Evaluates the carcinogenic risks to humans posed by the use of four antiretroviral agents four DNA topoisomerase II inhibitors used in the treatment of cancer and an additional three pharmaceutical agents (hydroxyures phenolphthalein and vitamin K substances). The volume marks the first IARC evaluation of nucleoside analogs that act as antiviral agents. The evaluation responds in part to recent findings that zidovudine (AZT) an effective antiretroviral agent now being given to pregnant HIV-infected women to prevent maternal-to-fetal transmission of the virus is a transplacental carcinogen in mice. The opening monograph evaluates the carcinogenicity to humans of the antiretroviral nucleoside analogs zidovudine (AZT) zalcitabine (ddC) and didanosine (ddI) and the antiherpesvirus drug aciclovir. Of these aciclovir and didanosine could not be classified on the basis of available data. For zidovudine transplacental administration to mice resulted in an increased incidence and multiplicity of lung and liver tumours and in an increased incidence of female reproductive tract tumours in one study but not in another involving treatment at a lower dose. Despite observation of toxic effects in some studies of humans human carcinogenicity data were judged to provide inadequate evidence of carcinogenicity in humans. Zidovudine was classified as possibly carcinogenic to humans. Similar weaknesses in human carcinogenicity data for zalcitabine which consistently induces thymic lymphomas in mice resulted in its classification as possibly carcinogenic to humans. The second monograph evaluates four DNA topoisomerase II inhibitors: etoposide teniposide mitoxantrone and amsacrine. Of these etoposide - one of the most widely used and effective cytotoxic drugs in combination therapy - was classified as probably carcinogenic to humans and etoposide in combination with cisplatin and bleomycin was judged to be carcinogenic to humans. Teniposide was classified as probably carcinogenic to humans and mitoxantrone and amsacrine were classified as possibly carcinogenic to humans. Of the three pharmaceutical agents evaluated in the final monograph hydroxyurea which is widely used in cancer treatment and increasingly in combination with didanosine in HIV infection could not be classified. Phenolphthalein a widely used laxative now being withdrawn from the market in many countries because of toxicological concerns was classified as possibly carcinogenic. Vitamin K substances could not be classified on the basis of available evidence.

Get the latest information on antineoplastic use and patient care when you purchase your copy of the essential chemotherapy resource for cancer-care professionals. Newly updated, revised, and expanded, the third edition of the Clinical Guide to Antineoplastic Therapy: A Chemotherapy Handbook serves as an up-to-date reference for clinicians at every level from students and novices to the most seasoned nurses and other healthcare professionals involved in the care of patients receiving chemotherapy. Edited by Mary Magee Gullatte, this comprehensive guide features chapters on the fundamentals of antineoplastic therapy, commonly used regimens for specific cancers, clinical trials, reimbursement for chemotherapy, botanicals and other complementary and alternative therapies, vascular access devices, and symptom management, as well as an easy-to-use A Z guide of more than 150 chemotherapy, biotherapy, and hormonal therapy agents. New to this edition are chapters on patient navigati

Medicinal Chemistry of Anticancer Drugs, Second Edition, provides an updated treatment from the point of view of medicinal chemistry and drug design, focusing on the mechanism of action of antitumor drugs from the molecular level, and on the relationship between chemical structure and chemical and biochemical reactivity of antitumor agents. Antitumor chemotherapy is a very active field of research, and a huge amount of information on the topic is generated every year. Cytotoxic chemotherapy is gradually being supplemented by a new generation of drugs that recognize specific targets on the surface or inside cancer cells, and resistance to antitumor drugs continues to be investigated. While these therapies are in their infancy, they hold promise of more effective therapies with fewer side effects. Although many books are available that deal with clinical aspects of cancer chemotherapy, this book provides a sorely needed update from the point of view of medicinal chemistry and drug design. - Presents information in a clear and concise way using a large number of figures - Historical background provides insights on how the process of drug discovery in the anticancer field has evolved - Extensive references to primary literature

The past decades have seen major developments in the understanding of the cellular and molecular biology of cancer. Significant progress has been achieved regarding long-term survival for the patients of many cancers with the use of tamoxifen for treatment of breast cancer, treatment of chronic myeloid leukaemia with imatinib, and the success of biological drugs. The transition from cytotoxic chemotherapy to targeted cancer drug discovery and development has resulted in an increasing selection of tools available to oncologists. In this Special Issue of Pharmaceuticals, we highlight the opportunities and challenges in the discovery and design of innovative cancer therapies, novel small-molecule cancer drugs and antibody–drug conjugates, with articles covering a variety of anticancer therapies and potential relevant disease states and applications. Significant efforts are being made to develop and improve cancer treatments and to translate basic research findings into clinical use, resulting in improvements in survival rates and quality of life for cancer patients. We demonstrate the possibilities and scope for future research in these areas and also highlight the challenges faced by scientists in the area of anticancer drug development leading to improved targeted treatments and better survival rates for cancer patients.

Written by the foremost authority in the field, this volume is a comprehensive review of the multifaceted phenomenon of hepatotoxicity. Dr. Zimmerman examines the interface between chemicals and the liver; the latest research in experimental hepatotoxicology; the hepatotoxic risks of household, industrial, and environmental chemicals; and the adverse effects of drugs on the liver. This thoroughly revised, updated Second Edition features a greatly expanded section on the wide variety of drugs that can cause liver injury. For quick reference, an appendix lists these medications and their associated hepatic injuries. Also included are in-depth discussions of drug metabolism and factors affecting susceptibility to liver injury.

The past decade has seen a significant increase of research aimed at discovering new drugs for treating cancer, and the increasing number of new antineoplastic drugs approved by regulatory agencies reflects this. Until now, details on the synthesis of these newer agents have been scattered in various journals and in US and European patents. This timely volume deals with the organic chemistry involved in the synthesis of the agents found within antineoplastic drugs, including descriptions of the synthetic schemes for the preparation of over 200 compounds that have been granted non-proprietary names. Compounds are collected in chapters based on the mechanism of action rather than on their chemical structures. Each individual chapter is preceded by a brief description of that mechanism and includes detailed flow charts of the preparation of those compounds accompanied by discussions of the organic chemistry involved in each step. The first half of this volume is dedicated to the syntheses of established chemotherapy drugs. Kinase inhibitors occupy the following chapters with the largest single chapter dealing with the fifty compounds that inhibit tyrosine kinase. This class stands out since over twenty compounds in this group have been approved for treating patients; a rare track record compared to any other class of therapeutic agents. Antineoplastic Drugs: Organic Syntheses is written to appeal to organic and medicinal chemists in industry and academia. It is beneficial to those composing grant proposals for NCI and related organizations. The book is accessible to advanced undergraduates as well as graduates and researchers as well as those with a thorough grasp of organic chemistry.