- LPCN 1144 was well tolerated over 72-week exposure with no
observed safety signals
- Liver injury markers were reduced and maintained with extended
LPCN 1144 treatment
- Observed liver histology improvements support further
development
SALT
LAKE CITY, May 12, 2022 /PRNewswire/ -- Lipocine Inc.
(NASDAQ: LPCN), a biopharmaceutical company leveraging its
proprietary technology to develop innovative products to treat
neuroendocrine and metabolic disorders, announces positive topline
results from its Open Label Extension study, OLE. LPCN 1144
comprises an orally delivered prodrug of testosterone.
Twenty-five subjects were enrolled (OLE Safety Set, OLE-SS) of
whom 16 subjects from LiFT study continued LPCN 1144 treatment for
additional 36 weeks (total of 72 weeks) and nine subjects initiated
LPCN 1144 treatment for 36 weeks after placebo run-in for 36 weeks
in the LiFT study. The OLE-SS were evaluated for safety and
tolerability of LPCN 1144, as well as overall subject health at
weeks 6, 12, 24, and 36 of OLE treatment. Twenty-three subjects
completed the study, and one subject discontinued due to a non-drug
related treatment emergent adverse event (TEAE). Six subjects (OLE
Biopsy Set, OLE-BS) elected to have an optional liver biopsy at the
end of the OLE at week 72.
LPCN 1144 was well tolerated over 72-week exposure with no
observed safety signals
In the OLE-SS, the frequency and severity of TEAEs were
comparable to those observed in the LiFT study. There were no
reported cases of cardiovascular events, thromboembolic events,
hepatocellular carcinoma, or drug induced liver injury ("DILI").
Weight change from baseline was minimal and comparable to the LiFT
results. A GI adverse event was reported in one subject, and pedal
edema was also reported in one subject, neither of which were
considered related to study drug. Additionally, no clinically
meaningful changes in lipids were observed.
Liver injury markers were reduced significantly (p<0.05)
and maintained with extended LPCN 1144 treatment
Liver injury markers were reduced relative to baseline during
the initial 36 weeks of treatment with LPCN 1144 [OLE-SS, n = 25,
36 weeks in LiFT (n=16) and 36 weeks in OLE for subjects on placebo
in LiFT (n=9)] with the reduction (U/L) of ALT (alanine
aminotransferase), AST (aspartate aminotransferase), ALP (alkaline
phosphatase) and GGT (gamma-glutamyl transferase): 25.4 (from
61.8),12.2 (from 38.4), 10.6 (from 67.3), and 12.2 (from 50.1),
respectively.
Further, subjects exposed to 72-weeks of LPCN 1144 treatment
(n=16; 36 weeks of LPCN 1144 treatment in LiFT + 36 weeks of LPCN
1144 treatment in OLE) maintained the mean liver injury marker
reductions (U/L): ALT of 27.8 (from 65.9), AST of 13.3 (from 37.4),
ALP of 9.4 (from 69.8), and GGT of 14.3 (from 47.7).
Observed improvements in liver histology support further
development
Utilizing NASH CRN (Clinical Research Network) scoring, in the
limited number of biopsies LPCN 1144 treatment showed improved
efficacy upon extended treatment, and treatment post 36-week
placebo run-in demonstrated efficacy consistent with the LiFT study
results.
"The tolerability with no adverse safety signals and efficacy
results of LPCN 1144 over extended treatment duration are
promising. These data provides strong rationale for further
development of this novel approach as a treatment for NASH," said
Dr. Arun Sanyal, Professor in the Virginia Commonwealth
University ("VCU") Department of Internal Medicine and
Education Core Director in the VCU Center for Clinical and
Translational Research.
Dr. Mahesh Patel, Chairman,
President, and CEO of Lipocine Inc. commented, "We are
delighted by the continued tolerability and efficacy results of
LPCN 1144 treatment from the OLE study, which we believe along with
the previous LiFT results support LPCN 1144's potential to be the
'best in class' option for treating NASH with a differentiated
benefit-to-risk profile. We look forward to the End of Phase 2
meeting with FDA to discuss the pivotal study design."
About the LiFT study
The LiFT clinical study (NCT04134091), a prospective,
multi-center, randomized, double-blind, placebo-controlled,
multi-arm, multi-site trial in the United States, enrolled biopsy-confirmed
hypogonadal or eugonadal male NASH subjects with stage
F1-F3 fibrosis and a NAFLD Activity Score ≥ 4 for a 36-week
treatment period. Subjects with advanced fibrosis
(F2-F3) and steatohepatitis (inflammation on liver biopsy) were
also eligible. Subjects were randomized 1:1:1 to one of three
arms. More information on study design and results were
announced on August 25, 2021.
