RTL1000 is an experimental therapy developed by researchers at the Oregon Health & Science University (OHSU) Multiple Sclerosis Center, in collaboration with Artielle Immunotherapeutics, for the treatment of relapsing-remitting multiple sclerosis (RRMS).

How RTL1000 works

In MS, the immune system mistakenly directs immune cells, such as T-cells, to attack myelin (a protective sheath surrounding nerve fibers) in the brain and spinal cord, causing inflammation and damage. This results in disrupted nerve signaling and eventual permanent nerve damage.

RTL1000 is a recombinant T-cell receptor ligand. A ligand can bind and interact with specific receptors, triggering a specific response. RTL1000 is an artificially designed ligand, constructed from parts of multiple proteins involved in immune response.

By interacting with receptors on the surface of immune cells, RTL1000 can change the activity of the immune system. By binding to T-cells and other immune cells, RTL1000 is predicted to reduce inflammation and promote remyelination (repair of the myelin sheath) by reducing the production of two cytokines called CXCL1 and 2 implicated in multiple sclerosis. (Cytokines are small secreted proteins that are involved in the immune response).

Administering RTL1000 to a mouse model of MS prevented or reversed the clinical signs such as inflammatory lesions and further demyelination.

RTL1000 in clinical trials

Artielle completed a randomized, double-blind, placebo-controlled Phase 1 study (NCT00411723) testing the tolerability and safety profile of different doses of RTL1000 in 34 people with MS.

RTL1000 or a placebo was administered as an injection into a vein as a single escalating dose between two and 100 mg. The participants were observed in the hospital during the infusion and for 24 hours thereafter. They were followed to evaluate safety parameters every week for 28 days, and then one and two months after treatment. The results of the study were published in the scientific journals Autoimmune Diseases and the Journal of Neuroimmunology.

RTL1000 was well-tolerated up to a dose of 60mg, with no serious adverse events reported due to the treatment. Artielle is currently planning further studies with RTL1000 in MS.

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