indium In-111 capromab pendetide

Action and Spectrum

Actions and Spectrum: 

indium In-111 capromab pendetide comprises a monoclonal antibody (7E11-C5.3) attached to the radionuclide indium-111. The monoclonal antibody targets the prostate-specific membrane antigen (PSMA), a protein expressed on the surface of prostate cancer cells. PSMA is overexpressed in prostate cancer and is not typically found in significant amounts in normal tissues. 

When indium In-111 capromab pendetide is administered intravenously, the monoclonal antibody selectively binds to the PSMA on prostate cancer cells. The attached indium-111 emits gamma radiation, which can be detected by a gamma camera or other imaging devices during nuclear medicine scans. 

Spectrum of Activity 

indium In-111 capromab pendetide is specifically designed to detect prostate cancer, and its spectrum of activity is limited to imaging PSMA-expressing prostate cancer cells. It is not used for therapeutic purposes and has no direct therapeutic effects on cancer cells. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Antibody development 

1-10% 

Hypotension 

Hypertension 

Increased serum bilirubin 

<1% 

Dysgeusia 

Fever 

Burning sensation (thigh), 

Dyspnea 

Headache 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

Hypersensitivity 

Caution: 

• Radiation Exposure: indium In-111 capromab pendetide is a radioactive substance, and patients will be exposed to ionizing radiation during the imaging procedure. The potential benefits of the imaging should be weighed against the radiation exposure, especially in patients who may be more sensitive to radiation, such as pregnant women and children. 
• Impaired Renal Function: The radiopharmaceutical is eliminated primarily through the kidneys. Patients with impaired renal function may have reduced clearance of the radioactive substance, leading to increased radiation exposure and potential adverse effects.  
• Interference with Subsequent Treatments: indium In-111 capromab pendetide imaging may interfere with subsequent treatments, such as certain targeted or radionuclide therapies.

Pregnancy / Lactation

Pregnancy consideration: It is not advised to use in women. 

Lactation: It is not advised to use in women. 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

The pharmacology of indium In-111 capromab pendetide (ProstaScint®) involves its use as a diagnostic radiopharmaceutical agent for imaging prostate-specific membrane antigen (PSMA)-expressing prostate cancer cells.  

• Radiopharmaceutical Agent: indium In-111 capromab pendetide is a radiopharmaceutical composed of a monoclonal antibody (7E11-C5.3) coupled to the radionuclide indium-111. 
• Targeting PSMA: The monoclonal antibody component of indium in-111 capromab pendetide specifically targets and binds to PSMA, a protein highly expressed on the surface of prostate cancer cells. 
• Gamma Emissions: indium-111 is a gamma-emitting radionuclide. Once bound to PSMA-expressing prostate cancer cells, the indium-111 emits gamma radiation. 
• Scintigraphy: The gamma emissions from indium In-111 capromab pendetide can be detected by a gamma camera or other nuclear medicine imaging devices using scintigraphy, a type of nuclear medicine imaging. 
• Diagnostic imaging: indium In-111 capromab pendetide is administered intravenously for nuclear medicine imaging in patients with suspected or confirmed prostate cancer. The gamma emissions from the radiopharmaceutical allow for the detection and localization of PSMA-expressing prostate cancer cells. 

Pharmacodynamics:  

The pharmacodynamics of indium In-111 capromab pendetide involves its specific interactions with prostate-specific membrane antigen (PSMA)-expressing prostate cancer cells and the effects of gamma radiation emitted by the attached indium-111 radionuclide. 

Pharmacokinetics: 

Absorption 

indium In-111 capromab pendetide is administered intravenously, typically as an injection into the bloodstream. It is radiopharmaceutical and is not absorbed through the gastrointestinal tract like conventional drugs. 

Distribution 

The volume of distribution (Vd) of the drug ranges from approximately 2 to 6 liters (L).  

Metabolism 

The drug undergoes decay by electron capture during its metabolism. Electron capture is a type of radioactive decay where an electron is captured by a proton-rich nucleus, transforming the nucleus and releasing radiation.  

Elimination and Excretion 

The drug has two half-life values: a physical half-life of 67.2 hours and a terminal half-life of approximately 56 to 78 hours. The drug is primarily excreted in the urine, with approximately 10% of the administered dose being eliminated over 72 hours. 

Adminstartion

Administration: 

Intravenous administration 

• Administer for at least 5 minutes. Do not combine with other drugs.  
• For each imaging session lasting 72 to 120 hours, provide a cathartic the night before and a cleaning enema just before the imaging.  
• Catheterization and irrigation of the bladder are also recommended.  
• Approximately 30 minutes after the infusion should pass before the first imaging session. Two to four hours following the infusion should pass before the second imaging session. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: indium In-111 capromab pendetide 

Why do we use indium In-111 capromab pendetide? 

indium In-111 capromab pendetide is a radiopharmaceutical used for specific diagnostic purposes in prostate cancer. Its primary clinical use is for imaging and staging prostate cancer, particularly in cases where conventional imaging techniques have limitations. The primary uses of indium In-111 capromab pendetide are as follows: 

• Imaging of Prostate Cancer: indium In-111 capromab pendetide is used to detect and visualize prostate cancer cells that express prostate-specific membrane antigens (PSMA). PSMA is a protein highly expressed on the surface of prostate cancer cells but is not typically found in significant amounts in normal tissues.  
• Detection of Recurrent Prostate Cancer: The radiopharmaceutical is particularly useful in suspected recurrent prostate cancer cases, especially when prostate-specific antigen (PSA) levels rise after initial therapy.  
• Staging of Prostate Cancer: For patients with newly diagnosed prostate cancer, indium In-111 capromab pendetide imaging aids in staging the disease.  
• Assessment of Metastatic Disease: indium In-111 capromab pendetide can be used to assess the extent and distribution of metastatic prostate cancer, helping to guide treatment decisions and monitoring disease progression.