Workshop B: Enhancing Oral Bioavailability of Bivalent Degraders to Improve Patient Exposure & Maximise Therapeutic Efficacy
Time: 1:00 pm - 3:00 pm
day: Workshop B
Details:
The development of PROTACs and other heterobifunctionals holds immense promise for targeted therapies. However, their large molecular size presents significant challenges in achieving oral bioavailability. Traditional methods for ensuring bioavailability, such as the rule of five, do not apply to these larger bifunctional molecules. This workshop will delve into the complexities of making PROTACs orally bioavailable, exploring the current hurdles and innovative strategies to overcome them.
- Learn about the specific difficulties in achieving oral bioavailability for large bifunctional molecules like PROTACs and gain insights into optimising these properties for better absorption
- Discover high-throughput methods and the potential of leveraging extracellular receptors to enhance oral bioavailability, ensuring a more consistent and effective approach
- Gain practical knowledge on optimising current in vitro assays and models to predict the solubility and permeability of your drugs to achieve the desired exposure in patients
