Preclinical pharmacokinetics of KBF611, a new antituberculosis agent in mice and rabbits, and comparison with thiacetazone

Xenobiotica

Volumn 40, Issue 3, 2010, Pages 225-234

  Shahab, F M ^a   Kobarfard, F ^a   Shafaghi, B ^a   Dadashzadeh, S ^a  

^a SHAHID BEHESHTI UNIVERSITY OF MEDICAL SCIENCES   (Iran)

Author keywords

KBF611; Pharmacokinetics; Thiacetazone; Tuberculosis

Indexed keywords

4 ACETAMIDO 3 FLUOROBENAZLDEHYDE THIOSEMICARBAZONE; 4 AMINO 3 FLUOROBENZALDEHYDE THIOSEMICARBAZONE; DRUG METABOLITE; KBF 611; THIOACETAZONE; TUBERCULOSTATIC AGENT; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANTIBIOTIC THERAPY; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DEACETYLATION; DOSE RESPONSE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG DOSE COMPARISON; DRUG EXCRETION; DRUG HALF LIFE; DRUG METABOLISM; DRUG PROTEIN BINDING; DRUG PURIFICATION; DRUG STRUCTURE; DRUG SYNTHESIS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IN VIVO STUDY; LIQUID CHROMATOGRAPHY; LIVER METABOLISM; MALE; MASS SPECTROMETRY; MEAN RESIDENCE TIME; MOUSE; NONHUMAN; PLASMA CLEARANCE; PLASMA CONCENTRATION-TIME CURVE; RABBIT; SPECIES DIFFERENCE; STRUCTURE ACTIVITY RELATION; URINARY EXCRETION;

ACETYLATION; ADMINISTRATION, ORAL; ANIMALS; ANTITUBERCULAR AGENTS; BLOOD PROTEINS; DRUG EVALUATION, PRECLINICAL; INJECTIONS, INTRAVENOUS; MICE; PROTEIN BINDING; RABBITS; SPECIES SPECIFICITY; THIOACETAZONE; TIME FACTORS;

ANIMALIA; HUMAN IMMUNODEFICIENCY VIRUS; MUS; ORYCTOLAGUS CUNICULUS;

EID: 77149177377     PISSN: 00498254     EISSN: 13665928     Source Type: Journal    
DOI: 10.3109/00498250903461411     Document Type: Article

References (22)

1. Alahari A, Trivelli X, Guerardel Y, Dover LG, Besra GS, Sacchettini JC, Reynolds RC, Coxon GD, Kremer L. (2007). Thiacetazone, an antitubercular drug that inhibits cyclopropanation of cell wall mycolic acids in mycobacteria. PLoS ONE 2:e1343.
2. Bailer AJ. (1988). Testing for the equality of area under the curves when using destructive measurement techniques. J Pharmacokin Biopharm 16(3):303-309
3. Bermudez LE, Reynolds R, Kolonoski P, Aralar P, Inderlied CB, Young LS. (2003). Thiosemicarbazole (thiacetazone-like) compound with activity against Mycobacterium avium in mice. Antimicrob Agent Chemother 47:2685-2687
4. Cock KMD, Chaisson RE. (1999). Will DOTS do it? A reappraisal of tuberculosis control in countries with high rates of HIV infection. Int J Tuberculosis Lung Dis 3:457-465
5. Custodio JM, Wu CY, Benet LZ. (2008). Predicting drug disposition, absorption/elimination/transporter interplay and the role of food on drug absorption. Adv Drug Del Rev 60: 717-733
6. Dover LG, Alahari A, Gratraud P, Gomes JM, Bhowruth V, Reynolds RC, Besra GS, Kremer L. (2007). EthA, a common activator of thiocarbamide-containing drugs acting on different mycobacterial targets. Antimicrob Agent Chemother 51:1055-1063
7. Dukes CS, Sugarman J, Cegielski JP, Lallinger GJ, Mwakyusa DH. (1992). Severe cutaneous hypersensitivity reactions during treatment of tuberculosis in patients with HIV infection in Tanzania. Trop Geograph Med 44:308-311
8. Duncan K. (2003). Progress in TB drug development and what is still needed. Tuberculosis (Edinb) 83:201-207
9. Frieden TR, Sterling TR, Munsiff SS, Watt CJ, Dye C. (2003). Tuberculosis. Lancet 362:887-899
10. Gibaldi M, Perrier D. (1982). Pharmacokinetics, 2nd ed. New York, NY: Marcel Dekker.
11. Gupta RA, Gupta AK, Soni LK, Kaskhedikar SG. (2007). Rationalization of physicochemical characters of oxazolyl thiosemicarbazone analogs towards multi-drug resistant tuberculosis: a QSAR approach. Eur J Med Chem 42:1109-1116
12. Gupta UD, Katoch VM. (2005). Animal models of tuberculosis. Tuberculosis 85:277-293
13. Henderson MC, Siddens LK, Morre JT, Krueger SK, Williams DE. (2008). Metabolism of the anti-tuberculosis drug ethionamide by mouse and human FMO1, FMO2 and FMO3 and mouse and human lung microsomes. Toxicol Appl Pharmacol 233:420-427
14. Ipuge YAI, Rieder HL, Enarson DA. (1995). Adverse cutaneous reactions to thiacetazone for tuberculosis treatment in Tanzania. Lancet 346(8976):657-660
15. Janmohamed A, Hernandez D, Phillips IR, Shephard EA. (2004). Cell-, tissue-, sex- and developmental stage-specific expression of mouse flavin-containing monooxygenases (FMOs). Biochem Pharmacol 68:73-83.
16. Kirishna R, Yu L. (2007). Biopharmaceutics applications in drug development. New York, NY: Springer. p. 1-25.
17. Kobarfard F, Kauffman JM. (2003). Halogenated antituberculosis agents. US Patent 6624153 B2.
18. Orme I M. (2003). The mouse model as a useful model of tuberculosis. Tuberculosis 83:112-115
19. Peloquin CA, Nitta AT, Berning SE, Iseman MD, James GT. (1996). Pharmacokinetic evaluation of thiacetazone. Pharmacotherapy 16:735-741
20. Qian L, Ortiz de Montellano PR. (2006). Oxidative activation of thiacetazone by the Mycobacterium tuberculosis flavin monooxygenase EtaA and human FMO1 and FMO3. Chem Res Toxicol 19:443-449
21. Shahab FM, Kobarfard F, Dadashzadeh S. (2009). Simultaneous determination of a new antituberculosis agent KBF-611 and its de-acetylated metabolite in mouse and rabbit plasma by HPLC: application to preclinical pharmacokinetics. Arch Pharm Res 32:1453-1460
22. Vannelli TA, Dykman A, Ortiz de Montellano PR. (2002). The antituberculosis drug ethionamide is activated by a flavoprotein monooxygenase. J Biol Chem 277:12824-12829