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Volumn 11, Issue 4, 2014, Pages 1335-1344

Distinguishing between the permeability relationships with absorption and metabolism to improve BCS and BDDCS predictions in early drug discovery

Author keywords

biopharmaceutics classification system (BCS); biopharmaceutics drug disposition classification system (BDDCS); Caco 2; drug metabolism; intestinal absorption; PAMPA; permeability rate

Indexed keywords

METOPROLOL;

EID: 84898006099     PISSN: 15438384     EISSN: 15438392     Source Type: Journal    
DOI: 10.1021/mp4007858     Document Type: Article
Times cited : (65)

References (46)
  • 1
    • 0035313896 scopus 로고    scopus 로고
    • Screening for Human ADME/Tox Drug Properties in Drug Discovery
    • Li, A. P. Screening for Human ADME/Tox Drug Properties in Drug Discovery Drug Discov. Today 2001, 6, 357-366
    • (2001) Drug Discov. Today , vol.6 , pp. 357-366
    • Li, A.P.1
  • 2
    • 0028948839 scopus 로고
    • A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of in Vitro Drug Product Dissolution and in Vivo Bioavailability
    • Amidon, G. L.; Lennernas, H.; Shah, V. P.; Crison, J. R. A Theoretical Basis for a Biopharmaceutic Drug Classification: The Correlation of In Vitro Drug Product Dissolution and In Vivo Bioavailability Pharm. Res. 1995, 12, 413-420
    • (1995) Pharm. Res. , vol.12 , pp. 413-420
    • Amidon, G.L.1    Lennernas, H.2    Shah, V.P.3    Crison, J.R.4
  • 3
    • 0003455059 scopus 로고    scopus 로고
    • Waiver of in Vivo Bioavailability and Bioequivalence Studies for Immediate-Release Solid Oral Dosage Forms Based on a Biopharmaceutics Classification System
    • Food and Drug Administration: Rockville, MD.
    • Waiver of In Vivo Bioavailability and Bioequivalence Studies for Immediate-Release Solid Oral Dosage Forms Based on a Biopharmaceutics Classification System. FDA Guidance for Industry; Food and Drug Administration: Rockville, MD, 2000.
    • (2000) FDA Guidance for Industry
  • 4
    • 35649009910 scopus 로고    scopus 로고
    • Intestinal Permeability and its Relevance for Absorption and Elimination
    • Lennernas, H. Intestinal Permeability and its Relevance for Absorption and Elimination Xenobiotica 2007, 37, 1015-1051
    • (2007) Xenobiotica , vol.37 , pp. 1015-1051
    • Lennernas, H.1
  • 5
    • 13244298994 scopus 로고    scopus 로고
    • Caco-2 Replace or Refine?
    • Ungell, A. L. Caco-2 Replace or Refine? Drug Discov. Today Tech. 2004, 1, 423-430
    • (2004) Drug Discov. Today Tech. , vol.1 , pp. 423-430
    • Ungell, A.L.1
  • 7
    • 17644380257 scopus 로고    scopus 로고
    • Predicting Drug Disposition via Application of BCS: Transport/Absorption/ Elimination Interplay and Development of a Biopharmaceutics Drug Disposition Classification System
    • Wu, C. Y.; 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. 2005, 22, 11-23
    • (2005) Pharm. Res. , vol.22 , pp. 11-23
    • Wu, C.Y.1    Benet, L.Z.2
  • 8
    • 68149170038 scopus 로고    scopus 로고
    • The Role of Transporters in the Pharmacokinetics of Orally Administered Drugs
    • Shugarts, S.; Benet, L. Z. The Role of Transporters in the Pharmacokinetics of Orally Administered Drugs Pharm. Res. 2009, 26, 2039-2054
    • (2009) Pharm. Res. , vol.26 , pp. 2039-2054
