Digestive & weight SSTR-targeted radiopeptide
Lutetium Lu-177 dotatate
Regulatory status
Status at a glance
503A compounding status
Not nominated
We found no pending nomination for the 503A bulks list. Unless the substance has another legal pathway (for example, a USP monograph or use in an FDA-approved drug), 503A pharmacies generally may not compound with it.
- FDA approval
- An FDA-approved product contains this peptide
- 503B outsourcing
- Not determined
- Anti-doping (WADA)
- Not on the WADA Prohibited List
- DEA schedule
- Not a controlled substance
About peptide status
Most peptides discussed here are not FDA-approved for any use, and products labeled “research use only” are not for human use. Removal from Category 2 does not authorize compounding. PCAC votes are non-binding recommendations; FDA and HHS make the final decisions.
This is not medical or legal advice, and we do not publish dosing, sourcing or reconstitution information. Talk with a licensed clinician before using any peptide.
If you think you are having a medical emergency, call 911.
Key takeaway
Lutetium Lu-177 dotatate (sold as Lutathera) is a targeted radiation therapy that attaches a radioactive isotope to a somatostatin analog to deliver radiation directly to neuroendocrine tumors. It was the first peptide receptor radionuclide therapy approved in the United States. It has been FDA-approved in the U.S. since 2018 and is given as a series of intravenous infusions.
At a glance
- What it is
- A lutetium-177-labeled somatostatin analog delivering targeted radiation (peptide receptor radionuclide therapy)
- Approved for
- Somatostatin-receptor-positive gastroenteropancreatic neuroendocrine tumors
- Key fact
- In the NETTER-1 trial it markedly improved progression-free survival versus high-dose octreotide
- Route
- Intravenous infusion, four doses eight weeks apart
- Evidence strength
- FDA approved
Summary
Lutetium Lu-177 dotatate (Lutathera) is an FDA-approved radiation therapy for neuroendocrine tumors. See how it works, uses, and side effects.
What is lutetium Lu-177 dotatate?
Lutetium Lu-177 dotatate, sold under the brand Lutathera, uses the same tumor-seeking somatostatin analog as the imaging agent gallium-68 dotatate, but attaches a radiation-emitting isotope, lutetium-177, to treat rather than image. It is a form of peptide receptor radionuclide therapy (PRRT), and it was the first such therapy approved in the United States. It was approved in 2018.
How does lutetium Lu-177 dotatate work?
The dotatate peptide binds somatostatin receptor subtype 2 on neuroendocrine tumor cells and is taken inside them. Attached to it is lutetium-177, which emits beta particles, a short-range form of radiation. Because the tracer concentrates in receptor-rich tumor cells, the radiation is delivered largely where it is needed, damaging the DNA of the tumor cells and the cells immediately around them while sparing much of the healthy tissue.
This targeted delivery is the principle of PRRT, often described as a "theranostic" pairing with the gallium-68 imaging agent: the scan confirms the target before the therapy is given. In the NETTER-1 trial in advanced midgut neuroendocrine tumors, lutetium-177 dotatate markedly improved progression-free survival compared with high-dose octreotide. An amino-acid solution is infused alongside it to protect the kidneys.
Is it FDA-approved?
Editor’s note
Status: Yes. Lutetium Lu-177 dotatate (Lutathera) was approved by the FDA in 2018 for somatostatin-receptor-positive gastroenteropancreatic neuroendocrine tumors in adults, with later expansion to adolescents. It is given as four intravenous infusions about eight weeks apart.
Category: FDA-approved · Primary body area: Digestive & weight
Yes. Lutetium Lu-177 dotatate (Lutathera) was approved by the FDA in 2018 for somatostatin-receptor-positive gastroenteropancreatic neuroendocrine tumors in adults, with later expansion to adolescents. It is given as four intravenous infusions about eight weeks apart.
What is lutetium Lu-177 dotatate prescribed for?
It is prescribed for somatostatin-receptor-positive gastroenteropancreatic neuroendocrine tumors, including those of the foregut, midgut, and hindgut. Eligibility is confirmed with somatostatin-receptor imaging such as the gallium-68 dotatate scan.
What are the side effects?
According to the prescribing information, common side effects include:
- Nausea and vomiting, partly from the protective amino-acid infusion
- Fatigue
- Low blood counts
More serious considerations include:
- Bone-marrow suppression and a risk of secondary myelodysplastic syndrome or leukemia
- Kidney and liver toxicity
- A temporary surge of tumor hormones (neuroendocrine hormonal crisis)
- Allergic reactions, including swelling of the face or throat (angioedema)
- Radiation exposure and effects on fertility
Sources: FDA prescribing information for Lutathera; the NETTER-1 trial (Strosberg et al., New England Journal of Medicine, 2017, DOI: 10.1056/NEJMoa1607427), indexed on PubMed. This document is educational and does not constitute medical advice.
Registered human trials
0 registered human trials on ClinicalTrials.gov that we reviewed
Sources
- [1]
- [2]
approved (PDF)
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