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Semisynthetic synthesis of artemisinin

Biological production of artemisinic acid and chemical conversion of the acid to artemisinin could help supply first-line treatments for malaria infection at low cost. Artemisinin is naturally produced in the plant Artemisia annua. Saccharomyces cerevisiae expressing A. annua enzymes synthesized the artemisinin precursor artemisinic acid, which then was extracted from suspension at more than 10-fold higher titers than those produced by other methods. A 4-step chemical synthesis process was used to synthesize artemisinin from artemisinic acid with an overall yield of 40%-45% and with higher purity than plant-derived artemisinin. Next steps include commercializing the process to produce artemisinin-based combination therapies to treat malaria infection.
Novartis AG markets the artemisinin-based combination therapy Coartem artemether/lumefantrine to treat malaria.
Sigma-Tau Group and Pfizer Inc. market Eurartesim dihydroartemisinin/piperaquine to treat malaria.
Suda Ltd.'s ArTiMist, a sublingual aerosol formulation of artemisinin, is in Phase III testing for the indication.

SciBX 6(16); doi:10.1038/scibx.2013.394
Published online April 25, 2013

Patent status undisclosed; Amyris Inc. exclusively licensed the technology to the Institute for OneWorld Health, which has licensed it to Sanofi; available for licensing for non-malaria indications

Paddon, C.J. et al. Nature; published online April 10, 2013;
Contact: Chris J. Paddon, Amyris Inc., Emeryville, Calif.