PLUVICTO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for PLUVICTO (PLUVICTO).
Lutetium Lu 177 vipivotide tetraxetan is a radioligand therapeutic agent that binds to prostate-specific membrane antigen (PSMA), which is overexpressed on prostate cancer cells. After binding, the radioactive isotope lutetium-177 emits beta particles, causing DNA damage and cell death.
| Metabolism | Lutetium Lu 177 vipivotide tetraxetan undergoes minimal metabolism; it is primarily cleared via renal excretion as the intact drug. |
| Excretion | Primarily renal; approximately 60% of administered radioactivity excreted in urine within 24 hours, with gradual elimination thereafter. Biliary/fecal excretion accounts for <15%. |
| Half-life | Effective half-life of lutetium-177 is approximately 160 hours (6.67 days), reflecting both physical decay (T1/2 6.647 days) and biological clearance. Clinical context: Due to physical decay, therapeutic radioactivity decreases to <1% after about 45 days. |
| Protein binding | Approximately 43% bound to plasma proteins (mainly albumin and transferrin) in vitro. Binding is reversible and moderate. |
| Volume of Distribution | Mean Vd ~0.4 L/kg (range 0.2–0.6 L/kg), indicating distribution predominantly in extracellular fluid with some tissue binding. Large Vd suggests accumulation in PSMA-expressing tissues and reticuloendothelial system. |
| Bioavailability | Not applicable; administered exclusively as IV infusion. Oral bioavailability is zero. |
| Onset of Action | IV administration: Radiopharmaceutical uptake in target tissues occurs within minutes; radiation-induced DNA damage initiates within hours. Clinical response (PSA decline, symptom improvement) typically observed within 4–12 weeks. |
| Duration of Action | Radiation exposure to tissues continues during the physical half-life of 6.647 days. Treatment cycles are administered every 6 weeks (6–7 half-lives apart) to allow clearance and recovery. Clinical benefit may last months; cumulative toxicity (myelosuppression, renal) may persist longer. |
PLUVICTO (lutetium Lu 177 vipivotide tetraxetan) is administered intravenously at a dose of 7.4 GBq (200 mCi) every 6 weeks for up to 6 doses, in combination with a gonadotropin-releasing hormone (GnRH) analog or after prior unilateral orchiectomy.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment is recommended for mild (creatinine clearance [CrCl] 60–89 mL/min) or moderate (CrCl 30–59 mL/min) renal impairment. PLUVICTO has not been studied in patients with severe renal impairment (CrCl <30 mL/min) or end-stage renal disease; dosing recommendations cannot be provided. |
| Liver impairment | No formal studies have been conducted in patients with hepatic impairment. No dose adjustment is recommended for mild (Child-Pugh class A) or moderate (Child-Pugh class B) hepatic impairment. PLUVICTO has not been studied in patients with severe hepatic impairment (Child-Pugh class C); dosing recommendations cannot be provided. |
| Pediatric use | The safety and effectiveness of PLUVICTO in pediatric patients have not been established. No dosing recommendations can be made. |
| Geriatric use | Of the 735 patients treated with PLUVICTO in the VISION trial, 54% were ≥65 years of age and 16% were ≥75 years of age. No overall differences in safety or efficacy were observed between these patients and younger patients. No dose adjustment is recommended based on age. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for PLUVICTO (PLUVICTO).
| Breastfeeding | It is unknown whether PLUVICTO is excreted in human milk or if it affects milk production. Because of the potential for serious adverse reactions from radiation exposure in breastfed infants, women are advised not to breastfeed during treatment and for at least 7 months after the last dose. No M/P ratio available. |
| Teratogenic Risk | PLUVICTO (lutetium Lu 177 vipivotide tetraxetan) is a radioactive therapeutic agent. It emits beta and gamma radiation, and radiation exposure is associated with teratogenesis. Risk is highest during the first trimester when organogenesis occurs. Use is contraindicated in pregnancy. Fetal harm is expected if administered to a pregnant woman. No human data available; animal studies have not been conducted but based on mechanism, teratogenic risk is high across all trimesters. |
■ FDA Black Box Warning
None.
| Serious Effects |
["None known."]
| Precautions | ["Radiation exposure to patients and caregivers","Bone marrow suppression including anemia, thrombocytopenia, leukopenia, and neutropenia","Renal toxicity","Fertility impairment","Infertility","Secondary malignancies"] |
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| Fetal Monitoring | For women of reproductive potential, a pregnancy test should be performed prior to initiating therapy. Due to radiation exposure, fetal monitoring is not applicable as use is contraindicated in pregnancy. For non-pregnant patients, monitor complete blood counts and renal function periodically. |
| Fertility Effects | PLUVICTO may impair fertility in both males and females due to radiation effects on gonads. In males, it may cause oligospermia, azoospermia, and permanent infertility. In females, it may cause ovarian failure and premature menopause. Prior to treatment, fertility preservation options should be discussed. |