Blisibimod

Source: Wikipedia, the free encyclopedia.
Blisibimod
Clinical data
Other namesA-623
ATC code
  • none
Legal status
Legal status
  • Investigational
Identifiers
CAS Number
ChemSpider
  • none
UNII
KEGG
Chemical and physical data
FormulaC2836H4376N756O858S26
Molar mass63624.20 g·mol−1
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Blisibimod (also known as A-623, formerly AMG 623) is a selective antagonist of

systemic lupus erythematosus.[1] It is currently under active investigation in clinical trials.[2]

Mechanism of action

Blisibimod is a

binding domains fused to the N-terminus of the fragment crystallizable region (Fc) of a human antibody.[1]

BAFF is involved in

autoimmune diseases, including systemic lupus erythematosus,[4][5][6] lupus nephritis,[7] rheumatoid arthritis,[5][6] multiple sclerosis,[8] Sjögren syndrome,[9] Graves' disease,[10] and Hashimoto's thyroiditis.[10] Blisibimod binds to BAFF and inhibits interaction with BAFF receptors, thus decreasing B-cell survival and proliferation throughout the body.[1][3] Improvements in disease activity have been observed in patients with systemic lupus erythematosus[11] and rheumatoid arthritis[12]
following treatment with BAFF inhibitors in clinical trials.

Development

Blisibimod was initially developed by Amgen, with Phase I trials demonstrating comparable safety between the blisibimod and placebo treatments.[1] It was subsequently acquired by Anthera Pharmaceuticals,[13] who in 2010 initiated a global Phase II study called PEARL-SC to investigate the efficacy, safety, and tolerability of blisibimod in subjects with systemic lupus erythematosus.[2][14] The PEARL-SC study, completed in April 2012, yielded data that has been published.[15] Blisibimod is currently being tested in a Phase 3 study, CHABLIS-SC1, for systemic lupus erythematosus, and a Phase 2 study, BRIGHT-SC, for IgA nephropathy.

References

  1. ^ a b c d "A-623: BAFF Peptibody for the Treatment of Lupus". Anthera Pharmaceuticals, Inc. Archived from the original on 2011-09-02. Retrieved 2011-07-08.
  2. ^ a b "Anthera Initiates Expanded and Extended PEARL-SC Phase 2b Clinical Study in Lupus With A-623 - A Subcutaneous Dual Inhibitor of Membrane and Soluble B-Cell Activating Factor (BAFF or BLyS)" (Press release). Anthera Pharmaceuticals, Inc. 29 July 2010. Archived from the original on 3 June 2011. Retrieved 15 July 2011.
  3. ^
    S2CID 9159761
    .
  4. PMID 18668552
    .
  5. ^
    PMID 11407690
    .
  6. ^
    PMID 11123269
    .
  7. S2CID 11795623
    .
  8. PMID 15642740
    .
  9. PMID 19088870
    .
  10. ^
    PMID 19647102
    .
  11. S2CID 28952240
    .
  12. ^ Genovese M, Bojin S, Biagini M, Mociran E, Cristei D, Georgescu L, Sloan-Lancaster J (June 2010). "Effects on B cells, safety, and efficacy of LY2127399, a novel anti-BAFF MAB, in patients with active rheumatoid arthritis". Annals of the Rheumatic Diseases. 69 (Suppl3): 69. Archived from the original on 2011-10-02. Retrieved 2011-07-15.
  13. ^ "Anthera Pharmaceuticals acquires the worldwide rights to a BAFF inhibitor for the treatment of lupus and other autoimmune diseases" (Press release). Anthera Pharmaceuticals, Inc. 2008-01-08. Archived from the original on 2012-03-27. Retrieved 2011-07-15.
  14. ^ Clinical trial number NCT01162681 for "PEARL-SC Trial: A Study of the Efficacy, Safety, and Tolerability of A 623 Administration in Subjects With Systemic Lupus Erythematosus" at ClinicalTrials.gov
  15. S2CID 23122293
    .
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