Med. Chem. Commun., 2014, 5,408-431
DOI: 10.1039/C3MD00360D, Review Article
Christian Hess, Dario Venetz, Dario Neri
There is a trend in oncology towards the development of 'armed' antibody products. In this article,
some of the most advanced preclinical and clinical activities in the field of armed
antibodies are reviewed.
Monoclonal antibodies represent the largest and fastest growing type of biopharmaceuticals.
Their commercial and clinical success has fueled research activities aiming to improve safety
and efficacy. In oncology, there is a trend towards the development of ‘armed’ antibody products,
in which the immunoglobulin moiety serves for the selective in vivo pharmacodelivery
of bioactive payloads such as cytotoxic drugs, bispecific antibodies,
radionuclides or cytokines to sites of disease, thereby sparing healthy tissues.
In this article, we review some of the most advanced preclinical and clinical
activities in the field of armed antibodies and present a personal perspective
on the opportunities and challenges associated with the use of this type of anti-cancer therapeutics.
Synthesis, anti-tubulin and antiproliferative
structure–activity relationship of steroidomimetic dihydroisoquinolinones