Comparative bioavailability assessment between 2 x 10 mg R-178 tablets and 2 x 10 mg 2-amino-1,7-dihydro-6H-purine-6-thione tablets administered orally in healthy participants under fasting conditions.

Phase 1

Withdrawn

• Conditions: 2-amino-1,7-dihydro-6H-purine-6-thione is indicated for the maintenance treatment of inflammatory bowel disease (Crohn's disease or ulcerative colitis).; Oral and Gastrointestinal - Crohn's disease; Oral and Gastrointestinal - Inflammatory bowel disease

• Registration Number: ACTRN12622000579796
• Lead Sponsor: Zenith Technology Corporation Limited

Brief Summary

Not available

Detailed Description

Not available

Study Timeline

• Study Start: 2022-04-20
• Last Update Posted: 22 July 2024

Recruitment & Eligibility

• Status: Withdrawn
• Sex: All
• Target Recruitment: 14

Inclusion Criteria

Healthy participants.
Aged between 18 and 55
Non-smoker
BMI between 18 and 30
Healthy individuals in good health as determined by medical history, physical examination, ECG, blood pressure and laboratory tests
The absence of mental illness requiring medication or treatment by a physician.
Able to provide written informed consent

Exclusion Criteria

Concomitant drug therapy of any kind
Any history of mental illness requiring medication or treatment by a physician.
A deficient, low or intermediate TPMT ensyme activity by means of phenotyping found during medical screening
History of significant drug abuse within one year prior to screening or use of soft drugs (such as marijuana) within 3 months prior to the screening visit or hard drugs (such as cocaine, phencyclidine [PCP], crack, opioid derivatives including heroin, and amphetamine derivatives) within 1 year prior to screening.
History of Gilbert's Syndrome or Gout
Sensitive to the study drug
History of any conditions that might interfere with the absorption, distribution, metabolism or excretion of the drug
Smoker (anyone who has smoked in the last 6 months)
Participants of child- bearing potential who are pregnant and/or breastfeeding
History of alcohol abuse or dependency
Participation in a drug study within 60 days of the start of the study or donated blood within the 60 days preceding the study
Volunteers for whom the Clinical Investigator believer, for any reason, that participation would not be an acceptable risk

Study & Design

• Study Type: Interventional
• Study Design: Not specified

Primary Outcome Measures

Name	Time	Method
To evaluate the pharmacokinetics (as summarised by Cmax and AUC). All plasma samples will be assayed for 2-amino-1,7-dihydro-6H-purine-6-thione using fully validated LC/MS/MS methods. Validation will be conducted to comply with FDA guidelines.[ 0, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.25, 2.5, 2.75, 3, 3.5, 4, 5, 6, 7, 8, 10, 12, 14, 16, 20, 24 and 32 hours post dosing]

Secondary Outcome Measures

Name	Time	Method
Time to maximum peak concentration (Tmax) will be determined by plasma sample analysis. Tmax will be the time where the maximum concentration occurred in the sample points.[ 0, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 1.75, 2, 2.25, 2.5, 2.75, 3, 3.5, 4, 5, 6, 7, 8, 10, 12, 14, 16, 20, 24 and 32 hours post dosing]