Small Molecule Polymer Conjugates

This platform allows for the fine-tuning of the physicochemical properties of small molecule oral drugs to increase their therapeutic benefit. In addition, the approach can enable oral administration of parenterally-delivered small molecule drugs that have shown low bioavailability when delivered orally.

Benefits of this approach are: improved potency, increased oral bioavailability, modified biodistribution with enhanced pharmacodynamics, and reduced transport across specific membrane barriers in the body, such as the blood-brain barrier.

Through advanced medicinal chemistry, a polymer is conjugated to a small molecule drug via a stable linkage. The linkage is considered stable because it remains intact the entire time the drug is in vivo. The new orally-administered drug can pass through certain cell membranes, such as the gut epithelial layer, to act on a target receptor on the cell surface. Depending upon the type of polymer used, the drug can also be designed to have reduced transport across other specific barriers within the body, such as the blood-brain barrier in the CNS. In other cases, the drug can be engineered to cross cell membranes to reach an intracellular target. With various conjugation techniques, the drug could potentially show increased binding affinity with intracellular or extracellular targets.

Pro-Drug Conjugates »

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