History

1992
Compound Found

As a result of the dog trials, the team of Merck scientists had learned some valuable lessons. The medicinal chemists in West Point PA continued to tinker with compounds, adding and removing molecules to try and fine-tune the attack on HIV while avoiding the toxicity problems of their prior effort. In the meantime, process researchers in Rahway NJ worked to overcome the challenges of synthesizing protease inhibitors. After going through some 3,000 compounds, the team finally developed the compound L-735,524 in January 1992; this would come to be known as CRIXIVAN.

The biggest problem now was manufacturing enough of the drug for use in a human trial. The protease inhibitors, and CRIXIVAN in particular, had proven to be difficult and time-consuming to make. Merck began production in its research factory in Rahway. After receiving the first sample of CRIXIVAN from the medicinal chemists at Merck’s West Point research labs, it took 6 months for Merck’s process chemists in Rahway to produce 600 grams of CRIXIVAN for a 12-day safety trial in 12 volunteers not infected with HIV. The trial was to start in February 1993.