For the treatment inflammatory diseases, SynAct Pharma is researching a number of molecules, specifically with focus on melanocortin agonists, that is compounds that bind to and activate the melanocortin receptors (MCR).
Our proprietary series of phenyl pyrrole aminoguanidine compounds are well protected through our patent portfolio, specifically our lead compound resomelagon (AP1189) with patent protection until 2042.
Resomelagon
Resomelagon is the international nonproprietary name (INN) for the structure of our lead compound, being developed in clinical phase 2b. We have studied this compound intensively over the years and characterized it as a selective agonist for the MC1R and MC3R and as a biased agonist linked to ERK phosphorylation rather the cAMP activation.
It means that resomelagon binds to two specific receptors involved in the immune system’s regulation of inflammation, and that the compound activates one of the two signal pathways each of these receptors would stimulate when the natural endogenous agonists, the melanocyte stimulating hormones (MSH), binds to the receptors.
Activation of MC1R is related to pigmentation of the skin and is in some cases related to melanoma. However, this effect is linked to the c-AMP signal pathway that resomelagon does not activate, and our data has not indicated any such effect of resomelagon.
Resomelagon is also well characterized in our preclinical research, where we have demonstrated activity of the compound in animal models of various inflammatory diseases, and tested that the relevant effective doses are safe, even after prolonged dosing of the compound.
In the clinical Phase 1 trials we have demonstrated exposure of resomelagon and that the compound was well tolerated after dosing our immediate release tablet to healthy volunteers. Resomelagon is currently tested in clinical phase 2b.
The clinical research is being underpinned by our ongoing preclinical research and collaborations, including the RESOVIR collaboration, that has opened up to have a parallel development path with host-directed therapy in viral infection.
Concurrently, we are developing the production processes for the tablets used in the clinic, such that production of resomelagon as well as the tablets are scalable to meet the expected future demands. Both for supply in later clinical trials, but also eventually if the compound is successfully commercialized. This requires a control strategy, development of analytical methods, and demonstration of robustness and stability to make sure that the tablets are the same, are safe and effective each time they are dosed to patients.