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A Novel Approach to Identify Smooth Muscle Relaxants
Phone: () -
Email: NSIGAL@CYTOKINETICS.COM
DESCRIPTION (provided by applicant): Chronic obstructive pulmonary disease
(COPD) and especially asthma affect millions of Americans. As of 1995, an
estimated 14.9 million persons suffer chronic symptoms. Despite several
different therapeutic approaches, disease severity also is on the rise as
reflected by increasing mortality rates. The treatment of COPD and asthma
relies on long-term reduction of the chronic inflammatory response and acute
symptomatic control by the use of bronchodilators. In the latter class, inhaled
Beta adrenergic agents are most commonly used but suffer from reduced efficacy
with prolonged use secondary to receptor desensitization. We propose to begin
development of a new class of bronchodilators that act directly on the target
responsible for force generation, the motor protein smooth muscle myosin. We
plan to introduce this target into Cytokinetic's robust high throughput
screening technology to discover compounds that will act via this unique
mechanism. Using biochemical and physiological means, these compounds will be
screened for secondary undesirable properties and then tested in semi-intact
systems. We expect to identify chemical compounds that have the potential to
demonstrate proof of principle in relevant models of bronchoconstriction. These
compounds may then eventually lead to a novel pharmacologic class of smooth
muscle relaxants with applicability in other therapeutic areas.
PROPOSED COMMERCIAL APPLICATIONS:
Given the number of individuals that use bronchodilators in various lung diseases, the potential market is enormous. The estimated 2002 market size for the most widely used inhaled beta-adrenergic agents (albuterol and salmeterol) is $1.3 billion dollars (Med Ad News, 2000, Vol. 19, p. 59). Agents that directly target the contractile machinery could be used either as adjunctive therapy or potentially as a primary agent. In addition, a potent smooth muscle relaxant may have applications in the other large therapeutic areas such as hypertension, pre-term labor, and bladder spasmaticity leading to incontinence.
* Information listed above is at the time of submission. *