Title : Minimal contribution of the hepatic uptake transporter OATP1B1 to the inter-individual variability in SN-38 pharmacokinetics in cancer patients without severe renal failure.

Pub. Date : 2021 Sep

PMID : 34117512






6 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 PURPOSE: SN-38, a pharmacologically active metabolite of irinotecan, is taken up into hepatocytes by organic anion transporting polypeptide (OATP) 1B1. Irinotecan solute carrier organic anion transporter family member 1B1 Homo sapiens
2 PURPOSE: SN-38, a pharmacologically active metabolite of irinotecan, is taken up into hepatocytes by organic anion transporting polypeptide (OATP) 1B1. Irinotecan solute carrier organic anion transporter family member 1B1 Homo sapiens
3 The effects of functional OATP1B1 521T>C on the pharmacokinetics of SN-38 remain controversial. Irinotecan solute carrier organic anion transporter family member 1B1 Homo sapiens
4 Here, we prospectively examined the effects of OATP1B1 function on the area under the plasma total or unbound concentration-time curve (tAUC or uAUC) of SN-38 by assessing OATP1B1 521T>C and the plasma levels of endogenous OATP1B1 substrates, coproporphyrin (CP)-I and III, in cancer patients treated with irinotecan. Irinotecan solute carrier organic anion transporter family member 1B1 Homo sapiens
5 Here, we prospectively examined the effects of OATP1B1 function on the area under the plasma total or unbound concentration-time curve (tAUC or uAUC) of SN-38 by assessing OATP1B1 521T>C and the plasma levels of endogenous OATP1B1 substrates, coproporphyrin (CP)-I and III, in cancer patients treated with irinotecan. Irinotecan solute carrier organic anion transporter family member 1B1 Homo sapiens
6 CONCLUSION: The contribution of OATP1B1 activity to inter-patient variability in the systemic exposure to SN-38 is likely minimal in patients without severe renal failure. Irinotecan solute carrier organic anion transporter family member 1B1 Homo sapiens