PROSTASCINT
Clinical safety rating
cautionComprehensive clinical and safety monograph for PROSTASCINT (PROSTASCINT).
PROSTASCINT is a murine monoclonal antibody fragment (capromab pendetide) conjugated to the chelating agent glycyl-tyrosyl-lysyl-diethylenetriaminepentaacetic acid (GYK-DTPA) and labeled with indium-111. It binds to the intracellular epitope of prostate-specific membrane antigen (PSMA) expressed on prostate epithelial cells and is used for imaging prostate cancer.
| Metabolism | Capromab pendetide is a monoclonal antibody fragment; metabolism is via catabolism to amino acids and small peptides. The indium-111 label is not metabolized and decays physically. |
| Excretion | Renal: ~90% (predominantly as intact tracer), Fecal: <5% |
| Half-life | Terminal elimination half-life: 2.6 ± 0.7 days (requires 2 weeks for complete clearance; used for radioimmunodetection within 5–7 days post-injection) |
| Protein binding | ~90% (binding to plasma proteins, likely immunoglobulins and albumin) |
| Volume of Distribution | 5.5 L (not weight-adjusted; approximates intravascular space with slow distribution to extravascular tumor sites) |
| Bioavailability | IV: 100% (not administered via other routes) |
| Onset of Action | IV: Localization in tumor sites detectable by gamma camera within 24–48 hours (maximal target-to-background ratios at 5–7 days) |
| Duration of Action | IV: Tracer remains detectable in tumor tissue up to 14 days; optimal imaging window 5–7 days post-administration |
| Molecular Weight | 150000 |
5 mCi (185 MBq) intravenously over 5 minutes, single dose.
| Dosage form | VIAL |
| Renal impairment | No specific dose adjustment recommended; caution in severe renal impairment (GFR <30 mL/min) due to potential radiation clearance delay. |
| Liver impairment | No specific adjustment for Child-Pugh class; caution in severe hepatic impairment due to altered clearance. |
| Pediatric use | Safety and efficacy not established; not recommended for pediatric patients. |
| Geriatric use | No specific dose adjustment; follow standard adult dosing with consideration of renal function. |
| 1st trimester | Contraindicated due to risk of fetal harm from radiation exposure. |
| 2nd trimester | Contraindicated due to risk of fetal harm from radiation exposure. |
| 3rd trimester | Contraindicated due to risk of fetal harm from radiation exposure. |
Clinical note
Comprehensive clinical and safety monograph for PROSTASCINT (PROSTASCINT).
| Placental transfer | Expected to cross placenta due to low molecular weight and similarity to antibodies; direct exposure from radionuclide. |
| Breastfeeding | Discontinue breastfeeding due to potential radiation exposure to the infant via milk. |
| Lactation Rating | Avoid |
| Teratogenic Risk | PROSTASCINT (indium-111 capromab pendetide) is a murine monoclonal antibody labeled with indium-111 used for imaging. No adequate human data on fetal risk. Animal studies are not available. The radiopharmaceutical component emits radiation; fetal radiation exposure may increase the risk of congenital anomalies and childhood malignancies. Use in pregnant women is contraindicated unless potential benefit outweighs risks. First trimester exposure poses highest risk of teratogenesis; second and third trimester exposure may increase risk of childhood cancer. |
| Fetal Monitoring | Maternal: Monitor for allergic or hypersensitivity reactions (e.g., rash, urticaria, anaphylaxis) during and after infusion. Fetal: If inadvertently administered during pregnancy, assess fetal radiation dose estimate and consult radiation safety officer. Fetal monitoring for growth and development if exposure occurred. |
| Fertility Effects | Indium-111 capromab pendetide is a radiopharmaceutical. Animal reproductive studies have not been conducted. Radiation exposure can damage gonadal tissues, potentially impairing fertility in both males and females. The effect is dose-dependent; diagnostic doses are low but may carry a small risk of transient or permanent infertility. No specific human data on fertility effects. |
■ FDA Black Box Warning
Not applicable.
| Serious Effects |
Hypersensitivity to capromab pendetide or any componentPregnancyBreastfeeding
| Precautions | Risk of hypersensitivity reactions, including anaphylaxis, Use of murine antibodies may cause human anti-mouse antibody (HAMA) response, potentially affecting subsequent murine antibody-based diagnostics or therapeutics, Radiation exposure from indium-111; risk of secondary malignancies, Limited data in patients with renal impairment |
| Food/Dietary | No known food interactions. Maintain adequate hydration; no dietary restrictions required. |
| Clinical Pearls | Prostascint (capromab pendetide) is a radiolabeled monoclonal antibody used for imaging prostate-specific membrane antigen (PSMA) in patients with prostate cancer. For optimal imaging, allow 72 hours post-injection for clearance of unbound antibody. Use with caution in patients with known murine protein allergy; pre-medicate with antihistamines if prior reaction. False-positive scans may occur in benign prostatic hyperplasia or inflammation. Ensure adequate hydration to promote renal excretion of the radiopharmaceutical. |
| Patient Advice | This drug is a radioactive imaging agent that helps detect the spread of prostate cancer. · You will receive a single intravenous injection before your scan. · Drink plenty of water after the injection to help clear the radioactive material from your body. · Avoid close contact with pregnant women and young children for 24 hours after the scan. · Inform your doctor if you have had allergic reactions to mouse proteins or previous monoclonal antibody therapy. |
Loading safety data…