Availability of PSC833, a substrate and inhibitor of poglycoproteins, in various concentrations of serum

Journal of the National Cancer Institute

Volumn 90, Issue 15, 1998, Pages 1161-1166

  Smith, Alexander J ^a   Mayer, Ulrich ^a   Schinkel, Alfred H ^a   Borst, Piet ^a  

^a NETHERLANDS CANCER INSTITUTE   (Netherlands)

Author keywords

[No Author keywords available]

Indexed keywords

GLYCOPROTEIN P; VALSPODAR;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DRUG DETERMINATION; DRUG TRANSPORT; GENE EXPRESSION; GENETIC TRANSFECTION; MICHAELIS CONSTANT; MULTIDRUG RESISTANCE; NONHUMAN;

EID: 0032486795     PISSN: 00278874     EISSN: None     Source Type: Journal    
DOI: 10.1093/jnci/90.15.1161     Document Type: Article

References (34)

1. Juliano RL, Ling V. A Surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants. Biochim Biophys Acta 1976;455:152-62.
2. Endicott JA, Ling V. The biochemistry of P-glycoptorein-mediated multidrug resistance. Annu Rev Biochem 1989;58:137-71.
3. Gottesman MM, Hrycyna CA, Schoenlein PV, Germann UA, Pastan I. Genetic analysis of the multidrug transporter. Annu Rev Genet 1995; 29:607-49.
4. Germann UA. P-glycoprotein - a mediator of multidrug resistance in tumour cells. Eur J Cancer 1996;32A:927-44.
5. Ruetz S, Gros P. A mechanism for P-glycoprotein action in multidrug resistance: are we there yet? Trends Pharmacol Sci 1994;15: 260-3.
6. Borst P, Schinkel AH. Genetic dissection of the function of mammalian P-glycoproteins. Trends Genet 1997;13:217-22.
7. Tsuruo T, Iida H, Naganuma K, Tsukagoshi S, Sakurai Y. Promotion by verapamil of vincristine responsiveness in tumor cell lines inherently resistant to the drug. Cancer Res 1983; 43:808-13.
8. Tsuruo T, Iida H, Tsukagoshi S, Sakurai Y. Overcoming of vincristine resistance in P388 leukemia in vivo and in vitro through enhanced cytotoxicity of vincristine and vinblastine by verapamil. Cancer Res 1981;41:1967-72.
9. Ford JM, Hait WN. Pharmacology of drugs that alter multidrug resistance in cancer. Pharmacol Rev 1990;42:155-99.
10. Dalton WS, Crowley JJ, Salmon SS, Grogan TM, Laufman LR, Weiss GR, et al. A phase III randomized study of oral verapamil as a chemosensitizer to reverse drug resistance in patients with refractory myeloma. A Southwest Oncology Group study. Cancer 1995;75: 815-20.
11. Wishart GC, Bissett D, Paul J, Jodrell D, Harnett A, Habeshaw T, et al. Quinidine as a resistance modulator of epirubicin in advanced breast cancer: mature results of a placebo-controlled randomized trial. J Clin Oncol 1994; 12:1771-7.
12. Wilson WH, Bates SE, Fojo A, Bryant G, Zhan Z, Regis J, et al. Controlled trial of dexverapamil, a modulator of multidrug resistance, in lymphomas refractory to EPOCH chemotherapy. J Clin Oncol 1995;13:1995-2004.
13. Boesch D, Gaveriaux C, Jachez B, Pourtier-Manzanedo A, Bollinger P, Loor F. In vivo circumvention of P-glycoprotein-mediated multidrug resistance of tumor cells with SDZ PSC 833. Cancer Res 1991;51:4226-33.
14. Twentyman PR, Bleehen NM. Resistance modification by PSC-833, a novel non-immunosuppressive cyclosporin [published erratum appears in Eur J Cancer 1992;28:6160]. Eur J Cancer 1991;27:1639-42.
15. Boote DJ, Dennis IF, Twentyman PR, Osborne RJ, Laburte C, Hensel S, et al. Phase I study of etoposide with SDZ PSC 833 as a modulator of multidrug resistance in patients with cancer. J Clin Oncol 1996;14:610-8.
16. Sonneveld P, Marie JP, Huisman C, Vekhoff A, Schoester M, Faussat AM, et al. Reversal of multidrug resistance by SDZ PSC 833, combined with VAD (vincristine, doxorubicin, dexamethasone) in refractory multiple imeloma. A phase I study. Leukemia 1996;10: 1741-50.
