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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2018, Vol. 23 ›› Issue (9): 983-988.doi: 10.12092/j.issn.1009-2501.2018.09.003

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Absorption mechanism of a novel tubulin inhibitor,YMR-65, in Caco-2 cell model

Clinical Pharmacokinetics Laboratory, China Pharmaceutical University, Nanjing 211198, Jiangsu, China   

  1. Clinical Pharmacokinetics Laboratory, China Pharmaceutical University, Nanjing 211198, Jiangsu, China
  • Received:2018-05-14 Revised:2018-06-11 Online:2018-09-26 Published:2018-09-26

Abstract:

AIM: To study the uptake and transport characteristics of a novel tubulin inhibitor, YMR-65, in Caco-2 cells model and to provide ideas and methods for new drug development. METHODS: By establishing Caco-2 cell model, the effects of time, concentration and temperature on the uptake of YMR-65 were studied using intracellular uptake amount. Time, concentration or verapamil on its transport in Caco-2 cells were evaluated using apparent permeability coefficient (Papp). RESULTS:In Caco-2 uptake model, the cumulative amount of YMR-65 in Caco-2 cells increased in time- and concentration- manners without obvious saturation and it seemed that the uptake characteristics was unaffected by temperature. Time, concentrations or P-gp inhibitor showed no significant difference to the apparent permeability coefficient (Papp) in Caco-2 cells. CONCLUSION: YMR-65 is passively diffused into Caco-2 cells and it suggests that P-gp might not be involved in the intracellular transport of YMR-65 and it might not be the substrate of P-gp.

Key words: novel tubulin inhibitor, YMR-65, Caco-2 cells

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