Valrubicin drug data and news

Valrubicin drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Valrubicin
Brand Names/Synonyms AD 32; Antibiotic Ad 32; Valrubicin; Valrubicin [Usan]; Valstar; Valstar Preservative Free
Indication Bladder cancer
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Description Not Available
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.
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Dosage Forms LIQUID
Drug_Category Antineoplastic Agents; ATC:L01DB09
Absorption Not Available
Interactions -->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.

Toxicity Not Available
Organisms Affected Humans and other mammals
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
Molecular Weight 723.644 g/mol
Smiles String CCCCC(=O)OCC(=O)C1(CC(C2=C(C3=C(C(=C2C1)O)C(=O)C4=C(C3=O)C(=CC=C4)OC)O)OC5CC(C(C(O5)C)O)NC(=O)C(F)(F)F)O
Melting Point 116-117°C
Water Solubility insoluble
State Solid
LogP/Hphobicity 3.332
Isoelectric Point Not Available
Biotransformation Not Available
Half Life Not Available
Protein Binding [%] >99%
RxList Link RXlist
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Drug Reference http://www.drugs.com/cons/Valrubicin.html
http://www.rxlist.com/cgi/generic2/rubicin.htm
Drug Type Approved Drug
Accession No APRD00662
CAS Registry Number 56124-62-0
KEGG Compound ID Not Available
PubChem ID SID:182424
PharmGKB ID PA451847
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2242466

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