Pharmacokinetic Study of Oral Testosterone (T) Ester Formulations in Hypogonadal Men

Clarus Therapeutics

Status and phase: Completed; Phase 2

Conditions: Hypogonadism

Treatments: Drug: Oral testosterone undecanoate (TU) combined with testosterone enanthate (TE) (400 mg T equivalents/dose); Drug: Oral testosterone undecanoate (TU) (200 mg T equivalents/dose with and without food); Drug: Oral testosterone undecanoate (TU) (300 mg T equivalents/dose); Drug: Oral testosterone undecanoate (TU) combined with testosterone enanthate (TE) (300 mg T equivalents/dose)

Study type: Interventional

Funder types: Other; Industry

Identifiers

NCT00695110

CLAR-08005

Details and patient eligibility

About

The purpose of this pharmacokinetic study is to determine whether oral testosterone (T) ester formulations can be used effectively to treat men with low testosterone.

Full description

Determination of the steady-state serum T pharmacokinetic profiles for two oral formulations of T-esters [testosterone undecanoate (TU) and TU combined with testosterone enanthate (TE)] administered bis in die (BID) to 29 hypogonadal adult male subjects. TU was evaluated in total daily doses of 400 and 600 mg equivalents of T given twice daily for 7 or 8 days; TU + TE was evaluated in total daily doses of 600 and 800 mg equivalents of T given twice daily for 7 days. All subjects were enrolled into a single group and proceeded through the four Treatment Periods 1-4 in a sequential manner. In Treatment Period 3 the effect of food on the study-state pharmacokinetics profile of the TU formulation was evaluated.

Enrollment: 29 patients

Sex: Male

Ages: 18 to 68 years old

Volunteers: No Healthy Volunteers

Inclusion criteria

• Male, ages 18-68
• Serum total T less than or equal to 275 ng/dL

Exclusion criteria

• Significant intercurrent disease of any type, in particular, liver, kidney or heart disease, uncontrolled diabetes mellitus or psychiatric illness.
• Abnormal prostate digital rectal examination, elevated prostate-specific antigen (PSA), American Urological Association (AUA) symptom score of >15, and/or history of prostate cancer.
• Hematocrit of <35 or >50%
• Body mass index (BMI) >36
• Serum transaminases > 2 times upper limit of normal or serum bilirubin > 2.0 mg/dL

Trial design

Primary purpose: Treatment

Allocation: N/A

Interventional model: Single Group Assignment

Masking: None (Open label)

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29 participants in 1 patient group

All study participants

Experimental group

Description:

Treatment Period 1: Three capsules each containing 100 mg testosterone (T) as testosterone undecanoate (TU), twice daily (BID) for 7 days. Treatment Period 2: Two capsules each containing 200 mg T as TU and testosterone enanthate (TE), BID for 7 days. Treatment Period 3: Two capsules each containing 100 mg T as TU, BID for 8 days. Treatment Period 4: Two capsules each containing 150 mg T as TU and TE, BID for 7 days.

Treatment:

Drug: Oral testosterone undecanoate (TU) (200 mg T equivalents/dose with and without food)

Drug: Oral testosterone undecanoate (TU) (300 mg T equivalents/dose)

Drug: Oral testosterone undecanoate (TU) combined with testosterone enanthate (TE) (300 mg T equivalents/dose)

Drug: Oral testosterone undecanoate (TU) combined with testosterone enanthate (TE) (400 mg T equivalents/dose)