The use of rabbit intestinal permeability as an in vitro assay in the search for orally active GPIIb/IIIa antagonists

Advanced Drug Delivery Reviews

Volumn 23, Issue 1-3, 1997, Pages 133-142

  Samanen, James M ^a   Lee, Chao Pin ^a   Smith, Philip L ^a   Bondinell, William E ^a   Calvo, Raul R ^a   Jakas, Dalia R ^a   Newlander, Kenneth A ^a   Parker, Michael ^a   Uzinskas, Irene ^a   Yellin, Tobias O ^a   Nichols, Andrew J ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

absorption; bioavailability; GPIIb IIIa antagonists; oral activity; peptides; permeability; pharmacophore model; transport; Ussing Chamber

Indexed keywords

ABSORPTION; AMINO ACIDS; BIOASSAY; DRUG THERAPY; MODIFICATION; PHARMACOKINETICS; STRUCTURE (COMPOSITION);

BIOAVAILABILITY; INTESTINAL PERMEABILITY; ORALLY ACTIVE ANTAGONISTS; USSING CHAMBER;

DRUG PRODUCTS;

FIBRINOGEN RECEPTOR ANTAGONIST; MANNITOL; PEPTIDE;

ASSAY; CHEMICAL MODIFICATION; DOG; DRUG BIOAVAILABILITY; DRUG DESIGN; HUMAN; INTESTINE ABSORPTION; INTRADUODENAL DRUG ADMINISTRATION; MEMBRANE PERMEABILITY; NONHUMAN; PRIORITY JOURNAL; RABBIT; REVIEW; STRUCTURE ACTIVITY RELATION; THROMBOCYTE AGGREGATION;

EID: 0031031113     PISSN: 0169409X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0169-409X(96)00431-0     Document Type: Review

References (26)

