- Identified dosing regimen that enables reliance on a single
confirmatory pivotal pharmacokinetic (PK) study to establish
efficacy for postpartum depression (PPD) and support NDA
submission
- LPCN 1154 treatment was well-tolerated with no hypoxia or
sedation-related adverse events
- Lipocine plans to initiate the confirmatory pivotal PK study in
2H 2023
- Conference call and webcast today at 8:30am ET
SALT
LAKE CITY, May 16, 2023 /PRNewswire/ -- Lipocine Inc.
(NASDAQ: LPCN), today announced positive topline results from a
pilot clinical PK bridge study of LPCN 1154 (oral brexanolone) with
a comparator, IV brexanolone. The pilot study is an important step
in Lipocine's ongoing program to develop LPCN 1154 for PPD.
Lipocine is a biopharmaceutical company focused on treating Central
Nervous System (CNS) disorders by leveraging its proprietary
platform to develop differentiated products.
PPD is a major depressive disorder with onset either during
pregnancy or within four weeks of delivery, with symptoms
persisting up to 12 months after childbirth. LPCN 1154 is
targeted to be a differentiated oral option with rapid-onset,
robust efficacy, and short treatment duration as a mono or add-on
therapy for patients with unresolved depression symptoms.
Study Design and Results
The pilot PK bridge study was an open label, randomized, partial
crossover study in healthy postmenopausal women. The primary
objective of the study was to compare the PK (AUC∞ and
Cmax) of two LPCN 1154 oral multi-dose regimens (DR 1:
dosing regimen 1 for 3.5 days, DR 2: dosing regimen 2 for 2.5
days) and a continuous IV infusion dosing regimen of brexanolone
(per label for 2.5 days, up to 90 µg/kg/hr), to inform the dose
selection for the planned confirmatory pivotal PK registration
study. The secondary objective was to evaluate the safety and
tolerability of multidose regimens of LPCN 1154. The study enrolled
a total of twelve participants and was conducted at a single phase
1 unit in the US.
Ratios (%) of geometric mean - LPCN 1154 regimens vs IV
brexanolone regimens:
PK Parameter
|
DR 1 vs
IV 60 µg*
|
DR 1 vs
IV 90 µg
|
DR 2 vs
IV 60 µg*
|
DR 2 vs
IV 90 µg
|
AUC∞
|
98 %
|
77 %
|
106 %
|
83 %
|
Cmax
|
114 %
|
68 %
|
134 %
|
79 %
|
|
60 µg and 90 µg refer
to the maximum dose in the IV regimen (60 µg/kg/hr and 90
µg/kg/hr). *Interpolated from 90 µg/kg/hr IV infusion
data
|
- DR 1 regimen resulted in comparable brexanolone exposure
(Cmax and AUC∞) to IV brexanolone 60 µg/kg/hr
regimen
- DR 2 regimen resulted in exposure levels (Cmax and
AUC∞) within the two clinically-effective IV brexanolone
dosing regimens (60 µg/kg/hr and 90 µg/kg/hr)
- Dosing regimen identified for confirmatory PK study
Consistent with prior experience, LPCN 1154 appeared safe and
well-tolerated in this study. All AEs were mild or moderate in
severity, and similar across trial arms. No hypoxia,
sedation-related, or serious adverse events were observed.
The U.S. Food and Drug Administration (FDA) has agreed with
Lipocine's proposal for establishing the efficacy of LPCN 1154 in
women with PPD through a clinical PK bridge to the approved IV
infusion of brexanolone via anticipated 505(b)(2) NDA
filing and streamlined approval pathway. Lipocine plans to
initiate a single confirmatory pivotal PK study in the second half
of 2023 to establish efficacy, pending FDA feedback.
"The encouraging positive results from this pilot PK bridge
study support our development plan for LPCN 1154," said
Dr. Mahesh Patel, President and CEO of Lipocine. "The
days and weeks after childbirth are critical time periods for the
care of both mother and newborn. PPD is a serious condition in need
of a highly effective, oral, fast-acting and short treatment
duration option. We believe rapid relief matters and, if approved,
LPCN 1154 has the potential to be a differentiated preferred
treatment for PPD."
