2017
DOI: 10.3892/ol.2017.6560
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Bortezomib, carfilzomib and ixazomib do not mediate relevant transporter-based drug-drug interactions

Abstract: Abstract. In order to optimize the clinical application of an increasing number of proteasome inhibitors, investigations into the differences between their respective pharmacodynamic and pharmacokinetic profiles, including their ability to act as a perpetrator in drug-drug interactions, are warranted. Therefore, in the present in vitro study, it was investigated whether bortezomib, carfilzomib and ixazomib are able to alter the expression, and/or the activity, of specific drug transporters generally relevant f… Show more

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Cited by 8 publications
(9 citation statements)
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“…Alteration of cellular proteostasis by inhibition of the 26S proteasome has proven to be effective for targeting cancer cells. Unlike conventional chemotherapeutic drugs, proteasome inhibitors specifically target the 20S core particle of the 26S proteasome without affecting drug transporters [ 1 , 2 ]. These inhibitors can cause apoptosis, mainly through protein accumulation-mediated cellular stress or proteotoxicity [ 1 , 3 , 4 ].…”
Section: Introductionmentioning
confidence: 99%
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“…Alteration of cellular proteostasis by inhibition of the 26S proteasome has proven to be effective for targeting cancer cells. Unlike conventional chemotherapeutic drugs, proteasome inhibitors specifically target the 20S core particle of the 26S proteasome without affecting drug transporters [ 1 , 2 ]. These inhibitors can cause apoptosis, mainly through protein accumulation-mediated cellular stress or proteotoxicity [ 1 , 3 , 4 ].…”
Section: Introductionmentioning
confidence: 99%
“…Several proteasome inhibitors have been approved by the FDA or are undergoing clinical and pre-clinical studies for cancer therapy [ 5 10 ]. The primary applications of proteasome inhibitors in cancer therapy are for the treatment of multiple myeloma or mantle cell lymphoma [ 2 , 3 , 11 , 12 ]. To date, no proteasome inhibitor has been approved for the treatment of solid tumors.…”
Section: Introductionmentioning
confidence: 99%
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