    • Shugarts, S.1    Benet, L.Z.2
  • 11
    • 33846176619 scopus 로고    scopus 로고
    • A Provisional Biopharmaceutical Classification of the Top 200 Oral Drug Products in the United States, Great Britain, Spain, and Japan
    • Takagi, T.; Ramachandran, C.; Bermejo, M.; Yamashita, S.; Yu, L. X.; Amidon, G. L. A Provisional Biopharmaceutical Classification of the Top 200 Oral Drug Products in the United States, Great Britain, Spain, and Japan Mol. Pharmaceutics 2006, 3, 631-643
    • (2006) Mol. Pharmaceutics , vol.3 , pp. 631-643
    • Takagi, T.1    Ramachandran, C.2    Bermejo, M.3    Yamashita, S.4    Yu, L.X.5    Amidon, G.L.6
  • 12
    • 72949123710 scopus 로고    scopus 로고
    • Prediction of Solubility and Permeability Class Membership: Provisional BCS Classification of the World's Top Oral Drugs
    • Dahan, A.; Miller, J. M.; Amidon, G. L. Prediction of Solubility and Permeability Class Membership: Provisional BCS Classification of the World's Top Oral Drugs AAPS J 2009, 11, 740-6
    • (2009) AAPS J , vol.11 , pp. 740-746
    • Dahan, A.1    Miller, J.M.2    Amidon, G.L.3
  • 13
    • 62649128592 scopus 로고    scopus 로고
    • The Use of Drug Metabolism for Prediction of Intestinal Permeability
    • Chen, M. L.; Yu, L. The Use of Drug Metabolism for Prediction of Intestinal Permeability Mol. Pharmaceutics 2009, 6, 74-81
    • (2009) Mol. Pharmaceutics , vol.6 , pp. 74-81
    • Chen, M.L.1    Yu, L.2
  • 15
    • 84898009750 scopus 로고    scopus 로고
    • The Confounding FDA Redefinition of Intestinal Permeability in Terms of Extent of Absorption
    • Abstract W1840.
    • Larregieu, C. A.; Benet, L. Z. The Confounding FDA Redefinition of Intestinal Permeability in Terms of Extent of Absorption. AAPS J. 2009, 11, Abstract W1840.
    • (2009) AAPS J. , vol.11
    • Larregieu, C.A.1    Benet, L.Z.2
  • 16
    • 77955921793 scopus 로고    scopus 로고
    • The FDA Should Eliminate the Ambiguities in the Current BCS Biowaiver Guidance and Make Public the Drugs for Which BCS Biowaivers Have Been Granted
    • Benet, L. Z.; Larregieu, C. A. The FDA Should Eliminate the Ambiguities in the Current BCS Biowaiver Guidance and Make Public the Drugs for Which BCS Biowaivers Have Been Granted Clin. Pharmacol. Ther. 2010, 88, 405-407
    • (2010) Clin. Pharmacol. Ther. , vol.88 , pp. 405-407
    • Benet, L.Z.1    Larregieu, C.A.2
  • 18
    • 84877045938 scopus 로고    scopus 로고
    • Drug Discovery and Regulatory Considerations for Improving in Silico and in Vitro Predictions that Use Caco-2 as a Surrogate for Human Intestinal Permeability Measurements
    • Larregieu, C. A.; Benet, L. Z. Drug Discovery and Regulatory Considerations for Improving In Silico and In Vitro Predictions that Use Caco-2 as a Surrogate for Human Intestinal Permeability Measurements AAPS J. 2013, 15, 483-497
    • (2013) AAPS J. , vol.15 , pp. 483-497
    • Larregieu, C.A.1    Benet, L.Z.2
  • 19
    • 0032568397 scopus 로고    scopus 로고
    • Physicochemical High Throughput Screening: Parallel Artificial Membrane Permeation Assay in the Description of Passive Absorption Processes
    • Kansy, M.; Senner, F.; Gubernator, K. Physicochemical High Throughput Screening: Parallel Artificial Membrane Permeation Assay in the Description of Passive Absorption Processes J. Med. Chem. 1998, 41, 1007-1010
