Agouron Protease Inhibitor AG1343: Activity Reported



Early results from a handful of patients, reported at the
Santa Fe meeting of the International Society of Antiviral
Research, show that the protease inhibitor AG1343, being
developed by Agouron Pharmaceuticals of La Jolla, California,
does have biological activity against HIV in people. This
finding is important because another protease inhibitor,
produced by Searle, was recently abandoned after it was found
to have no antiviral activity in people despite good activity
in the laboratory. It is believed that the problem with the
Searle drug is that it bound to a protein in the blood.
Agouron presented the new data earlier than usual in Santa Fe,
in order to show that AG1343 does not have the same problem.

Agouron reported that 300 mg of AG1343 have been given three
times a day to eight patients, for periods ranging from three
to 28 days. No clinically significant adverse events, nor
adverse laboratory changes, have been seen; but clear evidence
of anti-HIV activity has been found in some patients. One had
a reduction of HIV in the blood by more than 99 percent, and
an increase in CD4 count of 116. Viral load results for the
others are not yet available.

Agouron specializes in the rational design of small-molecule
drugs based upon molecular structures of proteins.