Which oral?

I am often asked which oral would you prescribe? There is no simple answer to this question. The answer will depend on several factors some of which are still to emerge; to mention a few:

1. If and when these agents get licensed and the conditions of licensing; i.e. a first- or second-line indication.
2. The price and more importantly the cost-effectiveness of the agents; NICE will dictate the conditions of use in the UK.
3. Level of disease activity; inactive vs. active vs. highly-active disease.
4. Perceived long-term risk; infections and possible risk of malignancy.
5. Local infrastructure to start the orals.
6. Requirements and intensity of monitoring whilst on medication.
7. Fertility issues.
8. Previous use of other disease-modifying agents.
9. Underlying medical problems.
10. Etc, etc.

It is clear from the above that the decisions about which agent to use will be personalised and will depend largely on patient choice. It is important to ensure that patients have choice and that the choice is an informed one.

Prof G

Oral Fingolimod or Intramuscular Interferon for Relapsing Multiple Sclerosis

In patients with relapsing–remitting multiple sclerosis, oral fingolimod was more effective than intramuscular interferon beta-1a in reducing relapse rates. Adverse events associated with fingolimod included herpes virus infections, atrioventricular block, macular edema, skin cancer, and liver-enzyme elevation.

http://content.nejm.org/cgi/content/full/NEJMoa0907839

A Placebo-Controlled Trial of Oral Cladribine for Relapsing Multiple Sclerosis

Oral cladribine reduced relapse rates and lowered the risk of sustained disability in patients with relapsing–remitting multiple sclerosis. Patients who were treated with cladribine had large reductions in lymphocyte counts and more infections, including one death from reactivation of tuberculosis.

http://content.nejm.org/cgi/content/full/NEJMoa0902533

A Placebo-Controlled Trial of Oral Fingolimod in Relapsing Multiple Sclerosis

In patients with relapsing–remitting multiple sclerosis, oral fingolimod reduced the rates of relapse and disability progression, as compared with placebo. Adverse events included bradycardia, atrioventricular conduction block, macular edema, elevations in liver-enzyme levels, and mild hypertension.

http://content.nejm.org/cgi/content/full/NEJMoa0909494

SAFETY WARNING FOR NATALIZUMAB

EU RECOMMENDS MORE SAFETY WARNINGS FOR ELAN, BIOGEN’S TYSABRI
2010-01-21 18:28:09.776 GMT

21 January 2010; EMA/37607/2010: Press Office

European Medicines Agency recommends additional measures to better manage risk of progressive multifocal leukoencephalopathy (PML) with Tysabri. The risk of PML increases after two years, but benefits of Tysabri continue to outweigh risks for patients with highly active relapsing-remitting multiple sclerosis.

The European Medicines Agency has finalised a review of Tysabri (natalizumab) and the risk of progressive multifocal leukoencephalopathy (PML), a rare brain infection caused by the JC virus. The Agency’s Committee for Medicinal Products for Human Use (CHMP) has concluded that the risk of developing PML increases after two years of use of Tysabri although this risk remains low. However, the benefits of the medicine continue to outweigh its risks for patients with highly active relapsing-remitting multiple sclerosis, for whom there are few treatment options available.

Because it is important that PML is detected early, the Committee recommended that a number of measures be put in place to ensure that patients and doctors are fully aware of the risks of PML. These include:

* an update of the product information to add information about the increase in the risk of PML after two years of treatment and additional advice on how to manage patients who show signs of PML;
* forms to be signed by patients at the beginning of treatment with Tysabri, and again after two years of treatment, after in-depth discussions about the risk of PML with their doctor.

Measures to minimise the risk of PML were part of the initial marketing authorisation for Tysabri, issued in June 2006. Since then, they have been continuously updated and strengthened to increase awareness of the risk of PML.

The new measures are designed to complement the existing recommendations that patients, and their carers, partners and families should be made aware of the symptoms of PML and that patients should be closely monitored throughout treatment.

Notes

1. Tysabri, from Elan Pharma International Ltd, is used to treat relapsing-remitting multiple sclerosis in patients with high disease activity despite treatment with a beta-interferon or whose disease is severe and progressing rapidly.

