lutetium lu 177 vipivotide tetraxetan

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% 

Decreased leukocytes (56%) 

Decreased calcium (39%) 

Decreased lymphocytes (85%) 

Decreased hemoglobin (63%) 

Nausea (35%) 

Decreased platelets (45%) 

Fatigue (43%) 

Dry mouth (39%) 

Increased AST (28%) 

Increased potassium (24%) 

Decreased sodium (33%) 

Anemia (32%) 

Decreased appetite (21%) 

Decreased neutrophils (28%) 

Increased creatinine (24%) 

Constipation (20%) 

Thrombocytopenia (17%) 

Urinary tract infection (12%) 

Vomiting (19%) 

Diarrhea (19%) 

Increased sodium (11%) 

Weight loss (11%) 

Abdominal pain (11%) 

1-10% 

Decreased platelets (9%) 

Thrombocytopenia (8%) 

Decreased neutrophils (4.5%) 

Urinary tract infection (3.8%) 

Decreased leukocytes (7%) 

Fatigue (6%) 

Acute kidney injury (3.2%) 

Decreased calcium (2.5%) 

Constipation (1.1%) 

Abdominal pain (1.1%) 

Decreased appetite (1.9%) 

Nausea (1.3%) 

Increased AST (1.1%) 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 

Cautions 

• Renal impairment 
• Hematological toxicity 
• Myelodysplastic syndrome 
• Leukemia 
• Pregnancy 
• Lactation 

Pregnancy / Lactation

Pregnancy consideration:  

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

Breastfeeding warnings:  

No data is available regarding the excretion 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 vipivotide tetraxetan primarily focuses on its selective targeting of somatostatin receptors on neuroendocrine tumor cells, delivering radiation therapy to these specific tumor sites. By combining the radioactive properties of lutetium lu 177 with the tumor-targeting capabilities of vipivotide tetraxetan, this therapy offers a targeted approach to managing neuroendocrine tumors. 

Pharmacodynamics: 

The pharmacodynamics of lutetium lu 177 vipivotide tetraxetan are centered around its targeted radiation delivery to somatostatin receptor-positive neuroendocrine tumor cells. By combining the radioactive properties of lutetium lu 177 with the tumor-targeting capabilities of vipivotide tetraxetan, this therapy offers a focused approach to managing neuroendocrine tumors, leading to cell death and tumor regression. 

Pharmacokinetics: 

Absorption 

The peak plasma concentration is 6.58 ng/mL 

The AUC is 52.3 ng⋅hr/mL 

Distribution  

The protein-bound is 60-70% 

The volume of distribution is 123L 

The time for distribution of the drug is 2.5  hours 

Metabolism 

It is not metabolized in the body. 

Elimination and Excretion 

The elimination half-life is approximately 41.6% 

The rate of clearance is 2.04 L/hr 

Adminstartion

Administration: 

lutetium lu 177 vipivotide tetraxetan 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 vipivotide tetraxetan 

Pronounced: loo-TEE-shee-um-loo-177 vye-PIV-oh-tide-te-TRAX-e-tan 

Why do we use lutetium lu 177 vipivotide tetraxetan? 

lutetium lu 177 vipivotide tetraxetan is used to treat certain types of neuroendocrine tumors, particularly those originating in the gastroenteropancreatic system It is also used to treat castration-resistant prostate cancer.