Full Press Release Details
Announces Positive LPCN 1144 NASH Open Label
| 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 |
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.
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.
1144 was well tolerated over 72-week exposure with no observed safety signals
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
injury markers were reduced significantly (p<0.05) and maintained with extended LPCN 1144 treatment
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.
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).
improvements in liver histology support further development
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.
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.
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."
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.
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).
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.
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.
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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