February 15, 2024
November 9, 2023
Best Practices for Enhancing Selectivity in TPD Drug Optimization
This workshop focused on understanding how degrader inhibition influences selectivity, guiding participants in prioritizing key selectivity attributes, and determining effective monitoring methods. Additionally, the workshop played a pivotal role in fostering an industry consensus on acceptable selectivity parameters essential for the clinical development of TPD drugs.
August 10, 2023
Optimizing in vivo profiling for TPD drugs and predicting first dose in humans.
In the Searchlight Targeted Protein Development Workshop on 'Optimizing in vivo profiling for TPD drugs and predicting first dose in humans', participants gained insights on preferred dosing routes for sustained efficacy in vivo. They also delved into modeling the first human dose and discussed the differentiation between in vivo profiling of TPD drugs and traditional small molecule drugs. Attendees left equipped with the top 10 parameters for optimizing in vivo chemistry, rooted in industry experience.
May 11, 2023
Lessons Learned from Degraders that are Currently in the Clinic
In a recent TPD Searchlight workshop the network explored clinical insights on degraders currently in clinical trials. We looked at key approaches and considerations through two case studies, addressing critical questions such as predicting clinical responses from pre-clinical data, comparing PROTACs to traditional small molecule drugs, uncovering unexpected effects during the transition from in vitro to in vivo, and identifying common characteristics of compounds in the clinic.
Rational Design of Molecular Glues
E3 Ligase Selection
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