Propella Therapeutics Presents Non-Clinical Data on PRL-02 at 2022 ASCO Genitourinary (GU) Cancers Symposium
February 15 2022 - 7:00AM
Propella Therapeutics, Inc. (“Propella”), a private, clinical-stage
biopharmaceutical company developing best-in-class oncology
therapeutics, today announced that nonclinical data for its lead
product candidate, PRL-02, will be featured at the 2022 ASCO
Genitourinary (GU) Cancers Symposium, which is being held
in San Francisco, CA from February 17-19, 2022. The poster
will be presented by Dr. William Moore, President and Chief
Executive Officer of Propella Therapeutics. Details on the poster
presentation are provided below:
2022 ASCO Genitourinary (GU) Cancer
SymposiumSession Information: Poster Session A:
Prostate Cancer; February 17, 2022 from 11:30 AM-1:00 PM and 5:45
PM-6:45 PM PTAbstract Number:
160Abstract Title: “Abiraterone
decanoate (PRL-02): Pharmacology of a single intramuscular (IM)
depot injection compared to oral abiraterone acetate (AA) in intact
male rats”Presenting Author:
William Moore, Ph.D.
Dr. Moore will present results from nonclinical
studies in male rodent models that evaluated the systemic exposures
and pharmacologic activity (testosterone suppression, CYP17 enzyme
activity) of single-dose, long-acting PRL-02 compared to daily oral
abiraterone acetate (AA), the standard of care for metastatic
prostate, at 7 and 14 days after treatment start.
Key Findings from Poster Presentation:
- A single, intramuscular (IM)
injection of PRL-02 produced large reductions in serum testosterone
concentrations that were equivalent to those from daily abiraterone
acetate at the clinical dose
- A single injection of PRL-02
produced complete inhibition of testicular CYP17 enzyme, 14 days
following dose administration
- PRL-02 produced higher concentrations of the highly active
metabolite, Δ-4 abiraterone, than of abiraterone in the
adrenal and testes
- The persistent high concentrations of both Δ-4 abiraterone and
abiraterone from PRL-02 in the adrenal and testes predict a long
duration of clinical effect
- Total abiraterone exposures were
greater from IM PRL-02 than from oral AA in therapeutic target
tissues (e.g., adrenal, testes, lymph, bone) whereas exposures from
PO AA were greater in plasma and off-target tissues (e.g., liver,
brain)
- The relatively greater on-target to
off-target exposures of abiraterone equivalents from IM PRL-02
compared to PO AA may provide an improved therapeutic index, which
could lead to an improved safety and efficacy profile in patients
with advanced prostate cancer
According to Dr. William Douglas Figg, Sr, Head
of the Clinical Pharmacology Program and Deputy Chief of the
Genitourinary Malignancies Branch of the National Cancer Institute,
the federal government's principal agency for cancer research and
training and a PRL-02 development partner, “These data from the
male rat study, in combination with previous data from the gold
standard, non-human primate model, further justify the ongoing
clinical development of PRL-02 depot for the treatment of prostate
cancer.”
“The non-clinical data we are presenting at this
year’s ASCO GU conference continue to support the potential for
PRL-02 to become the best-in-class androgen biosynthesis inhibitor
for the treatment of advanced prostate cancer and other
hormone-driven cancers,” said Dr. Moore. “The results obtained to
date with PRL-02 reflect the potential advantages our unique
platform, which combines outstanding medicinal chemistry with
lymphatic delivery, can provide; that is, highly active oncology
drug candidates that also have a high safety margin. Thus far, we
are very encouraged with the evolving therapeutic profile of
PRL-02, as these data suggest that intramuscular delivery is
leading to increased bioavailability to the target tissues where
CYP17 enzyme is expressed, a reduced impact on the liver, and an
improved therapeutic index relative to abiraterone acetate. We look
forward to providing an update from our ongoing Phase 1/2 study of
PRL-02 later this year.”
PRL-02 is being evaluated in an ongoing Phase
1/2a study (NCT04729114) for patients with advanced prostate
cancer. The Phase 1 portion is an open-label, multi-center,
dose-escalation study designed to assess the safety, tolerability,
pharmacokinetics, and preliminary clinical activity of PRL-02 and
establish a recommended dose for the Phase 2a portion. The
recommended Phase 2 dose will be selected in Q2 2022 based upon
pharmacokinetic, safety, clinical pharmacology, and efficacy
results.
About ASCO GU Cancer
Symposium
The ASCO Genitourinary (GU) Cancers Symposium is
a three-day scientific and educational meeting designed to provide
attendees with in-depth, multidisciplinary analysis of the most
timely topics in the study, diagnosis, and treatment of GU
malignancies. All members of the cancer care and research community
will benefit from the Symposium's exploration of the latest science
in the field and its clinical application.
About Metastatic Prostate
Cancer
Prostate cancer is the most common non-skin
cancer in men, and the second leading cause of cancer death,
developing most often in older men. Metastatic disease occurs when
prostate cancer cells travel through the lymphatic system or blood
stream to other organs and tissues such as lymph nodes, bone,
liver, and lungs. While early or localized prostate cancer remains
highly curable, advanced prostate cancer remains difficult to
treat, with a 5-year survival rate of only 30%. Although there are
several pharmacological treatment options for metastatic prostate
cancer, the reduction of androgen activity remains the most
effective approach.
About PRL-02
PRL-02 is a next generation androgen
biosynthesis inhibitor being developed for the treatment of
prostate cancer. The only androgen biosynthesis inhibitor approved
for the treatment of prostate cancer blocks the CYP17 enzyme that
is required for the biosynthesis of androgens, including
testosterone. A large body of both historic and modern data support
a role for androgens in prostate cancer pathogenesis and
progression. PRL-02 is a patented prodrug of abiraterone designed
for the lymphatic targeting of tissues and tumors that express the
CYP17 enzyme. PRL-02 is an intramuscular depot that was engineered
to locally release the precise concentration of abiraterone needed
to continuously block CYP17 enzyme while avoiding adverse liver and
drug-drug interaction effects.
About Propella Therapeutics
Inc.
Propella Therapeutics is a biopharmaceutical
company that has developed a platform that combines lymphatic
targeting with a medicinal chemistry optimization process to create
best- or first-in-class oncology drugs starting from active
moieties that have validated MOAs and biological targets but suffer
efficacy limitations due to low bioavailability and / or safety
concerns due to overexposure to non-target tissues. Lymphatic
targeting enables therapies to be delivered directly to therapeutic
target tissues, thereby bypassing plasma compartment safety and
efficacy limitations and first-pass liver effects. This approach
provides increased bioavailability to tissues of interest including
lymph nodes and bone metastatic sites, increased pharmacological
activity, reduced liver effects, and an improved therapeutic index.
Propella is currently in the Phase 1 portion of a Phase 1/2a study
of its lead product candidate, PRL-02, for the treatment of
metastatic prostate cancer. The privately held development-stage
company, based in Pittsboro, N.C., is dedicated to meeting the
needs of cancer patients currently underserved by existing
standards of care.
propellatx.com
Media and Investor
Contact:Brendan Griffin, Chief Financial
Officerbgriffin@propellatx.com 855-225-6378