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Pharmacokinetics of non-traditional drug classes

We investigate how new therapeutic modalities can be designed to reach their intended targets in the body.

Small molecules (<500 Da) have conventionally been favored in drug development, due to a relatively simpler optimization of their pharmacokinetic properties, and because they are suited for of the types of pharmacological targets that have historically been pursued. However, many interesting target types are difficult to modulate with small molecule ligands, and non-traditional chemotypes are therefore increasingly explored. Prominent examples include macrocyclic molecules, targeted protein degraders (PROTACs), and RNA-based therapeutics, that could bring new regions of the human proteome into reach for drug development.

Currently, clinical progress is hampered by that the molecular properties of these new therapeutic modalities typically are incompatible with oral absorption and intracellular exposure. Using combinations of cell-based in vitro experiments, biophysical measurements and computational modeling, we study how such non-traditional drugs can be designed to cross membrane barriers and reach their sites of action.

Environment-dependent exposure of polar functionalities allows membrane penetration of large non-traditional drug molecules.


Environment-dependent exposure of polar functionalities allows membrane penetration of large non-traditional drug molecules.

Contact information

Pär Matsson
Professor

E-mail: par.matsson@gu.se

Page Manager: Webbredaktör|Last update: 12/12/2019
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