Synonyms: 90Y-DOTA-hLL2 | 90Y-epratuzumab tetraxetan | 90Y-hLL2 | AMG-412 | IMMU-hLL2 | LymphoCide® (proposed proprietary name)
Compound class:
Antibody
Comment: Epratuzumab is a humanized monoclonal antibody. It is derived from the murine IG2a monoclonal antibody, LL2 (EPB-2). Epratuzumab has antineoplastic and antiinflammatory actions [1].
The antibody can be conjugated with tetraxetan (DOTA) which allows chelation of radionucleotides such as yttrium-90 [5]. |
References |
1. Al Rayes H, Touma Z. (2014)
Profile of epratuzumab and its potential in the treatment of systemic lupus erythematosus. Drug Des Devel Ther, 8: 2303-10. [PMID:25429203] |
2. Carnahan J, Stein R, Qu Z, Hess K, Cesano A, Hansen HJ, Goldenberg DM. (2007)
Epratuzumab, a CD22-targeting recombinant humanized antibody with a different mode of action from rituximab. Mol Immunol, 44 (6): 1331-41. [PMID:16814387] |
3. Clowse ME, Wallace DJ, Furie RA, Petri MA, Pike MC, Leszczyński P, Neuwelt CM, Hobbs K, Keiserman M, Duca L et al.. (2017)
Efficacy and Safety of Epratuzumab in Moderately to Severely Active Systemic Lupus Erythematosus: Results From Two Phase III Randomized, Double-Blind, Placebo-Controlled Trials. Arthritis Rheumatol, 69 (2): 362-375. [PMID:27598855] |
4. Leonard JP, Goldenberg DM. (2007)
Preclinical and clinical evaluation of epratuzumab (anti-CD22 IgG) in B-cell malignancies. Oncogene, 26 (25): 3704-13. [PMID:17530024] |
5. Lindén O, Hindorf C, Cavallin-Ståhl E, Wegener WA, Goldenberg DM, Horne H, Ohlsson T, Stenberg L, Strand SE, Tennvall J. (2005)
Dose-fractionated radioimmunotherapy in non-Hodgkin's lymphoma using DOTA-conjugated, 90Y-radiolabeled, humanized anti-CD22 monoclonal antibody, epratuzumab. Clin Cancer Res, 11 (14): 5215-22. [PMID:16033839] |
6. Onuora S. (2016)
Systemic lupus erythematosus: Epratuzumab not effective in phase III trials. Nat Rev Rheumatol, 12 (11): 622. [PMID:27652506] |
7. Ramos-Casals M, Sanz I, Bosch X, Stone JH, Khamashta MA. (2012)
B-cell-depleting therapy in systemic lupus erythematosus. Am J Med, 125 (4): 327-36. [PMID:22444096] |
8. Rao V, Gordon C. (2014)
Evaluation of epratuzumab as a biologic therapy in systemic lupus erythematosus. Immunotherapy, 6 (11): 1165-75. [PMID:25496332] |
9. Sieger N, Fleischer SJ, Mei HE, Reiter K, Shock A, Burmester GR, Daridon C, Dörner T. (2013)
CD22 ligation inhibits downstream B cell receptor signaling and Ca(2+) flux upon activation. Arthritis Rheum, 65 (3): 770-9. [PMID:23233360] |