Use of pemirolast

a technology of pemirolast and pemirolast, which is applied in the field of new pharmaceutical use, can solve the problems of shortness of breath, chest tightness, and condition that may become life-threatening, and achieve the effect of positive underlying airway hyperresponsiveness

Inactive Publication Date: 2017-04-27
CARDOZ AB
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0016]We have previously found that pemirolast has a previously-undisclosed and unappreciated plasma concentration (exposure) profile which means that it can be employed safely in doses that are significantly higher than those presently employed in the prevention of asthma.
[0017]In a double-blind, randomised clinical trial with a primary objective to investigate the relative efficacy of high dose and low dose pemirolast versus placebo in the prevention of the severity of mannitol-induced asthma attacks in human asthmatic subjects, a highly surprising and unexpected effect was observed.

Problems solved by technology

There is presently no cure for asthma, and treatments often revolve around avoidance of known triggers, such as allergens, dust, pollutants, etc.
Symptoms include shortness of breath, wheezing, and tightness in the chest.
In severe cases, breathing may be significantly impaired such that the condition may become life-threatening.
Acute asthma attacks can often be brought on by infections, allergens, air pollution, exercise or insufficient or inappropriate medication use.
Additionally, there are drawbacks associated with all of the aforementioned drugs (particularly inhaled corticosteroids), including lack of efficacy, non-adherence to treatment regimens, tolerance dependence and safety profiles / side-effects.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

inetics of Pemirolast in Humans

[0065]This study comprised 18 healthy male subjects, 18-45 years of age, and was a single and multiple-dose, open study assessing the safety and tolerability of pemirolast potassium tablets (10 mg, Ulgixal™ tablets) with the doses 10, 30 and 50 mg (containing 8.5, 25.5 and 42.5 mg pemirolast free acid, respectively) b.i.d. (6 subjects in each dose group).

[0066]The subjects received a single dose on the first day, then b.i.d. for three days and a single dose on the fifth day. The study was performed at the Berzelius Clinical Research Center AB in Linköping, Sweden. All laboratory pharmacokinetic analyses were performed by Quintiles AB, Uppsala, Sweden. Pharmacokinetic calculations were performed by Pharm Assist Sweden AB, Uppsala, Sweden.

[0067]Mean Cmax data after multiple dosing are shown in and Table 1, and mean plasma concentrations over time on Day 5 are shown in FIG. 1.

TABLE 1Multiple dose pharmacokinetics of orally administered pemirolastpotassium...

example 2

etics of Pemirolast in the Dog

[0071]In a study in the Beagles, systemic pemirolast exposure was determined for orally administered pemirolast potassium at 75 mg / kg daily for 7 consecutive days in male and female dogs (75 mg / kg daily having been found to be a safe chronic dose in dogs). The study, including all analyses and calculations, were performed by WIL Research, France, in compliance with Good Laboratory Practices (GLP).

[0072]There were no major differences in kinetics between males and females. Mean Cmax is shown in Table 3.

TABLE 375 mg / kg repeated dose (7th day)VariablesMales (n = 3)Females (n = 3)Cmax (μg / mL)168150

example 3

Pemirolast of hERG Channels

[0073]This study was performed by PhysioStim, France, a GLP compliant facility.

[0074]The effects of pemirolast on hERG currents in HEK-293 cells stably expressing the hERG potassium channel were studied using patch-clamp technique. In these experiments, 2.7, 8.0, 26.6 and 79.9 μg / mL of pemirolast potassium concentration-dependently decreased hERG tail current amplitude by 5.4%, 10.2%, 14.1% and 19.0%, respectively.

[0075]The reference compound E-4031 (0.1 μmol / L), a selective hERG inhibitor, reduced hERG tail current amplitude by 82.0%, thus confirming the pharmacological sensitivity of the hERG potassium channel in these experiments. In conclusion, IC50 for pemirolast could not be calculated because the inhibition was less than 20% at the highest concentration tested.

[0076]These results show that pemirolast lacks potential to inhibit hERG channel (an important human “anti-target” that must be avoided during drug development to reduce the risk of certain po...

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Abstract

According to the invention there is provided a method for the treatment of airway hyperresponsiveness, which method comprises the administration of pemirolast, or a pharmaceutically acceptable salt thereof, to a patient in need of such treatment. Suitable lower doses of pemirolast are least about 110 mg per day.

Description

[0001]This application is a continuation of U.S. patent application Ser. No. 14 / 951,202, filed Nov. 24, 2015, which claims priority benefit of GB 1518831.1, filed Oct. 23, 2015.FIELD OF THE INVENTION[0002]This invention relates to a new pharmaceutical use.BACKGROUND AND PRIOR ART[0003]Asthma is one of the most common chronic inflammatory diseases, known to affect nearly 25 million citizens in the US alone. In childhood, it is the most common chronic disease, affecting in the region of an estimated 7 million US children.[0004]The pathophysiology of asthma is complex and involves airway inflammation, intermittent airflow obstruction, and bronchial (airway) hyper-responsiveness, resulting in shortness of breath, wheezing, coughing, chest tightness and / or pain, as well as other non-specific symptoms in young children, including recurrent bronchitis, bronchiolitis, or pneumonia and the like.[0005]Diagnosis may be made under guidelines from the (US) National Asthma Education and Preventio...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/519
CPCY10S514/826A61K31/519A61K45/06C07D487/04
Inventor RAUD, JOHANDALSGAARD, CARL-JOHANTORNLING, GORAN
Owner CARDOZ AB
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