Asmacure Highlights Four Presentations on Novel Pulmonary Development Compound ASM-024 Presented at American Thoracic Society 2013 International Conference

QUEBEC CITY, May 20, 2013 /PRNewswire/ -- Asmacure Ltee, a clinical-stage biopharmaceutical company focused on the development of novel, proprietary compounds that target cholinergic receptors for the treatment of pulmonary diseases, today announced presentations of four studies of ASM-024, Asmacure's lead compound in development for asthma and chronic obstructive pulmonary disease (COPD). The data were presented at the 2013 American Thoracic Society (ATS) International Conference in Philadelphia.

"We believe the combined data presented confirm the significant potential for our lead compound, ASM-024, to positively impact the treatment of asthma and other respiratory disorders," said Yvon Cormier, M.D., Asmacure's founder and chief medical officer. "ASM-024's novel dual mechanism of action, which has been shown to induce smooth muscle relaxation as well as anti-inflammatory and bronchodilating effects, may address a significant need as an adjunctive treatment with current standard of care in patients with moderate to severe asthma or chronic obstructive pulmonary disease. We anticipate moving ASM-024 into a phase 2 trial in COPD later this year."

Highlights of the studies presented follow below:
(Poster #B25)

• The first study positively evaluated the safety, tolerability and clinical activity of ASM-024 delivered as a solution for nebulization formulation in people with mild allergic asthma in a phase 2 allergen challenge clinical trial, representing the first clinical proof-of-concept data for ASM-024 in an asthma patient population. ASM-024 was shown to reduce methacholine airway responsiveness and improve baseline lung function. No serious adverse events were reported in the study with poor taste and cough observed as the most common side effects. ASM-024, significantly inhibited IgE-mediated activation of basophils in vitro and decreased allergen-induced CD203c expression on circulating basophils of mild asthmatic subjects after 9 days treatment.

(Poster #507)

• A second study evaluated ASM-024's ability to activate potassium channels and the sodium/potassium (NA+/K+) ATPase pump, which pumps sodium out of and potassium into cells to regulate resting potential, in guinea pig tracheal rings. Previous studies have shown that ASM-024 reduces airway resistance in mice and has smooth muscle relaxant properties in vitro by acting directly on airway smooth muscle cells by a mechanism independent of cGMP or cAMP pathways; however, ASM-024's action on potassium channels and Na+/K+ ATPase is unknown. Researchers measured changes in tension with cumulative doses of ASM-024 (0.1-1000 microns). To investigate the potential mechanisms involved in the relaxant activity of ASM-024, the tracheal rings were pretreated with channel and pump inhibitors. Results showed that ASM-024's relaxant properties are independent of ATP-sensitive potassium channels, calcium-sensitive potassium channels or Na+/K+-ATPase activation, and further confirmed that ASM-024's mechanism of action is linked to its interaction with the nicotinic receptor.

(Poster #F76)

• A third study explored and differentiated between ASM-024, which has dual nicotinic and muscarinic action, and commonly used short- and long-acting muscarinic acetylcholine receptor antagonists. These antagonists are used in COPD and severe asthma to reduce enhanced cholinergic activity, but may be less effective on bronchoconstriction induced by histamine. Researchers measured relaxant responses to methacholine or histamine contraction via isometric tension measurement of guinea pig tracheal rings, and found that ASM-024 not only induces in vitro smooth muscle relaxation of histamine-contracted tracheas, but also has an additive relaxant effect to muscarinic acetylcholine receptor agonists after methacholine-induced contraction, suggesting that ASM-024 has different functional activity from these drugs. The precise mechanisms of action of ASM-024 continue to be studied; data develop to date indicate that ASM-024 has effects at the nicotinic and muscarinic levels. The results further suggest that ASM-024 could be considered as an add-on agent to current standard of care in patients with poorly controlled asthma, and in COPD patients who present insufficient bronchodilator response to current medication.

(Poster #B41)

• A final study evaluated the relaxant effects of ASM-024 on Beta2-agonist desensitized guinea-pig tracheas. Inhaled Beta2-agonists are widely used in asthma and COPD; however, prolonged use of these agonists induces functional desensitization of the Beta2-adrenoreceptors, which may lead to reduced efficacy when used chronically. The study assessed ASM-024's efficacy in promoting the relaxation of guinea pig tracheas that were rendered unresponsive to Beta2-agonists. Findings showed that ASM-024 elicits relaxation of Beta2-desensitized tracheal preparations, suggesting that ASM-024 mediates smooth muscle relaxation through a different target and signaling pathway than conventional Beta2-adrenergic receptor agonists; ASM-024 could thus potentially be used as an add-on therapy in patients with insufficient bronchodilator response to currently available Beta2-agonists.

About Asthma
Asthma is a reversible obstructive lung disease, caused by increased reaction of the airways to various stimuli. It is a chronic inflammatory condition with acute exacerbations. Asthma can be a life-threatening disease if not properly managed.  According to the American Lung Association in 2011 it was estimated that 25.9 million Americans currently have asthma, including 7.1 million children under 18. Of these, 13.2 million Americans (4.1 million children) had an asthma attack.  Close to 2.1 million emergency room visits were attributed to asthma in 2009.

About ASM-024
The company's lead development compound, ASM-024, with its novel mechanism of action, has demonstrated the capabilities of inhibitory effects on inflammation, bronchoprotection and smooth muscle relaxation in pre-clinical asthma models. ASM-024 delivered as a solution for nebulization achieved proof of concept in the treatment of patients with asthma in a phase 2 clinical trial program.  The company is now focused on bridging from the ASM-024 solution formulation to the development of the compound in a dry powder for inhalation (DPI) dosage form.  Typically, DPI's are a preferred dosage form for pulmonary products by allowing for delivery of lower, more optimal dosing with greater lung deposition. 

ASM-024 demonstrated a highly-significant effect on FEV₁and methacholine PC₂₀ pre-allergen challenge in a phase 2 study utilizing the solution for nebulization formulation.  In pre-clinical asthma models, ASM-024 has demonstrated an adjunctive benefit when combined with long- and short-acting Beta-agonists and long- and short-acting muscarinic antagonists. 

Based on recent findings about the novel mechanism of action for ASM-024 with nicotinic and muscarinic effects, Asmacure will initiate a phase 2 study in COPD patients in the third quarter of this year.

About Asmacure
Asmacure Ltee is a clinical-stage biopharmaceutical company focused on the development of novel, proprietary compounds that target cholinergic receptors for the treatment of inflammation, notably pulmonary airway diseases.  The company's lead compound, ASM-024, has a novel mechanism with multi-functional properties at the nicotinic and muscarinic levels. Asmacure was founded by Dr. Yvon Cormier, a noted pulmonologist, and Evelyne Israel-Assayag in 2002 and is based in Quebec City, Quebec, Canada.  Asmacure is a privately-held company with the major investors including Domain Associates, Fonds de solidarite des travailleurs du Quebec (F.T.Q.) and Desjardins-Innovatech s.e.c. For more information visit www.asmacure.com.

Contact Information
E. Blair Schoeb           
Tel: 917-432-9275                                                        
[email protected]

SOURCE Asmacure

WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM?

440k+
Newsrooms &
Influencers

9k+
Digital Media
Outlets

270k+
Journalists
Opted In

GET STARTED