artefenomel

Ligand id: 9971

Name: artefenomel

Structure and Physico-chemical Properties

2D Structure
Click here for structure editor
Calculated Physico-chemical Properties
Hydrogen bond acceptors 5
Hydrogen bond donors 0
Rotatable bonds 5
Topological polar surface area 49.39
Molecular weight 469.28
XLogP 5.34
No. Lipinski's rules broken 1

Molecular properties generated using the CDK

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 [3]) 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.
Clinical Trials
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
Pharmacokinetics
Elimination
The estimated terminal half-life for elimination is 46 to 62 hours [4].