BasilioColligris, Jesús Pintor
160
BELIMUMAB
Belimumab
is a human monoclonal antibody inhibiting B-‐cell activating
factor (BAFF) and is developed by the University of Udine as a treatment for
Sjögren’s syndrome. Sjögren's syndrome is a systemic autoimmune disease
characterizedbyan increase inBAFF (BLyS) levels resulting inBcell hyperactivity.
B cells are involved in the pathogenesis of SS in both systemic and glandular
features, and B cell down regulation may lead to a decrease of disease activity.
Moreover, pathogenesis of SS is closed to that of systemic lupus erythematosus,
where
belimumab
has been proven to be effective. Currently the compound is
under Phase II clinical trials evaluation (ClinicalTrials.gov Identifier:
NCT01160666) andthe initial resultsarepromising (56).
RITUXIMAB
Rituximab
(CD20) is developedby IDECPharmaceuticals as a treatment for
Sjögren’s syndrome. CD20antigen is targeting cells of theB-‐cell lineage, leading to
transient bloodB-‐cell depletion, leaving aside stemcells (57).
Rituximab
is already
approved by the U.S. Food and Drug Administration in 1997 as a treatment of B-‐
cell non-‐Hodgkin lymphomas resistant to other chemotherapy regimens. The
compound currently is tested in Phase III clinical trials (ClinicalTrials.gov
Identifier:NCT00740948) tostudy the toleranceandefficacyof rituximab injection
inSjögren’sdisease (58, 59).
LOTEMAX
Bausch & Lomb, Inc. is re-‐purposing the already approved drug
Lotemax
with topical cyclosporine ophthalmic emulsion 0.05% (
Restasis
) as a possible
treatment of dry eye.
Lotemax
(loteprednoletabonate-‐LE) (Figure 7) (60) is an
ester corticosteroidwith a high therapeutic index, containing an ester rather than
a ketone, at carbon-‐20 of the prednisolone core structure. LE is indicated for the
treatment of steroid responsive inflammatory conditions associated to the
palpebral and bulbar conjunctiva, cornea, and anterior segment of the globe. Its
mechanism of action is to block the inflammatory mediators treating the
inflammation associated with the dry eye disease. Cyclosporine A as already
mentioned above is a standardmolecule against inflammationwith efficacy indry
eye disease, enhancing or restoring the lachrymal gland secretion in patients
suffering from this syndrome (61). An advantage of topical loteprednol
