PK Study of Testosterone Nasal Gel (TBS-2) in Healthy Premenopausal Women

Phase 1

Completed

• Conditions: Female Sexual Dysfunction
• Interventions: Drug: Medium dose testosterone nasal gel, single dose; Drug: High dose testosterone nasal gel, single dose; Drug: Low dose testosterone nasal gel, single dose; Drug: Medium dose testosterone nasal gel, multiple dose

• Registration Number: NCT01364623
• Lead Sponsor: Acerus Pharmaceuticals Corporation

Brief Summary

The purpose of this study was to assess the bioavailability of total testosterone through pharmacokinetic profiles obtained following (a) single administration of three doses of TBS-2 b) multiple administration TBS-2.

In addition, assessing the bioavailability of free testosterone, dihydrotestosterone, SHBG and estradiol through pharmacokinetic profiles was also conducted.

Detailed Description

This is a 2 Period study that requires overnight stays in clinic. Blood samples are required at all visits including sampling at predefined time periods during the overnight stays.

Period I

Subjects were checked-in on Day 1 Period I to start their baseline testosterone measurement (dependant on menstrual cycle, preferably within 48hr of start of the menstrual cycle). They remained institutionalized until Day 4 morning, and were checked out after the 48 hour blood draw and study close-out for those that did not continue with Period II.

Period II (Multi-Dose)

At the end of Period 1, a total of 8 subjects sampled from these 3 cohorts, who were willing and able to continue with the multiple-dose portion of the study were selected to participate in Period 2. Subjects were institutionalized starting on Day 1 of Visit 3 until Day 5 morning of Visit 3, and were checked out after the 48 hour blood draw and study close-out.

Study Timeline

• Study First Submitted: 2011-05-27
• Study First Submitted QC: 2011-06-01
• Study First Posted: 2011-06-02
• Study Start: 2011-09
• Primary Completion: 2012-01
• Study Completion: 2012-02
• Results First Submitted: 2018-03-09
• Results First Submitted QC: 2019-08-07
• Results First Posted: 2019-09-13
• Status Verified: 2019-10
• Last Update Submitted: 2019-10-04
• Last Update Posted: 2019-10-16

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Female
• Target Recruitment: 24

Inclusion Criteria

Not provided

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Exclusion Criteria

Not provided

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Study & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
Medium dose TBS-2 single dose	Medium dose testosterone nasal gel, single dose	TBS-2 dispensers prefilled with 0.48% testosterone gel to deliver a single dose of 600 μg of testosterone per nostril, for a total dose of 1200 μg given at 0800 hours (±30 minutes) on Day 2 of Period 1 for Cohort 2 (Medium dose testosterone nasal gel, single dose)
High dose TBS-2 single dose	High dose testosterone nasal gel, single dose	TBS-2 dispensers prefilled with 0.72% testosterone gel to deliver a single dose of 900 μg of testosterone per nostril, for a total dose of 1800 μg given at 0800 hours (±30 minutes) on Day 2 of Period 1 for Cohort 3 (High dose testosterone nasal gel, single dose)
Low dose TBS-2 single dose	Low dose testosterone nasal gel, single dose	TBS-2 dispensers prefilled with 0.24% testosterone gel to deliver a single dose of 300 μg of testosterone per nostril, for a total dose of 600 μg given at 0800 hours (±30 minutes) on Day 2 of Period 1 for Cohort 1 (Low dose testosterone nasal gel, single dose)
Medium dose TBS-2 multiple doses	Medium dose testosterone nasal gel, multiple dose	TBS-2 dispensers prefilled with 0.48% testosterone gel to deliver a single dose of 600 μg of testosterone per nostril, for a total dose of 1200 μg given t.i.d. daily at 0800 hours (± 30 minutes), 1600 hours (± 30 minutes), and 2400 hours (± 30 minutes) on Days 1 and 2 of Period 2, and once in the morning at 0800 hours (± 30 minutes) on Day 3 of Period 2 (Multi-dose group) (Medium dose testosterone nasal gel, multiple dose)

Primary Outcome Measures

Name	Time	Method
Bioavailability (Cmax) of Total Testosterone Through Pharmacokinetic Profiles	Based on blood samples collected -0.25, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, 16, 20, 23.5h relative to dosing	Cmax - maximum concentration of total testosterone observed after dosing of TBS-2
Bioavailability (AUC0-t) of Total Testosterone Through Pharmacokinetic (PK) Profiles	Based on blood samples collected -0.25, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, 16, 20, 23.5h relative to dosing	Area under the concentration time curve from time zero to the last measurable concentration time point (AUC0-t) for single dose and AUCtau shown for multiple dose.
Medium Dose TBS-2 Multiple Dose Average Steady-state Concentration (Cavg) of Total Testosterone	-0.25, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, 16, 20, 24, 32, 40, 48h after Day 3 dosing

Secondary Outcome Measures

Name	Time	Method
Area Under the Plasma Concentration Versus Time Curve (AUC) for Dihydrotestosterone Following TBS-2	Based on blood samples collected -0.25, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, 16, 20, 23.5h relative to dosing	AUCt shown for single dose and AUCtau for multiple dose.
Area Under the Plasma Concentration Versus Time Curve (AUC) for Estradiol Following TBS-2	Based on blood samples collected -0.25, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 12, 16, 20, 23.5h relative to dosing	AUCt shown for single dose and AUCtau for multiple dose.

Trial Locations

Locations (1)

Premier Research International LLC; 🇺🇸 Austin, Texas, United States