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radiolabeled SST peptide

Lutetium Lu-177 Dotatate

Published evidence · coverage incomplete
Anatomical contextAnatomy connections are not mapped yet.

No body region is highlighted until this profile has a supported anatomical connection. This does not mean the peptide has no biological effects.

Read published mechanism findings ↓

At a glance

What is it—and why does it matter?

This agent is a somatostatin analog peptide that is radiolabeled with lutetium-177, classifying it as a radiopharmaceutical targeting somatostatin receptors. The drug targets somatostatin receptors—preferentially SSTR2—on receptor-expressing cells and undergoes receptor-mediated internalization after binding. After administration, radioactive signal associated with treatment can be detected in urine for as long as 30 days, informing radiation safety precautions. The dosage form is an injectable solution with an activity concentration of 370 MBq/mL (10 mCi/mL), presented as a clear, colorless to slightly yellow solution in a single-dose vial.

Sources for this introduction: [1] [2] [3] [4]

This published profile is a reference in progress. Findings retain their source context; missing topics are marked below.

What is it?

A molecule, not a product name.

Identity

This agent is a somatostatin analog peptide that is radiolabeled with lutetium-177, classifying it as a radiopharmaceutical targeting somatostatin receptors.

Sources[1]dailymedThese highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018Lutetium Lu 177 dotatate is a radiolabeled somatostatin analog.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Lutetium Lu 177 dotatate is a radiolabeled somatostatin analog.”

    These highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018 · 11 DESCRIPTION

    dailymed:72d1a024-00b7-418a-b36e-b2cb48f2ab55:f580a78cab27:f580a78cab27

How does it work?

Target, response, and disposition.

Mechanism

The drug targets somatostatin receptors—preferentially SSTR2—on receptor-expressing cells and undergoes receptor-mediated internalization after binding.

Sources[1]dailymedThese highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018Lutetium Lu 177 dotatate binds to somatostatin receptors with highest affinity for subtype 2 somatostatin receptors (SSTR2). Upon binding to somatostatin receptor expressing cells, including malignant somatostatin receptor-positive tumors, the compound is internalized.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Lutetium Lu 177 dotatate binds to somatostatin receptors with highest affinity for subtype 2 somatostatin receptors (SSTR2). Upon binding to somatostatin receptor expressing cells, including malignant somatostatin receptor-positive tumors, the compound is internalized.”

    These highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018 · 12.1 Mechanism of Action

    dailymed:72d1a024-00b7-418a-b36e-b2cb48f2ab55:f580a78cab27:f580a78cab27

Pharmacokinetics

The drug’s elimination is predominantly renal, with time-dependent cumulative urinary excretion reported at 5, 24, and 48 hours post-administration.

Sources[1]dailymedThese highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018Lutetium Lu 177 dotatate is primarily eliminated renally with cumulative excretion of 44% within 5 hours, 58% within 24 hours, and 65% within 48 hours following LUTATHERA administration.
Reported result
44% within 5 hours; 58% within 24 hours; 65% within 48 hours
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Lutetium Lu 177 dotatate is primarily eliminated renally with cumulative excretion of 44% within 5 hours, 58% within 24 hours, and 65% within 48 hours following LUTATHERA administration.”

    These highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018 · 12.3 Pharmacokinetics

    dailymed:72d1a024-00b7-418a-b36e-b2cb48f2ab55:f580a78cab27:f580a78cab27

What has been studied?

What the evidence says.

This profile does not yet contain a published summary for this topic. This is a coverage gap, not evidence that no research exists.

Risks and interactions

Risks, organized for scanning.

Safety findings

After administration, radioactive signal associated with treatment can be detected in urine for as long as 30 days, informing radiation safety precautions.

Sources[1]dailymedThese highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018Radiation can be detected in the urine for up to 30 days following LUTATHERA administration.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Radiation can be detected in the urine for up to 30 days following LUTATHERA administration.”

    These highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018 · 5.1 Risk From Radiation Exposure

    dailymed:72d1a024-00b7-418a-b36e-b2cb48f2ab55:f580a78cab27:f580a78cab27

Products and regulatory status

Same ingredient. Different records.

