lutetium lu 177-dota-tate

Action and Spectrum

Actions and Spectrum: 

Actions 

lutetium lu 177 is a beta-emitting radionuclide, emitting beta particles during radioactive decay. These beta particles have a short range in tissue (a few millimeters), allowing for localized radiation therapy. The emitted beta particles deposit their energy in the tumor cells, causing DNA damage and ultimately leading to cell death.

lutetium lu 177 vipivotide tetraxetan is primarily used to treat certain neuroendocrine tumors, particularly those originating in the gastroenteropancreatic system. Neuroendocrine tumors express somatostatin receptors, making them suitable targets for this therapy. lutetium lu 177 vipivotide tetraxetan offers a targeted and systemic treatment option for patients with inoperable or metastatic neuroendocrine tumors.  

Spectrum 

lutetium lu 177 vipivotide tetraxetan has shown promising therapeutic efficacy in managing neuroendocrine tumors.  

lutetium lu 177 vipivotide tetraxetan is primarily used palliative treatment as an option for patients with advanced or metastatic neuroendocrine tumors. It aims to alleviate symptoms, such as pain, hormonal excess, and tumor-related complications, and improve the patient’s overall well-being. 

Drug Interaction

Adverse Reaction

Frequency not defined 

>10% 

Lymphopenia (90%) 

Anemia (81%) 

Increased GGT (66%) 

Creatinine increased (85%) 

Hyperglycemia (82%) 

Increased alkaline phosphatase (65%) 

Thrombocytopenia (53%) 

AST increased (50%) 

ALT increased (43%) 

Nausea (65%) 

Leukopenia (55%) 

Vomiting (53%) 

Fatigue (38%) 

Blood bilirubin increased (30%) 

Hypokalemia (26%) 

Hyperuricemia (34%) 

Hypocalcemia (32%) 

Abdominal pain (26%) 

Diarrhea (26%) 

Hypernatremia (17%) 

Headache (17%) 

Dizziness (17%) 

Peripheral edema (16%) 

Neutropenia (26%) 

Decreased appetite (21%) 

Hyperkalemia (19%) 

Hypoglycemia (15%) 

Flushing (14%) 

Renal failure (12%) 

Alopecia (12%) 

Back pain (13%) 

Anxiety (12%) 

Hypertension (12%) 

Cough (11%) 

Pain in extremity (11%) 

1-10% 

Hyperuricemia (6%) 

Nausea (5%) 

Vomiting (7%) 

Alkaline phosphatase increased (5%) 

Hyperglycemia (4%) 

Hypokalemia (4%) 

AST increased (5%) 

ALT increased (4%) 

Renal failure (3%) 

Back pain (2%) 

Hypertension (2%) 

Leukopenia (2%) 

Abdominal pain (3%) 

Diarrhea (3%) 

Neutropenia (3%) 

Blood bilirubin increased (2%) 

Cough (1%) 

Thrombocytopenia (1%) 

Anxiety (1%) 

Atrial fibrillation (1%) 

Fatigue (1%) 

Creatinine increased (1%) 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 
• Pregnancy 
• Lactation 

Cautions 

• Bone marrow suppression 
• Previous radiation therapy 
• Renal impairment 
• Hepatic impairment 

Pregnancy / Lactation

Pregnancy consideration:  

No data is available regarding the usage of this drug during pregnancy. 

Breastfeeding warnings:  

No data is available regarding the presence of this drug in breast milk. 

Pregnancy category: 

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester. 
• Category B: No evidence of risk to the fetus is found in animal reproduction studies, and there are not enough studies on pregnant women.    
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a human product; Pregnant women must take care of the potential risks. 
• Category D: There is adequate data with sufficient evidence of human fetal risk from various platforms. However, despite potential dangers may be used only in emergencies for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. The drug is not for pregnant women. 
• Category N: No data for the drug under this category is available. 

Pharmacology

Pharmacology:
The pharmacology of lutetium lu 177-DOTA-TATE (Lutathera) involves understanding its pharmacokinetics and its interaction with somatostatin receptors in neuroendocrine tumor cells. Here are the critical aspects of its pharmacology: 

• Somatostatin Receptor Binding: lutetium lu 177-DOTA-TATE is a radiolabeled peptide that binds to somatostatin receptors, which are overexpressed on the surface of neuroendocrine tumor cells. The DOTA-TATE component of the molecule serves as a carrier that specifically targets somatostatin receptor subtypes, primarily subtype 2 (SSTR2). 
• Internalization and Retention: Once lutetium lu 177-DOTA-TATE binds to somatostatin receptors on tumor cells, the complex is internalized and retained within the cells. This internalization mechanism ensures prolonged exposure of the tumor cells to the radiation emitted by lutetium lu 177. 
• Beta Particle Emission: lutetium lu 177 is a beta-emitting radionuclide. As it undergoes radioactive decay, it emits beta particles. These high-energy beta particles have a limited range and can penetrate a short distance into the surrounding tumor cells. 
• Radiation Damage: The beta particles emitted by lutetium lu 177 cause localized radiation damage within the tumor cells. The energy deposited by the beta particles leads to DNA strand breaks, disruption of cellular processes, and eventual cell death. The radiation damage is primarily confined to the tumor cells, minimizing the impact on surrounding healthy tissues. 
• Clearance and Elimination: lutetium lu 177-DOTA-TATE is cleared from the 

Pharmacodynamics: 

lutetium lu 177-DOTA-TATE is a radiopharmaceutical that targets somatostatin receptors, which are overexpressed on the surface of neuroendocrine tumor cells. The drug binds to these receptors, allowing for targeted radiation delivery to the tumor cells. 

lutetium lu 177-DOTA-TATE combines the therapeutic effects of lutetium lu 177, a beta-emitting radionuclide, with the targeting properties of DOTA-TATE. Once bound to the somatostatin receptors on tumor cells, lutetium lu 177 emits beta particles during radioactive decay. These beta particles penetrate the surrounding tumor cells and deposit energy, leading to DNA damage and cell death.  

Pharmacokinetics: 

Absorption 

The peak plasma concentration is 10 ng/mL 

The AUC is 41 ng⋅hr/mL 

Distribution  

The protein-bound is 43% 

The volume of distribution is 640L 

Metabolism 

It is not metabolized in the body. 

Elimination and Excretion 

The elimination half-life is approximately 3.5 hours 

The terminal half-life is 71 hours 

The rate of clearance is 4.5 L/hr 

Adminstartion

Administration: 

lutetium lu 177-dota-tate  is administered as an intravenous injection. A healthcare provider will insert a needle into a vein, typically in the arm, and slowly inject the radiopharmaceutical into the bloodstream. The injection process usually takes a few minutes. 

After the injection, the patient is monitored briefly to ensure no immediate adverse reactions or complications. Patients are typically instructed to report any discomfort or adverse effects they experience during this period. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: lutetium lu 177-dota-tate 

Pronounced: loo-TEE-shee-um-loo-177 doh-tah-tayt 

Why do we use lutetium lu 177-dota-tate? 

lutetium lu 177-DOTA-TATE (also known as Lutathera) treats certain types of neuroendocrine tumors, particularly those that express somatostatin receptors.