Artemisia Carvifolia is a common herb found in many parts of the world, and has been used by Chinese herbalists or more than 2000 years in the treatment of malaria. The earliest record dates back to 200 BC, in the "Fifty-two Prescriptions" unearthed from the Mawangdui Han Dynasty tombs. Its antimalarial application was first described, in Zhouhou Beiji Fang ("The Handbook of Prescriptions for Emergencies", Chinese: 肘后备急方), edited in the middle of the fourth century by Ge Hong; in that book, 43 malaria treatment methods were recorded. Images of the original scientific papers that record the history of the discovery, have been available online since 2006.

Results were published in the Chinese Medical Journal in 1979). The research was met with skepticism at first, partly because the chemical structure of artemisinin, particularly the peroxide portion, appeared to be too unstable to be a viable drug.

In the late 1990s, Novartis filed a new Chinese patent for a combination treatment with artemether and lumefantrine, providing the first artemisinin-based combination therapies (ACTs) (Coartem) at reduced prices to the World Health Organisation.In 2006, after artemisinin had become the treatment of choice for malaria, the WHO called for an immediate halt to single-drug artemisinin preparations in favor of combinations of artemisinin with another malaria drug, to reduce the risk of parasites developing resistance.

In 2011, Tu Youyou was awarded the prestigious Lasker-DeBakey Clinical Medical Research Award for her role in the discovery and development of artemisinin. The New York Times notes that the discovery of artemisinin is under consideration for a future Nobel Prize in Physiology or Medicine.