Pilot Pharmacokinetic Study of Oral Testosterone Ester Formulations in Hypogonadal Men
Condition: Hypogonadism
MeSH terms: Hypogonadism
Intervention: Testosterone undecanoate; Testosterone enanthate
Intervention description: Single-day dose as QD or BID for 3 of 5 crossover periods; Single-day dose for 2 of 5 crossover periods
Intervention MeSH terms: Methyltestosterone; Testosterone; Testosterone undecanoate; Testosterone enanthate; Testosterone 17 beta-cypionate
Phase: Phase 2
Study type: Interventional
Primary purpose: Treatment
Allocation: Non-Randomized
Intervention model: Crossover Assignment
Masking: None (Open Label)
Enrollment: 12.0
Sex: Male
Minimum age: 18 Years
Maximum age: 65 Years
Healthy volunteers: No
Keywords: testosterone; male hypogonadism; low testosterone

Summary:

      Determine the serum pharmacokinetic profile for two oral formulations of T-esters (one TE and
      one TU) administered once -(QD) and twice-daily (BID) to hypogonadal men.
    

Eligibility criteria:

        Inclusion Criteria:

        Male, ages 18 to 65 Serum total testosterone less than or equal to 250 ng/dL Naive to
        androgen replacement therapy Subject must be on stable doses of thyroid or adrenal
        replacement hormones for at least 14 days prior to enrollment

        Exclusion Criteria:

        Significant intercurrent disease of any type, in particular, liver, kidney or heart
        disease, uncontrolled diabetes mellitus or psychiatric illness. Patients with treated
        hyperlipidemia will not be excluded provided they have been stable on their lipid-lowering
        mediation for at least three months. For non-insulin dependent diabetic subjects, HbA1c>9%.

        Abnormal prostate digital rectal examination, elevated PSA (serum PSA >4ng/mL), AUA Sympton
        Score greater than or equal to 15 points, and a history or prostate cancer.

        Serum transaminases >2X upper limit of normal (ULN) or serum bilirubin >2.0 mg/dL.

        History of severe or multiple allergies, severe adverse drug reaction or leucopenia. Known
        hypersensitivity to lidocaine or all surgical dressings.

        History of abnormal bleeding tendencies. Oral, topical, or buccal T therapy within the
        previous week, or intramuscular T injection within the previous 4 week.

        Use of dietary supplements that may increase serum T, such as androstenedione or DHEA,
        within the previous 4 weeks.

        Know malabsorption syndrome and/or current treatment with oral lipase inhibitors, bile
        acid-binding resins, colestipol, fibric acid derivatives, gemfibrozil, and probucol.

        Smokers who are unable to refrain from smoking during confinement periods. History of, or
        current evidence of, abuse of alcohol or any drug substance. Poor compliers or those
        unlikely to attend. Receipt of any drug as part of a research study within 30 days of
        inital dose administration in this study.

        Blood donation (usually 550 mL) within the 12-week period before the initial study dose.

        Hematocrit less than 35%. Known clinical polycythemia or hematocrit greater than 50%.
        Current use of paroxetine and clomipramine, antiandrogens, estrogens, p450 enzyme inducers,
        or barbiturates.

        History of sleep apnea.