Putting DMPK Where It Matters Most: Enabling Exposure-Driven Lead Selection

About this poster

Drug metabolism and pharmacokinetics (DMPK) often enter drug discovery too late, allowing potent compounds with poor exposure to advance and fail in later stages. This poster presents IRBM’s exposure-driven DMPK framework, which integrates early in vitro profiling and in vivo pharmacokinetics into a structured, multiparametric decision process that weighs unbound exposure and developability criteria alongside potency. Applied to a small-molecule SHP2 inhibitor program, the approach supported the assessment of CNS potential and guided optimization toward a CNS-active candidate with efficacy in an orthotopic glioblastoma model. Download the poster to explore the decision framework and in vivo characterization in detail.