Lutathera

Approved Indications

Lutathera is used to treat a group of cancers known as gastroenteropancreatic neuroendocrine tumors (GEP-NETs). These tumors may be located in the stomach, intestines, or pancreas.

This medication is specifically for tumors that are:

• Somatostatin receptor-positive: The cancer cells must have specific receptors that allow the drug to target them.
• Unresectable: The tumor cannot be completely removed through surgery.
• Metastatic: The cancer has spread from its original site to other parts of the body.

Healthcare providers typically confirm that the cancer is somatostatin receptor-positive using an imaging test before beginning treatment. This ensures the medication can effectively reach and bind to the tumor cells.

Targeted Therapy

Lutathera belongs to a class of drugs known as peptide receptor radionuclide therapy (PRRT). It works by combining a targeting molecule with a radioactive isotope to deliver treatment directly to cancer cells.

How It Targets Cancer

Many neuroendocrine tumors have a high number of proteins on their surface called somatostatin receptors. Lutathera is designed to recognize and bind specifically to these receptors. Once the drug attaches to the receptor, the cancer cell absorbs the medication.

Destroying Tumor Cells

After entering the cell, the radioactive part of the medicine, called lutetium-177, releases energy in the form of radiation. This radiation travels a short distance to damage the DNA within the tumor cell and nearby cells. This damage prevents the cancer cells from reproducing and eventually leads to cell death.

Common Side Effects

• Nausea and vomiting
• Fatigue
• Decreased appetite
• Muscle, bone, or joint pain
• Dizziness
• Abdominal pain
• Diarrhea or constipation
• Cough
• Headache

Serious Side Effects

• Low blood cell counts: This medication can cause a significant drop in red blood cells, white blood cells, and platelets, which may increase the risk of infection, bleeding, or anemia.
• Kidney problems: Changes in kidney function can occur during or after treatment.
• Liver problems: Some patients may experience liver damage or inflammation.
• Secondary cancers: There is a long-term risk of developing certain blood cancers, such as myelodysplastic syndrome or acute leukemia, due to radiation exposure.
• Hormonal crisis: In some cases, the treatment can cause a sudden release of hormones from the tumor (carcinoid crisis), leading to symptoms like flushing, diarrhea, or low blood pressure.
• Infertility: Radiation exposure from the drug may affect fertility in both men and women.

Radiation Exposure

Lutathera is a radiopharmaceutical that contributes to a patient's cumulative radiation exposure. Healthcare providers follow specific protocols to minimize radiation risks to the patient and their contacts.

Myelosuppression

Treatment can cause severe decreases in blood cell counts, including anemia, thrombocytopenia, and leukopenia. Monitoring of complete blood counts is required before each dose and during follow-up care. Dose adjustments or treatment delays may be necessary if blood counts fall too low.

Secondary Malignancies

Exposure to Lutathera increases the risk of developing secondary cancers, specifically myelodysplastic syndrome (MDS) and acute leukemia.

Renal and Hepatic Toxicity

Radiation from the drug can cause damage to the kidneys and liver. An amino acid solution is administered intravenously during the infusion to help protect the kidneys. Regular monitoring of kidney and liver function through blood tests is necessary during treatment.

Neuroendocrine Hormonal Crisis

The release of hormones from tumor cells can cause a carcinoid crisis. Symptoms may include severe flushing, diarrhea, hypotension, and breathing difficulties. Patients are monitored for these symptoms, and medications like corticosteroids may be used for prevention or treatment.

Embryo-Fetal Toxicity and Fertility

Lutathera can cause harm to a developing fetus. Females of reproductive potential should use effective contraception during treatment and for 7 months after the last dose. Males with female partners of reproductive potential should use effective contraception during treatment and for 4 months after the last dose. Radiation exposure may also lead to infertility in both males and females.

Pregnancy

Lutathera is a radiopharmaceutical that can cause harm to a fetus. Due to the risk of radiation exposure, healthcare providers will typically verify that a patient is not pregnant before starting treatment. If you are pregnant or become pregnant during treatment, it is important to discuss the potential risks to the fetus with your medical team.

Patients of reproductive potential should use effective birth control during treatment and for a period of time after the final dose:

• Females: Use effective contraception during treatment and for 7 months after the last dose.
• Males: Use effective contraception during treatment and for 4 months after the last dose if you have a female partner who could become pregnant.

Breastfeeding

There is no information regarding whether Lutathera is present in human breast milk or how it might affect a nursing infant. Because radiation exposure poses a risk of serious adverse reactions in infants, breastfeeding is not recommended during treatment and for 2.5 months after the final dose.

Dosage Forms

Lutathera is a radiopharmaceutical supplied as a sterile, clear, colorless to slightly yellow solution. It is administered by a healthcare professional as an intravenous injection.

Strengths

This medication is provided in a single-dose vial. The strength is determined by the level of radioactivity at the time of calibration and administration:

• Each single-dose vial contains a total radioactivity of 7.4 GBq (200 mCi) at the time of injection.
• The concentration is 370 MBq/mL (10 mCi/mL) at the time of calibration.

FDA Approval History

Lutathera (lutetium Lu 177 dotatate) was first approved by the U.S. Food and Drug Administration (FDA) in January 2018. It was the first peptide receptor radionuclide therapy (PRRT) approved to treat somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs), which include tumors of the foregut, midgut, and hindgut.

Expanded Pediatric Approval

In April 2024, the FDA expanded the approval of Lutathera to include pediatric patients 12 years of age and older with somatostatin receptor-positive GEP-NETs. This expansion made it the first radiopharmaceutical approved for pediatric patients with these specific types of tumors.

Regulatory Classification

Lutathera is a prescription medication classified as a radiopharmaceutical. Due to its radioactive components, it is subject to specific regulatory requirements regarding its handling, storage, and administration. It must be administered by qualified healthcare professionals in clinical settings equipped for nuclear medicine. There are currently no Boxed Warnings or Risk Evaluation and Mitigation Strategies (REMS) associated with this drug.

Estimated Costs

Lutathera is a specialized radiopharmaceutical medication with a high list price. A single dose is estimated to cost approximately $58,000. However, the actual price paid by patients or insurance providers often varies significantly from the list price based on negotiated rates and coverage details.

Factors Affecting Price

• Facility and Administration Fees: Because Lutathera must be administered in a specialized nuclear medicine setting, total costs include fees for the medical staff, radiation safety equipment, and facility use.
• Insurance Coverage: Most private insurance plans, Medicare, and Medicaid typically cover Lutathera for its FDA-approved uses. Patients may still be responsible for out-of-pocket costs such as deductibles, copayments, or coinsurance.
• Treatment Course: A standard treatment course usually involves four doses given every eight weeks. The total cost of therapy is determined by the completion of this full series.

Financial Assistance Programs

The manufacturer may provide patient assistance programs or co-pay assistance for eligible patients to help reduce out-of-pocket expenses. Patients are encouraged to consult with their healthcare provider or a financial counselor at their treatment center to identify available support options.