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LPCN 1111 is a next-generation, novel ester prodrug of testosterone which uses the Lip'ral technology to enhance solubility and improve systemic absorption. A Phase 1 single dose randomized, open label, crossover pharmacokinetic study was completed in eight (8) postmenopausal women which suggested feasibility of once-daily dosing. Based on the results of this study, Lipocine now completed a Phase 2a study of LPCN 1111 in hypogonadal males. The primary objectives of the study was to determine safety, tolerability, single and steady state pharmacokinetics of testosterone following oral administration of LPCN 1111 in hypogonadal males.

This open-label, dose-escalating single and multiple dose study enrolled 12 males. These subjects had serum total testosterone < 300 ng/dL based on two blood draws on two separate days. Subjects received doses of LPCN 1111 as a single dose of 330 mg, 550 mg, 770 mg, followed by once daily administration of 550 mg for 28 days in 10 subjects, and once daily administration of 770 mg for 28 days in eight subjects.

Top line results from this study demonstrated feasibility of once daily dosing with LPCN 1111 in hypogonadal men and a good dose response. Additionally, the clinical study confirmed that steady state is achieved by day 14 with consistent inter-day performance observed on days 14, 21 and 28. No subjects exceeded peak serum testosterone concentration ("Cmax") of 1500 ng/dL at any time during the 28 day dosing period on multi-dose exposure. Overall, LPCN 1111 was well tolerated with no serious adverse events.

Responder analysis for average 24 hour serum testosterone concentration ("Cavg") and Cmax from this study for the 550 mg dose and the 770 mg dose at day 28 are shown below:

Responder analysis (Cavg and Cmax)

Measure

550mg QD

770mg QD

Typical FDA targets for approval of TRT

% subjects with Cavg within normal range

67%

88%

≥ 75%

% of subjects with Cmax ≤1500ng/dL

100%

100%

≥ 85%

% of subjects with Cmax between 1800ng/dL and 2500mg/dl

0%

0%

≤ 5%

% of subjects with Cmax > 2500ng/dL

0%

0%

0%

Based on these positive results, a Phase 2b study is planned to begin in the first quarter of 2015 with the objective of determining the optimal once daily dosing regimen of LPCN 1111.