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Precision Oncology Comes of Age: Designing Best-in-Class Small Molecules by Integrating Two Decades of Advances in
Darrin D Stuart1, Angel Guzman-Perez1, Natasja Brooijmans1
1Scorpion Therapeutics, Boston, Massachusetts.
Abstract:
Small-molecule drugs have enabled the practice of precision oncology for genetically defined patient populations since the first approval of imatinib in 2001. Scientific and technology advances over this 20-year period have driven the evolution of cancer biology, medicinal chemistry, and data science. Collectively, these advances provide tools to more consistently design best-in-class small-molecule drugs against known, previously undruggable, and novel cancer targets. The integration of these tools and their customization in the hands of skilled drug hunters will be necessary to enable the discovery of transformational therapies for patients across a wider spectrum of cancers.
Significance:
Target-centric small-molecule drug discovery necessitates the consideration of multiple approaches to identify chemical matter that can be optimized into drug candidates. To do this successfully and consistently, drug hunters require a comprehensive toolbox to avoid following the "law of instrument" or Maslow's hammer concept where only one tool is applied regardless of the requirements of the task. Combining our ever-increasing understanding of cancer and cancer targets with the technological advances in drug discovery described below will accelerate the next generation of small-molecule drugs in oncology.
Insights
Advances in cancer research and technology are enabling the design of targeted small-molecule drugs for more patients. Skilled drug hunters integrating these tools can accelerate the discovery of new cancer therapies.
Area of Science:
- Oncology
- Medicinal Chemistry
- Data Science
Background:
- Precision oncology has advanced significantly since 2001, driven by small-molecule drugs targeting specific genetic mutations.
- Over two decades, scientific and technological progress has transformed cancer biology, drug design, and data analysis.
Purpose of the Study:
- To highlight the evolution of small-molecule drug discovery in oncology.
- To emphasize the necessity of integrating diverse tools and knowledge for future cancer therapies.
Main Methods:
- Review of scientific and technological advances in cancer biology, medicinal chemistry, and data science.
- Discussion of target-centric drug discovery approaches and the importance of a comprehensive "toolbox" for drug hunters.
Main Results:
- Current advances allow for more consistent design of best-in-class small-molecule drugs against various cancer targets.
- Integration of advanced tools and knowledge is crucial for developing next-generation oncology drugs.
Conclusions:
- The convergence of understanding cancer biology and technological progress is key to accelerating small-molecule drug discovery.
- Skilled drug hunters leveraging integrated tools can enable transformative cancer therapies for a broader patient population.
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