Antimalarial drugs: what’s new in the patents?

ABSTRACT

Introduction

The efficacy of current therapeutic warheads in preventing malaria transmission or treating the disease is often hampered by the emergence of drug-resistance. No effective vaccines are available to date, and novel drugs able to counteract drug-resistant forms of malaria and/or to target multiple stages of the parasite’s lifecycle are urgently needed.

Areas covered

This review covers patents that protect antimalarial small molecules bearing the artemisinin or other chemical scaffolds, as well as vaccines, that have been published in the period 2015–2022. Literature was searched in public databases of articles and patents. Patents protecting small molecules that prevent malaria transmission are not discussed herein.

Expert opinion

Significant progress has been made in the design of antimalarial agents. Most of these candidates have been tested in standardized strains, with the use of Plasmodium clinical isolates for testing still underdeveloped. Several compounds have been profiled in in vivo mouse models of malaria, including humanized mice. Despite having different efficacy, these new molecules might further progress the field and hopefully will advance to clinical development soon.

KEYWORDS:

• Malaria
• artemisinin
• antimalarial
• vaccines
• drugs

Article highlights

• Plasmodium drug resistance is compromising malaria eradication worldwide.

• Novel and effective antimalarials are urgently needed to overcome drug resistance.

• This review focus on patented antimalarials and vaccines from 2015 to 2022.

• Most relevant strategies focus on targeting host proteins or P. falciparum drug-resistant proteins.

• Molecules endowed with multiple mechanisms of action are expected to overcome drug resistance.

• Artemisinin derivatives are under development to increase the effectiveness of artemisinin combination therapies, and to decrease its susceptibility to drug resistance.

Acknowledgments

MMM Santos and E Lopes thank FCT (Fundação para a Ciência e Tecnologia) for funding through iMed.ULisboa (UIDB/04138/2020) and PhD fellowship SFRH/BD/137544/2018 (E. A. Lopes).

Declaration of interests

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Author contributions

E. A. Lopes – writing and revision; M. M. M. Santos – writing and revision; M. Mori – conception, writing and revision.

Data availability statement

Data sharing is not applicable to this article as no new data were created or analyzed in this study.

Additional information

Funding

This paper was not funded.