Lipocine, a specialty pharmaceutical company, announced positive top-line results from a phase 2a clinical study of LPCN 1111, a novel testosterone replacement therapy (TRT) candidate, in hypogonadal males. The primary objective of the study was to determine the feasibility of once daily dosing of LPCN 1111 in hypogonadal males.

"We are pleased that the results in the hypogonadal subject population confirmed our phase 1 findings that LPCN 1111 is a candidate for once daily oral testosterone replacement therapy," said Dr. Mahesh Patel, president and chief executive officer, of Lipocine Inc. "Additionally, these results, along with our positive top-line efficacy phase 3 results for our lead asset, LPCN 1021, a twice-a-day oral TRT, are particularly important in establishing Lipocine's leadership in providing "best in class" patient friendly oral TRT options. We believe that oral TRT will significantly increase patient compliance and overcome many of the inconvenience and transference issues associated with today's marketed TRT products."

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.

Results from this study demonstrated the feasibility of a 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 day 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.

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.

The current testosterone market is dominated by topical products that are associated with poor patient compliance and FDA "black box" warnings related to inadvertent transfer of testosterone.  LPCN 1111 is a novel ester prodrug of testosterone, being developed as a next-generation testosterone replacement therapy product candidate.   LPCN 1111 uses the Company's proprietary solubilisation technology to improve systemic absorption to give effective testosterone levels upon once daily dosing.