Abstract
Antibody–drug conjugates (ADCs), constructed with monoclonal antibodies (mAbs), linkers, and natural cytotoxins, are innovative drugs developed for oncotherapy. Owing to the distinctive advantages of both chemotherapy drugs and antibody drugs, ADCs have obtained enormous success during the past several years. The development of highly specific antibodies, novel marine toxins’ applications, and innovative linker technologies all accelerate the rapid R&D of ADCs. Meanwhile, some challenges remain to be solved for future ADCs. For instance, varieties of site-specific conjugation have been proposed for solving the inhomogeneity of DARs (Drug Antibody Ratios). In this review, the usages of various natural toxins, especially marine cytotoxins, and the development strategies for ADCs in the past decade are summarized. Representative ADCs with marine cytotoxins in the pipeline are introduced and characterized with their new features, while perspective comments for future ADCs are proposed.
Highlights
While cancer is one of the most serious diseases threatening human life, traditional chemotherapy and common antibody tumor therapy offer low efficacy due to weak target selectivity and tumor-killing efficiency
The named anti-PSMA antibody–drug conjugates (ADCs) whose monoclonal antibodies (mAbs) connect with cytotoxins via a stable thioether linker has already finished phase II clinical trials in patients with metastatic castration-resistant prostate cancer [18,19]
Due to its antineoplastic activity of inherent antibody-dependent cell-mediated cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC), IgG1 is commonly used in ADCs; more improved IgGs have been proposed for new generation of ADCs
Summary
While cancer is one of the most serious diseases threatening human life, traditional chemotherapy and common antibody tumor therapy offer low efficacy due to weak target selectivity and tumor-killing efficiency. As an innovative therapeutic choice, antibody–drug conjugates (ADCs) demonstrate distinctive advantages of both cytotoxin drugs and antibody drugs in cancer treatment. Eighty‐seven years after Dr Ehrlich’s proposal, the first ADC, Mylotarg® Eighty‐seven years after Dr Ehrlich’s proposal, the first ADC, Mylotarg® (Pfizer, gemtuzumab ozogamicin), was approved for the treatment of acute myelocytic leukemia (AML). ® (Pfizer, Eighty-seven years after Dr. Mylotarg gemtuzumab ozogamicin), was approved for Ehrlich’s the treatment of acute (AML). By the US Food and Drug Administration (FDA) in 2000 Though it was withdrawn from the market in 2010 for ozogamicin), approved for the treatment of acuteitmyelocytic leukemia by thein. ~10 new ADCs will come by Research & Markets), ~10 new ADCs will come into the clinical market in the decade, and the of overall.
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