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The Story of Zetia

Harry R. Davis, Jr., Ph.D.
Margaret van Heek, Ph.D.
Kevin B. Alton

The 2006 Discoverer’s Award, the highest scientific honor in the pharmaceutical industry, goes to Harry R. Davis, Jr., Ph.D., Margaret van Heek, Ph.D. and Kevin B. Alton, for their discovery of Zetia®. This drug represents the first breakthrough in cholesterol treatment since the discovery of statins over twenty years ago and is a major advancement in the treatment of cardiovascular disease.


The discovery of Zetia happened almost by chance. Davis had been working with his team on treating cholesterol by inhibiting an enzyme believed to play a role in absorbing cholesterol. While the drug did not block the intended enzyme, the surprising result was that it did still lower cholesterol in animals.

Meanwhile, van Heek was examining the effect of the same compound on cholesterol absorption in rats and had made some important discoveries about the impact of the rats’ bile on the compound. In a chance hallway meeting, van Heek discussed these findings with Alton, another scientist who was doing work with that compound. Working together, they discovered how an interaction with a component in the rat bile was making their compound more effective. Using this knowledge, they uncovered another drug that was 400 times more potent; this would come to be known as Zetia.

Davis then made a vital contribution to the work of van Heek and Alton with the discovery that this new drug could be used in combination with existing statins, resulting in a stronger effect than if either treatment was used separately. With the convergence of the research of these three scientists, a major scientific breakthrough was born. As a cholesterol absorption blocker, Zetia is very successful at lowering cholesterol levels on its own, but when used in combination with statins, which inhibit cholesterol production, the results are nothing short of extraordinary.

Zetia is significant in its ability achieve a reduction in cholesterol levels previously unheard of in the medical community. In particular, studies have shown that 72% of patients who were unable to get their cholesterol under control on statins alone achieved their goal when Zetia was added to their treatment regime. On its own, Zetia also offers an alternative to statins that has few side effects. In addition to many saved lives, the development of Zetia was a critical step for scientists to finally understand the process through which cells absorb cholesterol, laying the groundwork for future discoveries in the field. Through a combination of individual discoveries and collaborative efforts, persistence and intuition, Davis, van Heek, and Alton made a major contribution to the lives of millions of patients.