UCT, Swiss scientists in potential malaria drug breakthrough

[Techne]

http://www.timeslive.co.za/scitech/...ntists-in-potential-malaria-drug-breakthroughhttp://www.timeslive.co.za/scitech/2012/08/28/uct-swiss-scientists-in-potential-malaria-drug-breakthrough

University of Cape Town scientists in collaboration with Swiss-based colleagues are onto a possible breakthrough in the fight against malaria, Science and Technology Minister Naledi Pandor announced on Tuesday.

"I have the pleasure to announce the discovery of a compound which will be the first ever clinical candidate researched on African soil as part of a modern pharmaceutical industry drug discovery programme," she said in a statement.

The recently discovered compound, from the aminopyridine class, not only had the potential to become part of a single-dose cure for all strains of malaria, but might also be able to block transmission of the parasite from person to person, she said.

This followed a research collaboration involving the Medicines for Malaria Venture (MMV), based in Switzerland, and the Drug Discovery and Development Centre (H3-D) at UCT.

On the basis of initial results it had been selected by MMV for further development.

"The candidate molecule is novel, potent, and has the potential to have a significant impact on global malaria control and eradication," Pandor said.

The science and technology department had invested R25 million in this pioneering programme between MMV and UCT.

"This is a powerful demonstration of how much can be accomplished when open minded researchers come together for the sake of the greater good of humanity.

"The discovery that we announce today is a significant victory in the battle to alleviate the burden of disease in Africa.

"Clearly the war on disease is not yet won, but I am excited by the role that our excellent scientists have played in finding a potential single-dose cure for malaria and possibly preventing its transmission."

South Africa in general had built considerable strength in clinical research over the past decade. The main focus had been on HIV/Aids and TB.

This development had occurred together with significant growth in the basic sciences that underpinned infectious disease research (immunology, virology, microbiology, biochemistry, and genetics), Pandor said.

Quite big news:
http://www.sanews.gov.za/news/12/12082814151001

 

[empirex]

Wow, amazing.

Would love to know how the drug works.

 

[Techne]

I think this is the peer-reviewed article:
3,5-Diaryl-2-aminopyridines as a Novel Class of Orally Active Antimalarials Demonstrating Single Dose Cure in Mice and Clinical Candidate Potential

The compounds:

A novel class of orally active antimalarial 3,5-diaryl-2-aminopyridines has been identified from phenotypic whole cell high-throughput screening of a commercially available SoftFocus kinase library. The compounds were evaluated in vitro for their antiplasmodial activity against K1 (chloroquine and drug-resistant strain) and NF54 (chloroquine-susceptible strain) as well as for their cytotoxicity. Synthesis and structure–activity studies identified a number of promising compounds with selective antiplasmodial activity. One of these frontrunner compounds, 15, was equipotent across the two strains (K1 = 25.0 nM, NF54 = 28.0 nM) and superior to chloroquine in the K1 strain (chloroquine IC50 K1 = 194.0 nM). Compound 15 completely cured Plasmodium berghei-infected mice with a single oral dose of 30 mg/kg. Dose–response studies generated ED50 and ED90 values of 0.83 and 1.74 mg/kg for 15 in the standard four-dose Peters test. Pharmacokinetic studies in the rat indicated that this compound has good oral bioavailability (51% at 20 mg/kg) and a reasonable half-life (t1/2 7–8 h).

It was discovered after high throughput screening of a library of compounds and then optimization through synthesis of various analogues. It does not appear that they know exactly which protein it interacts with, which is interesting, as once they discover it, there may be chance for even more optimization. They know it cures mice of malaria and these compounds do not appear to have much side-effects.

Good stuff .

 

[empirex]

I think this is the peer-reviewed article:
3,5-Diaryl-2-aminopyridines as a Novel Class of Orally Active Antimalarials Demonstrating Single Dose Cure in Mice and Clinical Candidate Potential

The compounds:

It was discovered after high throughput screening of a library of compounds and then optimization through synthesis of various analogues. It does not appear that they know exactly which protein it interacts with, which is interesting, as once they discover it, there may be chance for even more optimization. They know it cures mice of malaria and these compounds do not appear to have much side-effects.

Good stuff .

Wow ok. Well keep us updated with news, be fascinating to know just how it knocks those little buggers on their ass

 

[RiaX]

:wtf: I didnt even know this was going on LOL. Epic stuff