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

Phase 2

Completed

• Conditions: Hypogonadism
• Interventions: Drug: Oral testosterone undecanoate (TU) (300 mg T equivalents/dose); 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) combined with testosterone enanthate (TE) (300 mg T equivalents/dose)

• Registration Number: NCT00695110
• Lead Sponsor: Clarus Therapeutics, Inc.

Brief Summary

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.

Detailed 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.

Study Timeline

• Study Start: 2008-06
• Study First Submitted: 2008-06-09
• Study First Submitted QC: 2008-06-10
• Study First Posted: 2008-06-11
• Primary Completion: 2008-12
• Study Completion: 2009-08
• Disposition First Submitted: 2010-08-17
• Disposition First Submitted QC: 2010-08-17
• Disposition First Posted: 2010-08-19
• Results First Submitted: 2021-04-06
• Status Verified: 2021-06
• Results First Submitted QC: 2021-06-23
• Last Update Submitted: 2021-06-23
• Results First Posted: 2021-06-24
• Last Update Posted: 2021-06-25

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 29

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

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: SINGLE_GROUP

Arm && Interventions

Group	Intervention	Description
All study participants	Oral testosterone undecanoate (TU) (300 mg T equivalents/dose)	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.
All study participants	Oral testosterone undecanoate (TU) (200 mg T equivalents/dose with and without food)	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.
All study participants	Oral testosterone undecanoate (TU) combined with testosterone enanthate (TE) (400 mg T equivalents/dose)	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.
All study participants	Oral testosterone undecanoate (TU) combined with testosterone enanthate (TE) (300 mg T equivalents/dose)	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.

Primary Outcome Measures

Name	Time	Method
Serum Testosterone Area Under Curve (AUC) (0-24) (ng•hr/dL)	30 minutes pre-dose and 0, 1, 2, 4, 8, 12 hours and 0,1, 2, 4, 8, and 12 hours post respective AM/PM doses	Sampling to determine serum T AUC post AM and PM doses and for 24 hours in Treatment Periods 1, 2, and 4. Sampling to determine serum T AUC with food (Day 7) and fasting (Day 8) in Treatment Period 3.
Serum Testosterone Average Concentration (Cavg) (ng/dL)	30 minutes pre-dose and 0, 1, 2, 4, 8, 12 hours and 0,1, 2, 4, 8, and 12 hours post respective AM/PM doses	Sampling to determine serum T Cavg post AM and PM doses and for 24 hours in Treatment Periods 1, 2, and 4. Sampling to determine serum T Cavg post AM dose with food (Day 7) and fasting (Day 8) in Treatment Period 3.

Trial Locations

Locations (4)

Alabama Internal Medicine; 🇺🇸 Birmingham, Alabama, United States

Alabama Clinical Therapeutics; 🇺🇸 Birmingham, Alabama, United States

dgd Research, Inc.; 🇺🇸 San Antonio, Texas, United States

Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center; 🇺🇸 Los Angeles, California, United States