Recommendations for bioequivalence testing of cyclosporine generics revisited

Therapeutic Drug Monitoring

Volumn 22, Issue 3, 2000, Pages 330-345

  Christians, Uwe ^a   First, M Roy ^b   Benet, Leslie Z ^a  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b UNIVERSITY OF CINCINNATI MEDICAL CENTER   (United States)

Author keywords

Bioequivalence; Cyclosporine; Cyclosporine generics; Individual bioequivalence; Therapeutic drug monitoring

Indexed keywords

CYCLOSPORIN; CYCLOSPORIN A;

AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; CLINICAL TRIAL; CONCENTRATION RESPONSE; DOSE RESPONSE; DRUG EFFICACY; DRUG FORMULATION; DRUG SAFETY; HUMAN; IMMUNOSUPPRESSIVE TREATMENT; INDIVIDUALIZATION; META ANALYSIS; PRACTICE GUIDELINE; PRIORITY JOURNAL;

CHEMISTRY, PHARMACEUTICAL; CYCLOSPORINE; DRUG EVALUATION; DRUGS, GENERIC; HUMANS; IMMUNOSUPPRESSIVE AGENTS; INDIVIDUALITY; THERAPEUTIC EQUIVALENCY; UNITED STATES; UNITED STATES FOOD AND DRUG ADMINISTRATION;

EID: 0034129695     PISSN: 01634356     EISSN: None     Source Type: Journal    
DOI: 10.1097/00007691-200006000-00017     Document Type: Article

References (95)

