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To minimize its toxicities, we linked ibrutinib to a cell\u2010targeted, internalizing antibody. To this end, we synthesized a poly\u2010anionic derivate, ibrutinib\u2010Cy3.5, that retains full functionality. This anionic inhibitor is complexed by our anti\u2010CD20\u2010protamine targeting conjugate and free protamine, and thereby spontaneously assembles into an electrostatically stabilized vesicular nanocarrier. The complexation led to an accumulation of the drug driven by the CD20 antigen internalization to the intended cells and an amplification of its pharmacological effectivity.\n                    <jats:italic>In\u2005vivo<\/jats:italic>\n                    , we observed a significant enrichment of the drug in xenograft lymphoma tumors in immune\u2010compromised mice and a significantly better response to lower doses compared to the original drug.\n                  <\/jats:p>","DOI":"10.1002\/anie.202109769","type":"journal-article","created":{"date-parts":[[2021,11,2]],"date-time":"2021-11-02T03:21:36Z","timestamp":1635823296000},"update-policy":"https:\/\/doi.org\/10.1002\/crossmark_policy","source":"Crossref","is-referenced-by-count":14,"title":["Tumor\u2010Cell\u2010Specific Targeting of Ibrutinib: Introducing Electrostatic Antibody\u2010Inhibitor Conjugates 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