Interactions of janus kinase inhibitors with drug transporters and consequences for pharmacokinetics and toxicity

Introduction: Janus kinase inhibitors (JAKinibs) constitute an emerging and promising pharmacological class of anti-inflammatory or anti-cancer drugs, used notably for the treatment rheumatoid arthritis some myeloproliferative neoplasms.Areas covered: This review provides overview interactions between marketed JAKinibs major uptake efflux drug transporters. Consequences regarding pharmacokinetics, drug-drug toxicity are summarized.Expert opinion: interact in vitro with transporters various ways, as substrates regulators transporter expression. may theoretically result (DDIs), acting perpetrators victims, toxicity, via impairment thiamine transport. Clinical significance terms DDIs JAKinib-transporter remains however poorly documented. In this context, vivo unbound concentration is likely a key parameter to consider evaluating clinical relevance JAKinibs-mediated inhibition. Additionally, interplay metabolism well possible importance time-dependent inhibition have be taken into account. The role play controlling cellular JAKinib concentrations efficacy target cells also issue interest.