Mechanism of action<unk>  is a μ- and κ-opioid receptor agonist and δ-opioid receptor antagonist that acts locally in the enteric nervous system, possibly decreasing adverse effects on the central nervous system. Pharmacokinetics In the in vitro studies,<unk>  was found to be transported by OAT3 (SLC22A8), OATP1B1 (SLCO1B1) and BSEP (ABCB11) at the highest concentrations tested (400 ng/ml which is 162-fold larger than the observed Cmax of the highest therapeutic dose of 100 mg). However, it was not to be transported by OCT1 POU2F1, OAT1 Organic anion transporter 1, OCT2, OATP1B3 (SLCO1B3), P-gp (P-glycoprotein), or BCRP (ABCG2). Multidrug resistance-associated protein 2 (MRP2)-vesicular accumulation of<unk>  was observed, indicating that the drug is a substrate of MRP2.<unk>  was not found to inhibit BCRP-, BSEP-, MRP2-, OCT1-, OCT2-, OAT1-, OAT3-, or OATP1B3-mediated transport of probe substrates but inhibited the transport of probe substrates of OATP1B1 and P-gp. Also in the in vitro studies, it was observed that<unk>  is an in vivo substrate of OATP1B1, OAT3, and MRP2. Finally, no inhibition or induction of cytochrome P450 enzymes was observed. Following a 100 mg dose of<unk> , the Cmax was about 2 to 4 ng/ml and AUC was 12-22 ng.h/ml.<unk>  has linear pharmacokinetics with no accumulation upon repeated twice daily dosing. Taking<unk>  with high fat meal decreased the Cmax by 50% and AUC by 60%.
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