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Phase II biotransformations are detoxification mechanisms that conjugate xenobiotics with endogenous substances, neutralizing their toxicity.
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Methylation is a phase II biotransformation process involving the attachment of a methyl group to a substrate. Enzymes known as methyltransferases orchestrate this reaction.
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Clinical development focuses on how the drug will interact with the human body and encompasses four key phases of clinical trials, each serving a specific purpose in assessing the safety and effectiveness of new drugs. These phases overlap and build upon one another. Phase I involves a small group of healthy volunteers (typically 20-80 individuals) or, in cases where significant toxicity is expected, patients with the targeted disease, such as cancer or AIDS. The volunteers are tested for...
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Antimalarial compounds in Phase II clinical development.

Jana Held1, Sankarganesh Jeyaraj, Andrea Kreidenweiss

  • 1Institut für Tropenmedizin, Eberhard Karls Universität , Wilhelmstraße 27, D-72074 Tübingen , Germany +49 7071 29 85569 ; +49 7071 295189 ; janaheld@hotmail.de.

Expert Opinion on Investigational Drugs
|January 8, 2015
PubMed
Summary

Novel antimalarial compounds are in development to combat drug resistance. While most candidates show initial safety, their efficacy is still under evaluation, with several promising new options emerging.

Keywords:
AQ-13DF02DSM265KAE609KAF156OZ439Phase IIPlasmodium falciparumPlasmodium vivaxSAR97276artemisonechemotherapydrug developmentferroquinefosmidomycinmethylene bluesevuparintafenoquine

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Area of Science:

  • Malariology
  • Medicinal Chemistry
  • Clinical Pharmacology

Background:

  • Malaria remains a significant global health challenge, necessitating effective chemotherapy.
  • Current treatments predominantly rely on artemisinins, facing increasing resistance.
  • Development of novel antimalarial drugs is crucial for malaria eradication efforts.

Purpose of the Study:

  • To review antimalarial compounds in Phase II clinical development.
  • To present the findings from investigations of these novel antimalarial candidates.

Main Methods:

  • Review of antimalarial compounds undergoing Phase II clinical trials.
  • Analysis of safety and efficacy data for emerging antimalarial drug candidates.

Main Results:

  • Several promising antimalarial compounds are in the drug development pipeline.
  • Initial safety data are available for most candidates, but efficacy remains largely unconfirmed.
  • KAE609, KAF156, and DSM265 represent novel chemical scaffolds, diversifying treatment options.

Conclusions:

  • A diverse range of antimalarial compounds are progressing through development.
  • While no single drug is a guaranteed breakthrough, multiple candidates offer future control strategies.
  • New chemical scaffolds like KAE609, KAF156, and DSM265 are particularly noteworthy for diversifying malaria chemotherapy.