Ion channels (Kv1.3, Nav1.7)

With the aim to extend the application of PEM Technology to other target classes, such as ion channels, Polyphor has entered in a collaboration with Milan, Italy-based Axxam. The aim of this collaboration is to access Axxam’s advanced screening technologies in the field.

The voltage-gated potassium channel Kv1.3 has been known for considerable time to play an important role in the pathogenesis of autoimmune diseases like rheumatoid arthritis, multiple sclerosis, type 1 diabetes mellitus and psoriasis. This ion channel is highly expressed in effector memory T-cells in the immune disease and its blockade can alleviate these diseases in animal models. Treating autoimmune diseases with an ion channel blocker represents a novel approach, very distinct from the wealth of antibodies being developed or marketed for these indications.

The voltage dependent sodium channel Nav1.7 is expressed only in afferent neurons signaling pain. When mutations occur in humans which result in a non-functional channel, these patients show reduced pain sensitivity. This makes Nav1.7 a very attractive, pain specific drug target. Attempts to identify blockers have been hampered so far by the lack of ion channel selectivity.

In the collaboration with Axxam, several novel PEM ion channels blockers have been identified. This illustrates the high potential of PEM Technology to be applied on many different target classes, which are difficult to address by the small molecule approach. Polyphor is seeking partners for these ion channel blocker programs, which are at the hit to lead stage.