Merrion Pharmaceuticals Ltd.

The objective of MER-101-03 is to examine the effects of two different dosing regimens of MER-101 20mg tablets versus Zometa 4mg IV infusion once-monthly therapy. The effects will be monitored on a weekly basis by measuring various markers of bone metabolism. Patients to be enrolled will be those who have not received any previous bisphosphonate therapy. The study will be carried out on prostate cancer patients who are no longer on hormone therapy. Treatment in the study will be for a 2-month period.

We propose oral dosing of gastrointestinal permeation enhancement technology [GIPET] enhanced oral acyline at 20 mg everyday for one week to determine the steady-state (multiple-dose) pharmacokinetics of oral acyline in four normal, healthy young men.

In this study, we propose oral dosing of GIPET enhanced oral acyline (MER-104) to determine if this potentially useful compound is safe and effective at suppression of gonadotropins after oral dosing in man.
Hypothesis: A single dose of Acyline will suppress gonadotropins, and testosterone, estradiol and dihydrotestosterone (DHT) for 24 hours in man, and the magnitude and duration of the suppression will increase with increasing doses of Acyline.