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452 Pages·2002·10.793 MB·English
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TUMOR TARGETING IN CANCER THERAPY CANCER DRUG DISCOVERY AND DEVELOPMENT Beverly A. Teicher, Series Editor Tumor Targeting in Cancer Therapy, edited by Michel Page, 2002 Chemoradiation in Cancer Therapy, edited by Hak Choy, 2002 Targets for Cancer Chemotherapy: Transcription Factors and Other Nuclear Proteins, edited by Nicholas B. La Thangue and Lasantha R. Bandara, 2002 Endocrine Therapy in Breast and Prostate Cancer, edited by V. Craig Jordan and Barrington J. A. Furr, 2002 Tumor Models in Cancer Research, edited by Beverly A. Teicher, 2002 Tumor Suppressor Genes in Human Cancer, edited by David E. Fisher, 2001 Matrix Metalloproteinase Inhibitors in Cancer Therapy, edited by Neil J. Clendeninn and KrzysztoJ Appelt, 2001 Farnesyltransferase Inhibitors in Cancer and Cardiovascular Therapy, edited by Saiä M. Sebti and Andrew D. Hamilton, 2001 Platinum-Based Drugs in Cancer Therapy, edited by Lloyd R. Kelland and Nicholas P. Farrell, 2000 Apoptosis and Cancer Chemotherapy, edited by John A. Hickman and Carotine Dive, 1999 Signal Transduction and Cell Cycle Inhibitors in Cancer Therapy, edited by J. Silvio Gutkind, 1999 Antifolate Drugs in Cancer Therapy, edited by Ann L. Jackman, 1999 Antiangiogenic Agents in Cancer Therapy, edited by Beverly A. Teicher, 1999 Anticancer Drug Development Guide: Preclinical Screening, Clinical Trials, and Approva~ edited by Beverly A. Teicher, 1997 Cancer Therapeutics: Experimental and Clinical Agents, edited by Beverly A. Teicher, 1997 TUMOR T ARGETING IN CANCER THERAPY Edited by MICHEL PAGE, PhD 0/ Department Medical Biology, 0/ Faculty Medicine, Universite Lava/, Sainte-Foy, Quebec, Canada ~ ~ Springer Science+Business Media, LLC © 2002 Springer Science+Business Media New York Originally published by Humana Press Inc. in 2002 Softcover reprint ofthe hardcover 1st edition 2002 www.humanapress.com All rights reserved. No part of this book may be reproduced. stored in a retrieval system, or transmitted in any form or by any means, electronic, mechanical, photocopying, microfilming, recording, or otherwise without written permission from the Publisher. All articles, comments, opinions, conclusions, or recommendations are those ofthe author(s), and do not necessarily reflect the views of the publisher. Cover design by Patricia F. Cleary. Cover illustration: From Fig. 4B in Chapter 21 "Internalization of Antibodies," by Jairo Jaime Correa. Production Editor: Kim Hoather-Potter. This publication is printed on acid-free paper.Q ANSI Z39.48-1984 (American National Standards Institute) Permanence of Paper for Printed Library Materials For additional copies, pricing for bulk purchases, andlor information about other Humana titles, contact Humana at the above address or at any of the following numbers: Tel.:973-256-1699; Fax: 973-256-8341; Email: humanapr.com; or visit our Website: http://humanapress.com Photocopy Authorization Policy: Authorization to photocopy items for internal or personal use, or the internal or personal use of specific clients, is granted by Springer Science+Business Media, LLC, provided that the base fee of US $10.00 per copy, plus US $00.25 per page, is paid directly the Copyright Clearance Center at 222 Rosewood Drive, Danvers, MA 01923. For those organizations that have been gran ted a photocopy license from the CCC, a separate system of payment has been arranged and is acceptable to Springer Science+Business Media, LLC. The fee code for users of the Transactional Reporting Service is: [0-89603-919-6/02 $10.00 + $00.25]. 10 9 8 7 6 5 4 3 2 1 Library of Congress Cataloging-in-Publication Data Tumor targeting in cancer therapy/edited by Michel Page. p.;cm.-(Cancer drug discovery and development) ISBN 978-1-61737-251-3 ISBN 978-1-59259-167-1 (eBook) DOI 10.1007/978-1-59259-167-1 1. Cancer-Immunotherapy. 2. Cancer-Chemotherapy. 3. Drug targeting.1. Page, Michael. 11. Series. [DNLM: . Neoplasms-immunology. 2. Antibodies, Neoplasm-therapeutic use. 3. Antineoplastic Agents-therapeutic use. 4. Drug Delivery Systems. 