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Antibody-Drug Conjugates: A Historical Review

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Book cover Antibody-Drug Conjugates

Part of the book series: AAPS Advances in the Pharmaceutical Sciences Series ((AAPS,volume 17))

Abstract

This chapter reviews the development of antibody–drug conjugates (ADCs) before 1980s. Focus is on the early exploratory approaches to prove the concept of antibody-mediated “magic bullets.” Progress of ADC development correlated closely with the advances of the knowledge and technology in immunology, conjugation chemistry, molecular biology, and cell biology. Results from diverse studies in different scientific disciplines during the past half century have slowly established ADCs as a new category of biotherapeutics in cancer treatment.

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References

  • Allen TM, Brandeis E, Hansen CB, Kao GY, Zalipsky S (1995) A new strategy for attachment of antibodies to sterically stabilized liposomes resulting in efficient targeting to cancer cells. Biochim Biophys Acta 1237:99–108

    Article  PubMed  Google Scholar 

  • Bird RE, Hardmann KD, Jacobson JW, Johnson S, Kaufman BM, Lee S, Lee T, Pope SH, Riordan GS, Whitlow M (1988) Single-chain antigen-binding proteins. Science 242:423–426

    Article  CAS  PubMed  Google Scholar 

  • Blair AH, Ghose TI (1983) Linkage of cytotoxic agents to immunoglobulins. J Immunol Methods 59:129–143

    Article  CAS  PubMed  Google Scholar 

  • Blattler WA, Kuenzi BS, Lambert JM, Senter PD (1985) A new heterobifunctional protein crosslinking reagent that forms an acid labile link. Biochemistry 24:1517–1524

    Article  CAS  Google Scholar 

  • Dillman RO, Johnson DE, Shawler DI, Koziol JA (1988) Superiority of an acid-labile daunorubucin-monoclonal antibody immunoconjugate compared to free drug. Cancer Res 48:6097–6102

    CAS  PubMed  Google Scholar 

  • Ducry L, Stump B (2010) Antibody-drug conjugates: linking cytotoxic payloads to monoclonal antibodies. Bioconjug Chem 21:5–13

    Article  CAS  PubMed  Google Scholar 

  • Duncan R, Lloyd JB, Kopecek J (1980) Degradation of side chains of N-(2-hydroxypropyl) methacrylamide copolymers by lysosomal enzymes. Biochem Biophys Res Commun 94:284–290

    Article  CAS  PubMed  Google Scholar 

  • Gallego J, Price MR, Baldwin RW (1984) Preparation of four daunomycin-monoclonal antibody 791T/36 conjugates with anti-tumor activities. Int J Cancer 33:737–744

    Article  CAS  PubMed  Google Scholar 

  • Garnett MC, Baldwin RW (1986) An improved synthesis of a methotrexate-albumin-791T/36 monoclonal antibody conjugate cytotoxic to human osteogenic sarcoma cell lines. Cancer Res 46:2407–2412

    CAS  PubMed  Google Scholar 

  • Ghose T, Blair AH (1978) Antibody-linked cytotoxic agents in the treatment of cancer: current status and future prospects. J Natl Cancer Inst 61:657–676

    CAS  PubMed  Google Scholar 

  • Ghose T, Nigam SP (1972) Antibody as carrier of chlorambucil. Cancer 29:1398–1400

    Article  CAS  PubMed  Google Scholar 

  • Ghose T, Guclu A, Tai J (1975) Suppression of an AKR lymphoma by antibody and chlorambucil. J Natl Cancer Inst 55:1353–1357

    CAS  PubMed  Google Scholar 

  • Ghose T, Norvell ST, Guclu A, Bodurtha A, Tai J, MacDonald AS (1977) Immunochemotherapy of malignant melanoma with chlorambucil-bound anti-melanoma globulins: preliminary results in patients with disseminated disease. J Natl Cancer Inst 58:845–852

    CAS  PubMed  Google Scholar 

  • Hurwitz E, Levy R, Maron R, Wilchek M, Arnon R, Sela M (1975) The covalent binding of daunomycin and adriamycin to antibodies, with retention of both drug and antibody activites. Cancer Res 35:1175–1181

    CAS  PubMed  Google Scholar 

  • Jones PT, Dear PH, Foote J, Neuberger MS, Winter G (1986) Replacing the complementarity-determining regions in a human antibody with those from a mouse. Nature 321:522–525

    Article  CAS  PubMed  Google Scholar 

  • Kim KJ, Li B, Winer J, Armanini M, Gillet N, Phillips HS, Ferrara N (1993) Inhibition of vascular endothelial growth factor-induced angiogenesis suppresses tumor growth in vivo. Nature 362:841–844

    Article  CAS  PubMed  Google Scholar 

  • Kohler G, Milstein C (1975) Continuous cultures of fused cells secreting antibody of predefined specificity. Nature 256:495–497

    Article  CAS  PubMed  Google Scholar 

  • Manabe Y, Tsubota T, Haruta Y, Kataoka K, Okazaki M, Haisa S, Nakamura K, Kimura I (1984) Production of a monoclonal antibody-methotrexate conjugate utilizing dextran T-40 and its biologic activity. J Lab Clin Med 104:445–454

