ADME PK metabolism study after oral and iv dosing of 14C/13C-RO4998452

• Research type

  Research Study

• Full title

  Single-center, open-label study investigating the excretion balance, pharmacokinetics and metabolism of a single oral dose of [14C]-labeled RO4998452 and an intravenous microdose of [13C]-labeled RO4998452 in healthy male volunteers

• IRAS ID

  31941

• Sponsor organisation

  F.Hoffmann-La Roche Ltd.

• Eudract number

  2009-013043-11

• Research summary

  Study drug RO4998452 is under development for the treatment of Type 2 diabetes mellitus.RO4998452 inhibits sodium glucose co-transporter 2 (SGLT2) in the blood. By inhibiting SGLT2 less glucose it re-absorbed back into the blood and more glucose is excreted in the urine thereby reducing blood glucose levels.Further development of RO4998452 is required for which greater knowledge of the metabolism (breakdown) and excretion (elimination) in man is required. This study will provide information on the levels of RO4998452 in the blood and how the body breaks down and eliminates RO4998452. Six healthy men will participate and receive one oral dose of 20 mg [14C]-RO4998452 (carbon 14[14C]) is a radiolabelled marker, and one 15 minute intravenous infusion of 0.1 mg 13C RO4998452. After taking [14C]-RO4998452 all urine and faeces will be collected, from which the radiolabelled marker Carbon 14 will be measured showing how much RO4998452 is eliminated in urine and in faeces. The 13C iv microdose allows comparison of the availability of RO4998452 to the body when given orally and intravenously.As well as collecting urine and faeces, blood samples will be collected to measure the amount of RO4998452 in the blood and plasma. Plasma will be also be analysed for breakdown products of RO4998452, known as metabolites.

• REC name

  Scotland A REC

• REC reference

  09/IEC02/22

• Date of REC Opinion

  2 Oct 2009

• REC opinion

  Favourable Opinion