Kv1.3 Blockers for Inflammatory Disorders
Bionomics is developing a new generation of treatments for inflammatory disorders, based upon blockers of the Kv1.3 potassium ion channel. Such compounds may prove useful to treat a wide variety of illnesses including Multiple Sclerosis, Rheumatoid Arthritis and Psoriasis. Bionomics is focusing on Multiple Sclerosis as an initial indication.
Kv1.3 is a key regulator of the effector-memory T-Cells of the immune system that are key mediators of inflammatory diseases. Kv1.3 is expressed in a limited range of tissues, lowering the likelihood of side-effects. Bionomics has identified what it believes to be the most promising inhibitors of Kv1.3 of any program in the world.
Key Competitive Advantages of Bionomics' Kv1.3 Blockers
- Excellent Potency. Some Bionomics Kv1.3 blockers have potency as low 5nM.
- Outstanding Specificity for Kv1.3 Over Other ion Channels. Bionomics compounds have approximately 25-fold or greater selectivity for related ion channels such as Kv1.1 or Kv1.5. All compounds evaluated to-date have at least 100-fold selectivity over the hERG channel, indicating that the risk of key toxicities is low.
- Proven Efficacy in Animal Models. Bionomics Kv1.3 blockers have been found efficacious in key models of inflammatory disorders such as Delayed Type Hypersensitivity DTH and Experimental Autoimmune Encephalomyelitis (EAE). and very drug-like characteristics.
- Low Risk of Drug-drug Interactions. Bionomics compounds cause minimal inhibition of Cyp450 enzymes, which are key mediators of drug metabolism. This low Cyp inhibition makes it unlikely that these compounds will have adverse effects upon the metabolism of other drugs, which is important as patients suffering from inflammatory disorders often require treatment with multiple medications.
- Oral Bioavailability. Bionomics clinical candidate will be suitable for treatment as a capsule or tablet. This is an important competitive advantage, as many leading treatments for inflammatory disorders (including all existing treatments for Multiple Sclerosis) are administered as injections.