    • (1998) J. Med. Chem. , vol.41 , pp. 1007-1010
    • Kansy, M.1    Senner, F.2    Gubernator, K.3
  • 20
    • 44749090398 scopus 로고    scopus 로고
    • A Novel Design of Artificial Membrane for Improving the PAMPA Model
    • Chen, X.; Murawski, A.; Patel, K.; Crespi, C. L.; Balimane, P. V. A Novel Design of Artificial Membrane for Improving the PAMPA Model Pharm. Res. 2008, 25, 1511-1520
    • (2008) Pharm. Res. , vol.25 , pp. 1511-1520
    • Chen, X.1    Murawski, A.2    Patel, K.3    Crespi, C.L.4    Balimane, P.V.5
  • 21
    • 0037173513 scopus 로고    scopus 로고
    • Prediction of Passive Intestinal Absorption Using Bio-Mimetic Artificial Membrane Permeation Assay and the Paracellular Pathway Model
    • Sugano, K.; Takata, N.; Machida, M.; Saitoh, K.; Terada, K. Prediction of Passive Intestinal Absorption Using Bio-Mimetic Artificial Membrane Permeation Assay and the Paracellular Pathway Model Int. J. Pharm. 2002, 241, 241-251
    • (2002) Int. J. Pharm. , vol.241 , pp. 241-251
    • Sugano, K.1    Takata, N.2    Machida, M.3    Saitoh, K.4    Terada, K.5
  • 22
    • 0036238280 scopus 로고    scopus 로고
    • A Comparative Study of Artificial Membrane Permeability Assay for High Throughput Profiling of Drug Absorption Potential
    • Zhu, C.; Jiang, L.; Chen, T. M.; Hwang, K. K. A Comparative Study of Artificial Membrane Permeability Assay for High Throughput Profiling of Drug Absorption Potential Eur. J. Med. Chem. 2002, 37, 399-407
    • (2002) Eur. J. Med. Chem. , vol.37 , pp. 399-407
    • Zhu, C.1    Jiang, L.2    Chen, T.M.3    Hwang, K.K.4
  • 23
    • 0002769936 scopus 로고    scopus 로고
    • Design and Optimization of Dosage Regimens: Pharmacokinetic Data
    • In, 9 th ed. Hardman, J. G. Limbird, L. E. Molinoff, P. B. Ruddon, R. W. Gilman. A. G. McGraw Hill: New York
    • Benet, L. Z.; Øie, S.; Schwarz., J. B. Design and Optimization of Dosage Regimens: Pharmacokinetic Data. In Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9 th ed.; Hardman, J. G.;; Limbird, L. E.;; Molinoff, P. B.;; Ruddon, R. W.;; Gilman., A. G.; McGraw Hill: New York, 1996; pp 1707-1792.
    • (1996) Goodman and Gilman's the Pharmacological Basis of Therapeutics , pp. 1707-1792
    • Benet, L.Z.1    Øie, S.2    Schwarz, J.B.3
  • 24
    • 0003344708 scopus 로고    scopus 로고
    • Design and Optimization of Dosage Regimens: Pharmacokinetic Data
    • In, 10 th ed. Hardman, J. G. Limbird, L. E. McGraw Hill: New York
    • Thummel, K. E.; Shen, D. D. Design and Optimization of Dosage Regimens: Pharmacokinetic Data. In Goodman and Gilman's The Pharmacological Basis of Therapeutics, 10 th ed.; Hardman, J. G.; Limbird, L. E., Eds.; McGraw Hill: New York, 2001; pp 1924-2023.
    • (2001) Goodman and Gilman's the Pharmacological Basis of Therapeutics , pp. 1924-2023
    • Thummel, K.E.1    Shen, D.D.2
  • 26
    • 79953061441 scopus 로고    scopus 로고
    • Greenwood Village, Colo: Thomson Reuters (Healthcare) Inc. (accessed Feb 2014); updated periodically.
    • DRUGDEX® System [Internet database]. Greenwood Village, Colo: Thomson Reuters (Healthcare) Inc.; http://www.rubali.com/new/index.php?option=com- content&view=article&id=6&Itemid=121 (accessed Feb 2014); updated periodically.
