Development of a subcutaneous formulation for trastuzumab - Nonclinical and clinical bridging approach to the approved intravenous dosing regimen

Arzneimittel-Forschung/Drug Research

Volumn 62, Issue 9, 2012, Pages 401-409

  Bittner, B ^a   Richter, W F ^a   Hourcade Potelleret, F ^a   McIntyre, C ^a   Herting, F ^b   Zepeda, M L ^c   Schmidt, J ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b ROCHE DIAGNOSTICS GMBH   (Germany)

^c Halozyme Therapeutics Inc   (United States)

Author keywords

clinical; dose finding; injection device; nonclinical; subcutaneous; trastuzumab

Indexed keywords

RECOMBINANT HYALURONIDASE; TRASTUZUMAB;

BREAST CANCER; CANCER INHIBITION; DOSAGE SCHEDULE COMPARISON; DRUG BLOOD LEVEL; DRUG COST; DRUG FORMULATION; DRUG SAFETY; DRUG TOLERABILITY; HUMAN; LOADING DRUG DOSE; LUNG NON SMALL CELL CANCER; MAINTENANCE DRUG DOSE; MINIPIG; NONHUMAN; OVERALL SURVIVAL; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); REVIEW; UNSPECIFIED SIDE EFFECT; XENOGRAFT;

EID: 84866292134     PISSN: 00044172     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0032-1321831     Document Type: Review

References (53)

