Title : Investigation of the functional role of P-glycoprotein in limiting the oral bioavailability of lumefantrine.

Pub. Date : 2014

PMID : 24189249






4 Functional Relationships(s)
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1 An in situ single-pass intestinal perfusion study in rats with the P-gp inhibitor verapamil or quinidine and an ATPase assay with human P-gp membranes indicated that lumefantrine is a substrate of P-gp which limits its intestinal absorption. Verapamil ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus
2 The increase in bioavailability of lumefantrine could be due to inhibition of P-gp and/or cytochrome P450 3A in the intestine/liver by verapamil. Verapamil ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus
3 Thus, the increase in lumefantrine bioavailability with verapamil is attributed in part to the P-gp-inhibitory ability of verapamil. Verapamil ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus
4 Thus, the increase in lumefantrine bioavailability with verapamil is attributed in part to the P-gp-inhibitory ability of verapamil. Verapamil ATP-binding cassette, subfamily B (MDR/TAP), member 1B Rattus norvegicus