Regulatory status

This product is indicated for SSTR-positive gastroenteropancreatic neuroendocrine tumors in adults and in pediatric patients at least 12 years old, including foregut, midgut, and hindgut primary sites.

Sources[1]dailymedThese highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018LUTATHERA is indicated for the treatment of adult and pediatric patients 12 years and older with somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs), including foregut, midgut, and hindgut neuroendocrine tumors.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “LUTATHERA is indicated for the treatment of adult and pediatric patients 12 years and older with somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs), including foregut, midgut, and hindgut neuroendocrine tumors.”

    These highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018 · 1 INDICATIONS AND USAGE

    dailymed:72d1a024-00b7-418a-b36e-b2cb48f2ab55:f580a78cab27:f580a78cab27

Administration context

The practical clinical context.

Administration

The labeled administration method excludes intravenous bolus injection; LUTATHERA is intended to be infused rather than pushed as a bolus.

Sources[1]dailymedThese highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018Do not administer LUTATHERA as an intravenous bolus.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Do not administer LUTATHERA as an intravenous bolus.”

    These highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018 · 2.5 Preparation and Administration

    dailymed:72d1a024-00b7-418a-b36e-b2cb48f2ab55:f580a78cab27:f580a78cab27

Dose records

The labeled regimen is a fixed activity dose of 7.4 GBq (200 mCi) administered on an 8-week cycle (± 1 week), repeated for 4 total administrations, in patients aged 12 years and older.

Sources[1]dailymedThese highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018The recommended LUTATHERA dosage for adult and pediatric patients 12 years and older is 7.4 GBq (200 mCi) every 8 weeks (± 1 week) for a total of 4 doses.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “The recommended LUTATHERA dosage for adult and pediatric patients 12 years and older is 7.4 GBq (200 mCi) every 8 weeks (± 1 week) for a total of 4 doses.”

    These highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018 · 2.2 Recommended Dosage

    dailymed:72d1a024-00b7-418a-b36e-b2cb48f2ab55:f580a78cab27:f580a78cab27

Dose records

The dosage form is an injectable solution with an activity concentration of 370 MBq/mL (10 mCi/mL), presented as a clear, colorless to slightly yellow solution in a single-dose vial.

Sources[1]dailymedThese highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018Injection: 370 MBq/mL (10 mCi/mL) of lutetium Lu 177 dotatate as a clear and colorless to slightly yellow solution in a single-dose vial.
Source records
1
Regulatory records
1

Evidence boundary: Applies only to the source-defined population, formulation, dose, and assessment period.

Exact passages, locators, and provenance
  1. supports · Source-backed record
    “Injection: 370 MBq/mL (10 mCi/mL) of lutetium Lu 177 dotatate as a clear and colorless to slightly yellow solution in a single-dose vial.”

    These highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018 · 3 DOSAGE FORMS AND STRENGTHS

    dailymed:72d1a024-00b7-418a-b36e-b2cb48f2ab55:f580a78cab27:f580a78cab27

Research status + gaps

What still needs better answers?

  • No publishable claim yet for: contraindication, effect, interaction
  • 17 compiled claim(s) withheld by automated assurance: assurance_score_below_0.58 (9), assurance_score_below_0.72 (8), current_regulatory_source_required (4), extraction_ambiguity (16), high_risk_requires_regulatory_or_two_independent_sources (8), no_direct_support (17)

These are the limits of this profile, not an exhaustive list of scientific uncertainties.

References + discovery

Open the records yourself.

  1. These highlights do not include all the information needed to use LUTATHERA safely and effectively. See full prescribing information for LUTATHERA.LUTATHERA®(lutetium Lu 177 dotatate) injection, for intravenous useInitial U.S. Approval: 2018 ↗

    dailymed · published 2026-01-15 · retrieved 2026-09-04T22:09:44Z

Publication history and provenance

Version 2 · Automated assessment · 2026-09-04T22:09:44Z

240e38471aa677d0bf9b3724610b16aedeb41e38bd3a36ab4f3fce6b6f6eca19