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Curr Pharm Biotechnol. 2017;18(14):1141-1150. doi: 10.2174/1389201019666180308091504.

Effects of a Series of Acidic Drugs on L-Lactic Acid Transport by the Monocarboxylate Transporters MCT1 and MCT4.

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Faculty of Pharmacy, Université de Montréal, Montreal, QC, Canada.
Centre de Recherche du Centre Hospitalier de l'Universite de Montreal (CRCHUM), Montreal, QC, Canada.
College of Pharmacy, University of Florida, Orlando, FL, United States.



Drug-induced myopathy is a serious side effect that often requires removal of a medication from a drug regimen. For most drugs, the underlying mechanism of drug-induced myopathy remains unclear. Monocarboxylate transporters (MCTs) mediate L-lactic acid transport, and inhibition of MCTs may potentially lead to perturbation of L-lactic acid accumulation and muscular disorders. Therefore, we hypothesized that L-lactic acid transport may be involved in the development of drug-induced myopathy. The aim of this study was to assess the inhibitory potential of 24 acidic drugs on L-lactic acid transport using breast cancer cell lines Hs578T and MDA-MB-231, which selectively express MCT1 and MCT4, respectively.


The influx transport of L-lactic acid was minimally inhibited by all drugs tested. The efflux transport was next examined: loratadine (IC50: 10 and 61 µM) and atorvastatin (IC50: 78 and 41 µM) demonstrated the greatest potency for inhibition of L-lactic acid efflux by MCT1 and MCT4, respectively. Acidic drugs including fluvastatin, cerivastatin, simvastatin acid, lovastatin acid, irbesartan and losartan exhibited weak inhibitory potency on L-lactic acid efflux.


Our results suggest that some acidic drugs, such as loratadine and atorvastatin, can inhibit the efflux transport of L-lactic acid.


This inhibition may cause an accumulation of intracellular L-lactic acid leading to acidification and muscular disorders.


Adverse drug reactions; drug-transporters; lactic acid; loratadine; monocarboxylate transporters; statins.

[Indexed for MEDLINE]

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