Bentiromide is not available in the United States or Canada; it was withdrawn in the US in October 1996.

[2] Headache and gastrointestinal disturbances have been reported in patients taking bentiromide.

It is broken down by the pancreatic enzyme chymotrypsin, yielding p-aminobenzoic acid (PABA).

The amount of PABA and its metabolites excreted in the urine is taken as a measure of the chymotrypsin-secreting activity of the pancreas.

The resulting L-amide is selectively hydrolyzed by sequential use of dimsyl sodium (NaDMSO) and dilute acid to give bentiromide (4).