthy Volunteers
Abstract
Purpose The aim of the study was to determine the steady-state pharmacokinetics of metformin in healthy volunteers with different numbers of reduced-function alleles in the organic cation transporter 1 gene (OCT1).Methods The study was conducted as part of a randomized cross-over trial. Thirty-four healthy volunteers with known OCT1 genotypes (12 with two wild-type alleles, 13 with one and 9 with two reduced-function alleles) were included. In one of the study periods, they were titrated to steady-state with 1 g metformin twice daily.Results Neither AUC(0-12), C(max) nor Cl(renal) were statistically significantly affected by the number of reduced-function alleles (0, 1 or 2) in OCT1: (AUC(0-12): 0, 1, 2: 14, 13 and 14 h ng/L (P = 0.61)); (C(max): 0, 1, 2: 2192, 1934 and 2233 ng/mL, (P = 0.26)) and (Cl(renal): 0, 1, 2: 31, 28 and 30 L/h (P = 0.57)) CONCLUSIONS: In a cohort of healthy volunteers, we found no impact of different OCT1 genotypes on metformin steady-state pharmacokinetics.
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With a plasma half-life of approximately 3 to 5 hours and subject to dosing schedule, it is unlikely that other than in gut enterocytes a significant cellular accumulation of metformin occurs when used for T2DM.
“However, with a plasma half-life of approximately 3 to 5 hours, and subject to the schedule of dosing, it is unlikely, that other than in gut enterocytes, a significant cellular accumulation of metformin occurs when the drug is used for the treatment of T2DM (34, 155, 156, 159, 160).”
From A Critical Review of the Evidence That Metformin Is a Putative Anti-Aging Drug That Enhances Healthspan and Extends Lifespan (2021) · cites this paper as [160]
When used to treat diabetes, peak plasma concentrations of metformin are usually less than 20 μM.
“As previously stated when used to treat diabetes peak plasma concentrations of metformin are usually less than 20 μM (155, 160).”
From A Critical Review of the Evidence That Metformin Is a Putative Anti-Aging Drug That Enhances Healthspan and Extends Lifespan (2021) · cites this paper as [160]
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References 45 · Cited by 62
- Authors
- Christensen, M. M. H., Højlund, K., Hother-Nielsen, O., Stage, T. B., Damkier, P., Beck-Nielsen, H., & Brøsen, K.
- Affiliations
- University of Southern Denmark (DK)
- Odense University Hospital (DK)
- Corresponding author
- Christensen, Mette Marie Hougaard
- Venue
- European Journal of Clinical Pharmacology
- Published
- 2015-05-05
- Volume
- 71
- Issue
- 6
- Pages
- 691-697
- ISSN
- 0031-6970 (ISSN-L)
- 1432-1041
- OpenAlex
- W2170852135
- Cited by
- 62
- References
- 45
- Citations by year
- 2026: 3 · 2025: 4 · 2024: 1 · 2023: 7 · 2022: 5 · 2021: 6 · 2020: 8 · 2019: 7 · 2018: 12 · 2017: 3 · 2016: 4 · 2015: 1
- FWCI
- 7.76
- Type
- journal article
- Language
- en
- Open access
- closed
- Licence
- www.springer.com/tdm (tdm)
- Locations
- European Journal of Clinical Pharmacology (publishedVersion)
- PubMed (publishedVersion)
- University of Southern Denmark Research Portal (University of Southern Denmark) (publishedVersion)
- Funders
- Odense Universitetshospital
- Sundhedsstyrelsen
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Health Sciences › Medicine › Oncology › Drug Transport and Resistance Mechanisms
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Metabolism, Diabetes, and Cancer
- Keywords
- metformin, OCT1, SLC27A1, genetic polymorphism, steady-state pharmacokinetics, renal clearance, drug metabolism, healthy volunteers
- MeSH terms
- Adult, Alleles, Female, Genotype, Humans, Hypoglycemic Agents, Male, Metformin, Polymorphism, Genetic, Cross-Over Studies, Organic Cation Transporter 1, Young Adult, Healthy Volunteers
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