II. Indications
- Bladder Cancer (BCG refractory, non-surgical candidate)
III. Mechanism
- See Antibiotic Chemotherapy
-
Anthracycline Antibiotic with antineoplastic activity
- Semisynthetic derivative of Doxorubicin
- Valrubicin is metabolized intracellularly to N-trifluoroacetyladriamycin (AD32)
- AD32 binds topoisomerase 2
- Inhibits DNA Replication and repair
- Inhibits RNA and Protein synthesis
- Cell Cycle arrested in G2 phase
- AD32 also inhibits Protein kinase C (PKC) in the cell cytoplasm
- AD32 binds topoisomerase 2
- Valrubicin is also effective when applied topically
- High tissue penetration
- Valrubicin (like Idarubicin) is highly lipophilic
- Allows Valrubicin to more easily cross cell membranes (more than other Anthracyclines)
- Valrubicin accumulates in cytoplasm more than other Anthracyclines
IV. Medications
- Valrubicin intravesical solution: 40 mg/ml in 5 ml vials
V. Dosing
- See other references for disease specific dosing protocols
- Instill 800 mg (four 5 ml vials) once weekly for 6 weeks
- Fluid should be retained in Bladder for 2 hours
VI. Pharmacokinetics
- Excreted unchanged in the urine
VII. Adverse Effects
- Less cardiotoxicity than Doxorubicin
- Bladder Irritability
- Alopecia
- Urine Discoloration (transient red coloration)
VIII. Safety
- Avoid in Lactation
- Avoid in pregnancy (all trimesters)
- Use reliable Contraception
IX. Efficacy
X. Resources
- Valrubicin Intravesical Solution (DailyMed)