Approved & therapeutic
Lutetium Lu 177 dotatate
Lutathera
Lutetium Lu 177 dotatate is a radiolabelled somatostatin analogue used for peptide receptor radionuclide therapy in somatostatin-receptor-positive gastroenteropancreatic neuroendocrine tumours. It uses a peptide purely as a delivery vehicle for radiation.
Also known as: 177Lu-DOTATATE, Lu-177 dotatate, PRRT
- Status
- Lutetium Lu 177 dotatate is approved by the U.S. FDA and has official prescribing information.
- Evidence
- Approved labeling. Official prescribing information exists, based on clinical trials in people.
- Half-life
- Approximately 3.5 days effective half-life; lutetium-177 has a physical half-life of 6.6 days.
- How it's taken
- Intravenous infusion in a nuclear medicine facility, four doses eight weeks apart
- Mechanism
- Other
- Pathways
- GH axis
How Lutetium Lu 177 dotatate works
The molecule couples a somatostatin analogue (octreotate) through a DOTA chelator to lutetium-177, a beta-emitting radionuclide. The peptide binds SSTR2 on tumour cells and is internalised, delivering beta radiation with a tissue range of about 2 mm directly into the tumour while largely sparing surrounding tissue. It is a targeted radiotherapy, not a receptor-mediated pharmacological effect.
What research has looked at
- The NETTER-1 trial showed a marked improvement in progression-free survival compared with high-dose octreotide LAR in midgut neuroendocrine tumours.
- The theranostic pairing is elegant in practice: a gallium-68 dotatate PET scan confirms receptor expression and therefore predicts which patients the therapy can reach.
- The short 2 mm tissue range of the beta emission concentrates dose within the tumour.
- Lutetium-177 also emits gamma photons, allowing post-treatment imaging to confirm where the dose actually went.
Evidence level: Approved labeling. Official prescribing information exists, based on clinical trials in people. These are areas studied or reported, not promised effects.
Reported side effects and risks
- Myelosuppression, and — importantly — myelodysplastic syndrome and acute leukaemia occur in a small percentage of patients as a delayed effect, sometimes years later.
- Renal toxicity from tubular reabsorption of the radiopeptide; an amino acid infusion is co-administered specifically to block this.
- Hepatotoxicity in patients with substantial liver metastases.
- Neuroendocrine hormonal crisis can be precipitated by the treatment.
- Nausea and vomiting, largely from the co-administered amino acid solution rather than the radiopharmaceutical.
- It requires radiation safety precautions and a licensed facility.
Sources
- FDA approved-drug listing for lutetium Lu 177 dotatate · U.S. Food & Drug Administration
- DailyMed prescribing information for lutetium Lu 177 dotatate · NIH · DailyMed
- PubMed research on lutetium 177 dotatate NETTER-1 PRRT · NIH · National Library of Medicine
- DrugBank record for lutetium Lu 177 dotatate · DrugBank
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Lutetium Lu 177 dotatate FAQ
What is Lutetium Lu 177 dotatate?
Lutetium Lu 177 dotatate is a radiolabelled somatostatin analogue used for peptide receptor radionuclide therapy in somatostatin-receptor-positive gastroenteropancreatic neuroendocrine tumours. It uses a peptide purely as a delivery vehicle for radiation.
How does Lutetium Lu 177 dotatate work?
The molecule couples a somatostatin analogue (octreotate) through a DOTA chelator to lutetium-177, a beta-emitting radionuclide. The peptide binds SSTR2 on tumour cells and is internalised, delivering beta radiation with a tissue range of about 2 mm directly into the tumour while largely sparing surrounding tissue. It is a targeted radiotherapy, not a receptor-mediated pharmacological effect.
Is Lutetium Lu 177 dotatate FDA approved?
Yes. Lutetium Lu 177 dotatate is approved by the U.S. FDA and has official prescribing information. Evidence level: approved labeling. Official prescribing information exists, based on clinical trials in people.
What is the half-life of Lutetium Lu 177 dotatate?
Reported half-life: Approximately 3.5 days effective half-life; lutetium-177 has a physical half-life of 6.6 days.
How is Lutetium Lu 177 dotatate taken?
Intravenous infusion in a nuclear medicine facility, four doses eight weeks apart.
What side effects have been reported with Lutetium Lu 177 dotatate?
Reported in the sources: Myelosuppression, and — importantly — myelodysplastic syndrome and acute leukaemia occur in a small percentage of patients as a delayed effect, sometimes years later; Renal toxicity from tubular reabsorption of the radiopeptide; an amino acid infusion is co-administered specifically to block this; Hepatotoxicity in patients with substantial liver metastases; Neuroendocrine hormonal crisis can be precipitated by the treatment; Nausea and vomiting, largely from the co-administered amino acid solution rather than the radiopharmaceutical; It requires radiation safety precautions and a licensed facility.
Educational summary compiled from the sources listed above. Not medical advice. Peptide Vault does not sell, source or recommend any compound. Talk to a qualified clinician before starting or changing anything.