POSLUMA
Clinical safety rating
cautionComprehensive clinical and safety monograph for POSLUMA (POSLUMA).
PSMA-targeted radiotherapeutic agent; emits beta radiation causing DNA damage and cell death in PSMA-expressing cells.
| Metabolism | Predominantly excreted renally; no significant hepatic metabolism. |
| Excretion | Renal: 0% (not significantly eliminated via kidneys); Biliary/Fecal: predominantly eliminated via hepatobiliary system with fecal excretion of intact complex and metabolites, though precise % not established for human. |
| Half-life | Terminal elimination half-life: approximately 25–30 minutes for [68Ga]Ga-PSMA-11; rapid clearance from blood pool due to renal and hepatobiliary elimination. |
| Protein binding | Approximately 30–40% bound to plasma proteins (albumin minimally implicated; major binding to serum proteins not fully characterized). |
| Volume of Distribution | Central Vd ~ 0.2–0.3 L/kg (limited extravascular distribution; primarily confined to blood pool and highly perfused organs); high uptake in kidney, liver, spleen, salivary glands. |
| Bioavailability | Intravenous: 100% (only route of administration). |
| Onset of Action | Intravenous: Diagnostic imaging agent; accumulation in PSMA-expressing tissues within minutes; optimal imaging at 60–120 minutes post-injection. |
| Duration of Action | Duration sufficient for PET imaging (scan acquisition performed 60–120 minutes post-injection); no prolonged therapeutic effect. |
| Molecular Weight | 1211.08 |
1.85 MBq (0.05 mCi)/kg intravenously as a single injection, followed by PET imaging approximately 60 minutes post-injection.
| Dosage form | SOLUTION |
| Renal impairment | No formal dose adjustment recommendations; use with caution in severe renal impairment (eGFR <30 mL/min) due to potential increased radiation exposure. |
| Liver impairment | No specific dose adjustment guidelines; no data in Child-Pugh classes. |
| Pediatric use | No approved pediatric indication; safety and efficacy not established in patients <18 years. |
| Geriatric use | No specific dose adjustment; consider age-related renal function decline and monitor for adverse effects. |
| 1st trimester | Use during first trimester is contraindicated due to risk of fetal harm from radiation exposure; consider alternative diagnostic methods. |
| 2nd trimester | Use during second trimester is contraindicated due to fetal radiation exposure; alternative imaging preferred. |
| 3rd trimester | Use during third trimester is contraindicated due to risk of fetal radiation exposure; alternative imaging preferred. |
Clinical note
Comprehensive clinical and safety monograph for POSLUMA (POSLUMA).
| Placental transfer | Gallium-68 PSMA-11 crosses the placenta; degree of transfer not quantified in humans, but expected due to small molecular weight and PSMA expression in placenta. |
| Breastfeeding | Breastfeeding should be discontinued for at least 48 hours after administration to minimize infant exposure to radiation; pump and discard milk during this period. |
| Lactation Rating | Avoid |
| Teratogenic Risk | POSLUMA (flortaucipir F 18) is a radioactive diagnostic agent. No human studies on fetal harm. Animal studies not conducted. All radiopharmaceuticals carry potential risk to fetus; radiation dose may cause fetal harm, especially during organogenesis (first trimester). Use only if benefit outweighs risk. Second and third trimester: lower risk but still consider cumulative radiation exposure. |
| Fetal Monitoring | Monitor for hypersensitivity reactions during administration. In pregnant women, ensure justification of radiation exposure; consider alternative imaging if possible. No specific maternal or fetal monitoring required beyond standard radiopharmaceutical administration precautions. |
| Fertility Effects | No human or animal data on fertility effects. Radiation exposure from diagnostic doses is unlikely to cause permanent infertility, but repeated high doses may theoretically affect gonadal function. Advise counseling for planned pregnancy. |
■ FDA Black Box Warning
None.
| Serious Effects |
Hypersensitivity to gallium-68 or any component of the productPregnancy
| Precautions | Bone marrow suppression: Grade 3-4 thrombocytopenia, neutropenia, and anemia reported. Monitor blood counts., Renal toxicity: Acute kidney injury and renal failure. Monitor renal function prior to and during therapy., Hypersensitivity reactions: Monitor for signs and symptoms., Radiation risks: Radiation exposure to patients, family, and healthcare providers; advise precautions. |
| Food/Dietary | No specific food interactions. Maintain adequate hydration before and after administration. No fasting required. |
| Clinical Pearls | POSLUMA (Flotufolastat F 18) is a radioactive diagnostic agent for PSMA PET imaging in prostate cancer. Administer as an IV bolus (3-7 mCi) followed by saline flush. Image 1-2 hours post-injection. No special patient preparation needed; assess for ability to lie still. Evaluate injection site for extravasation to avoid image artifacts. Report all adverse reactions to FDA MedWatch. |
| Patient Advice | This drug is a radioactive dye for PET scans to detect prostate cancer. · You will receive an injection into a vein, then wait about 1-2 hours before scanning. · Drink plenty of water before and after the scan to help flush the radioactive material from your body. · Tell your healthcare team if you are pregnant, breastfeeding, or have any allergies. · After the scan, avoid close contact with pregnant women and infants for several hours. · The radiation exposure is low and similar to other nuclear medicine tests. |
Loading safety data…