Meeting The Unmet Need in Drug DeliveryPartnering
Zaleplon GR for Insomnia

Current epidemiological data suggest that insomnia is one of the most common CNS disorders, affecting one-third of the general population.

In 2005, the Sleep in America poll found that 54% of adults reported one or more symptoms of insomnia at least a few nights a week, with one-third experiencing at least one symptom of insomnia every night or almost every night1

There are three key  attributes expected from an optimal insomnia drug:

1.  Rapid sleep onset
2.  Sleep maintenance
3.  No residual effects (hangover-like symptoms the following day)

An ideal treatment would be a modified-release formulation of a drug that is rapidly absorbed (therefore provides a rapid sleep induction) and has a very short half-life (associated with no residual effects). Continuous release of the drug overnight would provide efficient sleep maintenance.

Intec's product

Intec Pharma is developing a gastro retentive formulation of Zaleplon.

Zaleplon is the fastest and shortest acting drug of its class. It is absorbed rapidly, reaching peak blood levels within an hour after dosing and is rapidly cleared from the blood with a terminal half-life of 1 hour.  Accordingly, it is associated with rapid sleep induction and has minimum next-day residual effects.

The Accordion Pill enables a continuous duodenal infusion of Zaleplon throughout the night,  thereby prolonging the absorption phase and keeping a sufficient blood concentration for sleep maintenance over night.

Phase I

The Accordion Pill Zaleplon has demonstrated statistically significant superiority over the marketed Zaleplon (Sonata) 

Phase II

On September 14, 2010, Intec Pharma was informed that it received the approval of the US Food and Drug Administration (the "FDA") for the commencment of Phase II trials in the USA for the Accordion Zaleplon Pill.

On November 22, 2011, Intec Pharma reported  the results of the Phase II clinical trial of the Accordion-Zaleplon product (the "Trial").

The analysis of the Trial results showed that the primary objective (Primary End-Point) of the Trial was successfully achieved. The use of the Accordion Zaleplon product resulted in substantial improvement with statistical significance in the prolongation of the Total Sleep Time (TST) of patients suffering from chronic Insomnia. Additional important secondary End-points were also achieved successful with statistical significance:

Improvement of time to sleep onset (LPS) 

        (Latency to Persistent Sleep)

Prevention of side effects in the "next morning".

Improvement of the level of patient alertness in the "next morning".

Improvement of sleep quality.

Company's management believes that the clinical effect achieved with regard to the prolongation of the Total Sleep Time, along with the high safety profile shown in the Trial, points to the potential of the Accordion Zaleplon product to become a leading medication in the field of Insomnia treatment.

Eighty three Insomnia chronic patients, who suffer from difficulties in falling asleep and in maintaining a persistent sleep, participated in the Trial. The Trial was conducted in five leading sleep clinics in the U.S. (81 patients) and in the sleep clinic in Ramabam Medical Center in Israel (2 patients) (the "Subjects"). The Trial was conducted as a Double Blind study. The efficacy of the Accordion Zaleplon product versus a placebo was tested in a crossover design with the relevant Insomnia objective and subjective criteria.

These criteria included, inter alia, the use of Polysomnography (comprehensive sleep testing performed at night and includes, among other things, registration of brain waves, eye movements, etc.), memory and cognitive tests in the next morning, filling of questionnaires by patients, etc.

The analysis of the patients' brain waves records showed that the Total Sleep Time was substantially prolonged with statistical significance. It was also found that the latency to persistent sleep (LPS) was substantially shortened with statistical significance.

The analysis of the results of the objective tests for the evaluation of the patients' level of alertness in the next morning showed that no residual effects (Residual Sedation) were found with the patients who were treated with the Accordion Zaleplon product, in comparison to the placebo.

The results of the subjective tests (questionnaires handed out to the patient with regard to several parameters of sleep and with regard to the level of alertness in the morning) also indicated (with statistical significance) on substantial prolongation of the sleep duration and on improvement in its quality, on substantial shortening of the latency to persistent sleep and on improvement in the level of alertness in the next morning.

It is important to point out that currently, the Zaleplon medication is not approved for the indication of Sleep Maintenance. 

It is also important to point out that to the Company's best knowledge, there is an increasing concern among the regulatory authorities in the U.S. as to the residual effects, in the next morning, of currently approved sleep medications. In a recently held discussion, the FDA addressed the risk of sedatives and their link to next-day effects, such as dangerous sleep driving.

Sleep Disorders

Pursuant to public sources (Datamonitor, Forecast Insight, Insomnia, Aug 2008) the market for medications for sleep disorders was estimated at approximately 4.1 billion U.S. dollars in the year 2007 in the seven major markets (USA, Japan, UK, France, Germany, Switzerland and Italy). It is estimated that the market potential will grow to approximately 6.8 billion U.S. dollars in the seven major markets by the year 2017.

The Company's estimates regarding the future development and expected trials with respect to the Company's products are forward looking information based on the information that the Company has in its possession today pertaining to the potential of drugs development, and the indications the Company received from the relevant health care authorities. These estimates may not be realized, in whole or in part, and/or may be realized differently than estimated, as a result of different factors, including the failure to reach the objectives of the trials and/or schedules and/or to obtain the necessary funding for the continuation of development of the drugs as well as failure to obtain regulatory approvals required for further development, failure to reach agreements with international companies, other factors which are not within the Company's control and the materialization of any of the risk factors detailed in Section 5.31 of the Company`s shelf prospectus published on May 5, 2011. 

 

Sincerely,

Intec Pharma Ltd.

 


Intec's believes that the
continuous duodenal infusion,
throughout the night, offers
a superior insomnia solution,
to address a huge unmet need