1. Smith, P.L. (1995) Intestinal absorption and secretion: in vivo studies. In: T.S. Gaginella, (Ed.), Methods in Gastrointestinal Pharmacology: A Handbook, pp. 85-99.
2. Samanen, J., Wilson, G., Smith, P. L., Lee, C. -P., Bondinell, W., Ku, T., Rhodes, G. and Nichols, A. (1996) Chemical approaches to improve the oral bioavailability of peptidergic molecules. J. Pharm. Pharmacol. 48, 115-131.
3. Samanen, J., Ali, F.E., Barton, L., Bondinell, W., Burgess, J., Callahan, J., Calvo, R., Chen, W., Chen, L., Erhard, K., Heyes, R., Hwang, S.-M., Jakas, D., Keenan, R., Ku, T., Kwon, C., Lee, C.-P., Miller, W., Newlander, K., Nichols, A., Peishoff, C., Rhodes, G., Ross, S., Shu, A., Simpson, R., Takata, D., Yellin, T.O., Uzsinskas, I., Venslavsky, J., Wong, A., Yuan, C.-K. and Huffman, W. (1996) GPIIb/IIIa antagonists with long oral duration designed from cyclic peptides. In: P.T.P. Kaumaya, and R.S. Hodges, (Eds.), Peptides: Chemistry, Structure, and Biology (Proc. 14th Am. Peptide Symp.). Leiden: ESCOM, in press.
4. Nichols, A.J., Ruffolo Jr., R.R., Huffman, W.F., Poste, G. and Samanen, J. (1992) Development of GpIIb/IIIa antagonists as antithrombotic drugs. Trends Pharm. Sci. 13, 413-417.
5. Samanen, J. GPIIb/IIIa antagonists (1996) Annu. Rep. Med. Chem. Chapter 13, in press.
6. Ussing, H.H. and Zerahn, K. (1951) Active transport of sodium as the source of electric current in the short-circuited isolated frog skin. Acta Physiol. Scand. 23, 110-127.
7. Smith, P.L., Wall, D.A., Gochoco, C.H. and Wilson, G. (1992) Routes of delivery: case studies. (5) Oral absorption of peptides and proteins. Adv. Drug Del. Rev. 8, 253-290.
8. Marks, G.I., Ryan, F.M., Hidalgo, I.J. and Smith, P.L. (1991) Mannitol, as a marker for intestinal integrity in in vitro absorption studies. Gastroenterology 100, A697.
9. Swaan, P.W., Marks, G.J., Ryan, F.M. and Smith, P.L. (1994) Determination of transport rates for arginine and acetaminophen in rabbit intestinal tissues in vitro. Pharm. Res. 11, 283-287.
10. Hidalgo, I.H., Ryan, F.M., Marks, G.J. and Smith, P.L. (1993) pH-dependent transcellular transport of cephalexin in rabbit intestinal mucosa. Int. J. Pharm. 98, 83-92.
11. Ganapathy, V. and Leibach, F.H. (1985) Is intestinal peptide transport energized by a proton gradient? Am. J. Physiol. G153-G160.
12. Smith, P., L., Mirabelli, C., Fondacaro, J., Ryan, F. and Dent, J. (1988) Intestinal 5-fluorouracil absorption: use of Ussing chambers to assess transport and metabolism. Pharm Res. 5, 598-603.
13. Constantinides, P.P., Scalart, J., Lancaster, C., Marcello, J., Marks, G., Ellens, H. and Smith, P.L. (1994) Formulation and intestinal absorption enhancement evaluation of waterin-oil microemulsions incorporating medium-chain glycerides. Pharm. Res. 11, 1385-1390.
14. Laker, M.F., Bull, H.J. and Menzies, I.S. (1982) Evaluation of mannitol for use as a probe marker of gastrointestinal permeability in man. Eur. J. Clin. Invest. 12, 485-491.
15. Meunier, L.D., Kissinger, J.T., Marcello, J., Nichols, A.J. and Smith, P.L. (1993) A chronic access model for direct delivery of drugs into the intestine of conscious dogs. J. Lab. Animal Sci. 43, 466-470.
16. Ali, F.E., Bennett, D.B., Calvo, R.R., Elliott, J.D., Hwang, S.-M., Ku, T.W., Lago, M.A., Nichols, A.J., Romoff, T.T., Shah, D.H., Vasko, J.A., Wong, A.S., Yellin, T.O., Yuan, C.-K. and Samanen, J.M. (1994) Conformationally constrained peptides and semipeptides derived from RGD as potent inhibitors of the platelet fibrinogen receptor and platelet aggregation. J. Med. Chem. 37, 769-780.
17. Yeh, P.-Y., Smith, P.L. and Ellens, H. (1994) Effect of medium-chain glycerides on physiological properties of rabbit intestinal epithelium in vitro. Pharm. Res. 11, 1148-1154.
18. Constantinides, P. P., C. Lancaster, J. Marcello, D. Chiossone, D. Orner, I. Hidalgo, P. L. Smith and A. Sarkahian, S. Yiu and A. Owen (1994) Enhanced oral absorption of an RGD peptide from water-in-oil microemulsions of different composition and particle size, Proceed. Int. Symp. Control. Rel. Bioact. Mater. 21, 62-63.
19. Ku, T.W., Ali, F.E., Barton, L.S., W., B.J., Bondinell, W.E., Burgess, J.L., Callahan, J.F., Calvo, R.R., Chen, L., Eggleston, D.S., Gleason, J.G., Huffman, W.F., Hwang, S.M., Jakas, D.R., Karash, C.B., Keenan, R.M., Kopple, K.D., Miller, W.M., Newlander, K.A., Nichols, A., Parker, M.F., Peishoff, C.E., Samanen, J.M., Uzinskas, I. and Venslavsky, J.W. (1993) Direct design of a potent non-peptide fibrinogen receptor antagonist based on the structure and conformation of a highly constrained cyclic RGD peptide. J. Am. Chem. Soc. 115, 8861-8862.
20. Bondinell, W.E., Keenan, R.M., Miller, W.H., Ali, F.E., Allen, A.C., DeBrosse, C.W., Eggleston, D.S., Erhard, K.F., Haltiwanger, R.C., Huffman, W.F., Hwang, S.-M., Jakas, D.R., Koster, P.P., Ku, T.W., Lee, C.P., Nichols, A.J., Ross, ST., Samanen, J.M., Valocik, R.E., Vasko-Moser, J.A., Venslavsky, J.W.,Wong, A.S. and Yuan, C.-K. (1994) Design of a potent and orally active nonpeptide platelet fibrinogen receptor (GPIIb/IIIa) antagonist. Bioorg. Med. Chem. 2, 897-908.
21. Karls, M.S., Rush, B.D., Wilkinson, K.F., Vidmar, T.J., Burton, P.S. and Ruwart, M.J. (1991) Desolvation energy: a major determinant of absorption, but not clearance, of peptides in rats. Pharm. Res. 8, 1477-1481.
22. Bondinell, W.E., Callahan, J.F., Huffman, W.F., Keenan, R.M., Ku, T.F., Newlander, K.A., Samanen, J.M. and Uzinskas, I.N. (1995) Bicyclic fibrinogen receptor antagonists. World Patent WO 95/18619.
23. Bondinell, W., et al. (1996) manuscript in preparation.
24. Conradi, R.A., Hilgers, A.R., Ho, N.F.H. and Burton, P.S. (1991) The influence of peptide structure on transport across Caco-2 cells. Pharm. Res. 8, 1453-1459.
25. Frantantoni, J.C. and Poindexter, B.J. (1990) Measuring platelet aggregation with microplate reader. Am. J. Clin. Pharm. 94, 613-617.
26. Nichols, A.J., Vasko, J.A., Koster, P.F., Valocik, R.E., Rhodes, G.R., Miller-Stein, C., Boppana, V. and Samanen, J.M. (1994) The in vivo pharmacological profile of the novel glycoprotein IIb/IIIa antagonist, SK and F 106760. J. Pharm. Exp. Ther. 270, 614-621.