epratuzumab

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epratuzumab

GtoPdb Ligand ID: 8088

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]

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]