    CAS  PubMed  Google Scholar 

  • Mathé G (1969) Approaches to the immunological treatment of cancer in man. Brit Med J 4:7–10

    Article  PubMed Central  CAS  PubMed  Google Scholar 

  • Mathé G, Loc T, Bernard J (1958) Effet sur la leucemie 1210 de la souris d’un combinaison par diazotation d’A-methopterin et de γ-globulines de hamsters porteurs de cette leucemie par heterograffe. C R Acad Sci 216:1626–1628

    Google Scholar 

  • McCafferty J, Griffiths AD, Winter G, Chiswell DJ (1990) Phage antibodies: filamentous phage displaying antibody variable domains. Nature 348:552–554

    Article  CAS  PubMed  Google Scholar 

  • Monsigny M, Kieda C, Roche A-C, Delmotte F (1980) Preparation and biological properties of a covalent antitumor drug-arm-carrier (DAC conjugate). FEBS Lett 119:181–186

    Article  CAS  PubMed  Google Scholar 

  • Moolten FL, Cooperband SR (1970) Selective destruction of target cells by diphtheria toxin conjugated to antibody directed against antigens on the cells. Science 169:68–70

    Article  CAS  PubMed  Google Scholar 

  • Morrison SL, Johnson MJ, Herzenberg LA, Oi VT (1984) Chimeric human antibody molecules: mouse antigen-binding domains with human constant region domains. Proc Natl Acad Sci U S A 81:6851–6855

    Article  PubMed Central  CAS  PubMed  Google Scholar 

  • Oon CJ, Apsey M, Buckleton H, Cooke KB, Hanham I, Hazanika P, Hobbs JB, McLeod B (1974) Human immune γ-globulin treated with chlorambucil for cancer therapy. Behring Inst Mitt 56:228–255

    Google Scholar 

  • Ortho Multicenter Transplant Study Group (1985) A randomized clinical trial of OKT3 monoclonal antibody for acute rejection of cadaveric renal transplants. NEJM 313:1–7

    Article  Google Scholar 

  • Rowland GF, O’Neill GJ, Davies DAL (1975) Suppression of tumor growth in mice by a drug-antibody conjugate using a novel approach to linkage. Nature 255:487–488

    Article  CAS  PubMed  Google Scholar 

  • Shen WC, Ryser HJ-P (1979) Poly(L-lysine) and poly(D-lysine) conjugates of methotrexate: different inhibitory effect on drug resistant cells. Mol Pharmacol 16:614–622

    CAS  PubMed  Google Scholar 

  • Shen WC, Ryser HJ-P (1981) Cis-aconityl spacer between daunomycin and macromolecular carrier: a model of pH-sensitive linkage releasing drug from a lysosomotropic conjugate. Biochem Biophys Res Commun 102:1048–1054

    Article  CAS  PubMed  Google Scholar 

  • Shen WC, Ballou B, Ryser HJ-P, Hakala TR (1986) Targeting, internalization, and cytotoxicity of methotrexate-monoclonal anti-SSEA-1 antibody conjugates in cultured F-9 teratocarcinoma cells. Cancer Res 46:3912–3916

    CAS  PubMed  Google Scholar 

  • Strebhardt K, Ullrich A (2008) Paul Ehrlich’s magic bullet concept: 100 years of progress. Nat Rev Cancer 8:473–480

    Article  CAS  PubMed  Google Scholar 

  • Trouet A, Masquelier M, Baurain R, Deprez-De Campeneere (1982) A covalent linkage between daunomycin and protein that is stable in serum and reversible by lysosomal hydrolases, as required for a lysosomotropic drug-carrier conjugate: in vitro and in vivo studies. Proc Natl Acad Sci U S A 79:626–629

    Google Scholar 

  • van de Vijver MJ, Peterse JL, Mooi WJ, Wisman P, Lomans J, Dalesio O, Nusse R (1988) Neu-protein overexpression in breast cancer. Association with comedo-type ductal carcinoma in situ and limited prognostic value in stage II breast cancer. NEJM 319:1239–1245

    Article  PubMed  Google Scholar 

  • Vitetta ES, Uhr JW (1985) Immunotoxins. Ann Rev Immunol 3:197–212

    Article  CAS  Google Scholar 

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Authors and Affiliations

  1. Department of Pharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California, 90033, Los Angeles, CA, USA

    Wei-Chiang Shen

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  1. Wei-Chiang Shen
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Correspondence to Wei-Chiang Shen .

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Editors and Affiliations

  1. Western University of Health Sciences, Department of Pharmaceutical Sciences, Pomona, California, USA

    Jeffrey Wang

  2. University of Southern California, Department of Pharmacology and Pharmaceutical Sciences, Los Angeles, California, USA

    Wei-Chiang Shen

  3. University of Southern California, Department of Pharmacology and Pharmaceutical Sciences, Los Angeles, California, USA

    Jennica L. Zaro

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© 2015 American Association of Pharmaceutical Scientists

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Shen, WC. (2015). Antibody-Drug Conjugates: A Historical Review. In: Wang, J., Shen, WC., Zaro, J. (eds) Antibody-Drug Conjugates. AAPS Advances in the Pharmaceutical Sciences Series, vol 17. Springer, Cham. https://doi.org/10.1007/978-3-319-13081-1_1

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