Valstar
Valstar - General Information
Valstar (N-trifluoroacetyladriamycin-14-valerate, Valstar®) is a chemotherapy drug used to treat bladder cancer. Valstar is a semisynthetic analog of the anthracycline doxorubicin, and is administered by infusion directly into the bladder. [Wikipedia]
Pharmacology of Valstar
Valstar is a semisynthetic analog of the anthracycline doxorubicin, and is administered by infusion directly into the bladder.
Valstar for patients
Patients should be informed that ValstarÔ has been shown to induce complete responses in only about 1 in 5 patients, and that delaying cystectomy could lead to development of metastatic bladder cancer, which is lethal. They should discuss with their physician the relative risk of cystectomy versus the risk of metastatic bladder cancer and be aware that the risk increases the longer cystectomy is delayed in the presence of persisting CIS.
Patients should be informed that the major acute toxicities from ValstarÔ are related to irritable bladder symptoms that may occur during instillation and retention of ValstarÔ and for a limited period following voiding. For the first 24 hours following administration, red tinged urine is typical. Patients should report prolonged irritable bladder symptoms or prolonged passage of red-colored urine immediately to their physician.
Women of child-bearing potential should be advised not to become pregnant during treatment. Men should be advised to refrain from engaging in procreative activities while receiving therapy with ValstarÔ. All patients of reproductive age should be advised to use an effective contraception method during the treatment period.
Valstar Interactions
Because systemic exposure to ValstarÔ is negligible following intravesical administration, the potential for drug interactions is low. No drug interaction studies were conducted.
Valstar Contraindications
ValstarÔ is contraindicated in patients with known hypersensitivity to anthracyclines or CremophorÒEL (polyoxyethyleneglycol triricinoleate).
Patients with concurrent urinary tract infections should not receive ValstarÔ.
ValstarÔ should not be administered to a patient with a small bladder capacity, i.e., unable to tolerate a 75 mL instillation.
Additional information about Valstar
Valstar Indication: For the treatment of cancer of the bladder.
Mechanism Of Action: Valstar is an anthracycline that affects a variety of inter-related biological functions, most of which involve nucleic acid metabolism. It readily penetrates into cells, where it inhibits the incorporation of nucleosides into nucleic acids, causes extensive chromosomal damage, and arrests cell cycle in G2. Although valrubicin does not bind strongly to DNA, a principal mechanism of its action, mediated by valrubicin metabolites, is interference with the normal DNA breaking-resealing action of DNA topoisomerase II.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Valrubicin
Synonyms: Antibiotic Ad 32
Drug Category: Antineoplastic Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Valrubicin: Valstar; Valstar Preservative Free;
Absorption: Not Available
Toxicity (Overdose): The primary anticipated complications of overdosage associated with intravesical administration would be consistent with irritable bladder symptoms. Myelosuppression is possible if valrubicin is inadvertently administered systemically or if significant systemic exposure occurs following intravesical administration (e.g., in patients with bladder/rupture perforation). The maximum tolerated dose in humans by either intraperitoneal or intravenous administration is 600 mg/m2.
Protein Binding: >99%
Biotransformation: Valrubicin is metabolized to two primary metabolites: N-trifluoroacetyladriamycin and N-trifluoroacetyladriamycinol.
Half Life: Not Available
Dosage Forms of Valstar: Liquid Intravesical
Chemical IUPAC Name: [2-oxo-2-[(2S,4S)-2,5,12-trihydroxy-4-[5-hydroxy-6-methyl-4-[(2,2,2-trifluoroacetyl)amino]oxan-2-yl]oxy-7-methoxy-6,11-dioxo-3,4-dihydro-1H-tetracen-2-yl]ethyl] pentanoate
Chemical Formula: C34H36F3NO13
Valrubicin on Wikipedia: https://en.wikipedia.org/wiki/Valrubicin
Organisms Affected: Humans and other mammals
