ACY-7 Oral Administration of Acyline

Oral Administration of the GnRH Antagonist Acyline in Normal Men Part II: Multiple-dose Pharmacokinetics (Acyline-7/MER 104-02)

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.

The purpose of this study is to test how the body responds to a new oral form of acyline given for seven days and to also look at the safety of oral acyline.

Acyline temporarily blocks the production of the hormone testosterone in healthy men. It has been tested in over 100 men in an injection form. This study will be testing acyline in a pill form for seven days.

This study may help develop an oral form of testosterone-blocker which may be useful in the treatment of diseases such as prostate cancer, premature puberty and possibly in a male contraceptive.

This study will evaluate a single dose of oral acyline given once a day for seven days and subsequent effects on Testosterone, FSH and LH blood serum concentrations.

Inclusion Criteria:

• Healthy male
• 18-50 years of age
• Non-smoker
• Not taking any medications other than the study drug for the duration of the study.
• Must be willing to use an accepted method of contraception during the study.

Exclusion Criteria:

• BMI > 35
• Abnormal evaluation on screening exam and labs
• Known history of alcohol abuse, illicit drugs or steroids and/or use of more that 3 alcoholic beverages/day
• History of current testosterone use or infertility
• History of testicular disease or severe testicular trauma
• History of major psychiatric disorder or sleep apnea
• History of bleeding disorder or need for anticoagulation
• Current smoker or utilizing nicotine patches or gum
• Participation in a hormonal drug study within past month.