Beginning with the End in Mind: Risk Based Approach for Oral First in Human Formulation Development

“Fit-for-purpose” formulations such as solutions, suspensions, or powder in capsule dosage forms are frequently preferred to accelerate the initiation of first in human studies. However, these formulations often fail to illustrate oral bioavailability limitations and can significantly impact late-stage development.
Early evaluation of physico-chemical properties, preclinical PK, and biopharm modeling are crucial to identify oral absorption limitations and drive formulation technology selection.
Using a systematic risk-based approach, an optimized and well-characterized oral solid dosage form can be introduced in the early clinical studies while still balancing material requirements and timelines.