2. More information about the review of Tysabri is available in a
question-and-answer document. http://www.ema.europa.eu/humandocs/PDFs/EPAR/tysabri/Tysabri_A20-29_Q&A.pdf

3. More information about Tysabri is available in the European Public Assessment Report: http://www.ema.europa.eu/humandocs/Humans/EPAR/tysabri/tysabri.htm

4. This press release, together with other information on the work of the European Medicines Agency, can be found on the Agency’s website: http://www.ema.europa.eu

1st Barts and The London MS Research Day – 30th Jan 2010

We are holding an MS Research Day for people with MS and their families on the 30th January 2010. If you want to attend please RSVP to Maria Espasandin (M.Espasandin@qmul.ac.uk).

You can download an invitation and preliminary programme from the following link:

https://download.yousendit.com/TzY3c0w1Qk5tNEpMWEE9PQ

We look forward to seeing you on the 30th.

Prof G

Liberation therapy – CCSVI

I am a sceptic but remain open to the possibility, albeit remote, that CCSVI may be a real finding. I would definitely not recommend any surgical or radiological intervention at this stage. More research is needed to confirm of refute Zamboni’s findings before any prospective randomised trials are started. You may not be aware but I have been informed that two people with MS have died from the complications of stenting for possible CCSVI.

http://www.ctv.ca/servlet/ArticleNews/story/CTVNews/20091120/W5_liberation_091121/20091121?s_name=W5

http://watch.ctv.ca/news/latest/possible-cure/#clip238089

http://www.ctv.ca/servlet/ArticleNews/story/CTVNews/20091120/W5_liberation_091121/20091121?s_name=W5

http://www.ctv.ca/servlet/ArticleNews/story/CTVNews/20091120/W5_QandA_091121/20091121?hub=WFive

http://jnnp.bmj.com/content/80/4/392.full

http://www.ncbi.nlm.nih.gov/pubmed/19958985?dopt=Abstract

Prof G

2009 European Charcot Foundation Symposium

The 2009 European Charcot Foundation Symposium gathered many world opinion leaders in MS in Lisbon for a 3 day meeting to discuss “A new treatment era in multiple sclerosis: options, challenges and risks”.

Prof Lassmann
. In brain lesions in secondary progressive MS (SPMS), about 65% of cells are clonally expanded MHC class I CD8+ T cells that seem to escape apoptosis and outnumber CD4+T cells 10:1. There was little surprise that ustekinumab (anti-p40 IL-12/IL-23 antibody) trial in MS showed no benefit.Associated with the active demyelination, activated microglia/astroglia and cellular infiltrates are found in most types of lesions, there is evidence for oxidative damage from reactive oxygen species (ROS/RNI) and involvement of the mitochondrial complex IV in acute Balo type lesions (Mahad Brain 2008). The axonal injury is characterized by dissolution of the cytoskeleton, calpainopathy and disturbance of axonal transport. Na+ overload is observed, as in a channelopathy, which is the base for trials that block Na+ as a strategy for neuroprotection: Na+/Ca++ channel blockers, GluR blockers both in low doses (Frischer Brain2009). Overall, despite integrity of BBB, there is active inflammation: compartmentalization of inflammation in SP.
Prof Comi. The use of imaging techniques such as MTR can show sequential changes in new Gad enhancing lesions. This made it possible to see that in the same patients different lesions recover differently. The enhancement with a ring distribution is associated with worse evolution than when there is nodular enhancement and periventricular lesions evolve in a worse way than subcortical lesions (could it be because of the preferential location of stem cells in the periventricular area?)
Unlike Lassmann, he thinks there is imaging evidence for dissociation between inflammation and degeneration. In MRI, one can see evidence for primary anterograde and retrograde axonal degeneration in the NAWM.
He also emphasized the role of OCT (optical coherence tomography) in optic neuritis and CIS in particular.

Prof Edan. There emphasis on the difference between neurodegeneration due to focal or diffuse inflammation.
A bigger change in T2 lesion volume in the 1st 5 years is correlated with who will progress to SP stage (Fisniku LK & Miller).
In MS with progressive onset, phase I (time from EDSS 0 to EDSS 3) is much shorter that in RR-MS.
Both PP-MS and initially RR MS start phase II (EDSS 3 to EDSS 6) at about the same age.
At the end of day, the debate could reach a consensus about whether inflammation drives or is independent of neurodegeneration. Based on brain post-mortem pathology, there is inflammation behind the BBB; this compartment is not targeted by most drugs: even drugs with BBB penetration such as cladribine only achieve a concentration of about ¼ of the peripheral blood concentration, which may explain why SP-MS trials disappointment. Based on clinical cohorts and MRI studies, there is imaging evidence for neurodegeneration very early on in disease and in locations that do not seem to be affected by focal inflammation.

