II. Indications

  1. Bladder Cancer (BCG refractory, non-surgical candidate)

III. 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

IV. Medications

  1. Valrubicin intravesical solution: 40 mg/ml in 5 ml vials

V. 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

VI. Pharmacokinetics

  1. Excreted unchanged in the urine

VII. Adverse Effects

  1. Less cardiotoxicity than Doxorubicin
  2. Bladder Irritability
  3. Alopecia
  4. Urine Discoloration (transient red coloration)

VIII. Safety

  1. Avoid in Lactation
  2. Avoid in pregnancy (all trimesters)
    1. Use reliable Contraception

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Ontology: valrubicin (C0068314)

Definition (NCI_NCI-GLOSS) A drug used to treat bladder cancer that does not respond to BCG (Bacillus Calmette Guerin). It is an anthracycline and is a type of antitumor antibiotic.
Definition (NCI) A semisynthetic derivative of the antineoplastic anthracycline antibiotic doxorubicin. With a mechanism of action that appears to differ from doxorubicin, valrubicin is converted intracytoplasmically into N-trifluoroacetyladriamycin, which interacts with topoisomerase II, stabilizing the complex between the enzyme and DNA; consequently, DNA replication and repair and RNA and protein synthesis are inhibited and the cell cycle is arrested in the G2 phase. In addition, this agent accumulates in the cell cytoplasm where it inhibits protein kinase C (PKC). Valrubicin is less cardiotoxic than doxorubicin when administered systemically; applied topically, this agent shows excellent tissue penetration. Structurally, the trifluoro-acetyl moiety on the amino group of the glycoside and the valerate moiety appear to result in a lipophilicity that is greater than of doxorubicin, resulting in increased intracytoplasmic concentrations.
Concepts Organic Chemical (T109) , Antibiotic (T195)
MSH C016163
SnomedCT 116079002, 387002006
English (2S-cis)-pentanoic acid, 2-(1,2,3,4,6,11-hexahydro-2,5,12-trihydroxy-7-methoxy-6,11-dioxo-4-((2,3,6-trideoxy-3-((trifluoroacetyl)amino)-alpha-L-lyxo-hexopyranosyl)oxy)-2-naphth acenyl)-2-oxoethyl ester, N-Trifluoroacetyladriamycin-14-valerate, N-trifluoroacetyladriamycin-14-valerate, valrubicin (medication), valrubicin, VALRUBICIN, valrubicin [Chemical/Ingredient], Valrubicin (product), Valrubicin (substance), Valrubicin, N-trifluoroacetyladriamycin 14-valerate
Spanish valrrubicina (producto), valrrubicina, valrubicina (producto), valrubicina (sustancia), valrubicina, valrrubicina (sustancia)