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Hypha Discovery
What's New Q3 2023
Focus Feature - Active Metabolites of Ivermectin
It's now been shown that metabolites of ivermectin contribute to its anti-parasitic activity.
Ivermectin is a natural product derived macrocyclic lactone with broad spectrum antiparasitic drug, primarily deployed to combat parasitic worms in veterinary and human medicine. Due to its ability to kill the parasite Plasmodium falciparum that causes malaria, it has emerged as a potentially useful malaria transmission control tool. A recent paper looks at the activity of key metabolites of ivermectin to explain why the mosquito-lethal effect of ivermectin in clinical trials exceeds that predicted from in vitro laboratory experiments.
The three primary human ivermectin metabolites (M1, M3, and M6) investigated each have a mosquito-lethal effect similar to that of the ivermectin parent compound for two primary malaria vectors. This was the first time that the mosquito-lethal effect of ivermectin metabolites on Anopheles survival has been investigated in an in vitro system.
Hypha were asked to make the two metabolites resulting from demethylation of oligosaccharide sugar rings. M1 and M6 were made using microbial biotransformation since these metabolites could not easily be produced by chemical synthesis. Structures were confirmed by NMR spectroscopy.
Highlighted publications
You may have seen some of the papers around biotransformation and metabolism-led design of drugs we've highlighted on our LinkedIn page. We've added those featured so far this year to a page on Hypha's website in one handy location.
Read our latest blogs
Our “Metabolite Tales” blogs are science-focused articles on interesting aspects around metabolism and medicinal chemistry in drug discovery and development.
Metabolism of synthetic macrocycles approved by the FDA
Curious about metabolism of "beyond the Rule of 5" molecules such as macrocycles? In this blog we delve into the metabolism of some de novo-designed macrocyclic drugs approved by the FDA.
Metabolic cleavage of C-F bonds in drug compounds
In this blog we look at motifs and scaffolds of fluorine containing drugs subject to metabolism mediated defluorination, along with some drug design strategies chemist have used to circumvent this.
Other blog articles
Have a look at the blog articles we've published so far here.
Meet us
We'll be exhibiting at a number of events over the next couple of months, including the 25th North American ISSX meeting in Boston, the SCI/RSC Medicinal Chemistry symposium in Cambridge UK, with KRCC at the 44th KSNS Workshop in South Korea, and with BioBridge at the 2023 ICCP/JSSX Conference in Japan.
Stay tuned
If you're interested in keeping up with what's happening at Hypha Discovery, our blogs and paper picks, follow us on LinkedIn for regular updates.
