Role of P-Glycoprotein in intestinal absorption of FB2, a promising Abl/Src dual tyrosine kinase inhibitor

Drug Metabolism and Pharmacokinetics

Volumn 27, Issue 5, 2012, Pages 486-494

  Huang, Kai ^a   Hu, Jinping ^a   Li, Xue ^a   Li, Yan ^a  

^a INSTITUTE OF MATERIA MEDICA   (China)

Author keywords

Caco 2 cell; FB2; MDCK MDR1 cell; Pharmacokinetic; Single pass intestinal perfusion

Indexed keywords

ATENOLOL; DRUG METABOLITE; FB 2; GLYCOPROTEIN P INHIBITOR; METOPROLOL; MULTIDRUG RESISTANCE PROTEIN; PROTEIN TYROSINE KINASE INHIBITOR; UNCLASSIFIED DRUG; VERAPAMIL;

ANIMAL CELL; ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CELL STRAIN; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG STRUCTURE; DRUG TRANSPORT; FIRST PASS EFFECT; IN VITRO STUDY; IN VIVO STUDY; INTESTINE ABSORPTION; INTESTINE PERFUSION; MALE; MAXIMUM PLASMA CONCENTRATION; MEAN RESIDENCE TIME; MESENTERY; NONHUMAN; RAT; SINGLE DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION;

EID: 84869131339     PISSN: 13474367     EISSN: 18800920     Source Type: Journal    
DOI: 10.2133/dmpk.DMPK-11-RG-142     Document Type: Article

References (31)

