At Novartis, we are making the promise of next-generation medicines a reality today by leading the development of radioligand therapies (RLTs), a novel approach to cancer care.


Radioligand therapy explained

RLTs combine a targeting compound, the ligand, that binds to a specific marker, with a radioisotope. The ligand directs the radioisotope to the target cancer cells expressing the specific marker, even when they have spread throughout the body. This unique mechanism of action aims to damage or destroy target cancer cells or cells of the tumor microenvironment (TME) while limiting impact on nearby healthy cells. This precision approach aims to improve quality of life and extend people’s lives.

How RLT works

How is radioligand therapy developed?

Special instrument controlled by a production associate

RLTs have two primary components: the radioisotope and the targeting compound, or ligand. Radioisotopes are produced in special nuclear reactors or generators, then shipped to a production facility where they are then bonded to the ligand. The finished product is filled into vials, quality tested, packaged into special lead-shielded containers and certified shipping boxes and then shipped directly to the hospital or clinic. This intricate production process occurs all in a matter of days to account for the short life of the therapies. The finished product is a ready-to-use therapy for a specific day and time of administration. Due to the limited time window for administration, RLTs are produced in small batches on an "as ordered" basis for each individual patient.

Precision based approach to spot cancer cells using PET/CT scan

A precision-based approach

Radioligands can be used for diagnostic imaging and therapeutic applications, both of which have the same precision-based approach. By using specific markers expressed on the surface of target cells or in the tumor microenvironment, specialist healthcare professionals (HCPs) can directly identify and treat the cancer—a “see it, treat it” approach to cancer care. This approach allows HCPs to use radioligand imaging to visualize the marker and select specific patients eligible for RLT.

Three scientists working in a modern lab

The science behind RLTs

RLTs are the result of decades of scientific innovation. After scientists discovered that iodine naturally accumulates in the thyroid, they developed a radioactive version that became the first injected radiotherapy to treat thyroid diseases including certain types of cancer. Today, scientists have built on this concept, by engineering RLTs that can specifically target markers expressed in several cancers, including prostate and neuroendocrine tumors.

Portrait of an elder man

The future of radioligand therapy

There is no unique treatment approach for cancer because each cancer has a different underlying biology. This means we need to be agile with our thinking and scientific solutions, as there isn’t one approach that will work for all. With radioligand therapy, different isotopes and ligands can be combined to diagnose, monitor and/or treat various cancers—like interchangeable toy building blocks. Similar markers can be expressed on multiple tumor types, meaning one radioligand can potentially target various types of cancers. At Novartis, we are investigating these building blocks to understand the possibilities of RLTs in cancer care.