1. Bennett WM, Olayei AJ. Pharmacoeconomics of immunosuppressive agents in renal transplant patients. Transplant Proc 1999;31 (suppl. 3A):6S.
2. Coukell AJ, Plosker GL. Cyclosporin microemulsion (Neoral). Pharmacoeconomic review of its use compared with standard cyclosporin in renal and hepatic transplantation. Pharmacoeconomics 1998;14:692-708.
3. Drug Price Competition and Patent Term Restoration Act. Public law 98-417, 98, Stat. 1585-1605, 1984.
4. Code of Federal Regulations, 21, Food and Drugs, Part 314.94, Content and format of an abbreviated application, pp. 134, 1995.
5. Dighe SV. A review of the safety of generic drugs. Transplant Proc. 1999;31 (suppl. 3A):23S-24S.
6. Nightingale SL, Morrison JC. Generic drugs and the prescribing physician. JAMA 1987;258:1200-1204.
7. Nightingale SL. From the Food and Drug Administration: Generic substitution. JAMA 1998;279:645.
8. Benet LZ. Relevance of pharmacokinetics in narrow therapeutic index drugs. Transplant Proc 1999;31:1642-1644.
9. Benet LZ, Goyan JE. Bioequivalence and narrow therapeutic index drugs. Pharmacotherapy 1995;15:433-440.
10. Johnston A, Keown PA, Holt DW. Simple bioequivalence criteria: are they relevant to critical dose drugs? Experience gained from cyclosporine. Ther Drug Monit 1997;19:375-381.
11. Patnaik RN, Lesko LJ, Chen ML, Williams RL, FDA Individual Bioequivalence Working Group. Individual Bioequivalence: New concepts in the statistical assessment of bioequivalence metrics. Clin Pharmacokinet 1997;33:1-6.
12. Barr WH. The case for expanding bioequivalence criteria to include measures of individual bioequivalence in relevant population subsets. Transplant Proc 1999;31 (suppl. 3A):25S-30S.
13. Sabatini S, Ferguson RM, Helderman HJ, Hull AR, Kirkpatrick BS, Barr WH. Drug substitution in transplantation: A National Kidney Foundation white paper. Am J Kidney Dis 1999;33:389-397.
14. Kahan BD. Recommendations concerning the introduction of generic formulations of cyclosporine. Transplant Proc 1999;31: 1634.
15. Kahan BD, Welsh M, Rutzky LP. Challenges in cyclosporine therapy: the role of therapeutic drug monitoring by area under the curve monitoring. Ther Drug Monit 1995:17;621-624.
16. Food and Drug Administration (FDA), Division of Biopharmaceutics. Bioavailability and bioequivalence requirements. Fed Regist 1977;42:1624-1653.
17. CPMP (Committee for Proprietary Medicinal Products) Working Party in the Efficacy of Medicinal Products. Note for guidance: Investigation of bioavailability and bioequivalence. The Rule Governing Medicinal Products in the European Community. 1991;3: 149-167.
18. Kahan BD, Welsh M, Schoenberg L, et al. Variable oral absorption of cyclosporine. Transplantation 1996;62:599-606.
19. Inoue S, Beck Y, Nagao T, Uchida H. Early fluctuation in cyclosporine A trough levels affects long-term outcome of kidney transplants. Transplant Proc 1994;26:2571-2573.
20. Castañeda-Hernández G, Perez-Urizar J, Medeiros M. Current bioequivalence criteria are adequate for oral cyclosporin A formulations. Ther Drug Monit 1998;20:722-723.
21. Kahan BD. Discussion of recommendations concerning the introduction of generic formulations of cyclosporine. Transplant Proc 1999;31:1675-1684.
22. Vonderscher J, Meinzer A. Rationale for the development of Sandimmune Neoral. Transplant Proc 1994;26:2925-2927.
23. Olyaei AJ, deMattos AM, Bennett WM. Switching between cyclosporin formulations. What are the risks? Drug Saf 1997;16:366-373.
24. Kovarik JM, Mueller EA, Niese D. Clinical development of a cyclosporine microemulsion in transplantation. Ther Drug Monit 1996;18:429-434.
25. Noble S, Markham A. Cyclosporin. A review of the pharmacokinetic properties, clinical efficacy and tolerability of a microemulsion-based formulation (Neoral). Drugs 1995;50:924-941.
26. Mueller EA, Kovarik JM, Van Bree JB, Tetzloff W, Grevel J, Kutz K. Improved dose linearity of cyclosporine pharmacokinetics from a microemulsion formulation. Pharm Res 1994;11:301-304.
