- Guide to PHARMACOLOGY
Compound class: Synthetic organic
Comment: Artefenomel is a synthetic ozonide (synthetic peroxide), a class of compound that retains the endoperoxide bridge of the artemisinin class of antimalarials but also contains the sterically bulky amantadine ring, which increases blood plasma stability .
The Malaria tab on this ligand page provides additional curator comments of relevance to the Guide to MALARIA PHARMACOLOGY.
|No information available.|
|Summary of Clinical Use|
|Artefenomel has a longer elimination half-life than other antimalarial endoperoxides and therefore has potential as a single-dose treatment when used with a partner drug. A Phase 2 clinical trial in which artefenomel will be used in combination with ferroquine (NCT02497612) has commenced recruitment. Results from a trial with piperaquine (NCT02083380, published in ) did not reach target efficacy as a single-dose treatment and a trial in combination with DSM265 (NCT02573857) has been terminated. Click here to view the full list of artefenomel trials registered with ClinicalTrials.gov.|
|Mechanism Of Action and Pharmacodynamic Effects|
|The ozonide class are thought to act on the Plasmodium proteostatic stress response: initially disrupting haemoglobin metabolism and following extended exposure, to reflect clinically-relevant treatment periods, additional parasite biochemical pathways were found to be perturbed .|
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT02083380||Phase II Efficacy Study of Artefenomel & Piperaquine in Adults & Children With P. Falciparum Malaria.||Phase 2/Phase 3 Interventional||Medicines for Malaria Venture|
|NCT02497612||To Evaluate the Efficacy of a Single Dose Regimen of Ferroquine and Artefenomel in Adults and Children With Uncomplicated Plasmodium Falciparum Malaria||Phase 2 Interventional||Sanofi|
|NCT02573857||A Study to Characterise the Antimalarial and Transmission Blocking Activity of a Single Dose of DSM265 or OZ439 in Healthy Subjects With Induced Blood Stage Plasmodium Falciparum or Plasmodium Vivax Infection||Phase 1/Phase 2 Interventional||Medicines for Malaria Venture|
|The estimated terminal half-life for elimination is 46 to 62 hours .|