    • DRUGDEX® System [Internet Database]
  • 27
    • 0346216088 scopus 로고    scopus 로고
    • Development of a 7-day, 96-Well Caco-2 Permeability Assay with High-Throughput Direct UV Compound Analysis
    • Alsenz, J.; Haenel, E. Development of a 7-day, 96-Well Caco-2 Permeability Assay with High-Throughput Direct UV Compound Analysis Pharm. Res. 2003, 20, 1961-1969
    • (2003) Pharm. Res. , vol.20 , pp. 1961-1969
    • Alsenz, J.1    Haenel, E.2
  • 29
    • 36549002236 scopus 로고    scopus 로고
    • Development of in Vitro Pharmacokinetic Screens Using Caco-2, Human Hepatocyte, and Caco-2/Human Hepatocyte Hybrid Systems for the Prediction of Oral Bioavailability in Humans
    • Li, C.; Liu, T.; Cui, X.; Uss, A. S.; Cheng, K. C. Development of In Vitro Pharmacokinetic Screens Using Caco-2, Human Hepatocyte, and Caco-2/Human Hepatocyte Hybrid Systems for the Prediction of Oral Bioavailability in Humans J. Biomol. Screening 2007, 12, 1084-1091
    • (2007) J. Biomol. Screening , vol.12 , pp. 1084-1091
    • Li, C.1    Liu, T.2    Cui, X.3    Uss, A.S.4    Cheng, K.C.5
  • 30
    • 0031781430 scopus 로고    scopus 로고
    • Correlating Partitioning and Caco-2 Cell Permeability of Structurally Diverse Small Molecular Weight Compounds
    • Yazdanian, M.; Glynn, S. L.; Wright, J. L.; Hawi, A. Correlating Partitioning and Caco-2 Cell Permeability of Structurally Diverse Small Molecular Weight Compounds Pharm. Res. 1998, 15, 1490-1494
    • (1998) Pharm. Res. , vol.15 , pp. 1490-1494
    • Yazdanian, M.1    Glynn, S.L.2    Wright, J.L.3    Hawi, A.4
  • 32
    • 84874608792 scopus 로고    scopus 로고
    • Comparison of the Permeability of Metoprolol and Labetalol in Rat, Mouse, and Caco-2 Cells: Use as a Reference Standard for BCS Classification
    • Incecayir, T.; Tsume, Y.; Amidon, G. L. Comparison of the Permeability of Metoprolol and Labetalol in Rat, Mouse, and Caco-2 Cells: Use as a Reference Standard for BCS Classification Mol. Pharmaceutics 2013, 10, 958-966
    • (2013) Mol. Pharmaceutics , vol.10 , pp. 958-966
    • Incecayir, T.1    Tsume, Y.2    Amidon, G.L.3
  • 34
  • 35
    • 0024602746 scopus 로고
    • Amiloride Transport in Rabbit Renal Brush-Border Membrane Vesicles
    • Wright, S. H.; Wunz, T. M. Amiloride Transport in Rabbit Renal Brush-Border Membrane Vesicles Am. J. Physiol. 1989, 256, F462-F468
    • (1989) Am. J. Physiol. , vol.256
    • Wright, S.H.1    Wunz, T.M.2
  • 36
    • 0025046860 scopus 로고
    • Uptake of the Cephalosporin, Cephalexin, by a Dipeptide Transport Carrier in the Human Intestinal Cell Line, Caco-2
    • Dantzig, A. H.; Bergin, L. Uptake of the Cephalosporin, Cephalexin, by a Dipeptide Transport Carrier in the Human Intestinal Cell Line, Caco-2 Biochim. Biophys. Acta 1990, 1027, 211-217
    • (1990) Biochim. Biophys. Acta , vol.1027 , pp. 211-217
    • Dantzig, A.H.1    Bergin, L.2
  • 37
    • 0032189375 scopus 로고    scopus 로고
    • Estimation of Permeability by Passive Diffusion through Caco-2 Cell Monolayers Using the Drugs' Lipophilicity and Molecular Weight
    • Camenisch, G.; Alsenz, J.; van de Waterbeemd, H.; Folkers, G. Estimation of Permeability by Passive Diffusion through Caco-2 Cell Monolayers Using the Drugs' Lipophilicity and Molecular Weight Eur. J. Pharm. Sci. 1998, 6, 317-324
