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Valrubicin

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Valrubicin, Valstar

  • See Also
  1. Antibiotic Chemotherapy
  2. Chemotherapy
  • Indications
  1. Bladder Cancer (BCG refractory, non-surgical candidate)
  • Mechanism
  1. See Antibiotic Chemotherapy
  2. Anthracycline Antibiotic with antineoplastic activity
    1. Semisynthetic derivative of Doxorubicin
  3. Valrubicin is metabolized intracellularly to N-trifluoroacetyladriamycin (AD32)
    1. AD32 binds topoisomerase 2
      1. Inhibits DNA Replication and repair
      2. Inhibits RNA and Protein synthesis
      3. Cell cycle arrested in G2 phase
    2. AD32 also inhibits Protein kinase C (PKC) in the cell cytoplasm
  4. Valrubicin is also effective when applied topically
    1. High tissue penetration
  5. Valrubicin (like Idarubicin) is highly lipophilic
    1. Allows Valrubicin to more easily cross cell membranes (more than other Anthracyclines)
    2. Valrubicin accumulates in cytoplasm more than other Anthracyclines
  • Medications
  1. Valrubicin intravesical solution: 40 mg/ml in 5 ml vials
  • Dosing
  1. See other references for disease specific dosing protocols
  2. Instill 800 mg (four 5 ml vials) once weekly for 6 weeks
    1. Fluid should be retained in Bladder for 2 hours
  • Pharmacokinetics
  1. Excreted unchanged in the urine
  • Adverse Effects
  1. Less cardiotoxicity than Doxorubicin
  2. Bladder Irritability
  3. Alopecia
  4. Urine Discoloration (transient red coloration)
  • Safety
  1. Avoid in Lactation
  2. Avoid in pregnancy (all trimesters)
    1. Use reliable Contraception
  • Efficacy
  1. Curative in <20% of Bladder Cancers
    1. Dinney (2013) Urol Oncol 31(8):1635-42 +PMID: 22575238 [PubMed]
    2. Steinberg (2000) J Urol 163(3):761-7 +PMID: 10687972 [PubMed]
  • Resources
  1. Valrubicin Intravesical Solution (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=e96f30a0-6662-11de-8f80-0002a5d5c51b