Lipocine Announces Successful Phase 1 Results With LPCN 1107, Potentially the First Oral Product for the Prevention of Preterm

Lipocine Announces Successful Phase 1 Results With LPCN 1107, Potentially the
First Oral Product for the Prevention of Preterm Birth

  *Significant absorption upon oral dosing of LPCN 1107
  *Good dose response demonstrated
  *LPCN 1107 oral steady state 400mg BID exposure is about 55% of weekly
    250mg IM product

SALT LAKE CITY, May 15, 2014 (GLOBE NEWSWIRE) -- Lipocine Inc. (Nasdaq:LPCN),
a specialty pharmaceutical company, today announced the successful completion
of a Phase 1 study of LPCN 1107, the company's oral hydroxyprogesterone
caproate (HPC) product candidate. The study was designed to determine the
pharmacokinetics and bioavailability of LPCN 1107 relative to an intramuscular
(IM) HPC, as well as safety and tolerability, in healthy non-pregnant female

"We are pleased with the results of this study, as it confirms our
pre-clinical data by achieving meaningful drug levels after oral
administration of this highly insoluble drug," said Dr. Mahesh Patel,
President, CEO and Chairman of Lipocine Inc. "To our knowledge no significant
oral bioavailablity has ever been reported for this established drug.
Hydroxyprogesterone caproate is the only drug approved for prevention of
recurrent preterm birth, a leading cause of peri-natal mortality and morbidity
worldwide, but it is currently only available in an inconvenient injectable
form. We believe that an oral alternative will be a major contribution to
patient care and we are encouraged that LPCN 1107 has the potential to become
the first oral product for prevention of preterm birth."

In this Phase 1, pilot, open-label study, ten healthy non-pregnant female
subjects of child bearing age received in a randomized cross-over fashion
either one single dose of 400 mg of LPCN 1107 or two doses of 400 mg LPCN 1107
administered 12 hours apart, followed by a single dose of 250 mg IM HPC, with
a one week washout period between each treatment. Blood samples were collected
over 24 hours following the 400 mg QD dose, over 36 hours following the 400 mg
BID dose and over 30 days following the IM dose. Plasma samples were assayed
for HPC concentration by a validated LC-MS/MS method. The maximum
concentration (Cmax) and area under the curve (AUC) for the oral treatments
are shown in Table 1.

Table 1: Pharmacokinetic Parameters (geometric mean and associated ranges)

Dosing Regimen        C[max ](ng/ml) AUC [0-t ](ng.h/ml)
                      [range]        [range]
400mg , BID           23.1           173
(daily dose of 800mg) [8.5 – 72.1]   [82 – 443]
400mg, QD             13.5           69
                      [4.9 – 54.4]   [33-207]

Significant absorption of HPC following oral administration was noted. Both
mean Cmax and mean AUC increased significantly from the 400 mg QD to the 400
mg BID dose.

The steady state (week 5) pharmacokinetic parameters for the 400 mg BID and
the approved label dose of 250 mg IM weekly injection for the prevention of
recurrent preterm birth were simulated based on the single dose study data and
the simulated Cmax and AUC are shown in Table 2.

Table 2: LPCN 1107 Steady State Pharmacokinetic Parameters

Products / Dosing Regimen      C [ss,max ](ng/ml) AUC [SS- 1 ](ng.h/ml)
                               [range]            [range]
LPCN 1107 400mg BID            23.9               1348
                               [9.6 – 70.0]       [673 - 3381]
Intramuscular injection, 250mg 17.8               2468
                               [14.0 – 27.0]      [1840 - 3180]

Based on this steady state simulation, LPCN 1107 could match the HPC exposure
from the weekly IM injection at an appropriate oral dose.Based on these
results, a study is planned to assess the pharmacokinetics and bioavailability
of LPCN 1107 relative to IM in pregnant females to begin in the second half of

LPCN 1107 was well tolerated and the only significant treatment related
adverse events observed was abnormal menstrual effects in both the LPCN 1107
and IM arms in some subjects which is not an unexpected progestogenic effect
in non-pregnant females of child-bearing age.

About LPCN 1107

LPCN 1107 has the potential to become the first oral HPC product for the
prevention of preterm birth in women with a prior history of at least one
preterm birth. Potential benefits of our oral product candidate relative to
current injectable products include the elimination of pain and site reactions
associated with weekly injections, elimination of weekly doctor visits or
visits from the nurse, and elimination of interference/disruption of personal,
family or professional activities associated with weekly visits. LPCN 1107 has
completed PK studies in dogs showing oral exposure comparable to an
intramuscular injection.

About Lipocine

Lipocine Inc. is a specialty pharmaceutical company developing innovative
pharmaceutical products for use in men's and women's health using its
proprietary drug delivery technologies. Lipocine's lead product candidate,
LPCN 1021, currently in Phase 3 and is targeted to treat symptoms of low
testosterone for men in need of testosterone replacement therapy. Additional
pipeline candidates include LPCN 1111, a next generation oral testosterone
therapy product, and LPCN 1107, which has the potential to become the first
oral hydroxyprogesterone caproate product indicated for the prevention of
recurrent preterm birth.

Forward-Looking Statements

This release contains "forward looking statements" that are made pursuant to
the safe harbor provisions of the Private Securities Litigation Reform Act of
1995 and includes statements that are not historical facts relating to
expectations, clinical trials, the potential uses and benefits of Lipocine's
product candidates, and product development efforts. Investors are cautioned
that all such forward-looking statements involve risks and uncertainties,
including, without limitation, the risks related to the receipt of regulatory
approvals, the results of clinical trials, patient acceptance of Lipocine's
products, the manufacturing and commercialization of Lipocine's products, and
other risks detailed in Lipocine's filings with the U.S. Securities and
Exchange Commission (the "SEC"), including, without limitation, its Form 10-K
and other reports on Form 8-K, all of which can be obtained on the Company's
website at or on the SEC website at Lipocine
assumes no obligation to update or revise publicly any forward-looking
statements contained in this release, except as required by law.

CONTACT: Morgan Brown
         Executive Vice President & Chief Financial Officer
         Phone: (801) 994-7383
         John Woolford
         Phone: (443) 213-0500

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