Effect of OAT Inhibition on Baricitinib PK in Healthy subjects
Research type
Research Study
Full title
A Study to Investigate the Potential Impact of Organic Anion Transporter 3 Inhibition by Probenecid on the Pharmacokinetics of Baricitinib (LY3009104) in Healthy Subjects
IRAS ID
136851
Contact name
Ashley Brooks
Contact email
Sponsor organisation
Lilly UK
Eudract number
2013-002495-41
ISRCTN Number
N/A
Research summary
Baricitinib (formerly identified as LY3009104) is being developed for the treatment of inflammatory diseases including rheumatoid arthritis, psoriasis, and diabetic nephropathy.
Inflammation is a normal response in the body to harmful stimuli such as physical damage to cells, irritant chemicals or infections. The symptoms involve heat, redness and swelling to help repair damage or remove harmful bacteria. The process works by chemicals being released from cells and signalling the body to initiate an inflammatory response. If the body’s inflammatory response is abnormal or exaggerated this can lead to the development of various inflammatory diseases. Baricitinib works by regulating the chemicals which are responsible for the abnormal inflammatory response and therefore has the potential to reduce the unwanted inflammation.
This study is a drug interaction study, where we’ll be assessing the effect of probenecid on the pharmacokinetic properties (blood drug levels and rate of removal) of baricitinib when administered together. Probenecid is a drug which is licensed in many countries to treat gout, and was used in the past to inhibit the kidney excretion of several medications in order to increase their blood levels and prolong their effects. Probenecid works by inhibiting a certain protein called Organic Anion Transporter 3 (OAT3) which is responsible for the transport and excretion of various drugs from the body. Inhibition of OAT3 will therefore lead to reduced excretion and increased blood levels of drugs which are transported by this specific protein.
This is a single site study involving up to 18 healthy subjects. During this study, subjects will be receiving 2 single separate doses of baricitinib on Day 1 and Day 5 in addition to twice daily dosing with probenecid from Day 3 to Day 7.
Subject participation is expected to last up to 7 weeks from the time of screening until the last post-study visit.REC name
North East - York Research Ethics Committee
REC reference
13/NE/0217
Date of REC Opinion
15 Aug 2013
REC opinion
Favourable Opinion