About the OLE study
The OLE study (NCT04685993) was a multicenter study to provide
LPCN 1144 treatment to subjects from the LiFT study who chose to
participate. Subjects who completed the LiFT study from both the
placebo and LPCN 1144 treatment arms were eligible for the OLE. The
primary objective of OLE was to evaluate the safety and
tolerability of extended (up to 72 weeks) treatment with LPCN 1144
in subjects with biopsy-confirmed Nonalcoholic Steatohepatitis
(NASH).
About NASH
NASH is a more advanced state of non-alcoholic fatty liver
disease ("NAFLD") and can progress to a cirrhotic liver and
eventually hepatocellular carcinoma/liver cancer. Twenty-five to
thirty percent of the U.S. population is estimated to suffer from
NAFLD. NASH afflicts three to twelve percent of the U.S.
population, which is a substantially large population that lacks
effective therapy. Currently, there are no FDA approved treatments
for NASH. Approximately 50% of NASH patients are in adult males and
the number of NASH cases is projected to increase 63% from 16.5
million cases in 2015 to 27.0 million cases in 2030. NAFLD/NASH is
becoming more common due to its strong correlation with obesity and
metabolic syndrome, including components of metabolic syndrome such
as diabetes, cardiovascular disease and high blood pressure. In
men, especially with comorbidities associated with NAFLD/NASH,
testosterone deficiency has been associated with an increased
accumulation of visceral adipose tissue and insulin resistance,
which could be factors contributing to NAFLD/NASH.
About Lipocine
Lipocine is biopharmaceutical company leveraging its
commercially validated proprietary technology to develop innovative
products to treat neuroendocrine and metabolic disorders with high
unmet medical need. Our candidates target diseases with potential
for orphan drug designation, comprise endogenous actives for
favorable benefit to risk profile, and represent enablement of
patient friendly oral delivery option. Lipocine's clinical
development pipeline includes: LPCN 1148, LPCN 1144, LPCN 1111,
LPCN 1107 and oral neuroactive steroids including LPCN 1154 and
LPCN 2101. TLANDO, a novel oral prodrug of testosterone containing
testosterone undecanoate, is approved by the FDA for conditions
associated with a deficiency of endogenous testosterone, also known
as hypogonadism, in adult males. LPCN 1148 is an oral prodrug
of bioidentical testosterone targeted for the management of
symptoms associated with liver cirrhosis. LPCN 1144, an oral
prodrug of bioidentical testosterone, recently completed a Phase 2
clinical study demonstrating potential utility in the treatment of
non-cirrhotic NASH. LPCN 1111, a novel oral prodrug of
testosterone, originated and is being developed by Lipocine as a
next-generation oral testosterone product with potential for
once-daily dosing. In a phase 2 clinical evaluation when
administered as once or twice daily, LPCN 1111 met primary and
secondary endpoints. LPCN 1107 is potentially the first
oral hydroxyprogesterone caproate product candidate indicated for
the prevention of recurrent preterm birth and has been granted
orphan drug designation by the FDA. Neuroactive steroids are
currently being evaluated including LPCN 1154 for the potential
treatment of postpartum depression and LPCN 2101 for the potential
treatment of epilepsy. For more information, please
visit www.lipocine.com.
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 include statements that are not
historical facts regarding Lipocine's product candidates and
related clinical trials, the achievement of milestones within and
completion of clinical trials, the timing and completion of
regulatory reviews, outcomes of clinical trials of our product
candidates, the potential uses and benefits of our product
candidates, and our product development efforts. Investors are
cautioned that all such forward-looking statements involve risks
and uncertainties, including, without limitation, the risks that
the FDA will not approve any of our products, risks related to our
products, expected product benefits not being realized, clinical
and regulatory expectations and plans not being realized, new
regulatory developments and requirements, risks related to the FDA
approval process including the receipt of regulatory approvals, the
results and timing 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 SEC, including, without limitation, its Form 10-K and
other reports on Forms 8-K and 10-Q, all of which can be obtained
on the SEC website at www.sec.gov. Lipocine assumes no
obligation to update or revise publicly any forward-looking
statements contained in this release, except as required by
law.
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