Subcutaneous administration of biotherapeutics: Current experience in animal models

Current Opinion in Molecular Therapeutics

Volumn 12, Issue 4, 2010, Pages 461-470

  McDonald, Thomas A ^a   Zepeda, Monica L ^b   Tomlinson, Michael J ^c   Bee, Walter H ^b   Ivens, Inge A ^a  

^a BAYER CORPORATION   (United States)

^b Halozyme Therapeutics Inc   (United States)

^c Nova Pathology PC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BETA1A INTERFERON; BIOLOGICAL FACTOR; BIOTHERAPEUTICS; BUSERELIN; CANAKINUMAB; CERTOLIZUMAB PEGOL; FLOXURIDINE; GOLIMUMAB; GROWTH HORMONE; HUMAN GROWTH HORMONE; HUMAN RECOMBINANT HEMOGLOBIN; HYALURONIDASE; HYLENEX; IMMUNOGLOBULIN G; INSULIN; INSULIN GLARGINE; INSULIN GLULISINE; INSULIN LISPRO; INTERFERON BETA SERINE; INTERLEUKIN 1 RECEPTOR BLOCKING AGENT; NOVEL ERYTHROPOIESIS STIMULATING PROTEIN; PEGINTERFERON ALPHA2A; PEGINTERFERON ALPHA2B; PEGVISOMANT; PRAMLINTIDE; RECOMBINANT ENZYME; RECOMBINANT HUMAN HYALURONIDASE; RECOMBINANT PROTEIN; RECOMBINANT SOMATOMEDIN C; UNCLASSIFIED DRUG; UNINDEXED DRUG; USTEKINUMAB; BIOLOGICAL PRODUCT;

ANESTHESIA; BLOOD VESSEL WALL; CAPILLARY; CLINICAL TRIAL; DERMIS; DISEASE MODEL; DRUG ABSORPTION; DRUG DEGRADATION; DRUG DELIVERY SYSTEM; DRUG DIFFUSION; DRUG DISTRIBUTION; DRUG PENETRATION; DRUG TRANSPORT; DRUG UPTAKE; EPIDERMIS; HUMAN; INTERMETHOD COMPARISON; INTERSTITIUM; INTRAVENOUS DRUG ADMINISTRATION; MAXIMUM PLASMA CONCENTRATION; MOLECULAR WEIGHT; MUSCLE; NONHUMAN; PANNICULUS CARNOSUS MUSCLE; PARAMETER; PRECIPITATION; REVIEW; SKIN PERMEABILITY; SKIN STRUCTURE; SPECIES DIFFERENCE; SUBCUTANEOUS DRUG ADMINISTRATION; SUBCUTANEOUS TISSUE; ANIMAL; ANIMAL MODEL; BIOAVAILABILITY; DRUG DEVELOPMENT;

ANIMALS; BIOLOGICAL AVAILABILITY; BIOLOGICAL PRODUCTS; DRUG DISCOVERY; INJECTIONS, SUBCUTANEOUS; MODELS, ANIMAL;

EID: 77955447706     PISSN: 14648431     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (60)

