Peking University Team’s Breakthrough in Nuclear Drug Design for Advanced Cancer Metastasis Published in Nature After 50 Years

According to reports, the team has successfully developed targeted covalent radiopharmaceuticals (CTR).This is a disruptive technology in nuclear drug design, and has obtained excellent early clinical research data in tumor diagnosis and treatment, which is expected to rewrite the clinical diagnosis and treatment guidelines for related diseases..

Gamingdeputy learned from relevant introductions thatTargeted Radionuclide Therapy (TRT)It is a revolutionary treatment for advanced cancer metastasis. TRT uses radioligands with high affinity and selectivity for tumor-specific targets to deliver potent β or α radioactive therapeutic nuclides (with a range of only micrometers to millimeters) to the lesions for molecular-level precision radiotherapy. When the same ligand is combined with positron or single-photon radioactive diagnostic nuclides, it can locate the lesion and evaluate the treatment effect through PET and SPECT imaging technologies commonly used in nuclear medicine, thus achieving integrated diagnosis and treatment.


To make this molecular-level precision radiotherapy more effective, targeted radionuclide therapy needs to face at least the following challenges:

  • First, it allows the radionuclide to accurately find tumor cells (through ligand-target binding), i.e., excellent tumor targeting;

  • The second is to allow the radioactive nuclides to stay in the tumor cells for a longer period of time, so that the therapeutic radioactive nuclides can fully kill the tumor cells within a limited decay time;

  • The third is to ensure that the radioactive nuclides in normal organs are metabolized and excreted as quickly as possible to reduce the side effects of treatment.

It is reported that solving these three challenges simultaneously is difficult and is the key to further improving the efficacy of TRT.

Targeted covalent radiopharmaceuticals are a new form of drug that highly selectively fixes radioligands to tumors. This technology enhances tumor uptake and retention of radioligands and ensures low uptake in the blood circulation or healthy tissues.It is expected to overcome the problem that traditional nuclear medicines cannot achieve both safety and effectiveness.


Based on modern covalent drug molecular engineering, the research team verified the effectiveness of CTR at the molecular, cellular, mouse and patient levels. This new drug form,The company has overcome the bottleneck of poor efficacy of fibroblast activation protein (FAP, a pan-cancer target) targeted radioligands due to insufficient tumor uptake and retention, and has initially overcome the above challenges..

Targeted covalent radiopharmaceuticals (CTRs) have achieved three major breakthroughs.

  • Irreversible and selective covalent attachment of the pan-cancer target FAP

  • CTR-FAPI shows better PET imaging contrast

  • CTR enhances targeted radionuclide therapy by improving retention

The research team said that under the guidance of Peking University's one-stop scientific and technological innovation layout of basic research, applied research, and achievement transformation,The team is accelerating the development of targeted covalent radioactive drugs into a platform technology to enable functional transformation of conjugated drugsResearchers have recently used CTR-FAPI to make more accurate diagnoses in nearly 100 patients with medullary thyroid cancer to guide surgical treatment and achieved considerable clinical benefits.

In addition, the team is working with Peking University Cancer Hospital and Chinese Academy of Medical Sciences Cancer Hospital to verify the effectiveness of the drug in major cancers such as lung cancer, breast cancer, prostate cancer, head and neck cancer. The excellent clinical data has attracted many pharmaceutical companies to seek cooperation.

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