In vitro P-glycoprotein efflux ratio can predict the in vivo brain penetration regardless of biopharmaceutics drug disposition classification system class

Drug Metabolism and Disposition

Volumn 41, Issue 12, 2013, Pages 2012-2017

  Kikuchi, Ryota ^a   De Morais, Sonia M ^a   Kalvass, J Cory ^a  

^a ABBVIE INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMFEBUTAMONE; AMPRENAVIR; CAFFEINE; CARBAMAZEPINE; CETIRIZINE; CHLORPROMAZINE; CIMETIDINE; CITALOPRAM; CLOZAPINE; CYCLOBENZAPRINE; DESLORATADINE; DEXAMETHASONE; DIAZEPAM; DIGOXIN; DIPHENHYDRAMINE; ELETRIPTAN; ETHOSUXIMIDE; FEXOFENADINE; FLUOXETINE; FLUVOXAMINE; HALOPERIDOL; HYDROCODONE; HYDROXYZINE; INDINAVIR; LAMOTRIGINE; LOPERAMIDE; MULTIDRUG RESISTANCE PROTEIN; MULTIDRUG RESISTANCE PROTEIN 1A; MULTIDRUG RESISTANCE PROTEIN 1B; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANALYTICAL PARAMETERS; ARTICLE; BLOOD BRAIN BARRIER; CORRELATION ANALYSIS; DRUG DISPOSITION; DRUG METABOLISM; DRUG PENETRATION; DRUG RESEARCH; EFFLUX RATIO; HUMAN; IN VITRO STUDY; IN VIVO STUDY; MDCK CELL; NATIONAL HEALTH ORGANIZATION; NONHUMAN; PREDICTION; PRIORITY JOURNAL; PROTEIN TRANSPORT;

ANIMALS; BIOPHARMACEUTICS; BLOOD-BRAIN BARRIER; BRAIN; CENTRAL NERVOUS SYSTEM AGENTS; HUMANS; P-GLYCOPROTEINS; PERMEABILITY;

EID: 84888615911     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.113.053868     Document Type: Article

References (26)

1. Adachi Y, Suzuki H, and Sugiyama Y (2001) Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm Res 18:1660-1668.
2. Broccatelli F, Larregieu CA, Cruciani G, Oprea TI, and Benet LZ (2012) Improving the prediction of the brain disposition for orally administered drugs using BDDCS. Adv Drug Deliv Rev 64:95-109.
3. Chen C, Hanson E, Watson JW, and Lee JS (2003) P-glycoprotein limits the brain penetration of nonsedating but not sedating H1-antagonists. Drug Metab Dispos 31:312-318.
4. Clark DE (2003) In silico prediction of blood-brain barrier permeation. Drug Discov Today 8:927-933.
5. Di L, Umland JP, Chang G, Huang Y, Lin Z, Scott DO, Troutman MD, and Liston TE (2011) Species independence in brain tissue binding using brain homogenates. Drug Metab Dispos 39:1270-1277.
6. Doran A, Obach RS, Smith BJ, Hosea NA, Becker S, Callegari E, Chen C, Chen X, Choo E, and Cianfrogna J, et al. (2005) The impact of P-glycoprotein on the disposition of drugs targeted for indications of the central nervous system: evaluation using the MDR1A/1B knockout mouse model. Drug Metab Dispos 33:165-174.
7. Ecker GF and Noe CR (2004) In silico prediction models for blood-brain barrier permeation. Curr Med Chem 11:1617-1628.
8. Feng B, Mills JB, Davidson RE, Mireles RJ, Janiszewski JS, Troutman MD, and de Morais SM (2008) In vitro P-glycoprotein assays to predict the in vivo interactions of P-glycoprotein with drugs in the central nervous system. Drug Metab Dispos 36:268-275.
9. Fridén M, Winiwarter S, Jerndal G, Bengtsson O, Wan H, Bredberg U, Hammarlund-Udenaes M, and Antonsson M (2009) Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids. J Med Chem 52:6233-6243.
10. Giacomini KM, Massoud N, Wong FM, and Giacomini JC (1984) Decreased binding of verapamil to plasma proteins in patients with liver disease. J Cardiovasc Pharmacol 6:924-928.
11. Kalvass JC, Maurer TS, and Pollack GM (2007) Use of plasma and brain unbound fractions to assess the extent of brain distribution of 34 drugs: comparison of unbound concentration ratios to in vivo p-glycoprotein efflux ratios. Drug Metab Dispos 35:660-666.
12. Kalvass JC and Pollack GM (2007) Kinetic considerations for the quantitative assessment of efflux activity and inhibition: implications for understanding and predicting the effects of efflux inhibition. Pharm Res 24:265-276.
13. Kodaira H, Kusuhara H, Fujita T, Ushiki J, Fuse E, and Sugiyama Y (2011) Quantitative evaluation of the impact of active efflux by p-glycoprotein and breast cancer resistance protein at the blood-brain barrier on the predictability of the unbound concentrations of drugs in the brain using cerebrospinal fluid concentration as a surrogate. J Pharmacol Exp Ther 339:935-944.
14. Kusuhara H and Sugiyama Y (2005) Active efflux across the blood-brain barrier: role of the solute carrier family. NeuroRx 2:73-85.
15. Mahar Doan KM, Humphreys JE, Webster LO, Wring SA, Shampine LJ, Serabjit-Singh CJ, Adkison KK, and Polli JW (2002) Passive permeability and P-glycoprotein-mediated efflux differentiate central nervous system (CNS) and non-CNS marketed drugs. J Pharmacol Exp Ther 303:1029-1037.
16. Maurer TS, Debartolo DB, Tess DA, and Scott DO (2005) Relationship between exposure and nonspecific binding of thirty-three central nervous system drugs in mice. Drug Metab Dispos 33:175-181.
17. Norinder U and Haeberlein M (2002) Computational approaches to the prediction of the bloodbrain distribution. Adv Drug Deliv Rev 54:291-313.
18. Pajouhesh H and Lenz GR (2005) Medicinal chemical properties of successful central nervous system drugs. NeuroRx 2:541-553.
19. Pardridge WM (1999) Blood-brain barrier biology and methodology. J Neurovirol 5:556-569.
20. Park MS, Okochi H, and Benet LZ (2011) Is Ciprofloxacin a Substrate of P-glycoprotein? Arch Drug Inf 4:1-9.
21. Sasongko L, Link JM, Muzi M, Mankoff DA, Yang X, Collier AC, Shoner SC, and Unadkat JD (2005) Imaging P-glycoprotein transport activity at the human blood-brain barrier with positron emission tomography. Clin Pharmacol Ther 77:503-514.
22. Schinkel AH (1999) P-Glycoprotein, a gatekeeper in the blood-brain barrier. Adv Drug Deliv Rev 36:179-194.
23. Sun H, Dai H, Shaik N, and Elmquist WF (2003) Drug efflux transporters in the CNS. Adv Drug Deliv Rev 55:83-105.
24. Syvänen S and Hammarlund-Udenaes M (2010) Using PET studies of P-gp function to elucidate mechanisms underlying the disposition of drugs. Curr Top Med Chem 10:1799-1809.
25. Urquhart BL and Kim RB (2009) Blood-brain barrier transporters and response to CNS-active drugs. Eur J Clin Pharmacol 65:1063-1070.
26. Yamazaki M, Neway WE, Ohe T, Chen I, Rowe JF, Hochman JH, Chiba M, and Lin JH (2001) In vitro substrate identification studies for p-glycoprotein- mediated transport: species difference and predictability of in vivo results. J Pharmacol Exp Ther 296:723-735.