A Food-Drug Interaction Study of Serum Urate After Oral Inosine

A Phase 1, Open-label, Randomized, Two-period, Two-treatment, Crossover Study to Evaluate the Effects of Food on the Pharmacokinetics of Urate After a Single Dose of Inosine in Healthy Male Subjects

The purpose of this study is to assess the effects of food on the amount of urate in the body after a single oral dose of inosine.

Eighteen (18) eligible healthy male subjects will be randomly assigned to two groups with 9 subjects per group to receive a single oral dose of 1000 mg inosine with or without food on day 1 after an overnight fast. Subjects who receive inosine with food on day 1 will receive a second dose of inosine without food on day 8 after an overnight fast. Subjects who receive inosine without food on day 1 after an overnight fast will receive a second dose of inosine with food on day 8 after an overnight fast.

Subjects will be admitted to the clinic before dinner on days 0 and 7, the days before dosing, and will stay in the clinic for 48-h post-dose. During the clinic stay, blood samples will be taken for urate measurements.

Inclusion Criteria:

1. Healthy male subjects between the ages of 18 and 65 years
2. Body-mass index between 18.0 kg/m2 and 32.0 kg/m2
3. If not surgically sterile, willing to refrain from donating sperm and willing to use appropriate birth control when engaging in sexual intercourse for a period of 90 days following the last dose of the study medication
4. Serum urate < 6.1 mg/dL (approximately 360 μM) at screening
5. Non-smokers for at least 6 months prior to screening
6. Adequate venous access at multiple sites in both arms

Exclusion Criteria:

1. History of alcohol or drug dependence in the past 2 years
2. Had 400 mL of whole blood collection within four months or 200 mL of whole blood collection or who had blood component collection within one month of the screening test
3. Used prescription or over-the-counter (OTC) drugs within 14 days prior to screening
4. Used vitamin preparations or supplements (including St. John's Wort and ginseng) within 28 days prior to the screening test
5. Not willing to refrain from alcohol, grapefruit, grapefruit juice or related products, caffeine consumption (including chocolate), and strenuous exercise within 72 h prior to day 1 and through the end of the PK study
6. Treated with an investigational drug within 30 days or 7 half-lives of the investigational drug, whichever is longer, prior to the first dose of study drug
7. Previously received inosine supplement within three months from the screening or subjects who have had any inosine and suffered an adverse reaction due to it
8. Known HIV disease
9. Had a febrile illness within 5 days prior to the first dose of study medication
10. Vaccinated within 30 days prior to the first dose of medication
11. Has gout or a history or suspicion of kidney stones
12. Determined by the investigator or sub-investigator to be unsuitable for participating in the study based on medical conditions