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Radiopharmaceutical therapy is a targeted radioactive drug treatment. It links a radioactive atom (a radionuclide) to a molecule that recognizes a feature on, or near, cancer cells. After the drug is administered, the targeting molecule concentrates radiation at disease sites, where the radiation can damage tumor cells. Targeting may reduce exposure to some healthy tissue compared with delivering radiation without a molecular guide, but healthy tissue can still be affected and the treatment is not automatically curative.
The target, radionuclide, eligibility rules, dosing schedule and side effects depend on the specific cancer and product. A scan may be used first to show whether a tumor has the required target before treatment is offered.
The core idea: a radioactive atom guided to a tumor-associated target
The National Cancer Institute defines targeted radionuclide therapy as “a type of radiation therapy in which a radionuclide (a radioactive chemical) is linked to a cell-targeting molecule, such as a monoclonal antibody, and injected into the body.” NCI’s definition captures the two essential parts:
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- The radionuclide: the radioactive component that emits therapeutic radiation.
- The targeting molecule: a ligand, peptide, antibody or another molecule chosen because it binds to a feature associated with a particular tumor.
Once in the bloodstream, the compound travels through the body. Where the target is present, the targeting molecule binds or accumulates, bringing the radionuclide close to malignant cells. Radiation released at that location can injure cellular DNA and other structures. Some radiation can also reach nearby cells, which may help treat a cluster of disease rather than only the single cell to which the molecule is attached.
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“Targeted” describes the delivery strategy, not a promise that radiation reaches only cancer. Normal organs may express the same target, absorb part of the drug, or be exposed as the radionuclide circulates and clears. The expected balance between tumor dose and normal-tissue dose is therefore considered for each medicine and patient.
How different radiopharmaceuticals find cancer
PSMA-directed therapy for selected prostate cancer
Some prostate cancers display prostate-specific membrane antigen (PSMA) on their cells. A PSMA-binding ligand can carry a therapeutic radionuclide such as lutetium-177. The ligand attaches to PSMA-positive tumor cells, allowing the lutetium-177 radiation to act at metastatic sites that express the target. The Society of Nuclear Medicine and Molecular Imaging (SNMMI) prostate fact sheet describes lutetium-177 PSMA-617 as an example for selected prostate cancer patients.
Peptide receptor radionuclide therapy (PRRT)
Many neuroendocrine tumors carry somatostatin receptors. In PRRT, a radioactive peptide is designed to bind those receptors, delivering radiation to receptor-positive tumor cells. The NCI definition of peptide receptor radionuclide therapy describes this receptor-directed approach. The relevant receptor expression and the exact product determine whether PRRT is appropriate.
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Radium-223 and bone lesions
Radium-223 uses a different biological route. Rather than binding a tumor-cell receptor such as PSMA, it collects in areas of bone undergoing changes associated with prostate-cancer metastases. Its short-range alpha radiation can damage nearby tumor cells in those bone sites. It is therefore related to other radiopharmaceutical therapies but is not interchangeable with a PSMA ligand or a PRRT medicine. The prostate treatment overview from the NCI and the SNMMI fact sheet describe radium-223 as an example for prostate cancer with bone metastases.
Why imaging can determine whether treatment is possible
Some radiopharmaceutical programs use a diagnostic scan before therapy. The imaging agent is chemically related to the treatment’s targeting strategy, but it is not the therapeutic drug. A positron-emission-tomography (PET) tracer can show whether tumors express enough of the target for a treatment to have a reasonable chance of reaching them.
For PSMA-directed treatment, PSMA PET imaging is used to demonstrate PSMA expression. The tracer Locametz (gallium Ga 68 gozetotide) is one approved option. The U.S. Food and Drug Administration (FDA) announcement dated July 31, 2026 says that, for the newly approved population described there, patients receiving lutetium Lu 177 vipivotide tetraxetan with androgen-receptor pathway inhibitor therapy should be selected using Locametz or another approved PSMA PET product based on tumor PSMA expression.
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A positive scan is evidence that the target is present; it is not, by itself, a prescription. Doctors still evaluate the cancer type and stage, previous treatments, organ function, blood counts, overall health, competing treatment options and the product’s current label. A scan also may show mixed disease, with some lesions strongly target-positive and others weakly positive or negative. That pattern can affect the expected benefit.
Examples of radiopharmaceutical therapy
| Approach | Target or route | Cancer setting described by the sources | Schedule information |
|---|---|---|---|
| Lutetium-177 PSMA-617 | PSMA on prostate-cancer cells | Selected metastatic prostate cancer | SNMMI describes six injections, one every six weeks, for the therapy covered in its prostate fact sheet. This is a source-specific example, not a universal schedule. |
| Radium-223 | Areas of bone affected by metastatic disease | Prostate cancer with bone metastases | SNMMI describes six injections, one every four weeks, for the treatment discussed in its fact sheet. |
| Lutetium-177 radiolabeled peptides (PRRT) | Somatostatin receptors on certain neuroendocrine tumors | Selected receptor-positive neuroendocrine tumors | Protocols vary; the SNMMI neuroendocrine-tumor material does not establish one schedule for every product or patient. |
The table summarizes examples, not a treatment recommendation. Product names, indications and schedules can differ by country and can change as regulators update labeling. Confirm the current local prescribing information with the treating team.
Who might be considered for treatment?
Eligibility is clinical and product-specific. The general mechanism cannot establish that an individual qualifies. Teams commonly consider the following factors together:
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- Tumor target: imaging, pathology or other testing must show the molecular feature required by the therapy, such as PSMA or a somatostatin receptor.