27. Keown P, Niese D. Cyclosporine microemulsion increases drug exposure and reduces acute rejection without incremental toxicity in de novo renal transplantation. Kidney Int 1998;54:938-944.
28. Elder CA, Moore M, Chang CT, et al. Efficacy and pharmacokinetics of two formulations of cyclosporine A in patients with psoriasis. J Clin Pharmacol 1995;35:865-875.
29. Erkko P, Granlund H, Nuutinen M, Reitamo S. Comparison of cyclosporin A pharmacokinetics of a new microemulsion formation and standard oil preparation in patients with psoriasis. Br J Dermatol 1997;136:82-88.
30. Mueller EA, Kovarik JM, Van Bree JB, Lison AE, Kutz K. Pharmacokinetics and tolerability of a microemulsion formulation of cyclosporine in renal allograft recipients: A concentration-controlled comparison with the commercial formulation. Transplantation 1994;57:1178-1182.
31. Kovarik JM, Mueller EA, Van Bree JB, et al. Cyclosporine pharmacokinetics and variability from a microemulsion formulation. A multicenter investigation in kidney transplant patients. Transplantation 1994;58:658-663.
32. Curtis JJ, Lynn M, Jones PA. Neoral conversion from Sandimmune in maintenance renal transplant patients: an individual approach. J Am Soc Nephrol 1998;9:1293-1300.
33. Ruggenenti P, Perico N, Mosconi L, et al. Calcium channel blockers protect transplant patients from cyclosporine-induced daily renal hypoperfusion. Kidney Int 1993;43:706-711.
34. Taesch S, Niese D. Safety and tolerability of a new oral formulation of cyclosporin A. Sandimmun Neoral, in renal transplant patients. Transplant Int 1994;7:S263-S266, 1994.
35. Niese D. A double-blind randomized study of Sandimmun Neoral versus Sandimmun in new renal transplant recipients: results after 12 months. The International Sandimmun Neoral Study Group. Transplant Proc 1995;27:1849-1856.
36. Oellerich M, Armstrong VW, Kahan BD, et al. Lake Louise consensus conference on cyclosporin monitoring in organ transplantation: Report of the consensus panel. Ther Drug Monit 1995;17: 642-654.
37. United States Patent and Trademark Office. Patent No. 5,766,629.
38. Schroeder TJ, Cho MJ, Pollack GM, et al. Comparison of two cyclosporine formulations in healthy volunteers: Bioequivalence of the new Sang-35 formulation and Neoral. J Clin Pharmacol 1998;38:807-814.
39. First MR, Alloway R, Schroeder TJ. Development of Sang-35: a cyclosporine formulation bioequivalent to Neoral. Clin Transplant 1998;12:318-324.
40. Alloway RR. Generic immunosuppressants used in solid organ transplantation. Transplant Proc 1999;31 (suppl. 3A):2S-5S.
41. Canafax DM, Irish DM, Berger Moran H, et al. An individual bioequivalence approach to compare the intrasubject variability of two ciclosporin formulations. SangCya and Neoral. Pharmacology 1999;59:78-88.
42. U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research (CDER). Draft Guidance for Industry: In vivo bioequivalence studies based on population and individual bioequivalence approaches. Rockville, MD, October 1997.
43. First MR, Weiskittel P, Burton ML, et al. 9-Months safety and efficacy of Sang-35 in kidney transplant patients after conversion from Sandimmune. Transplant Proc 1998;30:1701-1705.
44. Lee YJ, Chung SJ, Shim CK. Bioequivalence of Neoplanta capsule to Sandimmune Neoral, microemulsion formulations of cyclosporin A in human subjects. Int J Clin Pharmacol Ther 1998;36:210-215.
45. Lee YJ, Chung SJ, Shim CK. Decreased oral availability of cyclosporin A at second administration. Br J Clin Pharmacol 1997; 44:343-345.
46. Park MS, Yu NC, Lee HK, Kim KH. Bioequivalence study of Cipol-N (cyclosporine microemulsion preparation) in healthy adults. Transplant Proc 1998;30:3541-3546.
47. United States Patent and Trademark Office. Cyclosporin-containing soft capsule composition. Patent No. 5,603,951.
48. Kim SC, Han DJ. Neoplanta as a new microemulsion formula of cyclosporine in renal transplantation: Comparative study with Neoral for efficacy and safety. Transplant Proc 1998;30:3547-3548.