Conference Call and Webcast
Lipocine management will host a conference call and webcast with
slides beginning at 8:30 a.m. Eastern
Time today to discuss the clinical bridge study results and
answer questions. To participate via telephone, please dial
1-877-451-6152 or 1-201-389-0879 (ex-U.S. toll dial-in number)
using the conference ID 13738729. Participants can also click the
Call me™ link,
https://callme.viavid.com/viavid/?callme=true&passcode=13738729&h=true&info=company&r=true&B=6,
for instant telephone access to the event. The Call me™ link
will be made active 15 minutes prior to scheduled start
time. To participate in the webcast a link is available at
https://viavid.webcasts.com/starthere.jsp?ei=1614938&tp_key=5a35eadcb6 and
also at www.lipocine.com. The webcast will be available for replay
for 180 days.
About LPCN 1154
LPCN 1154 is an oral formulation of brexanolone in development
targeted for rapid relief of postpartum depression (PPD).
Brexanolone is a bioidentical to naturally occurring neuroactive
steroid, allopregnanolone, a positive allosteric modulator of
y-aminobutyric acid (GABA) receptor. LPCN 1154 is expected to
have characteristics that could be particularly appealing to
patients with severe PPD, acutely elevated suicide risk, and in
whom rapid improvement is a priority while presenting no
significant risk of adverse reactions to breastfed infants from
exposure to brexanolone.
About Postpartum Depression and Unmet Needs
PPD is a major depressive disorder with onset either during
pregnancy or within four weeks of delivery, with symptoms
persisting up to 12 months after childbirth. Hormonal changes
leading to GABA dysfunction are common in depression and pregnancy.
Symptoms of PPD include hallmarks of major depression, including,
but not limited to, sadness, depressed mood, loss of interest,
change in appetite, insomnia, sleeping too much, fatigue,
difficulty thinking/concentrating, excessive crying, fear of
harming the baby/oneself, and/or thoughts of death or suicide.
Approximately 500,000 women are affected by PPD annually in
the United States. Traditional
antidepressants, not approved for PPD, have slow onset of action,
side effects such as sexual dysfunction and weight gain, and do not
demonstrate adequate remission post-acute treatment. The
current approved standard of care is continuous infusion of
intravenous brexanolone which requires inpatient administration
with significant limitations.
About Lipocine
Lipocine is a biopharmaceutical company leveraging its
proprietary technology platform to augment therapeutics through
effective oral delivery to develop products for CNS disorders.
Lipocine has candidates in development as well as candidates for
which we are exploring partnering. Our candidates represent
enablement of patient friendly oral delivery options for favorable
benefit to risk profile which target large addressable markets with
significant unmet medical needs.
Lipocine clinical development candidates include: LPCN 1154,
oral brexanolone, for the potential treatment of postpartum
depression, LPCN 2101 for the potential treatment of epilepsy and
LPCN 1148, an oral prodrug of bioidentical testosterone targeted
for the management of symptoms associated with liver cirrhosis.
Lipocine is exploring partnering opportunities for LPCN 1107, our
candidate for prevention of preterm birth, LPCN 1148, for the
management of cirrhosis, LPCN 1144, our candidate for treatment of
non-cirrhotic NASH, and LPCN 1111, a once-a-day therapy candidate
for testosterone replacement therapy (TRT). TLANDO, a novel oral
prodrug of testosterone containing testosterone undecanoate
developed by Lipocine, is approved by the FDA for conditions
associated with a deficiency of endogenous testosterone, also known
as hypogonadism, in adult males. 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 our product development efforts, the
anticipated uses and benefits of LPCN 1154, the timing of a
confirmatory pivotal PK study relating to LPCN 1154, the timing of
any submission of an NDA filing relating to LPCN 1154, our ability
to utilize the streamlined approval pathway under 505(b)(2), our
strategic plans for developing products to treat CNS disorders, our
ability to monetize non-core product candidates, including through
entering into partnering arrangements, the application of our
proprietary platform in developing new treatments for CNS
disorders, our 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, and the potential uses
and benefits of our product candidates. Investors are cautioned
that all such forward-looking statements involve risks and
uncertainties, including, without limitation, the risks that we may
not be successful in developing product candidates to treat CNS
disorders, including LPCN 1154, we may not have sufficient capital
to complete the development processes for our product candidates,
we may not be able to enter into partnerships or other strategic
relationships to monetize our non-core assets, 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 and
our ability to utilize a streamlined approval pathway for LPCN
1154, 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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SOURCE Lipocine Inc.