    • (1998) Eur. J. Pharm. Sci. , vol.6 , pp. 317-324
    • Camenisch, G.1    Alsenz, J.2    Van De Waterbeemd, H.3    Folkers, G.4
  • 38
    • 0141538249 scopus 로고    scopus 로고
    • Human Cytochromes P450 Associated with the Phase 1 Metabolism of Drugs and Other Xenobiotics: A Compilation of Substrates and Inhibitors of the CYP1, CYP2 and CYP3 Families
    • Lewis, D. F. Human Cytochromes P450 Associated with the Phase 1 Metabolism of Drugs and Other Xenobiotics: A Compilation of Substrates and Inhibitors of the CYP1, CYP2 and CYP3 Families Curr. Med. Chem. 2003, 10, 1955-1972
    • (2003) Curr. Med. Chem. , vol.10 , pp. 1955-1972
    • Lewis, D.F.1
  • 39
    • 28244461508 scopus 로고    scopus 로고
    • Effects of Grapefruit Juice on the Pharmacokinetics of Acebutolol
    • Lilja, J. J.; Raaska, K.; Neuvonen, P. J. Effects of Grapefruit Juice on the Pharmacokinetics of Acebutolol Br. J. Clin. Pharmacol. 2005, 60, 659-663
    • (2005) Br. J. Clin. Pharmacol. , vol.60 , pp. 659-663
    • Lilja, J.J.1    Raaska, K.2    Neuvonen, P.J.3
  • 40
    • 0014006229 scopus 로고
    • Urinary Excretion of Acetylsalicylic Acid in Man
    • Cummings, A. J.; King, M. L. Urinary Excretion of Acetylsalicylic Acid in Man Nature 1966, 209, 620-621
    • (1966) Nature , vol.209 , pp. 620-621
    • Cummings, A.J.1    King, M.L.2
  • 41
    • 0030916427 scopus 로고    scopus 로고
    • Contribution of Cytochrome P450 3A Pathway to Bromocriptine Metabolism and Effects of Ferrous Iron and Hypoxia-Re-Oxygenation on its Elimination in the Perfused Rat Liver
    • Matsubayashi, K.; Matsumoto, H.; Fukui, Y. Contribution of Cytochrome P450 3A Pathway to Bromocriptine Metabolism and Effects of Ferrous Iron and Hypoxia-Re-Oxygenation on its Elimination in the Perfused Rat Liver J. Pharm. Pharmacol. 1997, 49, 551-557
    • (1997) J. Pharm. Pharmacol. , vol.49 , pp. 551-557
    • Matsubayashi, K.1    Matsumoto, H.2    Fukui, Y.3
  • 42
    • 0025126914 scopus 로고
    • Clinical Pharmacokinetics of Ketoprofen and its Enantiomers
    • Jamali, F.; Brocks, D. R. Clinical Pharmacokinetics of Ketoprofen and its Enantiomers Clin. Pharmacokinet. 1990, 19, 197-217
    • (1990) Clin. Pharmacokinet. , vol.19 , pp. 197-217
    • Jamali, F.1    Brocks, D.R.2
  • 43
    • 0021324207 scopus 로고
    • Clinical Pharmacokinetics of Labetalol
    • McNeil, J. J.; Louis, W. J. Clinical Pharmacokinetics of Labetalol Clin. Pharmacokinet. 1984, 9, 157-167
    • (1984) Clin. Pharmacokinet. , vol.9 , pp. 157-167
    • McNeil, J.J.1    Louis, W.J.2
  • 44
    • 71949123177 scopus 로고    scopus 로고
    • PET Studies of Cerebral Levodopa Metabolism: A Review of Clinical Findings and Modeling Approaches
    • Kumakura, Y.; Cumming, P. PET Studies of Cerebral Levodopa Metabolism: a Review of Clinical Findings and Modeling Approaches Neuroscientist 2009, 15, 635-650
    • (2009) Neuroscientist , vol.15 , pp. 635-650
    • Kumakura, Y.1    Cumming, P.2
  • 46
    • 0029591968 scopus 로고
    • Metabolism of Zidovudine
    • Veal, G. J.; Back, D. J. Metabolism of Zidovudine Gen. Pharmacol. 1995, 26, 1469-1475
    • (1995) Gen. Pharmacol. , vol.26 , pp. 1469-1475
    • Veal, G.J.1    Back, D.J.2


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