Effects of Ketoconazole on the Pharmacokinetics of Lenvatinib (E7080) in Healthy Participants.

Author: AluriJagadeesh, FanJean, MartinezGresel, RenMin, ShumakerRobert, ThompsonGary A

Paper Details 
Original Abstract of the Article :
BACKGROUND: Lenvatinib is an oral, multitargeted, tyrosine kinase inhibitor under clinical investigation in solid tumors. In vitro evidence indicates that lenvatinib metabolism may be modulated by ketoconazole, an inhibitor of CYP3A4 and p-glycoprotein. METHODS: In this Phase I, single-center, rand...See full text at original site
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引用元:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4467237/

データ提供:米国国立医学図書館(NLM)

Exploring the Pharmacokinetic Interaction Between Lenvatinib and Ketoconazole

The research examines the potential [pharmacokinetic interaction] between [lenvatinib], a [multitargeted tyrosine kinase inhibitor] used to treat [solid tumors], and [ketoconazole], a [CYP3A4 and p-glycoprotein inhibitor]. The study utilizes a [Phase I, single-center, randomized, open-label, two-period, crossover] design to investigate the impact of [ketoconazole] on the [systemic exposure] to [lenvatinib] in [healthy participants]. The authors analyze the [plasma concentrations] of [lenvatinib] over time to assess the extent of [drug interaction] and its potential clinical significance.

Coadministration of Ketoconazole Slightly Increases Lenvatinib Exposure

The study reveals that [coadministration of ketoconazole] leads to a [slight increase] in [lenvatinib exposure], suggesting a potential [drug interaction]. However, the magnitude of the increase is [relatively small] and likely not [clinically meaningful], given that the [90% confidence interval] for [AUC] remained within the [prespecified bioequivalence interval]. This finding suggests that [ketoconazole] may have a [minimal effect] on the [pharmacokinetics] of [lenvatinib].

Navigating Drug Interactions: A Key Consideration in Cancer Treatment

This study emphasizes the importance of considering [potential drug interactions] when prescribing [anti-cancer medications]. Healthcare professionals must carefully evaluate the [pharmacokinetic profiles] of [drugs] and monitor patients closely for [adverse events] that may arise from [drug interactions].

Dr.Camel's Conclusion

This research is like a camel navigating a desert of drug interactions, carefully evaluating the impact of ketoconazole on lenvatinib. The study's findings suggest a minimal interaction, providing valuable insights for clinicians managing patients receiving these medications.

Date :
  1. Date Completed n.d.
  2. Date Revised 2019-11-20
Further Info :

Pubmed ID

26097795

DOI: Digital Object Identifier

PMC4467237

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Article Analysis
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Languages

English

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