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Valrubicin
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DRUG INFO
Valrubicin
Drug Name:
Valrubicin
Indication: Bladder cancer
Pharmacology: When 800 mg Valstar was administered intravesically to patients with carcinoma in situ, Valstar penetrated into the bladder wall. The mean total anthracycline concentration measured in bladder tissue exceeded the levels causing 90% cytoxicity to human bladder cells cultured in vitro. During the two-hour dose-retention period, the metabolism of Valstar to its major metabolites N-trifluoroacetyladriamycin and N-trifluoroacetyladriamycinol was neglible. After retention, the drug was almost completely excreted by voiding the instillate. Mean percent recovery of Valstar, N-trifluoroacetyladriamycin, and total anthracyclines in 14 urine samples from six patients was 98.6%, 0.4%, and 99.0% of the total administered drug, respectively. During the two-hour dose-retention period, only nanogram quantities of Valstar were absorbed into the plasma.
Mechanism Of Action: Valrubicin 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 Category: Antineoplastic Agents; ATC:L01DB09
Brand Names/Synonyms: AD 32; Antibiotic Ad 32; Valrubicin; Valrubicin [Usan]; Valstar; Valstar Preservative Free
Dosage Forms: LIQUID
Absorption: Not Available
Interactions:
DrugBank: Interactions for Valrubicin
Interactions for Valrubicin:
Because systemic exposure to ValstarÔ is negligible following intravesical
administration, the potential for drug interactions is low. No drug interaction studies were conducted.
Chemical IUPAC Name: [2-oxo-2-[2,5,12-trihydroxy-4-[5-hydroxy-6-methyl-4-(2,2,2-trifluoroacetyl)amino-tetrahydropyran-2-yl]oxy-7-methoxy-6,11-dioxo-1,2,3,4-tetrahydrotetracen-2-yl]-ethyl]pentanoate
Chemical Formula: C34H36F3NO13
Half Life: Not Available
Drug Type: Approved Drug
# Accession No: APRD00662
CAS Registry Number: 56124-62-0
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