1. Lin JH: Pharmacokinetics of biotech drugs: Peptides, proteins and monoclonal antibodies. Curr Drug Metab (2009) 10(7): 661-691.
2. McLennan DN, Porter CJ, Edwards GA, Martin SW, Heatherington AC, Charman SA: Lymphatic absorption is the primary contributor to the systemic availability of epoetin alfa following subcutaneous administration to sheep. J Pharmacol Exp Ther (2005) 313(1):345-351.
3. Porter CJ, Charman SA: Lymphatic transport of proteins after subcutaneous administration. J Pharm Sci (2000) 89(3):297-310.
4. Haller MF: Converting intravenous dosing to subcutaneous dosing with recombinant human hyaluronidase. Pharm Tech (2007):October 02.
5. Ponce R, Abad L, Amaravadi L, Gelzleichter T, Gore E, Green J, Gupta S, Herzyk D, Hurst C, Ivens IA, Kawabata T, et al.: Immunogenicity of biologically-derived therapeutics: Assessment and interpretation of nonclinical safety studies. Regul Toxicol Pharmacol (2009) 54(2):164-182.
6. Supersaxo A, Hein WR, Steffen H: Effect of molecular weight on the lymphatic absorption of water-soluble compounds following subcutaneous administration. Pharm Res (1990) 7(2):167-169.
7. Charman SA, Segrave AM, Edwards GA, Porter CJ: Systemic availability and lymphatic transport of human growth hormone administered by subcutaneous injection. J Pharm Sci (2000) 89(2):168-177.
8. Charman SA, McLennan DN, Edwards GA, Porter CJ: Lymphatic absorption is a significant contributor to the subcutaneous bioavailability of insulin in a sheep model. Pharm Res (2001) 18(11):1620-1626.
9. Porter CJ, Edwards GA, Charman SA: Lymphatic transport of proteins after s.c. injection: Implications of animal model selection. Adv Drug Deliv Rev (2001) 50(1-2):157-171.
10. McLennan DN, Porter CJ, Edwards GA, Heatherington AC, Martin SW, Charman SA: The absorption of darbepoetin alfa occurs predominantly via the lymphatics following subcutaneous administration to sheep. Pharm Res (2006) 23(9):2060-2066.
11. Draft guidance for industry and FDA staff: Technical considerations for pen, jet, and related injectors intended for use with drugs and biological products. FDA, Bethesda, MD, USA (2009). www.fda.gov/downloads/ RegulatoryInformation/Guidances/UCM147095.pdf
12. International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use-ICH Harmonised Tripartite Guideline: Preclinical Safety Evaluation of Biotechnology-Derived Pharmaceuticals (S6). International Conference on Harmonisation, Geneva, Switzerland (1997). www.ich.org/LOB/media/MEDIA503.pdf.
13. Tang L, Persky AM, Hochhaus G, Meibohm B: Pharmacokinetic aspects of biotechnology products. J Pharm Sci (2004) 93(9): 2184-2204.
14. Hargis AM, Ginn PE: The Integument. In: Pathologic Basis of Veterinary Disease. Zachary JF, McGavin MD (Eds), Mosby Elsevier, St Louis, MO, USA (2007):1107-1261.
15. Frost GI: Recombinant human hyaluronidase (rHuPH20): An enabling platform for subcutaneous drug and fluid administration. Expert Opin Drug Deliv (2007) 4(4):427-440.
16. Wells MY, Voute H, Bellingard V, Fisch C, Boulifard V, George C, Picaut P: Histomorphology and vascular lesions in dorsal rat skin used as injection sites for a subcutaneous toxicity study. Toxicol Pathol (2010) 38(2):258-266.
17. Bronaugh RL, Stewart RF, Congdon ER: Methods for in vitro percutaneous absorption studies. II. Animal models for human skin. Toxicol Appl Pharmacol (1982) 62(3):481-488.
18. Kurihara-Bergstrom T, Woodworth M, Feisullin S, Beall P: Characterization of the Yucatan miniature pig skin and small intestine for pharmaceutical applications. Lab Anim Sci (1986) 36(4):396-399.
19. Lavker RM, Dong G, Zheng PS, Murphy GF: Hairless micropig skin. A novel model for studies of cutaneous biology. Am J Pathol (1991) 138(3):687-697.
20. Yabuki A, Kamimura R, Setoyama K, Tottori J, Taniguchi K, Matsumoto M, Suzuki S: Skin morphology of the Clawn miniature pig. Exp Anim (2007) 56(5):369-373.
21. Ngawhirunpat T, Opanasopit P, Prakongpan S: Comparison of skin transport and metabolism of ethyl nicotinate in various species. Eur J Pharm Biopharm (2004) 58(3):645-651.
