The Role of Natural Product Chemistry in Drug Discovery Revisited

New review: “The Role of Natural Product Chemistry in Drug Discovery: Two Decades of Progress and Perspectives” just published in the Journal of Natural Products. The review is now online and comes with the raw tabulated data in XLS format (see Supporting Information).

More than 20 years ago, I wrote a review “The Role of Natural Product Chemistry in Drug Discovery” based on a talk given at the 43rd 2003 American Society of Pharmacognosy (ASP) meeting in New Brunswick, New Jersey. A great deal has changed since then.

In this new review, Jim La Clair and I identified and analysed 119 natural product–derived (NP-D) drugs, including 16 antibody–drug conjugates (ADCs), that received first global approval between January 2000 and September 2025. We also present six NP-D case studies and examine the representation of NP-D drugs among the top 200 brand-name medicines in 2006, 2015, and 2024.

Overall, we conclude that although NP-D drug sales have declined, agents such as dapagliflozin and empagliflozin demonstrate that blockbuster status remains achievable. While overall growth is modest, NPs continue to represent highly valuable active pharmaceutical ingredients (APIs). Importantly, substantial opportunities remain for drug-focused NP R&D, as many recently validated therapeutic targets are still underexplored for NP-D chemotypes.

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