1. Clifford A, Hudis M D. Trastuzumab, Mechanism of action and use in clinical practice. N Engl J Med: 2007; 357 39 51
2. Bystricky B, Okines AF C, Cunningham D. Targeting HER-2 in gastric cancer - incorporation of trastuzumab into the treatment of operable disease. Gastrointestinal Cancer: Targets and Therapy: 2011; 1 41 52
3. Poorter R L, Lauw F N, Bemelman W A et al. Complications of an Implantable Venous Access Device (Port-A-Cath®) During Intermittent Continuous Infusion of Chemotherapy. Eur J Cancer: 1996; 32 2262 2266
4. Shivakumar S P, Anderson D R, Couban S. Catheter-associated thrombosis in patients with malignancy. J Clin Oncol: 2009; 27 29 4858 4864
5. Piccart-Gebhart M J, Procter M, Leyland-Jones B et al. Trastuzumab after adjuvant chemotherapy in HER2-positive breast cancer. N Engl J Med: 2005; 353 16 1659 1672 (Pubitemid 41464705)
6. Bedell C H. A changing paradigm for cancer treatment: The advent of new oral chemotherapy agents. Clin J Oncol Nurs: 2003; 7 (6 SUPPL) 5 9
7. Liu G, Franssen E, Fitch M I et al. Patient preferences for oral versus intravenous palliative chemotherapy. J Clin Oncol: 1997; 15 110 115 (Pubitemid 27021524)
8. Laino C. Oral chemotherapy plus trastuzumab found safe, effective for breast cancer. Oncology Times: 2009; 31 09 28 30
9. Schweighofer C, Wendtner C. First-line treatment of chronic lymphocytic leukemia: role of alemtuzumab. OncoTargets and Therapy: 2010; 3 53 67
10. Fasth A, Nystroem J. Quality of life and health-care resource utilization among children with primary immunodeficiency receiving home treatment with subcutaneous human immunoglobulin. J Clin Immunol: 2008; 28 370 378
11. Barber N, Hoffmeyer U. Comparison of the cost-effectiveness of administering heparin subcutaneously or intravenously for the treatment of deep vein thrombosis. Annals of The Royal College of Surgeons of England: 1993; 75 430 433 (Pubitemid 23323452)
12. Kivitz A, Cohen S, Dowd J E et al. Clinical assessment of pain, tolerability, and preference of an autoinjection pen versus a prefilled syringe for patient self-administration of the fully human, monoclonal antibody adalimumab: the touch trial. Clin Ther: 2006; 28 1619 1629 (Pubitemid 44838895)
13. Akpinar R B, Celebioglu A. Effect of injection duration on bruising associated with subcutaneous heparin: a quasi-experimental within-subject design. International Journal of Nursing Studies: 2008; 45 812 817
14. Jorgensen J T, Romsing J, Rasmussen M et al. Pain assessment of subcutaneous injections. The Annals of Pharmacotherapy: 1996; 30 729 732 (Pubitemid 26243913)
15. Hunter J. Subcutaneous injection technique. Nursing Standard: 2008; 22 41 44
16. Bittner B, Schmidt J. Subcutaneous Administration of Monoclonal Antibodies in Oncology as Alternative to Established Intravenous Infusion. Pharm Ind: 2012; 74 04 638 643
17. Bookbinder L H, Hofer A, Haller M F et al. A recombinant human enzyme for enhanced interstitial transport of therapeutics. Journal of Controlled Release: 2006; 114 230 241 (Pubitemid 44291844)
18. Watson D. Hyaluronidase. Br J Anaesth.: 1993; 71 422 425 (Pubitemid 23268889)
19. Frost G I. Recombinant human hyaluronidase (rHuPH20): An enabling platform for subcutaneous drug and fluid administration. Expert Opinion in Drug Delivery: 2007; 4 427 440 (Pubitemid 47249140)
20. Chain E, Duthie E. Identity of hyaluronidase as spreading factor. Brit J Exper Pathol: 1940; 21 324 338
21. Pirrello R D, Ting Chen C, Thomas S H. Initial experiences with subcutaneous recombinant human hyaluronidase. J Palliat Med: 2007; 10 861 864 (Pubitemid 350030778)
22. Thomas D R, Cote T R, Lawhorne L et al. Understanding clinical dehydration and its treatment. J Am Med Dir Assoc: 2008; 9 05 292 301 (Pubitemid 351756273)
23. Deputy Division Director's Memorandum, NDA 21-859, 2005. Halozyme Therapeutics, Inc
24. Sanford M, McCormack P L. Ofatumumab. Drugs: 2010; 70 1013 1019
25. Bleeker W K, Munk M E, Mackus WJ M et al. Estimation of dose requirements for sustained in vivo activity of a therapeutic human anti-CD20 antibody. Br J Haematol: 2008; 140 03 303 312
26. Ribas A, Hanson D C, Noe D A et al. Tremelimumab (CP-675,206), a cytotoxic T lymphocyte - associated antigen 4 blocking monoclonal antibody in clinical development for patients with cancer. Oncologist: 2007; 12 07 873 883 (Pubitemid 47328230)
27. Ricart A D, Tolcher A W, Liu G et al. Volociximab, a chimeric monoclonal antibody that specifically binds alpha5beta1 integrin: A phase I, pharmacokinetic, and biological correlative study. Clin Cancer Res: 2008; 14 7924 7929
28. Harries M, Smith I. The development and clinical use of trastuzumab (Herceptin). Endocrine-Related Cancer: 2002; 9 75 85 (Pubitemid 34832161)
