Amakem’s ‘Localized Drug Action’ platform is designed to generate novel kinase inhibitor drugs which are contained locally and thus reduce or eliminate side effects. Kinases are crucial mediators of important disease pathways representing more than 22% of the drugable genome. However, kinases are present throughout the body and so there is a significant risk of toxicity due to on target effects in non-target organs and tissues if there is systemic exposure. This risk is acceptable in oncology indications, but not in others thus substantially reducing the potential of drugs targeting this class.

Amakem’s kinase inhibitors are designed to be rapidly inactivated outside the target organ. In indications that can be treated by topical administration, it is therefore possible to contain the drug locally as it becomes inactive before it can reach other organs or tissues if it leaks out of the target organ.

Localized Drug Action  is based on the inactivation of kinase inhibitors outside the target organ, e.g. in the bloodstream by specifically targeted enzymes. Each of Amakem’s kinase inhibitors brings together kinase specificity and enzymatic conversion specificity. When the drug candidate leaves the target organ it is converted to a functionally inactive metabolite. This inactive metabolite is then eliminated from the body.

The ‘Localized Drug Action’ platform can be applied to a wide range of kinase inhibitors in indications where local administration is viable: eye, skin, GI tract, ears and via local injections. Amakem has demonstrated proof-of-concept in glaucoma, where AMA0076 is the Company’s clinical candidate, and also in models of Chronic Obstructive Pulmonary Disease (COPD) and asthma where AMA0247 is an advanced lead compound.