5. Neoplasms-therapy. QZ 266 T9265 2002] RC271.I45 T86 2002 616.99'406---dc21 2001051657 PREFACE The purpose ofTumor Targeting in Cancer Therapy is to describe both experimental and clinical applications of antibodies for targeting tumors. Drug targeting has gone a long way since the initial concept of "magie bullets" was developed by Paul Ehrlich at the beginning of the 20th century. Twenty-five years after their discovery and after many years of failure to bring them to the bedside for therapeutic uses, monoclonal antibodies are now in a renaissance phase, both clinically and commercially. Monoclonal antibodies are theoretically ideal for the therapeutic area with all the required properties such as an extreme specificity and binding affinity that could be adjusted as needed, low cost commercial production, and a potential to be tailored to specific needs such as they could be made to fix, complement, be monomers, dimers, to be toxic or nontoxic; they could also be made to fix the same antigen on both arms of the antibody or different ones as needed. They have limitless applications in the therapeutic area. When Ehrlich proposed the concept of magie bullets for the treatment of cancer, he probably had in mind drug targeting with polyclonal antibodies, but with the development of other fields in cancer therapy and in biotechnology, the concept has now been applied to radioimmunotherapy, radioimmunodetection, therapy with cytotoxic antibodies, immunotoxins, enzyme-prodrug immunotherapy, immunotherapeutics with fusion proteins, and a whole range of applications that are discussed in Tumor Targeting in Cancer Therapy. Presently, more than 15 % of all drugs in development are deri ved from the monoclonal antibody technology. The drug industry has entered a new era, and products derived from biotechnology, and more specifically antibodies, are now applied to heart disease, can cer, and infectious diseases. The immunogenicity of monoclonal antibodies for humans, which was for a long time a stumbling block, and the short half-life in circulation are now better understood and controlled by various strategies such as chimerization, phage display technology, and humanization. These technologies have also permitted the affinity of monoclonal antibodies to be increased to the picomolar range. It must be remembered, however, that for cancer therapy the high affinity antibody is not always the best candidate. Many pharmaceutical companies have built on these technologies, and the number of clinical trials with monoclonal antibodies is still increasing. Tumor Targeting in Cancer Therapy is intended for scientists, clinicians, and phar maceutical investigators in cancer immunology and cancer therapeutics. It covers the various aspects of targeted cancer therapy, from fundamentals to biodistribution and clini cal applications. The contributors come from academic institutions, government, the drug industry, and the biotechnology industry. Each chapter covers a specific aspect of targeting without too many technical details. Tumor Targeting in Cancer Therapy is not an accumulation of scientific papers on the subject, but instead offers state-of-the-art reviews on each topic. For graduate students and for new scientists in the field, the first chapter gives a complete review on the subject. It also gives the necessary information to be able to evaluate technologies available to start new projects, and for teaching cancer therapeutics and immunology. v vi Preface It was a pleasure to edit this book and I thank all the authors for their collaboration. I also leamed as an editor new reasons for not respecting the deadline. Many that I had never used before. I thank you for writing these exceptional scientific papers and I wish all authors and readers good luck in their research. Michel Page, PhD CONTENTS Preface ............................................................................................................................ v Contributors ................................................................................................................... ix I. PART A REvIEw 1 The Current Status of Tumor Targeting: A Review .......................... 3 Tarunendu Ghose 2 Clinical Applications of Targeted Therapeutics ............................ 79 Tarunendu Ghose 11. PART T ARGETING TUMORS WITH DRUG ANTIBODY CONJUGATES 3 Targeting the CD22 Receptor with RNA Damaging Agents ...... 