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VALIDATION OF A NOVEL SARCOMERIC HIGH THROUGHPUT ASSAY

Award Information
Agency: Department of Health and Human Services
Branch: National Institutes of Health
Contract: N/A
Agency Tracking Number: 1R43HL066647-01
Amount: $99,900.00
Phase: Phase I
Program: SBIR
Solicitation Topic Code: N/A
Solicitation Number: N/A
Timeline
Solicitation Year: N/A
Award Year: 2001
Award Start Date (Proposal Award Date): N/A
Award End Date (Contract End Date): N/A
Small Business Information
280 E GRAND AVE, STE 2
SOUTH SAN FRANCISCO, CA 94080
United States
DUNS: N/A
HUBZone Owned: No
Woman Owned: No
Socially and Economically Disadvantaged: No
Principal Investigator
 FADY MALIK
 () -
Business Contact
Phone: (650) 624-3000
Email: NSIGAL@CYTOKINETICS.COM
Research Institution
N/A
Abstract

DESCRIPTION: (Investigator's abstract) The US. heart failure population numbers
approximately 5 million and is growing. Despite treatment with current medical
therapy, many patients remain symptomatic and require frequent hospitalization,
placing an enormous burden on our health care system. Currently, the most
ineffective arm of medical therapy are agents that modulate cardiac
contractility. These agents improve patients' quality of life and decrease
hospitalization rates, but have no effect on mortality rates.

We propose to start development of a new class of cardiac contractility
modulators acting directly on the force-producing cellular structure, the
sarcomere. We will leverage Cytokinetics' robust high throughput screening
technology to find compounds that modulate a reconstituted sarcomere. The
ability to introduce a complex, well characterized, functional protein machine
into a high throughput screen represents a significant advance in drug
discovery. Using biochemical and physiological means, these compounds will be
screened for secondary undesirable properties. This technology has already been
validated against molecular motors that power mitosis.

We expect to identify chemical compounds that have the potential to demonstrate
proof of principle in relevant animal models. These compounds may eventually
lead to a new class of contractility modulators that will play an important
role in treating heart failure.
PROPOSED COMMERCIAL APPLICATION:
No new agents that modulate cardiac contractility have come on the market in nearly 10 years.
The current market for digoxin, a 200 year old drug and the only one safe for chronic use in
heart failure, is roughly $150 million per year (IMS data). The sales of non-generic dobutamine
(Eli Lilly), used for acute heart failure, amounted to $86 million in 1998 (Paine Webber). Agents
that directly target the force generating apparatus could be expected to be more effective
and have fewer cellular toxicities. These properties may lead to improved patient outcomes.
Naturally, such agents would gain a strong foothold in a large and growing marketplace.

* Information listed above is at the time of submission. *

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