KIT develops nanodroplet chip to accelerate drug discovery with integrated synthesis, testing, and analysis

KIT develops nanodroplet chip to accelerate drug discovery with integrated synthesis, testing, and analysis

(IN BRIEF) Researchers at the Karlsruhe Institute of Technology (KIT) have created a nanodroplet-based chip platform that combines drug synthesis, biological testing, and chemical analysis in a single workflow. Each droplet measures only 200 nanoliters and contains 300 cells, enabling up to 1,000 experiments per chip. This approach cuts the cost and time of early drug discovery, which normally requires years and hundreds of millions of euros. In proof-of-concept tests, the team synthesized 325 potential MEK inhibitors within a week, identifying 46 compounds as effective as the cancer drug mirdametinib. By integrating advanced analysis tools such as MALDI-MSI and cell-based assays, the platform offers a faster and more resource-efficient path for academic labs and smaller biotech firms to participate in therapeutic development.

(PRESS RELEASE) KARLSRUHE, 22-Aug-2025 — /EuropaWire/ — The Karlsruhe Institute of Technology (KIT) has unveiled a groundbreaking miniaturized platform that integrates the synthesis, testing, and analysis of drug candidates onto a single chip, drastically reducing both costs and development time. The system operates with nanodroplets measuring only 200 nanoliters—roughly the size of a grain of sand—containing just 300 cells per test. This innovative approach enables thousands of experiments to be carried out on one chip and could redefine how cancer drugs and other therapies are discovered. The findings were published in Angewandte Chemie (DOI: 10.1002/anie.202507586).

Traditionally, drug discovery involves a sequence of costly and time-consuming steps for synthesizing, characterizing, and biologically testing new compounds. These processes demand extensive resources, often placing them beyond the reach of universities and smaller biotech firms. “In particular, academic and smaller industrial research institutions are not able to mobilize these resources,” explains Professor Pavel Levkin from KIT’s Institute of Biological and Chemical Systems (IBCS). “Our technology removes this barrier and could open the door for many more players to contribute to drug discovery.”

The new nanodroplet array platform developed by Levkin’s team in the Department of Biofunctional Materials reduces experimental scale by a factor of 1,000, moving from microliter to nanoliter volumes. Using this “direct-to-biology” workflow, researchers can test drug candidates immediately without lengthy preparation, allowing synthesis and biological assays to be performed in parallel.

To demonstrate the platform’s potential, the team focused on MEK inhibitors—compounds that target an enzyme implicated in cancers such as skin and colon cancer. Building on the molecular structure of mirdametinib, an established MEK inhibitor used in the treatment of rare tumors, they synthesized a library of 325 new candidates within seven days. Laboratory tests revealed that 46 of these worked as effectively as mirdametinib itself.

“By shrinking our tests to nanodroplet scale, we can produce and screen hundreds of candidate drugs in a fraction of the time and with far fewer resources,” said Levkin.

Doctoral researcher Liana Bauer, lead author of the study, noted that the experiments included cell-based assays using the colon cancer cell line HT-29, which is particularly sensitive to MEK inhibitors. For chemical characterization, the researchers collaborated with Professor Carsten Hopf’s team at TH Mannheim’s CeMOS center, using matrix-assisted laser desorption/ionization mass spectrometry imaging (MALDI-MSI) to analyze and visualize the molecular structures directly on the chip. In total, the group tested 975 samples in triplicate, confirming that the nanodroplet method remains reliable at extremely small scales.

By bringing together synthesis, testing, and analysis in one integrated system, the KIT platform offers a powerful tool for high-throughput drug discovery that is significantly faster, cheaper, and more accessible. It may allow smaller labs and startups to participate in early-stage drug research, ultimately speeding up the discovery of urgently needed treatments. “This is a big step toward faster, cheaper, and more efficient discovery of urgently needed new drugs,” Levkin emphasized.

Media Contacts:

Christian Könemann
Chief Press Officer
Phone: +49 721 608-41190
Fax: +49 721 608-43658
christian koenemann∂kit edu

Sandra Wiebe
Press Officer
Phone: +49 721 608-41172
sandra wiebe∂kit edu</a

SOURCE: Karlsruhe Institute of Technology (KIT)