109 Huaitian Liu, Dianne L. Newton, Hans 1. Hansen, Stanislaw M. Mikulski, David M. Goldenberg, Edward A. Sausville, and Susanna M. Rybak 4 The Development of Liposomes for Enhanced Delivery of Chemotherapeutics to Tumors ............................................. 119 Paul Tardi, Ludger fckenstein, Marcel Bally, and Lawrence Mayer 5 Overcoming Multiple Drug Resistance with Anti-Pgp Carrier ............................................................... 137 Brigitte Page and Michel Page 6 Targeting with Transferrin ............................................................ 151 Mandip Singh 7 Synthesis and Evaluation of Paclitaxel Immunoconjugate with Antitumor Activity In Vitro ............................................. 165 lairo laime Correa and Michel Page 8 The Use of Drug-Monoclonal Antibody Conjugates for the Treatment of Cancer ................................................................. 179 Geoffrey A. Pietersz and fan F. C. McKenzie 111. PART T ARGETING TUMORS WITH ANTIBODIES 9 Targeting Vascular Endothelium with Antibodies ....................... 199 Przemek Twardowski and Kim Margolin 10 Targeting B-Cell Non-Hodgkin's Lymphoma with Monoclonal Antibodies .................................................... 211 Christian Buske and W. Hiddemann 11 From Bench to Bedside: Development oJ Rituximab (Rituxan ®), A Monoclonal Antibody Jor the Therapy oJ Non-Hodgkin 's Lymphoma .................................................. 225 Roland Newman 12 Mylotarg: The First Antibody-Targeted Chemotherapy Agent ... 239 Philip R. Hamann and Mark S. Berger vii viii Contents P"ART IV. T ARGETING TUMORS WITH RADIOIMMUNOCONJUGATES 13 188Rhenium_ Labeled Trisuccin-LlCH2HuCC49 as a Radioimmunotherapy Model in Nude Mice ..................... 257 Ahmad Safavy and Donald 1. Buchsbaum PART V. T ARGETING TUMORS WITH IMMUNOTOXINS 14 General Approach for Targeting Toxins ...................................... 279 Manish Monga, Richard A. Messmann, and Edward A. Sausville 15 Antibody-Toxin Conjugates: Chemistry of Coupling and Purification ........................................................................ 289 Silvana Canevari, Maria Ines Colnaghi, Luigi Cattel, and Franco Dosio 16 Shiga-Like Toxins as Targeted Anticancer Agents ..................... 307 Paul LaPointe and lean Gariepy PART VI. T ARGETING TUMORS WITH ANTIBODY -ENZYME CONJUGATES (ADEPT) 17 Antibody-Directed Enzyme Prodrug Therapy with Carboxypeptidase G2: Clinical Studies ........................... 321 Kenneth D. Bagshawe PART VII. PHOTODYNAMIC THERAPY 18 Photodynamic Therapy: Targeting Cancer Cells with Photosensitizer-Bioconjugates ......................................... 329 Cynthia M. Allen, Wesley M. Sharman, and lohan E. van Lier 19 Tumor Targeting Using PEG-m-THPC for Photodynamic Therapy in a Rat Ovarian-Cancer Model ................................. 363 Rene Hornung PART VIII. T ARGETING TUMORS WITH MAGNETIC DRUGS 20 Targeting Tumors with Magnetic Drugs ..................................... 379 Andreas S. Lübbe, Christian Bergemann, and Christoph Alexiou PART IX. PRINCIPLES AND TECHNIQUES IN T ARGETING 21 Internalization of Antibodies ........................................................ 391 lairo laime Correa 22 Bioconjugation and Biodistribution ............................................ .411 Francesco M. Veronese and Paulo Caliceti 23 Principles of Antitumor Targeting of Cytotoxic Drugs ............... 431 Gene M. Dubowchik 24 Targeting by Antibody or Ligand: Wh ich Is Better? ................... 449 Douglas A. Lappi Index ........................................................................................................................... 459 CONTRIBUTORS CHRISTOPH ALEXIOU • Klinikum Rechts der Isar, Munich, Germany CYNTHIA M. ALLEN • Institute of Biological Sciences, National Research Council, Ottawa, Ontario, Canada KENNETH D. BAGSHAWE· Emeritus Professor of Medical Oncology, Imperial College School of Medicine, Charing Cross Campus, London, UK MARCEL BALLY • Department of Advanced Therapeutics, BC Agency, Celator Technologies Inc., Vancouver, British Columbia, Canada CHRISTIAN BERGEMANN • Chemicell Inc., Berlin, Germany MARK S. BERGER· Clinical Research and Development, Wyeth-Ayerst Research, Collegeville, PA DONALD J. BUCHSBAUM • Department of Radiation Oncology, Division of Radiation