Artemisinin Derivatives
Because artemisinin itself has physical properties such as poor bioavailability that limit its effectiveness, semisynthetic derivatives of artemisinin have been developed. These include:
- Artesunate (water-soluble: for oral, rectal, intramuscular, or intravenous use)
- Artemether (lipid-soluble: for oral, rectal or intramuscular use)
- Dihydroartemisinin
- Artelinic acid
- Artenimol
- Artemotil
There are also simplified analogs in preclinical research.
A synthetic compound with a similar trioxolane structure (ring containing three oxygen atoms) named arterolane showed promise in in vitro testing. Phase II testing in patients with malaria was not as successful as hoped, but the manufacturer decided to start Phase III testing anyway. A combination with piperaquine is also in development.
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