Safer anti-malarials

In the arms race against malaria, humans wield the biggest weapons, but their cost is great. In recent years, malaria has mutated and adapted to resist the drugs used to combat it. Caused by a parasite and transmitted by mosquitoes, malaria is an infectious disease that kills nearly one million people each year. Humans struggle to prevent malaria transmission and to treat those infected with the deadly disease.

Unfortunately, some of the malaria treatments are potentially deadly as well. "Amodiaquine was introduced as an antimalarial drug, but. . . withdrawn from the market when it became clear that the drug caused serious adverse effects in the form of liver damage and impaired immune system." The drug is still used in the most severe cases of drug-resistant malaria. It saves lives, but endangers them as well.

Endeavoring to create safer drugs, scientists at the University of Gothenburg, Sweden, studied the byproducts of drugs, looking for toxins. "A pharmaceutical in the body is, in the optimal case, broken down into harmless products (metabolites) that leave the body, for example via the urine. Some pharmaceuticals, however, can be converted into toxic products, which may result in serious adverse effects." Proposed by Tove Johansson Mali'n, the scientists uncovered a process that can "simulate the metabolism of pharmaceuticals in the body". In this way they can identify and characterize several potentially toxic products that arise as the metabolites of drugs". With the aid of this methond, Mali'n "has now managed to identify. . . previously unknown metabolites that may have caused, or contributed to, the adverse effects of amodiaquine."

"We hope that the method can simplify the work of identifying potentially toxic metabolites at an early stage, and thus facilitate the development of safe drugs," says Tove Johansson Mali'n.

Tove Johansson Mali'n, Lars Weidolf, Neal Castagnoli, Ulrik Jurva. P450-catalyzed vs. electrochemical oxidation of haloperidol studied by ultra-performance liquid chromatography/electrospray ionization mass spectrometry. Rapid Communications in Mass Spectrometry, 2010; 24 (9): 1231 DOI: 10.1002/rcm.4505
University of Gothenburg (2010, May 9). New method for developing safer drugs. ScienceDaily. Retrieved May 10, 2010, from http://www.sciencedaily.com¬ /releases/2010/05/100509202645.htm