Cynapsus Announces Successful Human Volunteer Pilot Proof-of-Concept Results For APL-130277
Marketwire, January 10, 2022
- Sublingual Thin Film Strips of Apomorphine are for the Treatment of Motor Fluctuations in Advanced Parkinson's Disease.
- A confirmatory Phase 1 Bioequivalence Study followed by a Safety Study, are expected to lead to a New Drug Application by late 2013 or early 2014.
TORONTO, CANADA – (Marketwire) – Cynapsus Therapeutics Inc. (CTH: TSX-V), a specialty pharmaceutical company, today announced positive headline data from its recently completed human volunteer pilot proof-of-concept trial for APL 130277, a sublingual thin film strip formulation of apomorphine. The study showed a pharmacokinetic (PK) profile that compared favorably to injected apomorphine with a mean T-max of 25 minutes and good tolerability, and therefore confirms that APL-130277 has the potential to treat motor fluctuations or "off episodes" in Parkinson's disease.
“The successful completion of this first in man study is an important derisking event for APL-130277 and sets the stage for completing the clinical requirements over the next two years to qualify for an accelerated New Drug Application. This significant achievement, combined with the recent announcement of our 500 neurologist survey (December 8, 2021) that confirmed a potentially expanded market for this acute rescue treatment of the debilitating daily freezing episodes, sets a firm foundation of credibility and potential value,” said Anthony Giovinazzo, President and CEO of Cynapsus.
Dr. Albert Agro, Chief Medical Officer at Cynapsus, commented: “We are encouraged by the safety and pharmacokinetic results obtained in this pilot study. The results confirm our hypothesis that a sublingual thin-film strip delivery of apomorphine is safe, well-tolerated and produces a rapid absorption profile that, after dose adjustment, mirrors that of a subcutaneous injection of apomorphine. Most importantly, the T-max of less than 25 minutes confirms that the sublingual delivery system is well equipped to provide therapeutic benefit to patients suffering from Parkinson’s disease who have ‘off episodes’. Planning is now underway for the final configuration of the film strip system, for the full bioequivalence study, and a subsequent safety study in patients, with Parkinson’s disease as vetted by the FDA.”
APL 130277 Trial Design, Results and Development Rationale
The pharmacokinetics and safety/tolerability of sublingual APL-130277 formulation (3 mg dose) were demonstrated in a Phase I pilot study in 15 healthy volunteers with 12 of 15 subjects receiving drug product and 3 of 15 receiving placebo. Following washout, patients were dosed in a second period with APL-130277 placing the drug in a different orientation under the tongue. The study determined that the sublingual orientation does impact the T-max and PK of APL-130277. In the majority of subjects, maximum blood levels were reached within 20 minutes of administration. A detailed analysis of the data is expected to be available within the next 30 days. Other pharmacokinetic parameters mirrored those seen with a subcutaneous injection of apomorphine after an expected dose adjustment.
APL-130277 product showed good tolerability. APL-130277 was safe and well-tolerated. Adverse events were mild in intensity with one subject having moderate nausea and dizziness post dosing. In placebo treated subjects, 33% had at least one adverse event during the treatment period, with 17% of subjects having at least one adverse event in the APL-130277 treatment group. The systemic adverse effects were typical of adverse effects that are commonly observed with apomorphine injection.
Apomorphine, a potent dopamine agonist, is currently the only drug approved specifically for the treatment of acute motor fluctuations/hypomobility (freezing or "off" episodes) in patients with advanced Parkinson's disease. Presently, apomorphine is administered by intermittent sc injection usually via a pre-filled injection pen, or by continuous (waking day or round the clock) infusion pump outside the US. Drawbacks associated with subcutaneous injection therapy for patients and care givers include the need for multiple injections, which can be painful and are often associated with the development of nodules at the injection site, and the requirement for a degree of manual dexterity that some PD patients find difficult.
APL-130277 is a solid dosage form of apomorphine hydrochloride that dissolves rapidly under the tongue (typically, 1-2min), is absorbed directly into the blood stream from the mouth and reproduces the blood levels typically obtained by injection. APL-130277 allows for easy self-administration without the injection site side effects. The results of this Phase 1 pilot study are consistent with the use of APl-130277 as an acute rescue treatment of hypomobility in advanced PD and illustrate the product's potential to replace apomorphine injections.
About Cynapsus Therapeutics
Cynapsus is a specialty pharmaceutical company developing an improved dosing formulation of an approved drug used to treat the symptoms of Parkinson’s disease. Parkinson’s disease is a chronic and progressive neurodegenerative disease that impacts motor activity, and its prevalence is increasing with the aging of the population. It is estimated that between 25 percent and 50 percent of patients experience “off episodes” in which they have impaired movement or speaking capabilities. Current medications only control the disease’s symptoms, and most drugs become less effective over time as the disease progresses.
Cynapsus’ lead drug candidate, APL-130277, is an easy-to-administer, fast-acting and oral reformulation of an approved drug, apomorphine, used to rescue patients from off episodes. Cynapsus is focused on rapidly maximizing the value of APL-130277 by completing pivotal studies in advance of a New Drug Application expected to be submitted in 2013 or 2014. Cynapsus anticipates out-licensing to an appropriate pharmaceutical partner before such an application is submitted.
More information about Cynapsus (CTH: TSX-V) is available at www.cynapsus.ca and at the System for Electronic Document Analysis and Retrieval (SEDAR) at www.sedar.com.
Contact Information
Cynapsus Therapeutics
Anthony Giovinazzo
President and CEO
(416) 703-2449 x225
[email protected]
Andrew Williams
COO & CFO
(416) 703-2449 x253
[email protected]
Media contacts:
Russo Partners LLC
Ian Stone
(619) 528-2220
[email protected]
Robert E. Flamm, Ph.D.
(212)-845-4226
[email protected]
Forward Looking Statements
This press release contains "forward-looking statements" within the meaning of applicable Canadian securities legislation. Generally, these forward-looking statements can be identified by the use of forward-looking terminology such as "plans", "expects" or "does not expect", "is expected", "budget", "scheduled", "estimates", "forecasts", "intends", "anticipates" or "does not anticipate", or "believes" or variations of such words and phrases or state that certain actions, events or results "may", "could", "would", "might" or "will be taken", "occur" or "be achieved". Forward-looking statements are subject to known and unknown risks, uncertainties and other factors that may cause the actual results, level of activity, performance or achievements of Cynapsus to be materially different from those expressed or implied by such forward-looking statements, including but not limited to those risks and uncertainties relating to Cynapsus’ business disclosed under the heading “Risk Factors” in Cynapsus' current Annual Information Form and its other filings with the various Canadian securities regulators which are available online at www.sedar.com. Although Cynapsus has attempted to identify important factors that could cause actual results to differ materially from those contained in forward-looking statements, there may be other factors that cause results not to be as anticipated, estimated or intended. There can be no assurance that such statements will prove to be accurate, as actual results and future events could differ materially from those anticipated in such statements. Accordingly, readers should not place undue reliance on forward-looking statements. Cynapsus does not undertake to update any forward-looking statements, except in accordance with applicable securities laws.
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