Patent issued for a novel anti-malaria target

BLACKSBURG, Va., Nov. 17, 2008 – Virginia Tech Intellectual Properties has announced that the U.S. Patent and Trademark Office has granted a patent for targets and methods to develop new drugs for malaria.

For decades, scientists have been searching for a way to target malaria-causing parasites that have infected the human body. Researchers from the Virginia Bioinformatics Institute at Virginia Tech discovered and characterized a protein the parasites make, called Heme Detoxification Protein (HDP), which is a key to doing just that. Dharmendar Rathore, formerly an assistant professor at the institute, led the effort, working closely with Dewal Jani, a molecular and protein biologist, and Rana Nagarkatti, protein biochemist and molecular biologist, to identify and isolate the protein that is so vital for the parasite's survival.

Every year 350-500 million people are infected and more than 1 million people die from malaria.

"New drugs developed with this discovery will have a huge impact," said Otto Folkerts, associate director of technology development at the Virginia Bioinformatics Institute. "It's an entirely new mechanism of action and can help with the increasing problem of drug resistance, for example, as part of a cocktail therapy with other existing drugs."

Once infected mosquitoes bite and transmit the parasite to the human body, the parasite replicates exponentially and infects the red blood cells, which are composed of approximately 90 percent hemoglobin. The parasite feeds on the globin component of the hemoglobin, and because the leftover free heme component is toxic, the parasite uses a protein to detoxify the heme and convert it into a new form called hemozoin. That protein is HDP.

"We've discovered the piece to the puzzle that was missing," said Rathore.

Prior to the discovery of HDP, scientists created drugs to target the free heme byproduct and prevent it from becoming hemozoin, thus keeping the molecule in its toxic form in order to kill the parasite. However, the anti-malaria drugs currently on the market tend to have adverse side effects and are progressively becoming ineffective due to increasing drug resistance.

Rathore explained that drugs used for malaria therapy today target a host (human) metabolic process, which involves the heme byproduct that is natural to the human body. The ideal target for an anti-infective drug is a pathogen protein, so that human metabolism is not disrupted.

"With HDP, you will be targeting a parasite-specific factor, which is absolutely unique, and that's a big plus in the field of drug discovery," he said. "If you can identify the target, that's a big achievement,” which is why Rathore's work is foundational for this new therapeutic approach.

Virginia Tech Intellectual Properties Inc. is seeking a pharmaceutical company to continue the drug development work that is needed in order to take Rathore's discovery to the next stage, and to test the effectiveness of drugs that are identified in the laboratory using the patented assays. The cost of any treatment for malaria will need to be very low or else it won't be affordable in the parts of the world where malaria is widespread and devastating. However, a licensee is still likely to want exclusive rights to develop the technology into a treatment, so securing a patent is an important first step. Large pharmaceutical companies have an interest in devoting a portion of their research and development to underserved humanitarian medical needs, so Virginia Tech Intellectual Properties is looking for a company with an interest in the area of malaria research and treatment to license the rights to this newly issued patent.

For more information about this product or to discuss licensing terms, please contact Jackie Reed with Virginia Tech Intellectual Properties at (540) 231-9217.

(Biological Sciences undergraduate Michelle A. Rivera of Blacksburg, Va., working as an intern for Virginia Tech Intellectual Properties, prepared this announcement.)