Relevance of in vitro and clinical data for predicting CYP3A4-mediated herb–drug interactions in cancer patients

Goey, Andrew K.L.; Mooiman, Kim D.; Beijnen, Jos H.; Schellens, Jan H.M.; Meijerman, Irma

doi:10.1016/j.ctrv.2012.12.008

Cited by 85 publications

(66 citation statements)

References 69 publications

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“…This result is consistent with our previous reports on imatinib, which is catalyzed mainly by CYP3A4 [20,21,22]; co-administration with apigenin would result in higher concentrations of imatinib in the short term. The result significantly increased the AUC and reduced the CL after administering imatinib and apigenin in rats at a single dose [11].…”

Section: Discussionsupporting

confidence: 82%

Inhibitory Effect of Apigenin on Pharmacokinetics of Venlafaxine in vivo and in vitro

Zhan

Liang²,

Gu³

et al. 2015

Pharmacology

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Objective: This study was conducted to investigate the effects of orally administered apigenin on the pharmacokinetics of venlafaxine (VEN) in rats and on the metabolism of VEN in human and rat liver microsomes in vitro. Methods: Ten healthy male SD rats were randomly divided into 2 groups: A group (control group), B group (a single dose of 250 mg/kg apigenin). A single dose of 20 mg/kg VEN was administered orally 30 min after administration of apigenin (250 mg/kg). VEN plasma levels were measured by HPLC with fluorescence detection, and pharmacokinetic parameters were calculated by DAS 3.0 software. Results: The single dose of 250 mg/kg apigenin significantly increased the AUC_0-t of VEN by 40.9% (p < 0.05) and obviously increased the peak plasma concentration (C_max) of VEN (p < 0.05). Furthermore, apigenin showed inhibitory effect on human and rat microsomes and the IC₅₀ of apigenin was 58.37 and 25.73 μmol/l, respectively. Conclusions: Our results indicated that an intake of apigenin could increase VEN plasma levels and some of its pharmacokinetic parameters (AUC, T_max). Thus, more attention should be paid when VEN was administrated combined with apigenin.

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Section: Discussionsupporting

confidence: 82%

Inhibitory Effect of Apigenin on Pharmacokinetics of Venlafaxine in vivo and in vitro

Zhan

Liang²,

Gu³

et al. 2015

Pharmacology

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“…The SupersomesV R CYP enzymes used in this study are not confounded by cellular uptake or other intracellular metabolic processes, and is the recommended approach to use for in vitro metabolic evaluation when looking at single enzymes (Bjornsson et al 2003;Parkinson et al 2010;FDA 2012;Goey et al 2013). However, the physiological hepatic environment and the influence on CYP metabolism will not be assessed with this approach (Bjornsson et al 2003).…”

Section: Discussionmentioning

confidence: 99%

“…(Araliaceae)] and milk thistle [Silibum marianum L. (Asteraceae)] (Goey et al 2013). As previously described, the total amount of rosavins is a more suitable quality control measurement for actual R. rosea content than any single constituents (Brown et al 2002;Ma et al 2011;Mudge et al 2013).…”

Section: Discussionmentioning

confidence: 99%

In vitro inhibition of cytochrome P-450 activities and quantification of constituents in a selection of commercial Rhodiola rosea products

Thu

Nilsen

Hellum

2016

Pharmaceutical Biology

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Context: Rhodiola rosea L. (Crassulaceae) products are popular natural remedies with a worldwide distribution. Recent studies have revealed potent CYP inhibition by R. rosea extracts both in vitro and in vivo, but information on in vitro CYP inhibition by commercial products are lacking. Variations in commercial R. rosea product quality have also been published. Objective: This study evaluates the variation of in vitro CYP inhibition potential and product quality of six commercially available R. rosea products. Materials and methods: Human CYPs isolated from baculovirus-infected cell system were incubated with testosterone (CYP3A4), dextromethorphan (CYP2D6) or phenacetin (CYP1A2). Positive CYP inhibitors ketoconazole (CYP3A4), quinidine (CYP2D6) and b-naphtoflavone (CYP1A2) were used as controls. Quantification of rosavin, rosarin, rosin, tyrosol and salidroside were used to evaluate R. rosea content. Results: IC 50 values ranged from 7.2-106.6 lg/mL for CYP3A4, 13.0-186.1 lg/mL for 2D6 and 10.7-116.0 lg/mL for 1A2. The tincture formulation of R. rosea was the strongest inhibitor giving the lowest IC 50 values of 7.2 ± 0.7, 13 ± 1.7 and 10.7 ± 5.6 lg/mL, respectively. CYP3A4 was significantly more inhibited by the different products than CYP1A2 (p < .05). One of the six products did not contain any rosavin, rosarin or rosin and is not a R. rosea product. Constituent concentrations were not linked to enzyme inhibition. Discussion and conclusion: The present results show a large variation in inhibitory potential between the products. Several of the products demonstrate similar inhibition levels as the product Arctic Root already proven to inhibit CYP enzyme activity in man.ARTICLE HISTORY

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“…Gaertner reviewed 200 patients in a palliative care setting and found 631 interactions in 151 charts; these were mainly pharmacodynamic-two drugs acting on the same receptor (Caraco 1996 ;Caruso 1998 ;Gaertner et al 2012 ;Goey et al 2013 ;Peng et al 2005 ;Rahimi and Abdollahi 2012 ;Sinclair 1973 ).…”

Section: Drug Interactions: Palliative Care and Oncologymentioning

confidence: 99%

Drug Interactions in Palliative Cancer Care and Oncology

Stehmer

Bernard²

2015

Palliative Care in Oncology

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Relevance of in vitro and clinical data for predicting CYP3A4-mediated herb–drug interactions in cancer patients

Cited by 85 publications

References 69 publications

Inhibitory Effect of Apigenin on Pharmacokinetics of Venlafaxine in vivo and in vitro

Inhibitory Effect of Apigenin on Pharmacokinetics of Venlafaxine in vivo and in vitro

In vitro inhibition of cytochrome P-450 activities and quantification of constituents in a selection of commercial Rhodiola rosea products

Drug Interactions in Palliative Cancer Care and Oncology

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