Raltegravir for RRMS

Raltegravir is an antiretroviral medicine currently used to treat HIV, under the brand name Isentress. It was investigated for its potential in treating relapsing-remitting multiple sclerosis (RRMS) patients in a small clinical trial sponsored by Merck, but failed to show benefits.

This drug’s potential as a MS treatment now appears to be on hold.

How Raltegravir works

In MS, the immune system mistakenly attacks the myelin sheath (a protective layer that surrounds nerve fibers), causingĀ damage and inflammation in the brain and spinal cord. The underlying trigger of these immune system attacks on the nervous system is not entirely known, although someĀ evidence suggests that, in some cases, they can beĀ due to the activation of human endogenous retroviruses (HERVs).

HERVs are a family of viruses present in the human genome. They are similar to retroviruses, such as HIV, but are generally inactive or present at levels too low to be consideredĀ a threat. Research has shown that HERVs that become active may be involved in MS pathology. For example, a subset calledĀ multiple sclerosis-associated retroviral element, or MSRV,Ā has been foundĀ in high levels in MS lesions. Once active, MSRV produces a protein called MSRV-envelope protein (MSRV-Env) that can induce an inflammatory response and prevent the developmentĀ of oligodendrocytes (cells that produce and repair myelin).

Other viruses, such as the Epstein-Barr virus (EBV),Ā are also suggested toĀ influence the heightened immune response seen in MS.Ā 

Because of a possible viral link to the disease, Merck decided to investigate whether the HIV drug, Raltegravir, could treat MS. The drug inhibits a viral protein called integrase, which is essential to inserting aĀ virus into the genome to promote its replication.Ā 

Raltegravir in clinical trials

A Phase 2b proof-of-concept trial called INSPIRE (NCT01767701)Ā aimed to determine whether Raltegravir mightĀ be effective inĀ easing diseaseĀ progression in RRMS patients. AboutĀ 23 participants took Raltegravir for three months and underwentĀ monthly MRI scans to assess changes in the number of MS lesions present in the brain. Results, however, found thatĀ Raltegravir failed to be of benefit;Ā no changes were seen in the development of lesions and no improvements in the level of disability or quality of life were reported in treated patients.

Currently, there are no updates concerning Raltegravir’s future as an MS treatment and no further clinical tests are being planned.

Note: Multiple Sclerosis News TodayĀ is strictly a news and information website about the disease. It does not provide medical advice, diagnosis, or treatment. This content is not intended to be a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition. Never disregard professional medical advice or delay in seeking it because of something you have read on this website.