Biology, University of Alabama at Birmingham, Birmingham, AL CHRISTIAN BUSKE • Department of Medicine III, Ludwig-Maximilians University, Munich, Germany PAULO CALICETI • Department of Pharmaceutical Sciences, University of Padua, Padova, Italy SILVANA CANEVARI· Department of Experimental Oncology, Istituto Nazionale Tumori, Milan, Italy LUIGI CATTEL· Department of Drug Science and Technology, Turin, Italy MARIA INEs COLNAGHI • Department of Experimental Oncology, Istituto Nazionale Tumori, Milan, Italy JAIRO JAIME CORREA· Department of Medical Biology, Faculty of Medicine, Universite Laval, Ste Foy, Quebec, Canada FRANCO DOSIO· DISCAFF, Novara, Italy GENE M. DUBOWCHIK • Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT JEAN GARIEPY • Department of Medical Biophysics, University ofToronto and The Ontario Cancer Institute, Princess Margaret Hospital, University Health Network, Toronto, Canada T ARUNENDU GHOSE • Professor Emeritus in Pathology, Dalhousie University, Halifax, Nova Scotia, Canada DAVID M. GOLDENBERG • Garden State Cancer Center, Belleville, NI PHrLlP R. lIAMANN • Oncology/Chemical Sciences, Wyeth-Ayerst Research, Pearl River, NY HANs J. HANSEN • Immunomedics Inc., Morris Plains, NI W. HIDDEMANN • Department of Medicine III, Ludwig-Maximilians University, Munich, Germany RENE HORNUNG • Beckman Laser Institute and Medical Clinic, University of Califomia, Irvine, CA; Department of Obstetrics and Gynecology, University Hospital Zurich, Zurich, Switzerland LUD GER IcKENSTEIN • Department of Advanced Therapeutics, BC Agency, Celator Technologies Inc., Vancouver, British Columbia, Canada PAUL LAPOINTE • Department of Medical Biophysics, University ofToronto and The Ontario Cancer Institute, Princess Margaret Hospital, University Health Network, Toronto, Canada ix x Contributors DOUGLAS A. LAPPI • Advanced Targeting Systems, San Diego, CA HUAITIAN LIU • Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, NCI-FCRDC, National Institutes of Health, Frederick, MD ANDREAS S. LÜBBE· Cecilien-Klinik, Bad Lippspring, Germany KIM MARGOLIN· Department of Medical Oncology and Therapeutics Research, City of Hope National Medical Center, Duarte, Canada LAWRENCE MAYER· Department of Advanced Therapeutics, BC Agency, Celator Technologies Inc., Vancouver, British Columbia, Canada IAN F. C. McKENZIE • The Austin Research Institute, Heidelberg, Victoria, Australia RICHARD A. MESSMANN • Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Bethesda, MD STANISLAW M. MIKULSKI· Alfacell Corp., Bloomfield, Ni MANISH MON GA • National Cancer Institute-Medicine Branch, Bethesda, MD ROLAND NEWMAN • IDEC Pharmaceuticals, San Diego, CA DIANNE L. NEwToN • SAIC Frederick, National Cancer Institute-Frederick Cancer Research and Development Center, Frederick, MD BRIGITTE PAGE· Biotechlab, Quebec, Canada MICHEL PAGE • Department of Medical Biology, Faculty of Medicine, Universite Laval, Sainte-Foy, Quebec, Canada GEOFFREY A. PIETERSZ • The Austin Research Institute, Heidelberg, Victoria, Australia SUSANNA M. RYBAK • Developmental Therapeutics Program, Division of Cancer Treatment, and Diagnosis, National Cancer Institute-Frederick Cancer Research and Development Center, National Institutes of Health, Frederick, MD AHMAD SAFAVY· Division of Radiation Biology, Department of Radiation Oncology, University of Alabama at Birmingham, Birmingham, AL EDWARD A. SAUSVILLE • Developmental Therapeutics Program, Division of Cancer Treatment, and Diagnosis, National Cancer Institute-Frederick Cancer Research and Development Center, National Institutes of Health, Frederick, MD WESLEY M. SHARMAN • Department of Nuclear Medicine and Radiobiology, Faculty of Medicine, Universite de Sherbrooke, Sherbrooke, Quebec, Canada MANDIP SINGH • College of Pharmacy, Florida A & M University, Tallahasee, FL PAUL TARDI· Celator Technologies Inc., Vancouver, British Columbia, Canada PRZEMEK TWARDOWSKI· Department of Medical Oncology and Therapeutics Research, City of Hope National Medical Center, Duarte, Canada JOHAN E. VAN LIER • Department of Nuclear Medicine and Radiobiology, Faculty of Medicine, Universite de Sherbrooke, Sherbrooke, Quebec, Canada FRANCESCO M. VERONESE • Department of Pharmaceutical Sciences, University of Padua, Padova, Italy

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