Canada-based Cynapsus has come up with the first sublingual option for the delivery of apomorphine to patients with Parkinson's disease to control their debilitating "off" episodes. The company this week heralded results from a study comparing the thin film strip with a subcutaneous injection of the same drug, noting a reduction in side effects.
The dopamine agonist apomorphine is an important drug for people with advanced Parkinson's and one of the only treatments that has been shown to get patients "unstuck" from "off" periods, in which it becomes extremely difficult for them to move. But the drug is unstable and has a host of side effects when injected under the skin. Cynapsus' delivery method attempts to curtail this with an acidity-changing process in the mouth.
"One of the limitations of apomorphine is it must be maintained in a highly acidic composition--otherwise it's very unstable," Cynapsus CEO Anthony Giovinazzo told FierceDrugDelivery over the phone from the J. P. Morgan Healthcare Conference in San Francisco. "What our strip system does is allow the drug to remain intact on the strip and change in acidity as it dissolves in the mouth. It allows it to penetrate in two minutes or less and get the drug into the bloodstream."
In the study, the company tested its sublingual thin film strips, called APL-130277, compared with injected apomorphine in healthy volunteers. The data showed that the strip was not as fast-acting as the injected apomorphine, but that it reduced adverse effects such as nausea and vomiting, which are reported in the subcutaneous version.
"Over the last 15 years, some 10 or more companies have tried to reformulate this in all other viable approaches, such as intranasal pumps, patches or suppositories," Giovinazzo said. "They all ran into two basic problems: They could not get enough of the drug into the bloodstream fast enough, and they had this irritation issue. We can provide not just a convenient delivery, but on top of that a delivery method that will produce fewer side effects for patients to deal with."
Last year, Civitas Therapeutics brought in $38 million to complete Phase II and move on to Phase III for its own Parkinson's treatment designed for "off" episodes, administering the drug levodopa, or L-dopa, to the lungs via inhalation. The market is a lucrative field, and one with a patient base looking for more effective and convenient delivery methods.
There's still a lot of work to do for Cynapsus, though. Giovinazzo said the company expects to finish the initial efficacy studies by the end of 2014 and another safety study by the end of 2015. They have spoken with the FDA in anticipation of filing an NDA by the middle of 2016.
Cynapsus does have the coveted blessing of the Michael J. Fox Foundation for Parkinson's Research, which granted the company almost $1 million about a year ago to move forward with the approval process. That comes with a certain amount of credibility, Giovinazzo mentioned.
- here's the release