Axiom Biotechnologies develops new, high-throughput screening paradigm for drug discovery on native cells.

SAN DIEGO--(BUSINESS WIRE)--Sept. 18, 1996--Management of privately held Axiom Biotechnologies Inc. Wednesday announced that the company has filed a patent application with the U.S. Patent and Trademark Office covering a new drug-screening technology, called high-throughput pharmacological screening (HT-PS), that allows for rapid screening of combinatorial libraries on a variety of cell types, including native cells, immortalized cells and transfected cells.

HT-PS represents a breakthrough in high-throughput screening of combinatorial libraries that could accelerate the drug-discovery process and reduce research costs by providing comprehensive pharmacological information on potential lead compounds before they enter into preclinical or clinical trials.

``Screening combinatorial libraries on native cells in a high- throughput format represents a new paradigm for drug discovery,'' said Pandi Veerapandian, Ph.D., president and chief scientific officer.

``By measuring the physiological response of cells, native or transfected, in real time, we can provide better insight into the true biological activity of lead compounds and, as a result, accelerate the identification of promising lead candidates.''

Veerapandian added that this patent represents an important milestone for Axiom, solidifying its technology position in the field of drug screening.

The patent application specifically describes the methods and instrumentation that allow for broad, high-throughput pharmacological profiling of combinatorial libraries on a variety of target cells.

The methods and instrumentation evaluate the response of target cells (e.g., calcium ion flux, pH changes, cAMP levels and other signals) to test compounds and can perform all three levels of compound characterization: functional screening, affinity profiling and selectivity profiling -- all in a high-throughput format.

When fully automated, the instrument can perform functional screening of as many as 8,000 to 10,000 compounds per day and affinity and selectivity profiling of as many as 400 compounds per day.

In addition, Axiom's HT-PS screening technology employs luminescent, fluorogenic and chromogenic markers that obviate the need for radioactive chemicals, thereby decreasing drug-discovery costs and reducing environmentally hazardous waste materials.

``The HT-PS screening technology affords very powerful and flexible drug discovery. With one device and one assay system, we can very rapidly perform all three levels of drug characterization necessary for preclinical drug development,'' said Ilya Okun, Ph.D., Axiom's vice president, cell pharmacology.

``As a result, HT-PS offers tremendous advantages in terms of accelerating the leads-identification process and reducing drug- discovery costs.''

Typically, first-level screening (functional) and second-level screening (affinity profiling) are conducted using high-throughput transfected cell-based assays which rely on expression of co-transfected reporter genes in non-native cell types. Activation or inactivation of cell signaling pathways is monitored by quantifying reporter-gene expression.

Since reporter-gene expression results from complicated intracellular signaling pathways stimulated by receptor activation, reporter-gene signals are often observed hours, or even days, after the primary physiological response takes place.

By contrast, Axiom's new screening technology allows drug- discovery teams to select and characterize compounds in minutes by evaluating the immediate physiological responses of native (nonengineered) cells, in real time in a high-throughput format.

Axiom Biotechnologies is an emerging leader in the field of drug discovery. The company's proprietary HT-PS capability allows the company and its partners to perform high-throughput drug discovery by screening combinatorial libraries on a wide variety of cells, including native cells.

The company also applies its proprietary expertise in molecular optimization to enhance the potency of lead compounds identified in the screening process. Axiom is utilizing these technologies to allow its customers and corporate partners to improve the probability of identifying successful lead compounds and to accelerate the optimization process leading to drug candidates.

CONTACT: Axiom Biotechnologies Inc., San Diego 

James Linton, 619/455-4500