

Glucokinase Receptor Activator
GKM-001 for Diabetes Mellitus
Impetis was among the pioneers in GKA research and has developed a highly differentiated and best-in-class activator of the target that holds the promise of providing long-term glucose control in patients of Type 2 Diabetes without several attendant adverse effects including Hypoglycemia. The program is ready for a human PoC and large scale clinical trials.

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Impetis' Glucokinase Receptor Activator includes the following
Robust and sustained efficacy
Demonstrated glucose Lowering without hypoglycemia in normal and Type II Diabetes Mellitus (T2DM) subjects in single ascending dose study and in T2DM in a 14 day multiple ascending dose (MAD) study despite an apparent 21 hours half life – early but strong evidence of proof of concept in humans GKM-001 is a novel Glucokinase activator (GKA) with a liver selective MoA -Robust fasting and post-prandial glucose lowering achieved without hypoglycemia validating pre-clinical efficacy and safety data – right balance of potency, liver selectivity and PK providing efficacy without hypoglycemia associated with pan GK activators Superior Safety profile -Unlike pan active GKAs, GKM-001 appears to have no effect on insulin secretion as evident from in vitro studies and the lack of increase in C-peptide in T2DM patients -In the MAD study in T2DM patients, no clinically relevant adverse events, changes in vital signs (including blood pressure) and changes in laboratory values were observed including liver enzymes & lipids – triglycerides, cholesterol and non-esterified fatty acids Ready for long term clinical trial -90-day safety studies successfully completed to initiate additional clinical studies including a 12-week Phase IIb (effect on HbA1c) study Clear IP position -US, EP Composition of Matter patent granted (US 8501955)