The staff at Macrocyclics has an international reputation in the field of medical chelation chemistry. Areas of expertise include the design of bifunctional ligands for radiopharmaceutical applications, magnetic resonance imaging contrast agents, and optical imaging probes based on metal chelates. We have hands on experience with the key challenges involved with early stage drug development projects and understand the necessity of integrating a sound quality system from the start.

Areas of Consulting:

• Choosing the appropriate chelating agent for specific applications – Not all ligands are created equally and deciding upon the best one to satisfy your objectives is not always an easy process. There are many aspects to consider when making this choice:
  • Matching the metal ion with an appropriate chelator
  • What type of environment will the chelate have to tolerate?
  • Factors relevant to in vitro or in vivo applications
  • Chelate stability – factors that can affect performance
  • Kinetics – How fast does complexation need to occur – a key point for nuclear medicine applications

• Deciding upon the correct bifunctional linker for optimal conjugation. Conjugation reactions can be challenging as each new targeting molecule is unique with respect to optimal conditions. In general there are three types of reactive functional groups used for the preparation of most conjugates:

  • Isothiocyante – reactive with primary amine residues
  • Activated NHS ester – reactive with primary amine residues
  • Maleimide – reactive with thiol groups.