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Effect of uptake transporters OAT3 and OATP1B1 and efflux transporter MRP2 on the pharmacokinetics of eluxadoline.

Davenport JM, Covington P, Bonifacio L, McIntyre G, Venitz J - J Clin Pharmacol (2015)

Bottom Line: The effects of OATP1B1, OAT3, and MRP2 on the pharmacokinetics of eluxadoline, an oral, locally active, opioid receptor agonist/antagonist being developed for treatment of IBS-d were assessed in vivo.Cyclosporine had little effect on renal clearance (CLren ) of eluxadoline whereas probenecid reduced CLren by nearly 50%.All treatments were safe and well tolerated.

View Article: PubMed Central - PubMed

Affiliation: Furiex Pharmaceuticals Inc., Morrisville, NC, USA.

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Mean (±SD) plasma concentrations of eluxadoline versus time.
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fig02: Mean (±SD) plasma concentrations of eluxadoline versus time.

Mentions: The average age of subjects was 31 years and ranged from 20 to 48 years. Seventy percent of the subjects (n = 21) were male; the mean (SD) weight was 75.9 kg (12.5); 20 subjects were white, whereas 10 were African American. For illustrative purposes, mean (±SD) eluxadoline plasma concentrations vs. time are presented on a semilogarithmic scale in Figure 2. Mean eluxadoline plasma concentrations were quantifiable through 72 hours after administration for eluxadoline alone and eluxadoline with cyclosporine, but were quantifiable through 48 hours only for eluxadoline with probenecid.


Effect of uptake transporters OAT3 and OATP1B1 and efflux transporter MRP2 on the pharmacokinetics of eluxadoline.

Davenport JM, Covington P, Bonifacio L, McIntyre G, Venitz J - J Clin Pharmacol (2015)

Mean (±SD) plasma concentrations of eluxadoline versus time.
© Copyright Policy - open-access
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4402028&req=5

fig02: Mean (±SD) plasma concentrations of eluxadoline versus time.
Mentions: The average age of subjects was 31 years and ranged from 20 to 48 years. Seventy percent of the subjects (n = 21) were male; the mean (SD) weight was 75.9 kg (12.5); 20 subjects were white, whereas 10 were African American. For illustrative purposes, mean (±SD) eluxadoline plasma concentrations vs. time are presented on a semilogarithmic scale in Figure 2. Mean eluxadoline plasma concentrations were quantifiable through 72 hours after administration for eluxadoline alone and eluxadoline with cyclosporine, but were quantifiable through 48 hours only for eluxadoline with probenecid.

Bottom Line: The effects of OATP1B1, OAT3, and MRP2 on the pharmacokinetics of eluxadoline, an oral, locally active, opioid receptor agonist/antagonist being developed for treatment of IBS-d were assessed in vivo.Cyclosporine had little effect on renal clearance (CLren ) of eluxadoline whereas probenecid reduced CLren by nearly 50%.All treatments were safe and well tolerated.

View Article: PubMed Central - PubMed

Affiliation: Furiex Pharmaceuticals Inc., Morrisville, NC, USA.

Show MeSH
Related in: MedlinePlus