Title : Isotretinoin and its metabolites alter mRNA of multiple enzyme and transporter genes in vitro but downregulation of OATP1B1 does not translate to the clinic.

Pub. Date : 2022 May 11

PMID : 35545255






3 Functional Relationships(s)
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1 Isotretinoin and its metabolites alter mRNA of multiple enzyme and transporter genes in vitro but downregulation of OATP1B1 does not translate to the clinic. Isotretinoin solute carrier organic anion transporter family member 1B1 Homo sapiens
2 Based on the EC50 and Emax-values and the known circulating concentrations of 13cisRA and its metabolites after isotretinoin dosing, a 55% decrease in OATP1B1 activity was predicted in vivo In vivo DDI potential was evaluated clinically in subjects dosed with isotretinoin for up to 20 weeks using coproporphyrin-I (CP-I) as an OATP1B1 biomarker. Isotretinoin solute carrier organic anion transporter family member 1B1 Homo sapiens
3 Based on the EC50 and Emax-values and the known circulating concentrations of 13cisRA and its metabolites after isotretinoin dosing, a 55% decrease in OATP1B1 activity was predicted in vivo In vivo DDI potential was evaluated clinically in subjects dosed with isotretinoin for up to 20 weeks using coproporphyrin-I (CP-I) as an OATP1B1 biomarker. Isotretinoin solute carrier organic anion transporter family member 1B1 Homo sapiens