Formulation and Quality – Biomolecular
2019 PharmSci 360
Oral dosing of biologics is one of the major challenges in biopharmaceutical development, there are major hurdles that need to be dealt with. In this presentation the results of 3 preclinical studies with a new oral delivery approach will be demonstrated that overcomes these hurdles.
The delivery technology has been extensively tested in CMC, in in-vitro experiments and in 3 preclinical studies and the results are very promising for bringing this new formulation to the clinic rapidly for existing therapies that use SC or IV dosing, and may serve as an alternative formulation for future NBE developments
The formulation utilizes existing manufacturing technologies and various GRAS excipients to obtain formulated monoclonal antibodies that are delivered to the GI tract in a capsule and subsequently taken up into circulation for systemic availability.
Omalizumab was the first Mab that was tested with this technology, formulations of which were tested in 3 preclinical studies with multiple dosing levels, and comparison with SC dosing. The studies provided outstanding PK results for the oral formulation, with linear pharmacokinetics and high bioavailability. It was also demonstrated that omalizumab as a molecule remained intact and functional regardless the administration route, demonstrating the absence of a potential first-pass effect.