ocrelizumab   Click here for help

GtoPdb Ligand ID: 7580

Synonyms: 2H7 | Ocrevus® | PRO70769 | RG1594
Approved drug Immunopharmacology Ligand
ocrelizumab is an approved drug (FDA (2017), EMA (2018))
Compound class: Antibody
Comment: Ocrelizumab is a humanized IgG1 anti-CD20 monoclonal antibody, approved for relapsing multiple sclerosis (RMS) and primary progressive multiple sclerosis (PPMS). This is the first therapeutic to gain approval for both of these forms of MS. Ocrelizumab is a modified version of rituximab, developed as a substitute in response to expiration of rituximab patent protection.
The submission documentation for the antibody's INN application contains the peptide sequences for the heavy and light chains of the antibody. BLAST searches of patented peptide sequences reveals identical matches with peptides claimed in patent WO2004056312, which resolve to clones 2H7.v16 and 2H7.v31 [1].
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Bioactivity Comments
Ocrelizumab depletes CD20+ B cells in the blood and lymphoid tissues of cynomolgus monkeys (Macaca fascicularis) [7]. B cell numbers recover to normal levels after one or two treatments [7]. Affinity data for clone 2H7.v16 is presented below. Clone 2H7.v31 exhibited 20-fold higher antibody-dependent cell-mediated cytotoxicity (ADCC) than the approved anti-CD20 monoclonal rituximab.
Selectivity at other protein targets
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
CD20 (membrane-spanning 4-domains, subfamily A, member 1) Primary target of this compound Hs Antibody Binding 9.1 pKd - 1
pKd 9.1 (Kd 8.4x10-10 M) [1]