B-Cell Modulation in Multiple Sclerosis Riley M. Bove, MD Partners Multiple Sclerosis Center, Brigham and Women’s Hospital, Harvard Medical School, Boston, Massachusetts A REPORT FROM THE 29TH CONGRESS OF THE EUROPEAN COMMITTEE FOR TREATMENT AND RESEARCH IN MULTIPLE SCLEROSIS (ECTRIMS 2013) © 2014 Direct One Communications, Inc. All rights reserved. 1 The Traditional View: Immunopathogenesis of Multiple Sclerosis The initial step in pathogenesis involves the peripheral activation of CD4+ T helper (Th) type 1 cells in response to a stimulating antigen. The assortment of molecules released, including costimulatory signals and cytokines, influences the response profile of the activated immune cells. The stimulating antigen, probably infectious, subsequently cross-reacts with a CNS antigen. Subsequently, activated T cells transmigrate across the blood-brain barrier by adhesion, chemoattraction, and active infiltration into the CNS. Chitnis T, Int Rev Neurobiol 2007;79:43 © 2014 Direct One Communications, Inc. All rights reserved. 2 The Traditional View: Immunopathogenesis of Multiple Sclerosis Transmigration of activated T cells across the bloodbrain barrier leads to reactivation of infiltrating cells within the CNS, which contributes to perivascular inflammation and injury. Release of additional CNS antigens may result in the recruitment of T cells with specificities for additional CNS antigens, called “epitope spreading,” which may further propagate a chronic immune response. Further modifications to this model include the appreciation of other factors, most importantly ThIL-17. Chitnis T, Int Rev Neurobiol 2007;79:43 © 2014 Direct One Communications, Inc. All rights reserved. 3 Back to the Bench: Further Discoveries Macrophage-mediated vesicular demyelination was replicated in New World monkeys, who developed chronic relapsing-remitting MS and occasionally progressive disease, with evidence of remyelination. Autoantibodies that recognize the immunizing antigen are deposited within the vesiculated myelin sheaths in this animal model of MS, and similar antibodies have been found in human MS lesions. This discovery implied that humoral immunity might be a key factor in MS pathogenesis. CD20+ B cells were then identified in MS lesions. Massaccesi L et al, J Clin Invest 1992;90:399; von Büdingen HC et al, Eur J Immunol 2004;34:2072; Genain CP et al, Nat Med 1999;5:170; von Büdingen HC et al, Curr Opin Immunol 2011;23:713 © 2014 Direct One Communications, Inc. All rights reserved. 4 A Possible Role for B Cells in MS Memory B cells, which can cross the blood-brain barrier, can trigger cellular-dependent and complement-dependent cytotoxic effects in the CNS. B cells can influence the priming of effector T cells by functioning as antigen-presenting cells. Abnormalities in B-cell cytokine responses have been reported in MS patients, and production of cytokines and chemokines by B cells may be involved in the formation of ectopic lymphoid-like structures. B cells may be the reservoir for Epstein-Barr virus (EBV); EBV infection is a known risk factor for MS. Hauser SL et al, N Engl J Med 2008;358:676; Kappos L et al, Lancet 2011;378:1779 © 2014 Direct One Communications, Inc. All rights reserved. 5 HERMES Trial: Rituximab in RRMS Phase 2, double-blind, 48-week trial in 104 patients diagnosed with relapsing-remitting MS (RRMS) who were randomized to receive rituximab or placebo Patients receiving rituximab had lower counts of gadolinium-enhancing lesions at 12, 16, 20, 24, and 48 weeks; fewer new gadolinium-enhancing lesions; a smaller T2 lesion volume; and fewer relapses at 24 and 48 weeks, compared with placebo. Patients receiving rituximab initially experienced more adverse events than did those receiving placebo (78% vs 40%, respectively) but not afterward, as treatment continued (20% vs 40%). Hauser SL et al, N Engl J Med 2008;358:676 © 2014 Direct One Communications, Inc. All rights reserved. 6 HERMES Trial: Rituximab in RRMS Number of gadolinium-enhancing lesions in patients receiving rituximab or placebo, from baseline to week 48. (A) Mean total number of gadolinium-enhancing lesions by week. (B) Mean number of new gadolinium-enhancing lesions by week. Missing values were imputed by averaging the available data. Baseline magnetic resonance imaging information was obtained 4 weeks before baseline. Hauser SL et al, N Engl J Med 2008;358:676 © 2014 Direct One Communications, Inc. All rights reserved. 7 HERMES Trial: Rituximab in RRMS The incidence of infection (eg, nasopharyngitis, upper respiratory tract infections, urinary tract infections, and sinusitis) was similar among the rituximab and placebo groups (70% vs 71%). More patients in the placebo group than in the rituximab-treated cohort discontinued therapy before week 48 (40% vs 16%). Rituximab treatment may lead to lysis of memory B cells in the peripheral blood and lymphoid tissues, as well as interfere with antigen presentation by B cells and activation of T cells or macrophages by proinflammatory B-cell cytokines. Hauser SL et al, N Engl J Med 2008;358:676 © 2014 Direct One Communications, Inc. All rights reserved. 8 OLYMPUS Trial: Rituximab in PPMS Double-blind, randomized clinical trial in which a total of 439 patients with primary progressive MS (PPMS) received rituximab or placebo every 24 weeks over a period of 96 weeks (four courses) There was no significant difference between rituximab and placebo in time to clinically definite progression, defined as an increase in EDSS score sustained over 12 weeks. Patients given rituximab had less of a decrease in T2 lesion volume, but total brain volume was similar in both patient groups. Hawker K et al, Ann Neurol. 