Antibody-drug conjugates-A new wave of cancer drugs

被引：154

作者：

Bouchard, Herve ^{[1
,2
]}

Viskov, Christian ^{[1
,2
]}

Garcia-Echeverria, Carlos ^{[2
]}

机构：

[1] Sanofi, Nat Prod & Prot Chem, F-94403 Vitry Sur Seine, France

[2] Sanofi, Lead Generat Compound Realizat, F-94403 Vitry Sur Seine, France

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 23期

关键词：

Oncology; Natural products; Bioorganic; Conjugate; Linkers; TRASTUZUMAB EMTANSINE; ANTITUMOR ANTIBIOTICS; BRENTUXIMAB VEDOTIN; BREAST-CANCER; CALICHEMICINS; OZOGAMICIN; CHEMISTRY; FAMILY;

D O I：

10.1016/j.bmcl.2014.10.021

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Antibody-drug conjugates (ADCs) consist of cytotoxic drugs covalently linked to monoclonal antibodies directed to antigens differentially overexpressed in tumor cells. These loaded antibodies are expected to selectively deliver lethal cargoes to tumor cells and provide sustained clinical benefit to pre-selected cancer patients while, at the same time, minimizing systemic toxicity. Although on-target adverse events are not completely avoided and the true efficacy of these innovative agents still requires further clarification, proof-of-concept has already been achieved in clinical settings with immunoconjugates containing calicheamicin, auristatin or maytansine-based cytotoxic payloads. In this present article we review the characteristics of the preceding cytotoxic platforms and their chemical conjugation approaches. (C) 2014 Published by Elsevier Ltd. This is an open access article under the CC BY-NC-ND license

引用

页码：5357 / 5363

页数：7

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