22. Vana G, Meingassner JG: Morphologic and immunohistochemical features of experimentally induced allergic contact dermatitis in Gottingen minipigs. Vet Pathol (2000) 37(6): 565-580.
23. Ikomi F, Schmid-Schonbein GW: Lymph transport in the skin. Clin Dermatol (1995) 13(5):419-427.
24. Swartz MA: The physiology of the lymphatic system. Adv Drug Deliv Rev (2001) 50(1-2):3-20.
25. Novakov SS, Yotova NI, Petleshkova TD, Muletarov SM: Sternalis muscle-A riddle that still awaits an answer. Folia Med (Plovdiv) (2008) 50(2):63-66.
26. Rose EH, Vistnes LM, Ksander GA: The panniculus carnosus in the domestic pig. Plast Reconstr Surg (1977) 59(1):94-97.
27. Kawamata S, Ozawa J, Hashimoto M, Kurose T, Shinohara H: Structure of the rat subcutaneous connective tissue in relation to its sliding mechanism. Arch Histol Cytol (2003) 66(3):273-279.
28. Cross SE, Roberts MS: Dermal blood flow, lymphatics, and binding as determinants of topical absorption, clearance and distribution. In: Dermal Absorption Models in Toxicology and Pharmacology. Riviere JE (Ed), Taylor and Francis Group, Boca Raton, FL, USA (2006):251-281.
29. Kota J, Machavaram KK, McLennan DN, Edwards GA, Porter CJ, Charman SA: Lymphatic absorption of subcutaneously administered proteins: Influence of different injection sites on the absorption of darbepoetin alfa using a sheep model. Drug Metab Dispos (2007) 35(12):2211-2217.
30. Aukland K, Reed RK: Interstitial-lymphatic mechanisms in the control of extracellular fluid volume. Physiol Rev (1993) 73(1): 1-78.
31. Day TD: The permeability of interstitial connective tissue and the nature of the interfibrillary substance. J Physiol (1952) 117(1):1-8.
32. Kojima K, Takahashi T, Nakanishi Y: Lymphatic transport of recombinant human tumor necrosis factor in rats. J Pharmacobiodyn (1988) 11(10):700-706.
33. Kagan L, Gershkovich P, Mendelman A, Amsili S, Ezov N, Hoffman A: The role of the lymphatic system in subcutaneous absorption of macromolecules in the rat model. Eur J Pharm Biopharm (2007) 67(3):759-765.
34. Bocci V, Muscettola M, Grasso G, Magyar Z, Naldini A, Szabo G: The lymphatic route. (1) Albumin and hyaluronidase modify the normal distribution of interferon in lymph and plasma. Experientia (1986) 42(4):432-433.
35. Drug approval package: PEGinterferon alfa-2a product approval information-Licensing action. Food and Drug Administration, Silver Spring, MD, USA (2002). www.fda.gov/Drugs/DevelopmentApprovalProcess/ HowDrugsareDevelopedandApproved/ApprovalApplications/ TherapeuticBiologicApplications/ucm080721.htm
36. Drug approval package: Somavert (pegvisomant) injectable. Food and Drug Administration, Silver Spring, MD, USA (2002). www.accessdata.fda.gov/ drugsatfda-docs/nda/2003/021106-somavert.cfm
37. Fishbane S, Pannier A, Liogier X, Jordan P, Dougherty FC, Reigner B: Pharmacokinetic and pharmacodynamic properties of methoxy polyethylene glycol-epoetin β are unaffected by the site of subcutaneous administration. J Clin Pharmacol (2007) 47(11):1390-1397.
38. Jensen JD, Jensen LW, Madsen JK: The pharmacokinetics of recombinant human erythropoietin after subcutaneous injection at different sites. Eur J Clin Pharmacol (1994) 46(4): 333-337.
39. Macdougall IC, Jones JM, Robinson MI, Miles JB, Coles GA, Williams JD: Subcutaneous erythropoietin therapy: Comparison of three different sites of injection. Contrib Nephrol (1991) 88:152-156; discussion 157-158.
40. Beshyah SA, Anyaoku V, Niththyananthan R, Sharp P, Johnston DG: The effect of subcutaneous injection site on absorption of human growth hormone: Abdomen versus thigh. Clin Endocrinol (1991) 35(5):409-412.
41. Drug approval package: Apidra (insulin glulisine [rDNA origin]) injection. Food and Drug Administration, Silver Spring, MD, USA (2004). www.accessdata.fda.gov/drugsatfda-docs/nda/2004/21-629-Apidra.cfm
