Drug-discovery collaboration discovers potential new antimalarial drug candidates

Overview

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• Source: Walter and Eliza Hall Institute


• Date: 23 Apr,2021

Potential new antimalarial drug candidates are being developed through an protracted drug-discovery collaboration between Australian medical research institute WEHI and Janssen Pharmaceutica NV. The collaboration was facilitated by Johnson & Johnson Innovation.

A collaborative research team discovered compounds with antimalarial activity within a collection of 80,000 drug-like molecules at the Janssen Jump-stARter Compound Library, a special collection of drug-like compounds designed to fast track the discovery of new medicines. Under the agreement, the most promising candidates are now being further developed by the researchers towards potential antimalarial drugs, which could lead to powerful new weapons in the international struggle against this disease.

In a glance

1.A drug-discovery cooperation between WEHI and Janssen Pharmaceutica NV has discovered new drug-like compounds with antimalarial activity.

2.The collaborative team, now involving the Medicines for Malaria Venture, are developing these compounds into possible new drugs that will be tested for their action against malaria, a disease that kills hundreds of thousands of individuals each year.

Collaborative drug discovery
Over 200 million people worldwide contract malaria each year. This mosquito-borne parasitic disease causes hundreds of thousands of deaths annually, and also puts an enormous burden on communities through illness.

“The evolution of resistance to currently used antimalarial drugs is among the greatest threats to global malaria control efforts, and new medicines are urgently needed,” said Professor Alan Cowman AC, who leads WEHI’s malaria research program. “Our group has focussed for more than 30 years on understanding the biology of the malaria parasite and its interactions with people, with the objective of creating new approaches to preventing or treating malaria.

With this collaboration, we have been able to access novel drug-like compounds that have the right properties to be developed into new medicines. Excitingly, our collaboration and additional support from Johnson & Johnson Innovation has shown this library contains multiple compound classes with antimalarial activity, suggesting they could be developed into new drug candidates.”

Professor Alan Cowman

“The discovery and development of new antimalarial drugs has been a central goal of WEHI’s malaria research.

The opportunity to get into the Jump-stARter Compound Library in late 2016, allowed WEHI scientists to rapidly progress their search for new antimalarial drugs. With the compounds identified, the WEHI team will now move forward to learn more about the key proteins in collaboration with Janssen.

WEHI medicinal chemist Dr Brad Sleebs led the next stage of the study, modifying the antimalarial compounds in the library, to enhance their activity, in addition to ensuring they had the right properties to be appropriate as a medication.

“We have worked closely with the Janssen Discovery Chemistry team to advance this stage of the research, and we finally have some really promising compounds,” Dr Sleebs said. “Our research team has also been able to pinpoint how some of these compound classes act to block the rise of malaria, a key step in enhancing their design.”

The research has been enhanced through the involvement of the not-for-profit foundation, the Medicines for Malaria Venture (MMV), whose goal is to reduce the burden of malaria in disease-endemic nations and ultimately to eradicate malaria.

“MMV has provided critical advice for this project, both in the chemical design of the new compounds, as well as ensuring the drugs we’re developing meet their Target Product Profile (TPP) and don’t replicate work underway at other malaria research facilities around the world. This has been a valuable addition to the collaboration, and we can be certain we are working in a exceptional research space. The cooperation with MMV has offered access to a global network of malaria researchers and assay platforms,” Dr Sleebs said.

Professor Cowman said the collaboration between WEHI, Janssen Pharmaceutica NV, Johnson & Johnson Innovation and MMV has created a powerful team.

“WEHI has a solid track record in malaria biology, as well as expertise in drug screening and medicinal chemistry, which has been complemented by skills brought to the table by our spouses. We’re thrilled that this has yielded some encouraging antimalarial drug candidates, which that are now being evaluated in preclinical models,” Professor Cowman said.