2009;66:460 © 2014 Direct One Communications, Inc. All rights reserved. 9 OLYMPUS Trial: Rituximab in PPMS Rituximab therapy of PPMS was associated with delayed time to clinically definite progression in: » Patients under 51 years of age » Patients with gadolinium-enhancing lesions on MRI These subpopulation analyses suggest that: » Some PPMS patients have evidence of inflammation early in the disease course, which influences the rate of progression. » Early, aggressive treatment of inflammation in PPMS may be beneficial. » Age-related neurobiologic changes (eg, immunosenescence) occur in MS and have implications for therapeutic decisions. Hawker K et al, Ann Neurol. 2009;66:460 © 2014 Direct One Communications, Inc. All rights reserved. 10 On the Horizon: Ocrelizumab Ocrelizumab, a recombinant humanized monoclonal antibody that selectively targets CD20+ B cells, might offer similar therapeutic benefits to rituximab in patients with MS with less risk of immunogenicity and infusion-site reactions. Ocrelizumab is biosimilar but not bioidentical to rituximab. In vitro, ocrelizumab demonstrates more antibodydependent, cell-mediated cytotoxicity than rituximab and less complement-dependent cytotoxicity. Kappos L et al, Lancet 2011;378:1779; ocrelizumab [data on file], Genentech, 2003 © 2014 Direct One Communications, Inc. All rights reserved. 11 On the Horizon: Ocrelizumab Kappos et al conducted a phase 2, placebo-controlled trial involving 220 patients with RRMS who were randomly assigned to receive 600 or 2,000 mg of ocrelizumab, interferon beta-1a, or placebo. At 24 weeks, when compared with the placebo group, patients given 600 or 2,000 mg of ocrelizumab had 89% or 96% fewer gadolinium-enhancing lesions on MRI; both doses of ocrelizumab were superior to interferon beta-1a in reducing the number of lesions. Two phase 3 pivotal trials in RRMS patients and the first phase 2 pivotal trial in PPMS patients (the ORCHESTRA trial) are ongoing Kappos L et al, Lancet 2011;378:1779 © 2014 Direct One Communications, Inc. All rights reserved. 12 On the Horizon: Ocrelizumab Number of gadolinium-enhancing lesions by week in patients receiving ocrelizumab, interferon beta-1a, or placebo. Vertical bars = 95% confidence interval. Kappos L et al, Lancet 2011;378:1779 © 2014 Direct One Communications, Inc. All rights reserved. 13 Recovery After B-Cell Depletion The prolonged benefits of B-cell depletion after exposure to rituximab suggest that protection may extend beyond the period of B-cell depletion. Immunologic changes in peripheral circulation: » Naïve and immature B cells predominate » Increase in the numbers of interleukin 10-secreting B regulatory cells and CD25+FoxP3+ T regulatory cells » Reduction in Th1 and Th17 proinflammatory responses Immunologic changes in cerebrospinal fluid: » Decrease in the number of T and B cells » Resting CD19+ bright B cells predominate © 2014 Direct One Communications, Inc. All rights reserved. 14 Emerging Studies: MOG Antigen There may be a repertoire of B-cell-dependent antigens that might help to elucidate the underlying triggers in MS. Myelin oligodendrocyte glycoprotein (MOG), for example, may be involved in either completion or maintenance of the myelin sheath; it has emerged as a potential antigen involved in the pathogenesis of MS. Studies in B-cell MHC II-deficient mice suggest that a simple substitution may induce a conformational change resulting in human MOG antigen becoming completely B-cell dependent; this protection could not be restored by injecting MOG antibody. Weber MS et al, Ann Neurol. 2010; 68:369 © 2014 Direct One Communications, Inc. All rights reserved. 15 Emerging Studies: Oligoclonal Bands Studies of IgG sequences reveal that oligoclonal B cells in CSF may be “fingerprints” for MS. Multiple different oligoclonal bands belong to the same clone and may respond to a smaller number of antigenic determinants than the bands would suggest. Members of these oligoclonal bands were identified in the CSF and peripheral blood mononuclear cells. Some B cells found only in the peripheral blood were associated with oligoclonal bands found only in the CSF, suggesting some exchange of B cells across the blood-brain barrier. von Büdingen HC et al, J Clin Invest. 2012;122:4533 © 2014 Direct One Communications, Inc. All rights reserved. 16 Emerging Studies: Oligoclonal Bands Lineage trees of multiple sclerosis IgG-VH sequences suggest ongoing B-cell exchange across the blood-brain barrier. IgG-VH lineages suggestive of ongoing B-cell exchange across the blood-brain barrier for patient MS-1 (A and C), MS-5 (B), and MS-6 (D). These lineages could also reflect affinity maturation occurring in both compartments in parallel. Blue nodes represents cerebrospinal fluid-derived IgG-VH sequences, red nodes represent PB-derived IgG-VH sequences, and green nodes represent identical sequences found in both compartments. von Büdingen HC et al, J Clin Invest. 2012;122:4533 © 2014 Direct One Communications, Inc. All rights reserved. 17 Summary Anti-CD20 trials have revealed that B cells are central players in the pathogenesis of focal lesions in MS. The mechanism of action likely involves blocking the activation of pathogenic T cells by B cells through a function of antigen-presenting cells, but it cannot exclude bystander cytokine effects or autoantibodies. Not all approaches based on B-cell manipulation are likely to be effective in MS; some may potentially worsen the disease. Targeting resident B cells may soon be feasible. A properly designed clinical trial could elucidate the role of B cells in progressive MS. © 2014 Direct One Communications, Inc. All rights reserved. 18