Metabolic profile of [14C]bendamustine in rat urine and bile: Preliminary structural identification of metabolites

Drug Metabolism and Disposition

Volumn 35, Issue 10, 2007, Pages 1744-1753

  Chovan, James P ^a   Li, Feng ^a   Yu, Erya ^a   Ring, Steven C ^a  

^a CEPHALON INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALKYLATING AGENT; ANTINEOPLASTIC AGENT; BENDAMUSTINE; CARBON 14; DRUG METABOLITE;

ANIMAL EXPERIMENT; ARTICLE; BILIARY EXCRETION; CANCER CHEMOTHERAPY; DRUG BILE LEVEL; DRUG METABOLISM; DRUG STRUCTURE; DRUG URINE LEVEL; HEMATOPOIETIC SYSTEM TUMOR; ISOTOPE LABELING; LIQUID CHROMATOGRAPHY; MALE; MASS SPECTROMETER; NONHUMAN; PRIORITY JOURNAL; RADIOACTIVITY; RAT; URINARY EXCRETION;

ACETYLCYSTEINE; ANIMALS; ANTINEOPLASTIC AGENTS; BILE; DEALKYLATION; GLUTATHIONE; MALE; NITROGEN MUSTARD COMPOUNDS; RATS; RATS, SPRAGUE-DAWLEY;

RATTUS;

EID: 34748858790     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.107.015958     Document Type: Article

References (8)

1. Bezek S, Scasnar V, Trnovec T, and Grupe R (1991) Hepatobiliary elimination of bendamustine (Cytostasan) in rats. Pharmazie 46:810-811.
2. Gandhi V (2002) Metabolism and mechanism of action of bendamustine: rationales for combination therapies. Semin Oncol 29:4-11.
3. Hinchman CA and Ballatori N (1994) Glutathione conjugation and conversion to mercapturic acids can occur as an intrahepatic process. J Toxicol Environ Health 41:387-409.
4. Pönisch W, Mitrou PS, Merkle K, Herold M, Assmann M, Wilhelm G, Dachselt K, Richter P, Schirmer V, Schulze A, et al. (2006) Treatment of bendamustine and prednisone in patients with newly diagnosed multiple myeloma results in superior complete response rate, prolonged time to treatment failure and improved quality of life compared with treatment with melphalan and prednisone: a randomized phase III study of the East German Study Group of Hematology and Oncology (OSHO). J Cancer Res Clin Oncol 132:205-212.
5. Smith MB and March J (2001) Advanced Organic Chemistry, pp 773-775, Wiley-Interscience, New York.
6. Teichert J, Baumann F, Chao Q, Franklin C, Bailey B, Hennig L, Caca K, Schoppmeyer K, Patzak U, and Preiss R (2007) Characterization of two phase I metabolites of bendamustine in human liver microsomes and in cancer patients treated with bendamustine hydrochloride. Cancer Chemother Pharmacol 59:759-770.
7. Teichert J, Sohr R, Baumann F, Henning L, Merkle K, Caca K, and Preiss R (2005) Synthesis and characterization of some new phase II metabolites of the alkylator bendamustine and their identification in human bile, urine, and plasma from patients with cholangiocarcinoma. Drug Metab Dispos 33:984-992.
8. Weber H, Amlacher R, Preiss R, and Hoffmann H (1991) Pharmacokinetics of bendamustine (Cytostasan) in B6D2F1-mice. Pharmazie 46:589-591.