Fulfilling the Promise of Natural Products with Technology: Discovering the Next Generation of Small Molecules

December 15, 2020

In twenty years of Big Pharma experience, I have seen both the promise of small-molecule Drug Discovery (helping take four molecules all the way from Lead Discovery through Preclinical Development, Clinical Trials, and Market Approval) and its challenges (most of the projects I’ve worked on failed to make a drug).  

There are good reasons why many Pharmaceutical companies prefer biologics to small Molecules.  But I firmly believe in small molecule drug discovery!  Many targets are not accessible to antibodies, and even when antibodies work, small molecules have tremendous advantages such as lower cost of goods for the manufacturer and the convenience of oral dosing.

“Natural products, especially plant-derived molecules, have huge untapped potential for exciting new small molecule drugs. Many marketed drugs are either molecules first isolated in plants or molecules made by medicinal chemistry programs that began with plant-derived scaffolds.”

But small molecule drug discovery is a slow, expensive, and failure-prone process.  I’ve seen projects fail for many reasons, most of which boil down to one of four main causes:

  1. Failure to translate from laboratory models to humans
  2. The target protein turned out not to be appropriate for therapeutic intervention
  3. Our compounds had serious safety issues
  4. The compound collection we used for High-Throughput Screening did not include molecules that selectively bound our target protein

Natural products, especially plant-derived molecules, have huge untapped potential for exciting new small molecule drugs because:

  1. The chemical diversity of phytochemicals is vastly greater than all the molecules human chemists have ever made
  2. Many plants have been used in humans for centuries, so both safety and translatability are “built-in” to phytochemicals
  3. There is a vast published literature on legacy uses of plants to treat symptoms associated with various diseases,

Many currently marketed drugs are either molecules first isolated in plants or molecules made by medicinal chemistry programs that began with plant-derived scaffolds.

However, many pharmaceutical companies have abandoned Natural Product Drug Discovery because historically it has been a very slow process.  Identifying bioactive molecules from a plant preparation and determining their mechanism of action used to take many years.

“Our platform overcomes the main bottlenecks that have held back Natural Product Drug Discovery.  In 2020, Enveda has made huge progress towards building the platform we envisioned.  We have built proof of concept for our model!”

When our CEO, Viswa, first described his ideas for what would become Enveda in the Summer of 2019 I was tremendously excited because our platform overcomes the main bottlenecks that have held back Natural Product Drug Discovery.  In 2020, Enveda has made huge progress towards building the platform we envisioned.  We have built proof of concept for our model!

What is that model?  We use Natural Language Processing to extract knowledge from the published literature around Medicinal Plants and combine it with the highest resolution biological and chemical map of these plants that has ever been built, thanks to advancements in OMICs technologies. Then, our team of Machine Learning experts generate testable hypotheses around scaffolds that we validate in the lab, and perform Medicinal Chemistry on the most promising compounds to generate novel chemical matter. Thus far, we have generated promising results across a variety of pathologies, and are eager to commence discussions with potential partners to advance our treatments to the clinic.

Our goal: to discover novel molecules and novel mechanisms with high potential to address unmet medical needs.

Written By:

Matt Healy
Matt spent 20+ years as part of drug-discovery teams at BMS and Regeneron. Matt is a Computational Biologist at Enveda.

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