Prestigious journal Cancers published the work of the scientists from the Research Group of Cancer Pharmacology, Department of Pharmacology and Toxicology. The paper entitled „Ensartinib (X-396) Effectively Modulates Pharmacokinetic Resistance Mediated by ABCB1 and ABCG2 Drug Efflux Transporters and CYP3A4 Biotransformation Enzyme” originated under the supervision by Dr. Jakub Hofman and is based on a tight cooperation between several inland as well as outland research teams. Namely, the colleagues from the Charles University, University of Hradec Králové, Brandenburg University of Technology Cottbus-Senftenberg (Germany) and National Center for Toxicological Research at U.S. FDA (USA) participated in this research. The journal Cancers with impact factor of 6.162 is ranked as 31st best one from the total of 230 journals in Oncology section.
The publication relates to the long-term research on the role of biotransformation enzymes CYP450 in the pharmacokinetic drug resistance. The work brings first direct evidence on the participation of CYP3A4 in this phenomenon and demonstrates that drug interaction on this enzyme can be exploited for the potentiation of the antiproliferative effect of docetaxel. Based on the paper results, CYP3A4 represents another important resistance mechanism next to drug transporters. The modulation of this drug metabolizing enzyme shows a potential for the improvement of clinical outcomes of combination anticancer pharmacotherapy. More information about the research work of the Research Group of Cancer Pharmacology can be found on its website.
Text: doc. PharmDr. Jaroslav Roh, Ph.D., Vice-Dean for Scientific Activity, Doctoral Studies and Technology Transfer
Pictures: Archive of Research Group of Cancer Pharmacology