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They offer a diverse chemical space that bridges the gap between small molecules and larger biologics, often exhibiting high potency, selectivity, and improved pharmacokinetic properties. The constrained and often rigid structures of macrocycles provide increased stability and binding affinity to their targets, enabling them to interact with challenging protein-protein interfaces or unconventional binding sites that traditional small molecules might struggle to access. Moreover, their larger size allows for more specific interactions with biological targets, reducing off-target effects.
Despite the success of macrocycles in modulating challenging drug targets across various therapeutic areas, their significant potential as valuable candidates in drug discovery and development pipelines remains relatively untapped, mostly because of synthetic challenges. Macrocycles are more complex than the average small molecule developed in pharma and are often seen as more challenging to start a medicinal program with due to the long synthetic sequences required to synthesize them. This usually translates into a reduced frequency of design, make, test (DMT) cycles and more demand on the synthetic chemistry resources of the project.
Macrocycles offer a diverse chemical space that bridges the gap between small molecules and larger biologics, often exhibiting high potency, selectivity, and improved stability.
Our robust technology platform allows us to greatly alleviate this concern and to produce the first iterations of DMT optimization in just a few weeks per cycle. With our recent acquisition of Cyclenium Pharma in Montreal, we are combining our synthetic excellence and their proprietary CMRT (Customized Macrocycles for Recognition of Topologies) technology for the creation of diverse libraries of macrocyclic compounds.
We also leverage our existing unique library of over 8,000 ready-to-screen macrocycles (SpiroQUEST library) to generate advanced starting points for medicinal chemistry endeavors.
By integrating our macrocycle capabilities with innovative analytical tools, we provide a comprehensive approach that accelerates the development of novel therapeutics. Our platform's flexibility allows us to tailor macrocycles to specific targets, ensuring high efficacy and selectivity. This approach enhances the success of drug discovery programs, pushing the boundaries of what can be achieved in drug discovery.
Our macrocycle services include:
By leveraging our deep knowledge and state-of-the-art facilities, SpiroChem provides innovative solutions that address the most complex challenges in drug discovery. Our commitment to excellence ensures that our clients receive the highest quality support, accelerating their research and development processes.
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