ArticleClinical and translational science2018
Effect of Dose and 5α-Reductase Inhibition on the Circulating Testosterone Metabolite Profile of Men Administered Oral Testosterone.
Article in Clinical and translational science, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
7 citing papers in PubMed, 13 citations in OpenAlex.
- Relevance of Human Aldoketoreductases and MicrobialDrug metabolism and disposition: the biological fate of chemicals · 2023Article
- Dimethandrolone, a Potential Male Contraceptive Pill, is Primarily Metabolized by the Highly Polymorphic UDP-Glucuronosyltransferase 2B17 Enzyme in Human Intestine and Liver.Drug metabolism and disposition: the biological fate of chemicals · 2022Article
- Impact of Microbiome on Hepatic Metabolizing Enzymes and Transporters in Mice during Pregnancy.Drug metabolism and disposition: the biological fate of chemicals · 2020Article
- Normalized Testosterone Glucuronide as a Potential Urinary Biomarker for Highly Variable UGT2B17 in Children 7-18 Years.Clinical pharmacology and therapeutics · 2020Article
- The gut microbiota is a major regulator of androgen metabolism in intestinal contents.American journal of physiology. Endocrinology and metabolism · 2019Article
- Major glucuronide metabolites of testosterone are primarily transported by MRP2 and MRP3 in human liver, intestine and kidney.The Journal of steroid biochemistry and molecular biology · 2019Article
- Quantitative characterization of UDP-glucuronosyltransferase 2B17 in human liver and intestine and its role in testosterone first-pass metabolism.Biochemical pharmacology · 2018Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
Development of an oral testosterone therapy has proven extremely challenging because of extensive and variable first-pass metabolism. We investigated the in vivo metabolism of testosterone with increasing oral doses of testosterone, both alone and with the co-administration of dutasteride (5α-reductase inhibitor) by liquid-chromatography tandem mass spectrometry (LC-MS/MS). In eugonadal men prior to dosing, the circulating concentration of testosterone, androstenedione, etiocholanolone-glucuronide, and androsterone-glucuronide was 8.6, 20.9, 9.1, and 55.3%, respectively, of the total testosterone-related species, whereas testosterone-glucuronide was ∼1%. When testosterone was dosed orally to men with experimental hypogonadism, a proportion of testosterone-glucuronide increased to 13%. Dutasteride treatment significantly decreased levels of androsterone and its metabolites. This work reveals extensive metabolism of orally dosed testosterone to androsterone glucuronide via androstenedione, with testosterone-glucuronide appearing to be the second most important metabolite. This information is of importance in the development of an effective oral testosterone therapy and may have implications for testosterone doping research.
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Registered trials
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