Ublituximab (Briumvi)
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
- 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
- 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
Also known as
LFB-R603, TG-20, TGTX-1101