- Cancer type and disease state: an approved indication may be limited to a particular tumor type, metastatic pattern or line of therapy.
- Prior and concurrent treatment: previous systemic therapy, androgen-receptor pathway treatment or other medicines can be part of the indication and safety assessment.
- Ability to tolerate radiation and the drug: blood counts, kidney or other organ function, performance status and the distribution of disease may influence the decision.
- Expected benefit versus alternatives: the oncology and nuclear-medicine teams compare potential tumor control with risks, logistics and other available treatments.
For example, the FDA’s July 31, 2026 announcement concerns adults with PSMA-positive metastatic prostate cancer that is androgen-pathway modulation-naïve or -sensitive, in combination with androgen-receptor pathway inhibitor therapy. That U.S. approval should not be generalized to every person with prostate cancer, every PSMA result or every country.
What the treatment process generally involves
Exact procedures differ by radiopharmaceutical and facility, but a typical pathway has distinct decision points:
- Confirm the diagnosis and treatment question. The oncology team identifies the cancer setting, prior therapy and goal of treatment.
- Verify the target. A diagnostic scan or other approved test determines whether the tumor expresses the target required by the product. For PSMA therapy, this may involve an approved PSMA PET agent such as Locametz.
- Review safety factors. Clinicians assess blood counts, relevant organ function, medicines, symptoms and the extent and location of disease. They also explain radiation-related precautions and follow-up requirements appropriate to the product.
- Administer the radiopharmaceutical. These treatments are given in a specialized clinical setting, commonly by injection into a vein. The facility follows procedures for handling and monitoring radioactive medicines.
- Monitor during the course. The team checks for acute problems and schedules laboratory tests, examinations and imaging as needed before later doses.
- Reassess after or between doses. Decisions about continuing, delaying or stopping treatment depend on the product protocol, side effects, laboratory results and how the cancer is responding.
Do not assume that one product’s preparation, observation time, radiation-safety instructions or number of visits applies to another. Ask the treating center for written instructions specific to the medicine being offered.
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Schedules and side effects are not interchangeable
The SNMMI prostate fact sheet lists fatigue, dry mouth and decreased blood counts among effects associated with the lutetium-177 PSMA-617 therapy it discusses. It lists decreased blood counts for radium-223. These examples are not a complete risk list and do not describe every radiopharmaceutical.
| Therapy example | Schedule example in SNMMI material | Effects specifically listed in that material |
|---|---|---|
| Lutetium-177 PSMA-617 | Six injections every six weeks | Fatigue, dry mouth and decreased blood counts |
| Radium-223 | Six injections every four weeks | Decreased blood counts |
| PRRT for neuroendocrine tumors | Protocol varies | The cited SNMMI neuroendocrine material does not provide one universal side-effect list for all protocols. |
Individual risk depends on the drug, cumulative radiation, disease burden, baseline organ function and other treatments. The current prescribing information and the patient’s own oncology and nuclear-medicine team are the appropriate sources for complete warnings, dose changes and instructions about symptoms that require urgent attention.
Potential advantages and important limits
What targeting can offer
- Radiation is carried toward cells that display a selected molecular feature rather than being aimed only from outside the body.
- Multiple sites of target-positive disease can be reached through the bloodstream, including metastatic locations that are difficult to treat with a single local procedure.
- A diagnostic scan can provide a treatment-selection signal by showing whether the target is present.
What targeting does not guarantee
- It does not spare every healthy cell. Normal organs can receive radiation, and some toxicities are expected or possible.
- It does not work for tumors that lack, lose or unevenly express the required target.
- It is not automatically curative. The purpose and expected outcome depend on the disease setting and the specific product.
- It is not the same as diagnostic imaging. A PET tracer such as Locametz helps identify PSMA expression; a therapeutic radionuclide delivers treatment radiation.
The dated U.S. approval example readers should understand
On July 31, 2026, the FDA announced approval of lutetium Lu 177 vipivotide tetraxetan (Pluvicto) with androgen-receptor pathway inhibitor therapy for adults with PSMA-positive metastatic androgen-pathway modulation-naïve or -sensitive prostate cancer. The announcement specifies selection with Locametz or another approved PSMA PET product based on PSMA expression in tumors. This is a U.S. regulatory decision for the population described in that announcement, not a blanket approval for all prostate cancer or all radiopharmaceutical therapies. Read the current FDA labeling and local guidance before applying the example to a particular case.
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- Which target does my tumor need to express, and how was that confirmed?
- Is the scan being used for diagnosis, treatment selection or both, and which agent was used?
- What exact product and indication are being considered in my country and cancer setting?
- How many administrations are planned, at what interval, and what could cause a dose to be delayed or changed?
- Which blood tests and organ-function checks are required before each dose?
- What side effects are most important for this specific product, and whom should I call if they occur?
- How will response be assessed, and what alternatives exist if the target is absent or the treatment is not tolerated?
Bottom line
Radiopharmaceutical therapy combines a tumor-seeking molecule with a radioactive atom so radiation is delivered near cells bearing a selected target. PSMA-directed therapy, receptor-directed PRRT and bone-seeking radium-223 illustrate three different ways that principle is applied. A target-confirming scan, the exact cancer setting, prior treatment and product-specific safety criteria determine whether therapy is appropriate; no single schedule, side-effect list or approval applies to every radiopharmaceutical.
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