Κυριακή, 14 Φεβρουαρίου 2016

TAKE ERLOTINIB WITH COCA-COLA?

NEW YORK (Reuters Health) - Taking the tyrosine kinase inhibitor (TKI) erlotinib with an acidic cola beverage increases its absorption in patients with non-small-cell lung cancer (NSCLC), researchers from the Netherlands report.
"Stomach protectors, like proton pump inhibitors (PPIs) are often prescribed in combination with TKIs," Dr. Roelof W.F. van Leeuwen, from Erasmus University Medical Center, Rotterdam, told Reuters Health by email. "Since concomitant use of PPIs is associated with decreased TKI efficacy, prescribers are posed (with) a great dilemma whether or not to continue the combined treatment and patients may be deprived of optimal therapy. A glass of coke may be a practical and easy-to-implement way to optimize erlotinib blood levels."
When intragastric pH levels are elevated, erlotinib shifts from its ionized to its non-ionized, less soluble form, and drug absorption decreases.
Dr. van Leeuwen's team investigated whether taking erlotinib with 250 mL of Coca-Cola Classic (pH 2.5) would favorably alter the absorption of erlotinib in patients with NSCLC (with and without PPI treatment with esomeprazole).
The overall absorption of erlotinib, as measured by area under the curve 0-12h in patients taking esomeprazole was 39% higher when taken with cola than when taken with water. The maximum concentration (Cmax) was 42% higher with cola, according to the study released February 8 and scheduled for online publication in the Journal of Clinical Oncology.
Overall absorption of erlotinib was also increased in patients not taking esomeprazole (by 9% versus water), but the Cmax was not significantly changed.
Erlotinib was well tolerated when taken with cola or water, even in patients with known gastroesophageal reflux disease.
"Potentially, the effects of cola on erlotinib exposure may be extrapolated to other TKIs with a pH-dependent solubility (e.g., dasatinib, gefitinib, nilotinib), but this remains to be evaluated in future studies," the researchers wrote. "Furthermore, other acidic beverages (i.e., orange juice, other carbonated drinks) may have similar effects as cola and should be explored in future trials."
"In this study we were really looking for a simple and practical solution for this everyday problem," Dr. van Leeuwen said. "The most surprising finding was that the answer to all our problems appeared to be lying in something as simple as taking the pill with a glass of coke. When taken with a glass of coke (instead of water), the stomach is temporarily acidified and, as a result, erlotinib blood levels in patients who were also taking stomach protectors increased by an average of almost 40%. In some patients this increase was even by more than 100%."
"Although it was shown that a glass of coke significantly increased erlotinib blood levels (compared to intake with water), the guidelines committee will need to assess whether it will be better from now on to take erlotinib with coke rather than with water," he concluded. "For now, the researchers advise patients to consult their treating physician before taking their medication with coke instead of water."
Stichting de Merel and Roche funded this research. Four coauthors reported disclosures.
SOURCE: http://bit.ly/1g1ZgXh
J Clin Oncol 2016.

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