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Our Exciting Journey to ACT-451840
Christoph Boss1, Sergio Wittlin2
1Drug Discovery and Preclinical Development, Idorsia Pharmaceuticals Ltd, Hegenheimermattweg 91, CH-4123 Allschwil, Switzerland,
Chimia
|November 20, 2021
Summary
A novel antimalarial drug, ACT-451840, demonstrates efficacy in preclinical models and human trials. This compound offers a new mode of action against malaria parasites.
Area of Science:
- Medicinal Chemistry
- Parasitology
- Pharmacology
Background:
- Malaria remains a significant global health challenge, necessitating the development of new antimalarial drugs.
- Existing treatments face challenges due to drug resistance and side effects, highlighting the need for novel therapeutic agents.
Purpose of the Study:
- To identify and characterize a novel antimalarial compound, ACT-451840.
- To evaluate the efficacy and safety of ACT-451840 in preclinical and clinical settings.
Main Methods:
- In vitro and in vivo characterization of ACT-451840.
- Pharmacokinetic (PK) studies in rats.
- Efficacy testing in Plasmodium berghei mouse malaria models.
- Clinical investigation in an experimental human malaria infection model.
Main Results:
- ACT-451840 demonstrated a novel mode of action against malaria parasites.
- Complete cure in a P. berghei mouse model was achieved with oral doses of 300 mg/kg for 3 days.
- Therapeutic effects were observed in a human malaria infection model.
Conclusions:
- ACT-451840 is a promising novel antimalarial drug candidate.
- The compound exhibits efficacy in both animal models and human trials, supporting further development.
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