Case Study

Predicting Effective Drug Formulations Before Phase 1 Clinical Trials: How Roche Used GastroPlus® to Investigate the Impact of Solubility & Permeability on Bioavailability


Roche was developing a drug, R1315, and needed to determine first-in-human (FIH) dosage and a formulation strategy before designing phase 1 clinical trials.

3 factors analyzed
dosage form, food effect & dose strength
2 formulations

“It can therefore be concluded that GastroPlus™ computer simulation in conjunction with a factorial design of the pharmacokinetic animal trials let to a deeper mechanistic understanding which resulted in considerable resource savings.”

Martin Kuenz, Sonja Nick, Neil Parrott, Dieter Rothlisberger

During development of the drug, it was profiled to have low solubility and high permeability. Before selecting a formulation strategy for phase 1 clinical trials, researchers decided to investigate what kind of impact the solubility and permeability would have on the drug’s bioavailability.