42. Drug approval package: Humalog (insulin lispro [rDNA origin] injection), Food and Drug Administration, Silver Spring, MD, USA (1997). www.accessdata.fda.gov/drugsatfda-docs/nda/97/020563a- s003-071697.pdf
43. Scientific discussion: Lantus. European Medicines Agency, London, UK (2003). www.ema.europa.eu/docs/en-GB/document-library/EPAR-Scientific- Discussion/human/000284/WC500036075.pdf
44. Hizentra: Highlights of prescribing information. CSL Behring, King of Prussia, PA, USA (2010). www.hizentra.com/docs/hizentraPI.pdf
45. Thomas JR, Yocum RC, Haller MF, von Gunten CF: Assessing the role of human recombinant hyaluronidase in gravity-driven subcutaneous hydration: The INFUSE-LR study. J Palliat Med (2007) 10(6):1312-1320.
46. Allen CH, Etzwiler LS, Miller MK, Maher G, Mace S, Hostetler MA, Smith SR, Reinhardt N, Hahn B, Harb G: Recombinant human hyaluronidase-enabled subcutaneous pediatric rehydration. Pediatrics (2009) 124(5):e858-E867.
47. Prescribing information. HYLENEX recombinant (hyaluronidase human injection). Baxter Healthcare Corp, Deerfield, IL, USA (2010). www.hylenex.com/pdf/prescribe.pdf
48. Bookbinder LH, Hofer A, Haller MF, Zepeda ML, Keller GA, Lim JE, Edgington TS, Shepard HM, Patton JS, Frost GI: A recombinant human enzyme for enhanced interstitial transport of therapeutics. J Control Release (2006) 114(2):230-241.
49. Leesch VW, Johnson BA, Cook CS, Yocum RC, Schiff RI, Muchitsch EM, Teschner W: 30-Day pharmacokinetic evaluation of IV versus subcutaneous administration of immunoglobulin with and without recombinant human hyaluronidase in dogs. J Allergy Clin Immunol (2009) 123(2 Suppl 1):S10.
50. Bee WH, Nekoroski T, Zhang L, Kang D, Teschner W, Schwarz HP, Muchitsch EM: Effects of recombinant human hyaluronidase (rHuPH20) on subcutaneous administration of 10% and 20% IgG in Yucatan mini pigs. American Academy of Allergy, Asthma and Immunology Annual Meeting, New Orleans, LA, USA (2010):Abs 547.
51. Drugs@FDA: FDA approved drug products. Food and Drug Administration, Silver Spring, MD, USA (2010). www.accessdata.fda. gov/scripts/cder/drugsatfda
52. EPARs for authorised medicinal products for human use. European Medicines Agency, London, UK (2010). www. ema.europa.eu/ema/index.jsp ? curl=pages/medicines/landing/epar-search.jsp&murl=menus/medicines/medicines. jsp&mid=WC0b01ac058001d124
53. Drug approval package: PEGinterferon alfa-2b approval information-Licensing action. Food and Drug Administration, Silver Spring, MD, USA (2009). www.fda.gov/Drugs/Development Approval Process/How Drugsare Developed and Approved /ApprovalApplications/TherapeuticBiologicApplications/ ucm080727. htm
54. Drug approval package: Simponi (golimumab) injection. Food and Drug Administration, Silver Spring, MD, USA (2009). www.accessdata. fda.gov/drugsatfda-docs/nda/2009/125289s0000TOC.cfm
55. Drug approval package: Stelara (ustekinumab) injection. Food and Drug Administration, Silver Spring, MD, USA (2009). www.accessdata. fda.gov/drugsatfda-docs/nda/2009/125261s000TOC.cfm
56. Drug approval package: Arcalyst (rilonacept) vial. Food and Drug Administration, Silver Spring, MD, USA (2008). www.accessdata.fda. gov/drugsatfda-docs/nda/2008/125249s000TOC.cfm
57. Drug approval package: Betaseron (interferon β-1b) subcutaneous. Food and Drug Administration, Silver Spring, MD, USA (1993). www.accessdata.fda.gov/drugsatfda-docs/nda/pre96/103471s0000TOC.cfm
58. Scientific discussion: Betaferon. European Medicines Agency, London, UK (2003). www.ema.europa.eu/docs/en-GB/document-library/EPAR-Scientific- Discussion/human/000081/WC500053087.pdf
59. Drug approval package: PEGinterferon alfa-2b approval information ? Licensing action. Food and Drug Administration, Silver Spring, MD, USA (2001). www.fda.gov/Drugs/Development Approval Process/HowDrugsareDevelopedandApproved /ApprovalApplications/TherapeuticBiologicApplications/ucm080727. htm
60. Drug approval package: Neulasta (pegfilgrastim) injection. Food and Drug Administration, Silver Spring, MD, USA (2001). www. accessdata.fda.gov/ drugsatfda-docs/nda/2002/125031-0000- NeulastaTOC.cfm