1. Liu, H., Li, H., Feng, Z., Tai, J., Meng, Y., Wang, H., Xin, H., Zhang, S., Zuo, M., Zhang, Y. and Chen, X.: Activity of FB2, a novel dual Abl/Src tyrosine kinase inhibitor, against imatinibresistant chronic myeloid leukemia in vivo and in vitro. Leuk. Lymphoma, 50: 437-446 (2009).
2. Yuan, X., Zhang, Y., Zhang, H., Jin, J., Li, X., Liu, H., Feng, Z. and Chen, X.: Activity of the potent dual Abl/Src tyrosine kinase inhibitor FB2 against Bcr-Abl positive cell lines in vitro and in vivo. Leuk. Res., 35: 237-242 (2011).
3. Ayrton, A. and Morgan, P.: Role of transport proteins in drug absorption, distribution and excretion. Xenobiotica, 31: 469-497 (2001).
4. Cummins, C. L., Salphati, L., Reid, M. J. and Benet, L. Z.: In vivo modulation of intestinal CYP3A metabolism by P-glycoprotein: studies using the rat single-pass intestinal perfusion model. J. Pharmacol. Exp. Ther., 305: 306-314 (2003).
5. Zhang, J., Huang, M., Guan, S., Bi, H. C., Pan, Y., Duan, W., Chan, S. Y., Chen, X., Hong, Y. H., Bian, J. S., Yang, H. Y. and Zhou, S.: A mechanistic study of the intestinal absorption of cryptotanshinone, the major active constituent of Salvia miltiorrhiza. J. Pharmacol. Exp. Ther., 317: 1285-1294 (2006).
6. Crowe, A., Ilett, K. F., Karunajeewa, H. A., Batty, K. T. and Davis, T. M.: Role of P-glycoprotein in absorption of novel antimalarial drugs. Antimicrob. Agents Chemother., 50: 3504-3506 (2006).
7. Wu, C. Y. and Benet, L. Z.: Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm. Res., 22: 11-23 (2005).
8. Mahadevan, D. and List, A. F.: Targeting the multidrug resistance-1 transporter in AML: molecular regulation and therapeutic strategies. Blood, 104: 1940-1951 (2004).
9. Liu, Z. Q., Jiang, Z. H., Liu, L. and Hu, M.: Mechanisms responsible for poor oral bioavailability of paeoniflorin: Role of intestinal disposition and interactions with sinomenine. Pharm. Res., 23: 2768-2780 (2006).
10. Kim, W. Y. and Benet, L. Z.: P-glycoprotein (P-gp/MDR1)-mediated efflux of sex-steroid hormones and modulation of P-gp expression in vitro. Pharm. Res., 21: 1284-1293 (2004).
11. Varma, M. V. and Panchagnula, R.: Enhanced oral paclitaxel absorption with vitamin E-TPGS: effect on solubility and permeability in vitro, in situ and in vivo. Eur. J. Pharm. Sci., 25: 445-453 (2005).
12. Petri, N., Tannergren, C., Rungstad, D. and Lennernas, H.: Transport characteristics of fexofenadine in the Caco-2 cell model. Pharm. Res., 21: 1398-1404 (2004).
13. Singhal, D., Ho, N. F. and Anderson, B. D.: Absorption and intestinal metabolism of purine dideoxynucleosides and an adenosine deaminase-activated prodrug of 2$,3$-dideoxyinosine in the mesenteric vein cannulated rat ileum. J. Pharm. Sci., 87: 569-577 (1998).
14. Tan, W., Chen, H., Zhao, J., Hu, J. and Li, Y.: A study of intestinal absorption of bicyclol in rats: active efflux transport and metabolism as causes of its poor bioavailability. J. Pharm. Pharm. Sci., 11: 97-105 (2008).
15. Neerati, P., Ganji, D. and Bedada, S. K.: Study on in situ and in vivo absorption kinetics of phenytoin by modulating Pglycoprotein with verapamil in rats. Eur. J. Pharm. Sci., 44: 27-31 (2011).
16. Fromm, M. F., Kim, R. B., Stein, C. M., Wilkinson, G. R. and Roden, D. M.: Inhibition of P-glycoprotein-mediated drug transport: A unifying mechanism to explain the interaction digoxin and quinidine. Circulation, 99: 552-557 (1999).
17. Venkatesh, G., Ramanathan, S., Nair, N. K., Mansor, S. M., Sattar, M. A., Khan, M. A. and Navaratnam, V.: Permeability of atenolol and propranolol in the presence of dimethyl sulfoxide in rat single-pass intestinal perfusion assay with liquid chromatography/ UV detection. Biomed. Chromatogr., 21: 484-490 (2007).
18. Dahan, A., Miller, J. M., Hilfinger, J. M., Yamashita, S., Yu, L. X., Lennernas, H. and Amidon, G. L.: High-Permeability Criterion for BCS Classification: Segmental/pH Dependent Permeability Considerations. Mol. Pharm., 7: 1827-1834 (2010).
19. Schellens, J. H., Malingre, M. M., Kruijtzer, C. M., Bardelmeijer, H. A., van Tellingen, O., Schinkel, A. H. and Beijnen, J. H.: Modulation of oral bioavailability of anticancer drugs: from mouse to man. Eur. J. Pharm. Sci., 12: 103-110 (2000).
20. Yamashita, S., Tanaka, Y., Endoh, Y., Taki, Y., Sakane, T., Nadai, T. and Sezaki, H.: Analysis of drug permeation across Caco-2 monolayer: implication for predicting in vivo drug absorption. Pharm. Res., 14: 486-491 (1997).
21. Hoppu, K.: Prehepatic metabolism of drugs-a mechanism for low and variable oral bioavailability. Pediatr. Nephrol., 13: 85-89 (1999).
22. Wang, Y., Cao, J., Wang, X. and Zeng, S.: Stereoselective transport and uptake of propranolol across human intestinal Caco-2 cell monolayers. Chirality, 22: 361-368 (2010).
23. Sutton, S. C., Rinaldi, M. T., McCarthy, J. M. and Vukovinsky, K. E.: A statistical method for the determination of absorption rate constant estimated using the rat single pass intestinal perfusion model and multiple linear regression. J. Pharm. Sci., 91: 1046-1053 (2002).
24. Dackson, K., Stone, J. A., Palin, K. J. and Charman, W. N.: Evaluation of the mass balance assumption with respect to the tworesistance model of intestinal absorption by using in situ single-pass intestinal perfusion of theophylline in rats. J. Pharm. Sci., 81: 321-325 (1992).
25. McKinnon, R. A., Burgess, W. M., Hall, P. M., Roberts-Thomson, S. J., Gonzalez, F. J. and McManus, M. E.: Characterisation of CYP3A gene subfamily expression in human gastrointestinal tissues. Gut, 36: 259-267 (1995).
26. Pérez-Tomás, R.: Multidrug resistance: retrospect and prospects in anti-cancer drug treatment. Curr. Med. Chem., 13: 1859-1876 (2006).
27. Iannetti, P., Spalice, A. and Parisi, P.: Calcium-channel blocker verapamil administration in prolonged and refractory status epilepticus. Epilepsia, 46: 967-969 (2005).
28. Candussio, L., Decorti, G., Crivellato, E., Granzotto, M., Rosati, A., Giraldi, T. and Bartoli, F.: Toxicologic and pharmacokinetic study of low doses of verapamil combined with doxorubicin. Life Sci., 71: 3109-3119 (2002).
29. Bansal, T., Mishra, G., Jaggi, M., Khar, R. K. and Talegaonkar, S.: Effect of P-glycoprotein inhibitor, verapamil, on oral bioavailability and pharmacokinetics of irinotecan in rats. Eur. J. Pharm. Sci., 36: 580-590 (2009).
30. Kruijtzer, C. M., Beijnen, J. H., Rosing, H., ten Bokkel Huinink, W. W., Schot, M., Jewell, R. C., Paul, E. M. and Schellens, J. H.: Increased oral bioavailability of topotecan in combination with the breast cancer resistance protein and P-glycoprotein inhibitor GF120918. J. Clin. Oncol., 20: 2943-2950 (2002).
31. Haouala, A., Widmer, N., Duchosal, M. A., Montemurro, M., Buclin, T. and Decosterd, L. A.: Drug interactions with the tyrosine kinase inhibitors imatinib, dasatinib, and nilotinib. Blood, 117: e75-e87 (2011).