The first example in literature of a termination of an oral drug based on IV microdose data

What is it about?

This is an example of the application of microdosing in circumstances where pre-clinical data are not sufficient to provide accurate information to guide first-in-human (FIH) study design (in this case, conflicting PK data from 3 species: mouse, rat, and dog), thus limiting the value of traditional development and enhancing a unique advantage of microdosing . The drug was not administered orally because it is a known P-glycoprotein (P-gp) substrate, therefore exposing it to potential non-linear absorption from the GI tract. The half-life (17 hrs) was determined insufficient for the desired clinical management leading to termination of development.

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Why is it important?

As far as I am aware this is the first example in the literature of a termination of an oral drug based on IV microdose data.

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