Searching for new antimalarial medicines
World Class Quality, Indigenously African
Egbogi Therapeutics is searching for new antimalarial medicines from African science, starting with a parasite enzyme that could offer a new way to treat malaria.
WHY NEW MEDICINES ARE NEEDED
Why search for new antimalarials?
Malaria care still depends on a small number of treatments. A new approach, found carefully, could matter.
Malaria burden
Malaria still places a heavy burden on Nigeria and across Africa, especially on young children. New medicines are part of a long term response.
Parasite resistance
The malaria parasite has developed resistance to medicines before. Relying on a small number of treatments leaves care exposed if resistance spreads.
No new mechanism
Many current antimalarials work in similar ways. A different target could, in time, offer a genuinely new way to treat malaria.
Local science
The search starts with African science, building research skill and knowledge where the burden is highest.
Link to manufacturing
Discovery is linked from the start to Egbogi's API manufacturing work, so a future candidate would have a local route to production in view.
THE TARGET
One parasite enzyme, studied closely
The research focuses on one clear target first, rather than spreading effort across many ideas at once.
Plasmodial transketolase
An enzyme the malaria parasite needs. It is the starting point for the search, chosen because blocking it could disrupt the parasite.
Selectivity
The aim is to find compounds that act on the parasite enzyme. Selectivity is the question the work is testing, not a result it has shown.
From discovery to manufacturing
The long route from a research idea to a manufactured medicine is kept in view from the start. No medicine has made that journey yet.
OUR RESEARCH TARGET · TRANSKETOLASE
One enzyme the malaria parasite cannot do without
Transketolase is an enzyme in Plasmodium falciparum, the parasite behind the most deadly form of malaria. Egbogi is studying whether blocking this one enzyme could stop the parasite growing, while leaving the human version of the enzyme alone.
Enzyme · transketolase
Pathway · pentose phosphate
Needs · vitamin B1 form, TPP
Aim · block the parasite, spare the person
Progress · inhibitors identified, in optimization
What transketolase does
It sits in the pentose phosphate pathway, a set of chemical reactions the parasite uses to build and power new cells. The enzyme moves a two carbon unit between sugar molecules, and it needs thiamine pyrophosphate, a working form of vitamin B1, to do it.
Why the parasite needs it
That pathway produces ribose 5 phosphate, a building block for DNA and RNA. A parasite that is copying itself quickly needs a steady supply, which is why published research describes this enzyme as vital for the parasite’s survival and replication.
Why it may be a selective target
The parasite enzyme differs from human transketolase in structure and in how it behaves. That difference is the opportunity: a blocker shaped for the parasite version may have little effect on the human one, and it is the basis for the selective inhibitors Egbogi has now identified.
What Egbogi is doing with it, step by step
Study the target
Working from the published science on plasmodial transketolase, and on where it differs from the human enzyme.
Design on computer
Modelling compounds that could fit the parasite enzyme and block it, before anything is made in the lab.
Make and test
Preparing the selected compounds and testing whether they slow or stop the parasite enzyme.
Check selectivity
Testing the same compounds against the human enzyme. A blocker that also stops the human version is not useful.
PROGRESS SO FAR
Novel selective inhibitors, already identified. We have already identified some novel selective active inhibitors, and they are currently being refined and optimized.
HOW WE WORK
From a question to a tested candidate
Five stages, in order. Work moves to the next stage only when the evidence supports it.
Question
Start with a clear question about the parasite and the target.
Computational design
Model possible compounds against the target before making them.
Medicinal chemistry and synthesis
Test how the compounds behave against the parasite target.
Biological evaluation
Test how the compounds behave against the parasite target.
Lead optimisation and preclinical development
Improve the strongest candidates and prepare them for preclinical work.
QC worker checking equipment with a batch record
