Evaluation of the Antitumor Mechanism of Armed Antibodies: 2nd Edition

Dear Colleagues,

More than 120 years ago, Paul Ehrlich had a dream of the “magic bullet” that would seek out and specifically attack the pathogens. “Magic bullets” can identify their target molecules without harming the other normal tissues. This concept was also applied to cancer treatment, and the discovery of monoclonal antibody (mAb) producing hybridoma technology was developed. After this success to obtain target specific mAbs easily, the “missile therapy” or the “immunoconjugate” was developed for clinical use in the late 1980’s. In the 1990’s, antibody engineering technologies that allowed genetic modification of murine antibodies to produce chimeric mouse-human antibodies or humanized antibodies were developed and these mAbs are less likely to be recognized by the host immune system as a foreign antigen, and have half-lives similar to those of natural human IgG. From the late 2000’s, these mAbs were again applied to the immunoconjugate, named the “antibody drug conjugate; ADC”. ADCs are categorized as the armed antibodies which means the antibodies have the “weapons”, and the antibodies are used for delivery carriers of the weapons, such as anticancer drugs and radioisotopes. As of November 2022, 12 ADCs and one radioimmunotherapy (RIT) drug are approved by FDA: gemtuzumab ozogamicin (CD33, calicheamicin; Mylotarg), brentuximab vedotin (CD30, MMAE; Adcetris), trastuzumab emtansine (HER2, DM1; Kadcyla), inotuzumab ozogamicin (CD22, calicheamicin; Besponsa), polatuzumab vedotin (CD79b, MMAE; Polivy), enfortumab vedotin (nectin-4, MMAE; Padcev), trastuzumab deruxtecan (HER2, exatecan derivative; Enhertu), sacituzumab govitecan (TROP-2, SN38; Trodelvy), belantamab mafodotin (CD269, MMAF; Blenrep), loncastuximab tesirine (CD19, PBD dimer; Zynlonta), tisotumab vedotin (TF, MMAE; Tivdak), mirvetuximab soravtansine (FRα, DM4; Elahere) and Ibritumomab tiuxetan (CD20, Yttrium-90; Zevalin). Photoimmunotherapy (PIT) or antibody conjugated nanoparticles (micelles and liposomes) are listed as the armed antibodies which can deliver a photoactivating chemical or anticancer drug incorporated nanoparticles to the cancer cells, respectively. Bispecific antibodies, especially T cell-engaging (bispecific) antibodies, are also categorised into armed antibodies which can infiltrate the T cells to the cancer tissue and connect T cells to cancer cells. Thus, armed antibodies are one of the most exciting area for cancer therapeutics. In this Special Issue of Pharmaceuticals, original research, mini-review, and review articles regarding armed antibodies are invited. This Special Issue focuses on the therapeutic antibodies in vitro, in vivo, and clinical studies.

Dr. Yoshikatsu Koga
Dr. Hiroki Takashima
Dr. Ryo Tsumura
Guest Editors

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• antibody drug conjugate (ADC)
• photoimmunotherapy (PIT)
• radioimmunotherapy (RIT)
• antibody
• conjugated nanoparticle
• bispecific antibody
• CAR-T cell therapy