AntriaBio’s lead diabetes product candidate, AB101, is a once-a-week injectable basal insulin that is currently in preclinical development. AB101 is to be administered by subcutaneous injection and is intended for use in patients with Type 1 and Type 2 diabetes who require basal insulin for the control of hyperglycemia.
The formulation has been designed to release human insulin slowly and uniformly over a period of approximately one week without an adverse initial burst of insulin. The release profile results in a sustained and near peak-less insulin level over the intended treatment period, which supplements the effects of endogenous and exogenous insulin and complements the effects of orally administered hypoglycemic agents. AB101 has the potential to be a clearly differentiated product which would represent a significant advance in basal insulin therapy.
Unlike existing basal insulin replacement therapies which use synthetic insulin analogues, AB101 is formulated from human recombinant insulin. The extended duration of action is the result of the PEGylation (PEG) of human insulin which is then encapsulated into poly-lactic, poly-glycolic (PLGA) microspheres. Typically, PEGylated biomolecules use large molecular weight PEG chains to decrease clearance and therefore reduce injection frequency. However, in our patented formulation we use a very small molecular weight PEG for AB101 to modify the solubility of insulin, permitting encapsulation of the drug into a biodegradable polymer which determines the extended release profile.
After injection, the PEGylated insulin is slowly released at the injection site as the polymer microspheres are broken down by simple hydrolysis. As a result of our unique formulation capabilities, AB101 extends the duration of action of human insulin without the use of any new excipients. Regulatory authorities have already approved numerous products using PEG or biodegradable polymers such as PLGA.
In addition to the proprietary technology for PEGylation of insulin and incorporation of the PEGylated insulin, we use a proprietary microparticle manufacturing technology which ensures production of a very tight particle size distribution with uniformly small microparticles. Our efficient manufacturing capability allows us to maintain high yields as well as to facilitate patient comfort by producing microspheres that can be injected through 25 gauge or smaller needles.