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Rationale for Antiretroviral Therapy for Treatment of Multiple Sclerosis

Epstein-Barr virus causing multiple sclerosis has become irrefutable. Evidence indicating that EBV not only causes, but drives disease progression is growing. If EBV is a driver of MS then elimination of EBV would be a rational therapy for MS. There are licensed drugs with activity against EBV, such as the antiviral medication tenofovir alafenamide, which may be particularly effective as an inhibitor of EBV lytic reactivation.


See the following dropbox link for a number of scientific papers indicating that EBV is the cause and driver of MS disease activity, and on potential antiviral therapies.

Dropbox

Epstein-Barr Virus Causes MS

Multiple sclerosis is caused by EBV. The risk of MS increased 32-fold after infection with EBV. Serum levels of neurofilament light chain increased only after EBV infection. These findings suggest EBV as the leading cause of MS.
Longitudinal analysis reveals high prevalence of Epstein-Barr virus associated with multiple sclerosis


EBV as a driver of MS.

Epstein-Barr virus as a driver of multiple sclerosis

EBV as the “gluten of MS” hypothesis provides a rationale for trialing antiviral therapies

The case for targeting latent and lytic Epstein-Barr virus infection in multiple sclerosis

Early identification of individuals at risk for multiple sclerosis by quantification of EBNA-1381-452-specific antibody titers

Broader Epstein–Barr virus–specific T cell receptor repertoire in patients with multiple sclerosis

Unstable EBV latency drives inflammation in multiple sclerosis patient derived spontaneous B cells

Evaluation of IL-1β and IL-6 expression following EBNA-1 and BRLF-1 peptide treatment in EBV-positive MS patients

Seroreactivity against lytic, latent and possible cross-reactive EBV antigens appears on average 10 years before MS induced preclinical neuroaxonal damage

Targeting EBV is a viable therapeutic target in MS

EBV infection and HLA-DR15 jointly drive multiple sclerosis by myelin peptide presentation

Myelin antigen capture in the CNS by B cells expressing EBV latent membrane protein 1 leads to demyelinating lesion formation

Discoveries beyond molecular mimicry describe how EBV drives multiple sclerosis

EBV dysregulation is associated with immune imbalance in multiple sclerosis

 

Neurologist Gavin Giovannoni’s blog is a resource for additional information regarding MS and EBV.
MS-Selfie

Antiretroviral Therapy Case Reports

Tenofovir Inhibits EBV Reactivation

The patients in the above case reports are taking tenofovir prodrugs, tenofovir disoproxil fumarate (TDF) or tenofovir alafenamide fumarate (TAF). TAF may be particularly effective as an inhibitor of EBV lytic reactivation, and clinical studies are warranted.
Tenofovir prodrugs potently inhibit Epstein–Barr virus lytic DNA replication by targeting the viral DNA polymerase


The below chart has implications regarding TAF and TDF dose. Fig 5G indicates that the standard dose of TAF would reach a concentration needed to block ∼40% of DNA replication (EC40) mediated by the EBV polymerase after 40 min in their in vitro assay. This indicates that the standard dose of TAF may be lower than optimal for EBV, as the EC90 is a typical therapeutic target. This data comes from an in vitro assay and the optimal dose needs to be determined in humans. Even if the standard dose is lower than optimal for EBV, there are case reports of patients who presented indefinite remission or resolution of MS symptoms taking a standard dose of TAF or TDF.

Figure 5 - Tenofovir prodrugs potently inhibit Epstein–Barr virus lytic DNA replication by targeting the viral DNA polymerase


Descovy is a fixed-dose combination antiretroviral medication of tenofovir alafenamide 25mg / emtricitabine 200mg, commonly prescribed by PrEP clinics for HIV pre-exposure prophylaxis.
Descovy


Tenofovir alafenamide fumarate (TAF) and tenofovir disoproxil fumarate (TDF), are both tenofovir prodrugs that improve the absorption and delivery of tenofovir, which gets converted into its active form (TFV-DP) inside cells to stop viral replication. TAF is a newer generation prodrug designed for better tissue targeting, allowing for lower doses. A 25mg dose of TAF leads to higher tenofovir concentrations in lymphocytes compared to a 300mg dose of TDF. TDF at 300mg daily has been used for PrEP for over a decade. This may indicate that doses of TAF greater than 25mg are safe long term, however this needs further study.

Descovy Pharmacology


The authors of this paper created a list of therapies with anti-EBV effects.

Repurposing Licensed Drugs with Activity Against Epstein-Barr Virus for Treatment of Multiple Sclerosis: A Systematic Approach

Clinical Trials