49. Best NG, Trull AK, Tan KKC, et al. Blood cyclosporin concentrations and the short-term risk of lung rejection following heart lung transplantation. Br J Clin Pharmacol 1992;34:513-520.
50. Wahlberg J, Wilezek HE, Fauchald P, et al. Consistent absorption of cyclosporine from a microemulsion formulation assessed in stable renal transplant recipients over a one-year study period. Transplantation 1995;60:648-652.
51. Fahr A. Cyclosporin clinical pharmacokinetics. Clin Pharmacokinet 1993;24:472-495.
52. Christians U, Sewing KF. Ciclosporin metabolism in transplant patients. Pharmacol Ther 1993;57:291-345.
53. Wu C-Y, Benet LZ, Hebert MF, et al. Differentiation of absorption and first-pass gut and hepatic metabolism in humans: Studies with cyclosporine. Clin Pharmacol Ther 1995;58:492-497.
54. Wacher VJ, Wu CY, Benet LZ. Overlapping substrate specificities and tissue distribution of cytochrome P450 3A and p-glycoprotein: Implications for drug delivery and activity in cancer chemotherapy. Mol Carcinog 1995;13:129-134.
55. Wacher VJ, Silverman JA, Zhang Y, Benet LZ. Role of p-glycoprotein and cytochrome P450 3A in limiting oral absorption of peptides and peptidomimetics. J Pharm Sci 1998:87:1322-1330.
56. Lampen A, Christians U, Bader A, Hackbarth I, Sewing KF. Drug interactions and interindividual variability of ciclosporin metabolism in the small intestine. Pharmacology 1996;52:159-168.
57. Kolars JC, Awni WM, Merion RM, Watkins PB. First-pass metabolism of cyclosporine by the gut. Lancet 1991;331:1488-1490.
58. Lown KS, Mayo RR, Leichtmann AB, et al. Role of intestinal p-glycoprotein (mdr1) in interpatient variation in the oral bioavailability of cyclosporine. Clin Pharmacol Ther 1997;62:248-260.
59. Fricker G, Drewe J, Huwyler J, Gutmann H, Beglinger C. Relevance of p-glycoprotein for the enteral absorption of cyclosporin A, in vitro-in vivo correlation. Br J Pharmacol 1996;118:1841-1847.
60. Gleiter CH, Gundert-Remy U. Bioinequivalence and drug toxicity: How great is the problem and what can be done? Drug Saf 1994; 11:1-6.
61. Benet LZ. Understanding bioequivalence testing. Transplant Proc 1999;31 (suppl. 3A):7S-9S.
62. Food and Drug Administration (FDA). Bioavailability and bioequivalence requirements. Fed Resist 1992;57:17997-18001.
63. Schall R, Luus HG. On population and individual bioequivalence. Stat Med 1993;12:1109-1124.
64. Garbe E, Röhmel J, Gundert-Remy U. Clinical and statistical issues in therapeutic equivalence trials. Eur J Clin Pharmacol 1993; 45:1-7.
65. Sauter R, Steinijans VW, Diletti E, Böhm A, Schulz HU. Presentation of results from bioequivalence studies. Int J Clin Pharmacol Ther Toxicol 1992;30:233-256.
66. Midha KK, Rawson MJ, Hubbard JW. Individual and average bioequivalence of highly variable drugs and drug products. J Pharm Sci 1997;86:1193-1197.
67. Blume HH, McGilveray IJ, Midha KK. BIO-international 94, Conference on Bioavailability, Bioequivalence and Pharmacokinetic Studies. Eur J Pharm Sci 1995;3:113-124.
68. Sallas WM, Nedelman JR, Sheiner LB, Meligeni JA, Robinson WT. A non-linear mixed effect model comparing two formulations of cyclosporine in stable renal patients. J Pharmacokinet Biopharm 1995;23:495-514.
69. Ohashi Y, Izumo T. Comparison of intra-subject variability of different formulations by cross-over trials. In: Midha KK, Nagai K, eds. Bioavailability, Bioequivalence and Pharmacokinetic Studies. Tokyo: Business Center for Academic Societies 1996;113-118.
70. Keown P. Landsberg D. Halloran P, et al. A randomized, prospective multicenter pharmacoepidemiologic study of cyclosporine microemulsion in stable renal graft recipients. Transplantation 1996; 12:1744-1752.
71. Neoral. Physician's Desk Reference, ed. 52. Montvale: Medical Economics Data Production Co. 1998:1882-1889.
72. McGilveray IJ, Gallicano K. Generic drugs: the Canadian perspective. Transplant Proc 1999;31 (suppl. 3A):16S-18S.
