Drug Class: Anthracycline (rubicin derivative)
Use: Intravesical treatment of Bacillus Calmette-Guérin (BCG)-refractory carcinoma in situ (CIS) of the bladder in patients who are not candidates for cystectomy.
Mechanism of Action:
Valrubicin is a lipophilic anthracycline that interferes with DNA replication and RNA transcription by intercalating into DNA and inhibiting topoisomerase II. This leads to apoptosis of malignant urothelial cells.
Administration:
- Intravesical only (direct instillation into the bladder)
- Dose: 800 mg in 75 mL, once weekly for 6 weeks
- Minimal systemic absorption when given intravesically
- Metabolized hepatically; excreted mainly in urine
Common Side Effects:
- Local bladder irritation (dysuria, hematuria, urinary frequency)
- No systemic anthracycline toxicities (e.g., cardiotoxicity) due to poor absorption
Clinical Pearls:
- Not for IV use – strictly intravesical
- Red-colored solution, like other anthracyclines
- Handle with usual cytotoxic precautions
- Considered when BCG fails and surgery is not an option