Did you know? · Science & Medicine

Gertrude Elion's allopurinol still treats gout today

Allopurinol, developed in Gertrude Elion's laboratory, blocks the build-up of uric acid and remains a mainstay treatment for gout.

Gertrude Elion
Gertrude Elion · 1918–1999
Person
Gertrude Elion
Lived
1918–1999
Field
Pharmacology
From
American

The story

Gout is caused by uric acid crystals collecting in the joints, producing attacks of intense pain and, over years, joint damage and kidney stones. Uric acid is the end product of the body's breakdown of purines, the very molecules Gertrude Elion had spent her career studying at Burroughs Wellcome.

The route to a gout drug began with cancer. Elion's 6-mercaptopurine, introduced in the early 1950s, was broken down in the body by an enzyme called xanthine oxidase, the same enzyme that produces uric acid. Her group looked for ways to block that enzyme so that 6-mercaptopurine would last longer. One candidate was allopurinol, first synthesised by Roland Robins in 1956, which Wayne Rundles tested in collaboration with Elion's laboratory.

Allopurinol did not improve the response of leukaemia, but it did something else very well: it sharply reduced the body's production of uric acid. The team turned to gout. Instead of simply soothing the pain of an attack, the drug tackled the chemistry that caused the disease, and it proved safe for long-term use. The Nobel Assembly dates the result of this research to 1963, and on 19 August 1966 the US Food and Drug Administration approved allopurinol, sold by Burroughs Wellcome as Zyloprim.

Allopurinol is still one of the most commonly prescribed medicines. In 2023 it was the 45th most commonly prescribed medication in the United States, with more than 14 million prescriptions. It is used to prevent gout attacks and certain kidney stones and to control the rise in uric acid that can occur when cancer patients begin chemotherapy, and it is on the World Health Organization's List of Essential Medicines.

The story shows how Elion's method worked in practice. By understanding exactly which enzymes a drug met in the body, her team could turn an unsuccessful experiment in one disease into a lasting treatment for another.

Why it matters

Millions of people with gout have been spared painful attacks and joint damage by a drug that grew directly out of Elion's purine research.

About Gertrude Elion

Chemist without a doctorate who pioneered rational drug design and created drugs for leukaemia, transplants, gout and herpes, sharing the 1988 Nobel Prize in Physiology or Medicine.

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Gertrude Elion
1918–1999 · Pharmacology
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Another act of tikkun olam. This is part of tikkun olam, the Jewish idea of repairing the world, and every one of us can add to it.

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