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PCRs currently represent the most important and valuable class of drug targets. The success of GPCRs as drug targets over the past 20 years has spawned significant imitations in certain categories, such as beta-blockers against hypertension. Hence, by some estimates, GPCRs account for nearly 50% of all drugs on the market and 30% of the top 50 sellers (Scussa, F. World's best-selling drugs, Med Ad News No. 5, 2002) including such well-known brands as Claritin®, Zyprexa®, Zantac® and Cozaar®.

Examples of GPCR-
based drugs among the 200 best-selling prescriptions
, together with their GPCR targets.


While the Predix drug discovery process is widely applicable to numerous indications associated with GPCRs, the company is initially dedicated to developing therapeutics for indications that represent great unmet medical needs for psychiatric disorders (e.g. anxiety/depression and memory dysfunction), pain, and inflammatory diseases (e.g. asthma, COPD).

Arrhythmias and the Need for Novel Anti-Arrhythmic Agents

e've also been focused on modeling the physiology and pharmacology of cardiac ion channels to develop compounds for the treatment of ventricular arrhythmia. At the present time, patients with ventricular arrhythmias are treated palliatively with implantation of electrical devices called implantable cardioverter defibrillators (ICD), which deliver electrical shocks to the heart during episodes of arrhythmia. Patients may also be treated with medications such as Cordarone (amiodarone) or Sotacor (Betapace, sotalol) which act to suppress the occurrence of such arrhythmias. These treatments are highly inadequate (based on the continued high death rate), expensive (ICDs can run into tens of thousands of dollars), and have significant drug-related side effects. Therefore, the development of novel anti-arrhythmic agents is a critical unmet medical need, but poses substantial difficulties in development since the control of dynamic events is poorly understood in biology, generally, leading many large pharmaceutical companies to "wait and see" what new approaches emerge.    ^TOP

It is estimated that 295,000 people die in the United States yearly from sudden cardiac death linked to ventricular arrhythmia. Cost estimates for pharmaceuticals to treat ventricular arrhythmia approach US $350 million worldwide, approximately US $160 million of which is attributable to the U.S. market. In 1999, worldwide sales of pharmaceuticals to treat arrhythmias (primarily atrial) were approximately US$1.1 billion. The largest class in antiarrhythmic drug sales are Class I drugs (1999 sales of US$303 million) which block sodium channels in cardiac cells. Class I drug examples are Rhythmol, Tambocor and Quinaglute. Class II drugs (US$133 million) consist of beta blockers such as Inderol. Class III drugs (US$281 million) are potassium-channel blockers such as Cordarone and Betapace. Class IV drugs (US$255 million) are calcium-channel blockers such as Cardizem.    ^TOP