Novartis sponsored a Satellite Symposium
on “Fingolimod: SP1 receptor modulation” chaired by Prof Giovannoni.
Prof Antel. Fingolimod is a pro-drug that needs a converting enzyme to be activated; this enzyme is present in the blood and in the central nervous system. This drug is thought to work both on the inflammatory component of MS but also to have CNS effects. Fingolimod is a lipophiic molecule that crosses the BBB and binds to myelin. Interestingly, this raised the question whether the myelin pool is available to act on inflammatory cells. Nevertheless, it is measurable in the CSF.
S1P1 receptor is present in neural cells and astrocytic S1P1 signalling is critical for EAE. Physiologically, it is thought to modulate endogenous repair mechanisms; in mice cerebellar cultures, the oligodendrocyte precursor cells (OPC) put out and retract processes, depending on the timing and dose of the drug, with an impact on myelin maintenance and remyelination. This effect was not always protective.
In the periphery, fingolimod prevents naïve and central memory T cells to egress from lymph nodes; only naïve T cells (CCR7+CD45RA+), central memory T cells (Tcm or CCR7+CD45RA-) and B cells are affected, but effector memory T cells (Tem or CCR7-CD45RA- and CCR7-CD45RA+) are spared. This means that only selective T cell subsets are present in the circulation and they retain their functional properties.

Prof Vermersch. In the trials with fingolimod, the primary outcomes that were assessed were T1 hypointense lesion load, general atrophy and the visual system (anterior visual pathway / RNFL / macular volume).
The OCT was used to measure retinal nerve fibre layer (RNFL) thickness, which has been associated with relapse rate and progression in 52 PwMS, as well as associated with disease activity (measured as a 1 point increase in EDSS) and disability. The OCT measures were also correlated with MRI assessment of normalised brain volume.
The OCT uses a superluminescent diode as a near-infrared light source, uses interferometry measures and is able to penetrate significantly deeper into the scattering medium, for example ~3× deeper than confocal microscopy. It measured macular thickness and volume, but can also measure retinal ganglion density of different retinal regions.
In CIS patients, the temporal area of the retina was thinner, but not the average. In most measures, it was the external areas that showed significant differences, but this is similar to all types of damage, it is not specific for CIS/MS.
In contrast with MRI general brain volume, this measure was not affected by high dose pulsed steroids.

Prof Havrdova. Clinical trials with fingolimod
Initial results from the 2-year phase III FREEDOMS 1 study (~1300 patients) show that oral fingolimod was significantly superior to placebo in reducing both relapses and disability progression in patients with RRMS. There was no significant difference in efficacy between 0.5 mg and 1.25 mg doses. It reduced the relapse rate by 54% for the 0.5 mg dose and 60% for the 1.25 mg dose compared to placebo (both p<0.001). In addition, it reduced the progression of disability by 30% for patients on 0.5 mg (p=0.024) and 32% for those on 1.25 mg (p=0.017) compared to placebo over two years.
Results from the 1-year TRANSFORMS study (largest head-to-head Phase III study, vs Avonex) showed a reduction in relapse rates of 52% and 38% for fingolimod 0.5 mg and 1.25 mg respectively compared to interferon beta-1a (both p<0.001)
FREEDOMS II, currently under way, is a 2-year placebo-controlled Phase III study, similar to FREEDOMS 1.
INFORMS in PPMS patients in on-going.

Profs Kappos, Vermersch, Hartung and Montaban
discussed what to do in CIS or fulminant MS, the role of new drugs in RRMS and in progressive disease.
When CIS becomes MS with McDonald’s criteria through MRI in the first year, it seems reasonable to treat, as these are the patients at higher risk of developing a clinical relapse earlier.
The challenges with fulminant MS
Definition: 1. Rapid sequence of relapses with intervals shorter than 30 days or
2. A single catastrophic clinical manifestation with tumour-like MRI appearance – Marburg type – with encephalopathy that may be fatal and usually on the first attack.
Histology: greater number of T cells that recognise deiminated epitopes, increased citrullination in human MBP and developmentally immature MBP. If they have a Lassmann-Lucchinnetti type II pattern, there is good recovery with plasmapheresis (and possibly rituximab), but not if they are type I or III (Balo type). It must be stressed, however, that the existence of the Lassmann- Lucchinnetti classification has recently been questioned and is not accepted by all MS neuropathologists.
The differential diagnosis includes gliomas, multifocal gliomas, gliomatosis cerebri, lymphoma or rarely sarcoidosis. Treatment: high dose pulsed steroids: 1 to 5g of methylprednisolone daily for 5 to 10 days, followed by tapering
1. MRI shows no Gad+ve lesions and less T2 lesion load → Clinical and MRI follow-up → DMT
2. MRI with Gad +ve lesion or increased T2 lesion load → mitox 6 months → DMT
3. Clinical aggravation (15 days) → plasmapheresis (5 sessions) → mitox 6 months/rituximab (pattern II)

