Dose-dependent effects of Hedyotis diffusa extract on the pharmacokinetics of tamoxifen, 4-hydroxytamoxifen, and N-desmethyltamoxifen

Cheng, Yung Yi; Tuzo, Elise T.; Dalley, Jeffrey W.; Tsai, Tsong-Ru

doi:10.1016/j.biopha.2021.112466

Cited by 4 publications

(5 citation statements)

References 45 publications

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“…Based on the formula of metabolic conversion, the metabolic conversion of 4-hydroxytamoxifen, N -desmethyltamoxifen, and endoxifen was 19.6 ± 8.1%, 16.1 ± 2.4%, and 4.73 ± 2.27%, respectively. The metabolic conversion of 4-hydroxytamoxifen ranged from approximately 20% and was compatible with previous studies ( 24 ). However, the related studies rarely investigated the metabolic conversion of N -desmethyltamoxifen and endoxifen.…”

Section: Resultssupporting

confidence: 90%

“…Plasma drug levels are probably below the lowest detectable concentration of quantification, given that the bioavailability of tamoxifen was approximately 20% ( 23 ). The tamoxifen dosage orally administered in the present study is consistent with our previous work ( 24 ). Experimental animals were randomized into five groups: group 1 (sham group): tamoxifen 10 mg/kg, p.o.…”

Section: Methodssupporting

confidence: 92%

“…Male breast cancer is almost hormone receptor positive, and the use of endocrine therapy such as tamoxifen is routine for managing male breast cancer ( 30 ). In comparing our previous study ( 24 ) and the current study, the AUC of tamoxifen in female rats was about 1.2-fold higher than that in male rats. Moreover, the metabolic conversion ratio of 4-hydroxytamoxifen to N -desmethyltamoxifen in female rats was roughly onefold and the ratio of 4-hydroxytamoxifen to endoxifen conversion was 4- to 5-fold.…”

Section: Discussionsupporting

confidence: 59%

“…Moreover, the metabolic conversion ratio of 4-hydroxytamoxifen to N -desmethyltamoxifen in female rats was roughly onefold and the ratio of 4-hydroxytamoxifen to endoxifen conversion was 4- to 5-fold. However, our previous study demonstrated that the percentage of 4-hydroxytamoxifen conversion in male rats is only 26% ( 24 ). The endoxifen conversion ratio in female rats is significantly greater than that in male rats, implying that the endoxifen conversion ratio is higher in female rats than in male rats.…”

Section: Discussionmentioning

confidence: 98%

“…The sample injection volume was 5 μl. The MS/MS condition and analyte transition have previously been described ( 24 ). The coefficient correlation ( r 2 ) as the linearity standard was at least 0.995.…”

Section: Methodsmentioning

confidence: 99%

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Impact of Irradiation on the Pharmacokinetics and Biotransformation of Tamoxifen

et al. 2022

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BackgroundThe optimal procedure for combining radiotherapy (RT) with tamoxifen treatment is controversial as RT may alter the pharmacokinetics and biotransformation of tamoxifen. The present study investigated this potential interaction by assessing the pharmacokinetics of tamoxifen during concurrent and sequential RT.MethodPlasma tamoxifen concentration was measured in rats with or without RT 2.0 Gy (RT2.0Gy) or 0.5 Gy (RT0.5Gy) with ultra-high-performance liquid chromatography-tandem mass spectrometry after tamoxifen administration (10 mg/kg, p.o., n = 6). Tamoxifen was either administered 1 h after RT (concurrent condition) or 24 h after RT (sequential condition).ResultsPharmacokinetic data analysis demonstrated that the area under the curve (AUC) and half-life of tamoxifen were 2,004 ± 241 h ng/ml and 6.23 ± 1.21 h, respectively, after tamoxifen administration (10 mg/kg, p.o.). The respective conversion rate of 4-hydroxytamoxifen, N-desmethytamoxifen, and endoxifen for tamoxifen metabolism was 20%, 16%, and 5%. The AUC value of tamoxifen in the RT0.5Gy group was 1.5- to 1.7-fold higher than in the sham and RT2.0Gy groups. The relative bioavailability of tamoxifen at concurrent RT0.5Gy and RT2.0Gy groups ranged from 127% to 202% and from 71% to 152%, respectively. The magnitude of endoxifen, which converted from 4-hydroxytamoxifen and N-desmethyltamoxifen, increased 3- to 5-fold in the concurrent RT groups. By contrast, the AUC of tamoxifen decreased by roughly 24% in the sequential RT2.0Gy group. The conversion ratio of endoxifen was four times higher than that in the sequential RT2.0Gy group compared with rats not exposed to RT.ConclusionThe current study provides advanced pharmacokinetic data to confirm the interaction between RT and hormone therapy. Our findings indicate that RT facilitates the metabolism of tamoxifen to active metabolites and thus imply that combination RT-tamoxifen has potential benefits for the treatment of hormone-dependent breast cancer.

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Section: Resultssupporting

confidence: 90%

Section: Methodssupporting

confidence: 92%

Section: Discussionsupporting

confidence: 59%

Section: Discussionmentioning

confidence: 98%

Section: Methodsmentioning

confidence: 99%

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Impact of Irradiation on the Pharmacokinetics and Biotransformation of Tamoxifen

et al. 2022

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Simultaneous determination of raloxifene and tamoxifen using dispersive micro solid-phase extraction and HPLC method in real water, human hair and serum samples

Rezaei

Masrournia

Pordel

2022

International Journal of Environmental Analytical Chemistry

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Herb-Drug Interactions and Their Impact on Pharmacokinetics: An Update

Cheng

Xia

et al. 2023

CDM

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Herb medicine has a long history of application and is still used worldwide. With the development of complementary and alternative medicine, the interaction between herb and drugs has attracted more and more attention. Herb-drug interactions (HDI) could cause decreased efficiency, increased toxicity, and affect the drug absorption and disposition processes due to the interference of their pharmacological or pharmacokinetic effects. Hence, the mechanisms and results of herb-pharmacokinetic interactions should be comprehensively summarized. Here, we have summarized the mechanisms of HDI and pharmacokinetic interactions in the last ten years based on searching on PubMed, Science Direct, and Web of Science with different keywords. Besides, the pharmacokinetic interactions were related to nine commonly used herbs and drugs, including Ginseng, Salvia miltiorrhiza, Ginkgo biloba, Garlic, Coptis chinensis, St. John's wort, Ginger, Licorice, Silythistle and Fructus Schisandrae. This review provides an overview of HDI to provide a reference for the rational and safe clinical use of herbs and drugs.

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Dose-dependent effects of Hedyotis diffusa extract on the pharmacokinetics of tamoxifen, 4-hydroxytamoxifen, and N-desmethyltamoxifen

Cited by 4 publications

References 45 publications

Impact of Irradiation on the Pharmacokinetics and Biotransformation of Tamoxifen

Impact of Irradiation on the Pharmacokinetics and Biotransformation of Tamoxifen

Simultaneous determination of raloxifene and tamoxifen using dispersive micro solid-phase extraction and HPLC method in real water, human hair and serum samples

Herb-Drug Interactions and Their Impact on Pharmacokinetics: An Update

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