29. Baselga J, Phase I II. clinical trials of trastuzumab. Annals of Oncology: 2001; 12 ( SUPPL 1 ) S49 S55
30. Le X F, Mao W, Lu C et al. Specific Blockade of VEGF and HER2 pathways results in greater growth inhibition of breast cancer xenografts that overexpress HER2. Cell Cycle: 2008; 7 23 3747 3758
31. Baselga J, Carbonell X, Castañeda-Soto N J et al. Phase II study of efficacy, safety, and pharmacokinetics of trastuzumab monotherapy administered on a 3-weekly schedule. J Clin Oncol: 2005; 23 10 2162 2171 (Pubitemid 46218708)
32. Bruno R, Washington C B, Lu J F et al. Population pharmacokinetics of trastuzumab in patients with HER2-positive metastatic breast cancer. Cancer Chemother Pharmacol: 2005; 56 04 361 369 (Pubitemid 41095399)
33. Fukushima Y, Charoin J, Brewster M et al. Population pharmacokinetic analysis of trastuzumab (Herceptin) based on three different dosing regimens. Abstracts of the Annual Meeting of the Population Approach Group in Europe: 2007; 16 Abstr 1121
34. Mager D, Jusko W. General pharmacokinetic model for drugs exhibiting target-mediated drug disposition. J Pharmacokinetics Pharmacodynamics: 2001; 28 507 532 (Pubitemid 34289541)
35. Vogel C L, Cobleigh M A, Tripathy D et al. Efficacy and safety of trastuzumab as a single agent in first-line treatment of HER2-overexpressing metastatic breast cancer. J Clin Oncol: 2002; 20 719 726 (Pubitemid 34111379)
36. Friess T, Scheuer W, Hasmann M. Combination treatment with erlotinib and pertuzumab against humor tumor xenografts is superior to monotherapy. Clin Cancer Res: 2005; 11 5300 5308
37. Scheuer W, Friess T, Burtscher H et al. Strongly enhanced antitumor activity of trastuzumab and pertuzumab combination treatment on HER2-positive human xenograft tumor models. Cancer Res: 2009; 69 9330 9336
38. Bywaters EG L, Holborow E J, Keech M K. Reconstitution of the dermal barrier after hyaluronidase injection. Br Med J: 1951; 2 4741 1178 1183
39. Rose E H, Vistnes L M, Ksander G A. The panniculus carnosus in the domestic pig. Plast Reconstr Surg: 1977; 59 94 97 (Pubitemid 8020472)
40. Zheng Y, Tesar D B, Benincosa L et al. Minipig as a potential translatable model for monoclonal antibody pharmacokinetics after intravenous and subcutaneous administration. mAbs: 2012; 4 02 March/April
41. Kirshner S. Immunogenicity of therapeutic proteins: a regulatory perspective. In: Detection and Quantification of Antibodies to Biopharmaceuticals: Practical and Applied Considerations. Tovey M G. (Ed.). John Wiley and Sons Inc. NY, USA: 2011
42. Wynne C, Harvey V, Schwabe C et al. Comparison of subcutaneous and intravenous administration of trastuzumab: a phase I/Ib trial in healthy male volunteers and patients with HER2-positive breast cancer. J Clin Pharmacol Published online 22. Feb.: 2012; 10.1177/0091270012436560
43. Freireich E J, Gehan E A, Rall D P et al. Quantitative comparison of toxicity of anticancer agents in mouse, rat, dog, monkey, and man. Cancer Chemother Rep: 1966; 50 219 244
44. Egorin M J. Horseshoes, hand grenades, and body-surface area-based dosing: aiming for a target. Journal of Clinical Oncology: 2003; 21 02 182 183 (Pubitemid 46606144)
45. Bai S, Jorga K, Xin Y et al. A guide to rational dosing of monoclonal antibodies. Clinical Pharmacokinetics: 2012; 51 119 135
46. Mathijssen R H, de Jong F A, Loos W J et al. Flat-fixed dosing versus body surface area based dosing of anticancer drugs in adults: does it make a difference? Oncologist: 2007; 12 08 913 923 (Pubitemid 47359133)
47. Ng C M, Lum B L, Gimenez V et al. Rationale for fixed dosing of pertuzumab in cancer patients based on population pharmacokinetic analysis. Pharm Res: 2006; 23 06 1275 1284 (Pubitemid 43946149)
48. Wang D D, Zhang S, Zhao H et al. Fixed dosing versus body size-based dosing of monoclonal antibodies in adult clinical trials. J Clin Pharmacol: 2009; 49 1012 1024
49. Jackisch C, Stroyakovskiy D, Muehlbauer S et al. Subcutaneous administration of trastuzumab in patients with HER2-positive early breast cancer: Results from the Phase III randomised, open-label, multi-centre neoadjuvant-adjuvant HannaH study. European Breast Cancer Conference (EBCC-8): 2012; Abstr 1BA
50. Dani B, Platz R, Tzannis S T. High concentration formulation feasibility of human immunoglobulin G for subcutaneous administration. J Pharm Sci: 2007; 96 1504 1517 (Pubitemid 46953766)
51. Shire S J, Shahrokh Z, Liu J. Challenges in the development of high protein concentration formulations. J Pharm Sci: 2004; 93 1390 1402 (Pubitemid 38725014)
52. Adler M, Grauschopf U, Mahler H C et al. Subcutaneous anti-HER2 antibody formulations and uses thereof. Patent application US 2011/0044977 A1
53. Ratner M. Roche plans for more convenient-to-use Herceptin and Rituxan. Nature biotechnology: 2010; 28 04 289