The future anti-B-cell therapies were mentioned: ocrelizumab (humanized anti CD20 monoclonal antibody) and ofatumumab (Arzerra – HuMax-CD20, human mab, approved for non-responsive CLL, targets a different anti-CD20 epitope); atacicept (soluble form of the TACI receptor that binds to two ligands, BLyS and APRIL, that are implicated in B-cell survival, maturation and antibody production – not good in phase II MS trial), belimumab (Benlysta or LymphoStat-B is a fully human mab that specifically recognizes and inhibits the biological activity of B-lymphocyte stimulator -BLyS, also known as B-cell activation factor of theTNF family -BAFF.

The role of the new drugs in RRMS is a matter of intense debate: while some groups would offer them as first line treatment considering increased efficacy and easier administration other groups would use them in cases of failed IFNβ/glatimer acetate because of increased potential for serious side-effects.

There are still no positive trials for progressive MS. The OLYMPOS trial of rituximab in SPMS, MAESTRO (MBP8298 or dirucotide) in SPMS, and most of the trials have got the inadequate selection of patients, and bad outcome measures to show benefits.

Prof Meinl. The group has tested for antibodies against myelin glycoproteins, in particular neurofascin – an adhesion molecule required for the clustering of voltage gated Na+ channels at the node of Ranvier – as they are targets for auto-ab in MS patients. NF 186 and NF 155 may be implicated. The ab induces axonal injury in the animal model. There are detectable contactin-2 auto-abs in MS patients and the ab mediates gray matter pathology in animals. The ELISA technique is not optimal and they developed a FACS based technique and are testing their samples.

Prof Fujihara. The identification of NMO-Ig as anti-AQP4 antibodies and their presence in the serum of patients with neuromyelitis-optica was a major step in the research of neuroinflammation. Not unlike MS patients, patients with NMO have relapses of neurological deficits, usually with worse outcome. The a-AQP4-abs have been shown to destroy the AQP4 in the foot processes of astrocytes and the disease is now an independent entity, with more aggressive treatment. The highlights were the features of pain as a typical symptom, the possibility that abs become negative after steroid treatment and the presence of the typical antibodies many years prior to clinical attacks.

Prof Hemmer
. The mechanisms of pathogenic antibodies target 1. Inactivation of extra-cellular proteins, 2. Receptor blockade, 3. Cytotoxicity (through complement deposition or NK cell activity). The pathogenic antibodies bind in a conformational way to epitopes of the target protein. They have been testing for a-MOG abs in children and the younger the children are, the more a-MOG-abs they detect.
Also, in a study of children with demyelinating disease, the ones that went on to develop MS were the ones who were a-EBV-abs positive.

Dr Monica Calado-Marta

Immunology highlights ECTRIMS 2009

The highlight of ECTRIMs was the talk by the famous pathologist Prof John Prineas (Sydney, Australia), who was awarded the prestigious Charcot Prize for his unique contributions to the pathology of MS. The prize is named after the famous French neurologist also called “the Napoleon of the neuroses”. He was the first to describe multiple sclerosis as a distinct disease entity.

This talk highlighted the “astrocyte lesion” in neuromyelitis optica (NMO) and multiple sclerosis. NMO has been historically considered a subtype of MS and an autoimmune disease targeting astrocytes – star-shaped glial cells in the brain and spinal cord. Anti-aquaporin-4 antibodies, which are directed against this astrocytic water channel, are involved in the disease pathogenesis and used as diagnostic markers. Similar degenerative changes were also found in astrocytic endfeet in early MS lesions and Prof Prineas put forward the hypothesis that MS may not be a disease exclusively of oligodendrocytes and myelin, and suggested that future work should also focus on astrocytes.

One “hot topic session” of the conference was dedicated to Th17 cells. This cytokine was recently discovered and found to play a role MS and other autoimmune diseases. It is now known that axons express the IL-17 receptor and we saw very elegant experiments, using live cell imaging, looking at the trafficking capacity of these cells, which were found in close proximity to axons. This poses interesting questions about the pathogenic role of Th17 cells in MS.

Ute Meier, Post-doctoral Scientist