Advances in Radionuclides and Radiolabelled Peptides for Cancer Therapeutics

Radiopharmaceutical therapy, which can detect and treat tumours simultaneously, was introduced more than 80 years ago, and it has changed medical strategies with respect to cancer. Many radioactive radionuclides have been developed, and functional, molecularly modified radiolabelled peptides have been used to produce biomolecules and therapeutics that are vastly utilised in the field of radio medicine. Since the 1990s, they have smoothly transitioned into clinical application, and as of today, a wide variety of radiolabelled radionuclide derivatives have been examined and evaluated in various studies. Advanced technologies, such as conjugation of functional peptides or incorporation of radionuclides into chelating ligands, have been developed for advanced radiopharmaceutical cancer therapy. New radiolabelled conjugates for targeted radiotherapy have been designed to deliver radiation directly to cancer cells with improved specificity and minimal damage to the surrounding normal tissue. The development of new theragnostic radionuclides, which can be used for both imaging and therapy purposes, allows for more precise targeting and monitoring of the treatment response. The increased use of peptide receptor radionuclide therapy (PRRT) is also important in the targeting of specific receptors which are overexpressed in cancer cells. In this review, we provide insights into the development of radionuclides and functional radiolabelled peptides, give a brief background, and describe their transition into clinical application.

Automated summary

Radiopharmaceutical therapy, introduced over 80 years ago, has revolutionized cancer treatment by enabling simultaneous detection and treatment of tumors. Through the development of radioactive radionuclides and functional radiolabeled peptides, biomolecules and therapeutics have been produced and extensively utilized in radio medicine. Advanced technologies such as functional peptide conjugation and incorporation of radionuclides into chelating ligands have enabled precise and targeted cancer therapy while minimizing damage to surrounding normal tissue. Furthermore, the development of theragnostic radionuclides has allowed for more accurate targeting and monitoring of treatment response.