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Antimalarial Drug Design

Palumed, a company that specializes in antimalarial compounds, was created in 1999 by members of the CNRS Coordination Chemistry Laboratory (LCC) in Toulouse.1 After a 35-year career in academic research, the group leader, Bernard Meunier– President of CNRS between October 2004 and January 2006–decided to move into a more applied field. The antimalarials on which Palumed works today stem from research experience acquired by the LCC group over many years, resulting in the development of ten molecules, a patent, and some 20 frequently cited publications. In just a few years, Palumed has produced 120 compounds and filed two additional patents, in 2003 and 2006. “This type of pace is impossible to sustain in an academic research setting, and this is why I have decided to work full-time for Palumed,” explains Meunier.

The recent patents have to do with new antimalarial drugs called trioxaquines. How do they work? They are hybrid molecules, or “double-barreled guns,” that associate in a single molecule the advantages of two families of antimalarial drugs: artemisinin and chloroquine. Although both active in fighting the malaria parasite, each of these compounds raises specific problems: artemisinin is both rare and relatively expensive, and chloroquine is inactive against resistant parasite strains. By combining the advantages of these two substances into a single, novel compound, Palumed hopes to obtain a curative drug that would be effective on resistant strains, inexpensive, and could be orally consumed during malaria attacks, thus fulfilling all the requirements assigned by the World Health Organization (WHO).

“We performed in vitro tests on 120 active compounds generated by chemical synthesis, and then tested 70 of them on mice,” explains Meunier. After pharmacokinetics (residence time in the body) and bioavailability (passage through the intestinal barrier) measurements, performed in collaboration with Sanofi-Aventis, a compound called PA1103 was selected. It is still at the preclinical development stage, but Palumed, with its fourteen employees and €2.6 million in funding raised in 2006, now has the resources it needs to reach its objectives. A batch of that particular compound is scheduled for industrial production, and regulatory toxicology studies are under way, prior to human testing that will begin in early 2009. Market availability could become a reality by 2013.


Jean-François Haït






Notes :

1. Laboratoire de chimie de coordination (CNRS).

Contacts :

Bernard Meunier
Palumed, Labège.


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