We put innovative chemistry to work for a California startup, helping them streamline their antibody-drug conjugate (ADC) development process. This involved creating unique linker molecules custom-designed for their specific needs. By doing this, we accelerated their identification of promising lead compounds, significantly impacting their development timeline.

Identifying the issue

Finding the right linker molecule for a new ADC can be challenging. Testing different options to identify suitable linker molecules is time-consuming and expensive. Moreover, many existing linkers may be covered by intellectual property restrictions, hindering progress.

Methodology insight

Here is how Sigut Labs put its hands to work:

1. Design and synthesis of novel linkers: We began by designing and synthesizing linker molecules specifically for the client’s ADC. These linkers were unique and not covered by existing patents, providing the client with greater freedom in their development process.
2. Initial screening: Many linkers we produced were conjugated to the antibody and the activity and toxicity of the resulting ADCs were screened. This initial testing phase allowed us to quickly evaluate linker performance before proceeding to more complex stages.
3. Medicinal chemistry optimization: Based on the results of the first screening, we employed medicinal chemistry techniques to refine the linker structure. We considered biological activity and toxicity data to optimize the linker for both efficacy and safety. Screening and optimization processes were iterated until the best candidates were selected.
4. Lead compound and backup development: We synthesized a sufficient quantity of the novel linker molecules following optimization. This enabled the client to develop their lead ADC candidate efficiently and backup leads for further testing.
5. Technology transfer and verification: Once the optimal linker was identified, we transferred the manufacturing knowledge and procedures to a Contract Development and Manufacturing Organization (CDMO) for large-scale cGMP production. We closely monitored and followed CDMO throughout the process to ensure a quick successful outcome.
6. Quality control: Finally, we rigorously analyzed all compounds produced by the CDMO to verify their quality and purity, ensuring the client received compounds suitable for further development.

Positive outcome

Thanks to our innovative approach, the client’s ADC development journey got a significant boost. Designing novel linkers specifically tailored to their needs not only saved valuable time but also provided greater flexibility compared to using existing, potentially patented, linker technologies. This case study exemplifies the power of our chemistry expertise in facilitating the efficient and successful development of ADCs.