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Ublituximab (TG-1101)

Contents

Mechanism of action

From the NCI Drug Dictionary: A chimeric recombinant IgG1 monoclonal antibody directed against human CD20 with potential antineoplastic activity. Ublituximab specifically binds to the B cell-specific cell surface antigen CD20, thereby potentially inducing a B cell-directed complement dependent cytotoxicity (CDC) and antibody-dependent cell-mediated cytotoxicity (ADCC) against CD20-expressing B cells, leading to B cell apoptosis. CD20 is a non-glycosylated cell surface phosphoprotein that is exclusively expressed on B cells during most stages of B cell development and is often overexpressed in B-cell malignancies. Ublituximab has a specific glycosylation profile, with a low fucose content, that may enhance its ADCC response against malignant B cells.

Preliminary data

CLL

  1. Sharman JP, Farber CM, Mahadevan D, Schreeder MT, Brooks HD, Kolibaba KS, Fanning S, Klein L, Greenwald DR, Sportelli P, Miskin HP, Weiss MS, Burke JM. Ublituximab (TG-1101), a novel glycoengineered anti-CD20 antibody, in combination with ibrutinib is safe and highly active in patients with relapsed and/or refractory chronic lymphocytic leukaemia: results of a phase 2 trial. Br J Haematol. 2017 Feb;176(3):412-420. Epub 2016 Dec 16.link to original article PubMed
  2. Sawas A, Farber CM, Schreeder MT, Khalil MY, Mahadevan D, Deng C, Amengual JE, Nikolinakos PG, Kolesar JM, Kuhn JG, Sportelli P, Miskin HP, O'Connor OA. A phase 1/2 trial of ublituximab, a novel anti-CD20 monoclonal antibody, in patients with B-cell non-Hodgkin lymphoma or chronic lymphocytic leukaemia previously exposed to rituximab. Br J Haematol. 2017 Apr;177(2):243-253. Epub 2017 Feb 21. link to original article PubMed
  3. Abstract: Jeff Porter Sharman, Danielle M. Brander, Anthony R. Mato, Suman Kambhampati, John M. Burke, Frederick Lansigan, Marshall T. Schreeder, Scott D. Lunin, Nilanjan Ghosh, Alexander Zweibach, Mikhail Shtivelband, Patrick M. Travis, Jason Claud Chandler, Kathryn S. Kolibaba, Peter Sportelli, Hari P. Miskin, Michael S. Weiss, and Ian Flinn. Ublituximab and ibrutinib for previously treated genetically high-risk chronic lymphocytic leukemia: Results of the GENUINE phase 3 study. Journal of Clinical Oncology 2017 35:15_suppl, 7504-7504 link to abstract

Also known as

  • Code names: LFB-R603, TG-20, TGTX-1101