Natural products in modern drug discovery

Natural products (NPs) remain one of the most effective sources of therapeutic innovation, delivering unmatched chemical diversity and biological relevance. As novel technologies reveal previously inaccessible bioactive space, their role in the development of next‑generation therapies has become more significant than ever.

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The relevance of natural products today

NPs continue to yield first-in-class and best-in-class therapeutics, driving innovation across anti-infectives, oncology, and various other disease areas.

A recent audit of global approvals from 2014 to 2024 showed that 56 out of 579 drugs (9.7%) were NP or NP-derived. This comprises 44 NP and NP-derived NCEs and 12 NP-linked antibody-drug conjugates (ADCs) with an average of approximately five NP/NP-derived approvals annually.

As of December 2024, 125 NP and NP-derived compounds were reported in clinical trials or registration, reflecting a durable and active pipeline.¹

Complementary evaluations demonstrate higher progression rates for NP/NP-derived agents from Phase I to III relative to purely synthetic comparators, as well as lower predicted toxicity burdens. This context supports continued strategic focus on NP-derived therapeutics.²

NPs cover a wide variety of chemical entities originating from various biological sources, such as microorganisms (including actinomycetes, myxobacteria, and filamentous fungi), higher plants and botanicals, animals, and, in some cases, marine invertebrates and algae.

Among the primary structural classes of these NPs are peptides, polyketides, glycosides, terpenoids, phenolics, and alkaloids.³ These compounds are commonly used as either direct therapeutic agents or as scaffolds for semi-synthetic derivatives.

Historically, NPs have played significant roles in important pharmacological breakthroughs. Notable examples include morphine from Papaver somniferum and quinine from Cinchona bark, which have transformed pain management and anti-malarial treatment, respectively.⁴

Beyond these well-known molecules, NPs and their derivatives remain central for today’s drug pipelines, with substantial contributions to approved therapeutics and clinical-stage candidates across oncology, anti-infectives, and numerous other therapeutic fields.

This lasting impact reflects their unmatched structural diversity, stereochemical complexity, and ability to engage difficult biological targets, characteristics that synthetic libraries frequently struggle to replicate.

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Acknowledgments

Produced from materials originally authored by Jens Glaeser, PhD, Principal Scientist, Hit ID & Biophysics, Evotec.

References and further reading

1. Butler, M.S., et al. (2025). Natural product-derived compounds in clinical trials and drug approvals. Natural Product Reports. DOI:10.1039/d5np00031a. https://pubs.rsc.org/np/article-abstract/43/1/20/1249025/Natural-product-derived-compounds-in-clinical.
2. Domingo-Fernández, D., et al. (2024). Natural Products Have Increased Rates of Clinical Trial Success throughout the Drug Development Process. Journal of Natural Products, 87(7), pp.1844–1851. DOI:10.1021/acs.jnatprod.4c00581. https://pmc.ncbi.nlm.nih.gov/articles/PMC11287737/.
3. Walsh CT and Tang Y., (2022). Natural Product Biosynthesis, Chapter 1: Major Classes of Natural Product Scaffolds and Enzymatic Biosynthetic Machinery. The Royal Society of Chemistry eBooks, pp.1–21. DOI:10.1039/bk9781839165641-00001. https://books.rsc.org/books/monograph/2042/chapter/4662116/Major-Classes-of-Natural-Product-Scaffolds-and.
4. Dias, D.A., Urban, S. and Roessner, U. (2012). A Historical Overview of Natural Products in Drug Discovery. Metabolites, 2(2), pp.303–336. DOI:10.3390/metabo2020303. https://www.mdpi.com/2218-1989/2/2/303.

About Evotec

Evotec is a life science company that is pioneering the future of drug discovery and development. By integrating breakthrough science with AI-driven innovation and advanced technologies, we accelerate the journey from concept to cure – faster, smarter, and with greater precision. Our expertise spans small molecules, biologics, cell therapies and associated modalities, supported by proprietary platforms such as Molecular Patient Databases, PanOmics and iPSC-based disease modeling.

With flexible partnering models tailored to our customers’ needs, we work with all Top 20 Pharma companies, over 800 biotechs, academic institutions, and healthcare stakeholders. Our offerings range from standalone services to fully integrated R&D programs and long-term strategic partnerships, combining scientific excellence with operational agility.

Through Just – Evotec Biologics, we redefine biologics development and manufacturing to improve accessibility and affordability. With a strong portfolio of over 100 proprietary R&D assets, most of them being co-owned, we focus on key therapeutic areas including oncology, cardiovascular and metabolic diseases, neurology, and immunology.

Evotec’s global team of more than 4,500 experts operates from sites in Europe and the U.S., offering complementary technologies and services as synergistic centers of excellence. Learn more at www.evotec.com and follow us LinkedIn and X/Twitter @Evotec.

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