17. Schinkel AH, Mayer U, Wagenaar E, Mol CA, van Deemter L, Smit JJ, et al. Normal viability and altered pharmacokinetics in mice lacking mdr1-type (drug-transporting) P-glycoproteins. Proc Natl Acad Sci U S A 1997;94: 4028-33.
18. Mayer U, Wagenaar E, Dorobek B, Beijnen JH, Borst P, Schinkel AH. In vivo inhibitory activity and selectivity of SDZ PSC833 on mouse mdr1-type P-glycoproteins. J Clin Invest 1997;100:2430-36.
19. Lemaire M, Bruelisauer A, Guntz P, Sato H. Dose-dependent brain penetration of SDZ PSC 833, a novel multidrug resistance-reversing cyclosporin, in rats. Cancer Chemother Pharmacol 1996;38:481-6.
20. Naito M, Watanabe T, Tsuge H, Koyama T, Oh-hara T, Tsuruo T. Potentiation of the reversal activity of SDZ PSC833 on multi-drug resistance by an anti-P-glycoprotein monoclonal antibody MRK-16. Int J Cancer 1996;67: 435-40.
21. Archinal-Mattheis A, Rzepka RW, Watanabe T, Kokubu N, Itoh Y, Combates NJ, et al. Analysis of the interactions of SDZ PSC 833 ([3′-keto-Bmt1]-Val2]-Cyclosporine), a multidrug resistance modulator, with P-glycoprotein. Oncol Res 1995;7:603-10.
22. Schinkel AH, Wagenaar E, van Deemter L, Mol CA, Borst P. Absence of the mdr1a P-glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A. J Clin Invest 1995; 96:1698-705.
23. Schinkel AH, Kemp S, Dolle M, Rudenko G, Wagenaar E. N-glycosylation and deletion mutants of the human MDR1 P-glycoprotein. J Biol Chem 1993;268:7474-81.
24. Ueda K, Okamura N, Hirai M, Tanigawara Y, Saeki T, Kioka N, et al. Human P-glycoprotein transports cortisol, aldosterone, and dexamethasone, but not progesterone. J Biol Chem 1992; 267:24248-52.
25. Spoelstra EC, Westerhoff HV, Dekker H, Lankelma J. Kinetics of daunorubicin transport by P-glycoprotein of intact cancer cells. Eur J Cancer 1992;207:567-79.
26. Tiberghien F, Loor F. Ranking of P-glycoprotein substrates and inhibitors by a calcein-AM fluorometry screening assay. Anticancer Drugs 1997;7:568-78.
27. Tanigawara Y, Okamura N, Hirai M, Yasuhara M, Ueda K, Kioka N, et al. Transport of digoxin by human P-glycoprotein expressed in a porcine kidney epithelial cell line (LLC-PK1). J Pharmacol Exp Ther 1992;263:840-5.
28. Lehnert M, de Giuli R, Kunke K, Emerson S, Dalton WS, Salmon SE. Serum can inhibit reversal of multidrug resistance by chemosensitisers. Eur J Cancer 1996;32A:862-7.
29. Ludescher C, Eisterer W, Hilbe W, Hofmann J, Thaler J. Decreased potency of MDR-modulators under serum conditions determined by a functional assay. Br J Haematol 1995;91: 652-7.
30. Simon N, Dailly E, Combes O, Melaurie E, Lemaire M, Tillement JP, et al. Role of lipoproteins in the plasma binding of SDZ PSC 833, a novel multidrug-resistance reversing cyclosporine. Br J Clin Pharmacol 1998;45: 173-5.
31. Figg WD, Meadows B, Regis J, Tawfik E, Piscitelli S, Waldrop BA, et al. Oral bioavailability of PSC833, a P-glycoprotein antagonist. Pharmacotherapy 1994;14:362.
32. Giaccone G, Linn SC, Catimel G, Dumortier A, Foy M, Vermorken JB, et al. SDZ PSC833 in combination with doxorubicin: a phase I and pharmacologic study in solid tumors. Anticancer Drugs 1994;5:42-3.
33. Ayesh S, Shao YM, Stein WD. Co-operative, competitive and non-competitive interactions between modulators of P-glycoprotein. Biochim Biophys Acta 1996;1316:8-18.
34. Lyubimov E, Lan LB, Pashinsky I, Ayesh S, Stein WD. Saturation reversal of the multidrug pump using many reversers in low-dose combinations. Anticancer Drugs 1995;6:727-35.