# Second-Generation Novel Liver Stage Active Antimalarials

> **NIH NIH R01** · PORTLAND STATE UNIVERSITY · 2021 · $681,482

## Abstract

PROJECT SUMMARY/ABSTRACT
 The global impact of malaria remains staggering despite extensive efforts to eradicate the disease. We
have developed a novel antimalarial acridone chemotype with dual stage efficacy against both liver stage and
blood stage malaria, as well as single-dose cure ability and potential to prevent relapsing infection. The ability
to combat multiple stages of the infection represents a powerful tool, and one ideally suited to achieve the
broadest possible benefit as the malaria eradication effort proceeds. A rigorous optimization process has
produced a series of second-generation acridones with significant improvements in efficacy, metabolic stability,
pharmacokinetics, and safety profiles. Our overarching goal is to develop a novel antimalarial that is safe in
individuals with G6PD deficiency, and in the most vulnerable populations – pregnant women and children, thus
supporting world-wide elimination of the disease. The specific goal of this project is to conduct lead
optimization studies to produce second-generation candidates for full preclinical evaluation that retain the
broad-spectrum features and demonstrate enhanced efficacy, safety, solubility, and metabolic/pharmacokinetic
profiles; to investigate the propensity for drug resistance to selected acridone candidates and identify the
molecular target(s) through whole genome sequencing and analysis; and to explore mode(s) of action for these
liver stage active antimalarial acridones using functional assays and bioanalytical approaches.

## Key facts

- **NIH application ID:** 10180516
- **Project number:** 1R01AI158533-01
- **Recipient organization:** PORTLAND STATE UNIVERSITY
- **Principal Investigator:** JANE X KELLY
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2021
- **Award amount:** $681,482
- **Award type:** 1
- **Project period:** 2021-04-01 → 2026-03-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10180516

## Citation

> US National Institutes of Health, RePORTER application 10180516, Second-Generation Novel Liver Stage Active Antimalarials (1R01AI158533-01). Retrieved via AI Analytics 2026-05-24 from https://api.ai-analytics.org/grant/nih/10180516. Licensed CC0.

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