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Repurposing Drugs for Malaria through a Human Dose Prediction: A Case Study with Berzosertib.
Devasha Redhi1, Mwila Mulubwa2, Mmakwena M Mmonwa2
1South African Medical Research Council Drug Discovery and Development Research Unit, Department of Chemistry and Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Cape Town, South Africa.
Clinical Pharmacology and Therapeutics
|May 4, 2026
Summary
Repurposing the anticancer drug berzosertib shows promise for malaria treatment. A predicted effective dose for malaria is lower than its established cancer therapy dose, suggesting potential for drug repurposing.
Area of Science:
- Pharmacology
- Drug Repurposing
- Infectious Diseases
Background:
- Drug repurposing accelerates development of new malaria treatments.
- Berzosertib, an anticancer kinase inhibitor, is investigated for antimalarial potential.
Purpose of the Study:
- To assess if berzosertib can be repurposed for malaria treatment.
- To determine if the efficacious human dose for malaria falls within its safety profile.
Main Methods:
- Pharmacokinetic-pharmacodynamic (PK-PD) study in Plasmodium falciparum-infected humanized mice.
- Development of a human physiologically based pharmacokinetic (PBPK) model.
- Simulation of exposure-response relationships to predict effective human dose.
Main Results:
- Berzosertib's antimalarial activity depends on sustained concentrations above the minimum parasiticidal concentration (MPC).
- Predicted effective human dose: 75 mg daily IV for 6 days for uncomplicated malaria.
- This dose is lower than the maximum tolerated dose (440 mg IV twice weekly) used in cancer therapy.
Conclusions:
- Berzosertib shows potential for malaria drug repurposing.
- Further preclinical studies are required to validate its efficacy and safety for malaria.
- The predicted dose suggests a favorable therapeutic window for malaria treatment.
