Better, faster, cheaper drugs

Jeffrey Winkler

Jeffrey Winkler is into “making stuff,” as he put it. “Basically, what I do is develop new chemical reactions,” the professor of chemistry explained, “and then apply that to designing new ways to prepare substances of biological importance.” In other words, Winkler finds new and better ways of synthesizing drugs, including the anticancer drug Taxol and the drug Ritalin, used for treating hyperactive children.

Recently, Winkler won the 2000 Cope Scholar Award, one of chemistry’s highest honors, for his work in synthetic organic chemistry. One of his Cope nominators called Winkler “one of the most imaginative and scholarly of our emerging leaders in synthesis.”

A Chicago native who did undergraduate work at Harvard and graduate studies at Columbia, Winkler said he was always interested in science. As a kid, he recalled, “I burned my hair with the alcohol lamp in my chemistry set.”

The discovery of a new way of making Ritalin by Winkler’s lab made a big splash in the press last year, partly because there are so many children currently on Ritalin. “After the USA Today article came out, I can’t tell you how many private citizens have contacted me in total desperation because of their children being on Ritalin and having serious side effects,” Winkler said. “They’re desperate for a cleaner, more efficient drug.”

Winkler and his researchers worked in collaboration with Professor Hank Kung, in the radiology department, on the project. Led by former graduate student Jeffrey Axten, now at SmithKline Beecham, Winkler’s lab found a faster, cheaper way of producing the drug; in addition, the lab’s formulation is far more potent than previous forms.

“It reduces by half the amount of drug people have to take, and hopefully reduces the side effects,” Winkler said of his lab’s synthesis of Ritalin. “The structural modifications we can now make to the Ritalin molecule we hope will lead to a drug that will be more efficacious.”

The lab’s work also produced Ritalin analogs that seem to be promising cocaine addiction treatments. They apparently prevent the euphoria that comes from taking cocaine — users don’t get high, so the positive reinforcement for drug taking is be lost. (The Ritalin research is still in its early stages and has not undergone human trials.)

Winkler’s research on Taxol started in 1983, before it was known to be an important anticancer therapy (now the largest-selling one on the market). Its structure is unique and working to find an efficient way of preparing it was initially motivated by the intellectual puzzle. Only in 1989 was its medicinal importance made clear, “an added bonus,” Winkler said.

Winkler remarked that he is motivated in his work by both its intellectual discipline and its possible benefits to society. “It’s nice to have an intellectual challenge which has a real potential payoff in terms of helping people and doing something of importance for society,” he said.

Originally published on February 3, 2000