73. Hauck WW, Anderson S. Measuring switchability and prescribability: when is average bioequivalence sufficient? J Pharmacokinet Biopharm 1994;22:551-565.
74. Anderson S, Hauck WW. Consideration of individual bioequivalence. J Pharmacokinet Biopharm 1990;18:259-273.
75. Endrenyi L, Amidon GL, Midha KK, Skelly JP. Individual bioequivalence: attractive in principle, difficult in practice. Pharm Res 1998;15:1321-1325.
76. Laganière S, Lalonde RL, Potvin D, Kimanani EK. Comparison between individual (IB) and average bioequivalence (AB) for 3 highly variable drugs. Clin Pharmacol Ther 1998;63:145.
77. Kesten S, Scavuzzo M, Chaparro C, Szalai JP. Pharmacokinetic profile and variability of cyclosporine versus Neoral in patients with cystic fibrosis after lung transplantation. Pharmacotherapy 1998;18:847-850.
78. Cooney GF, Habucky K, Hoppu K. Cyclosporin pharmacokinetics in pediatric transplant recipients. Clin Pharmacokinet 1997;32: 481-495.
79. Schroeder TJ, Hariharan S, First MR. Variations in bioavailability of cyclosporine and relationship to clinical outcome in renal transplant subpopulations. Transplant Proc 1995:27:837-839.
80. Trull AK, Tan KKC, Tan L, Alexander GJM, Jamieson NV. Absorption of cyclosporine from conventional and new microemulsion oral formulations in liver transplant recipients with external biliary diversion. Br J Clin Pharmacol 1995;39:627-631.
81. Winkler M, Haller G, Oldhafer K, et al. Cyclosporin new oral formulation for early oral immunosuppressive therapy in liver transplant recipients. Transplantation 1996;62:1063-1068.
82. Serafinowicz A, Gaciong Z, Baczkowska T, Majchrzak J, Durlik M, Lao M. Cyclosporine (Sandimmun) pharmacokinetics in renal allograft recipients with diabetes mellitus. Polish J Immunol 1995; 20:437-439.
83. Yee GC. Dosage forms of cyclosporine. Pharmacotherapy 1991; 11:149S-152S.
84. Cavanak T, Sucker H. Formulation of dosage forms. Prog Allergy 1986;38:65-72.
85. Min DI, Hwang GC, Bergstrom S, et al. Bioavailability and patient acceptance of cyclosporine soft gealtin capsules in renal allograft recipients. Ann Pharmacother 1992;26:175-179.
86. Zehender C, Beveridge T, Nüesch E, Abisch A, Thiel G. Cyclosporin A capsules: bioavailability and clinical acceptance study in renal transplant patients. Transplant Proc 1988;20:641-643.
87. Bleck JS, Nashan B, Christians U, Schottmann R, Wonigeit K, Sewing KF. Single dose pharmacokinetics of cyclosporine and its main metabolites after oral cyclosporine as oily solution or capsule. Arzneimittelforschung 1990;40:62-64.
88. Nashan B, Bleck J, Wonigeit K, et al. Effect of application form of cyclosporine on blood levels: comparison of oral solution and capsules. Transplant Proc 1988;20:637-639.
89. Hildebrands LB, Hoitsma AJ, van den Berg JWO, Koene RAP. Cyclosporin A blood levels during use of cyclosporin as oral solution or in capsules: comparison of pharmacokinetic parameters. Transplant Int 1991;4:125-127.
90. Kovarik JM, Mueller EA, Johnston A, Hitzenberger G, Kutz K. Bioequivalence of soft gelatin capsules and oral solution new cyclosporine formulation. Pharmacotherapy 1993;13:613-617.
91. Benet LZ, Wu CY, Hebert MF, Wacher VJ. Intestinal drug metabolism and antitransport processes: A potential paradigm shift in oral drug delivery. J Controlled Release 1996;39:139-143.
92. Sridhar N, Schroeder TJ, Hariharan S, Pesce AJ, First MR. Influence of concomitant medication on cyclosporine dosage and blood concentrations in renal allograft patients. Clin Transplant 1991;6: 134-141.
93. First RM, Schroeder TJ, Michael A, Hariharan S, Weiskittel P, Alexander JW. Cyclosporine-ketoconazole interaction. Long-term follow-up and preliminary results of a randomized trial. Transplantation 1993;55:1000-1004.
94. Liu JP. Use of the repeated cross-oxer designs in assessing bioequivalence. Stat Med 1995;14:1067-1078.
95. Pidgen A. Bioequivalence and generic prescribing: an industrial view. J Pharm Pharmacol 1996;48:11-16.-