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A first-in-class treatment for multiple indications
Improves clinical score
In EAE model, treatment with relaxin showed greater improvement in clinical scores (from average of 2.0 to <0.5),co compared to the placebo treated group (from average of 2.0 to 1.5). It also reduced demyelination, the loss of neurons and gliosis (neural injury).Proinflammatory cytokines and chemokine receptors also decreased.
Promotes remyelination
Our studies showed that Relaxin treatment promotes differentiation and maturation of Oligodendrocyte Precursor Cells into mature myelin-producing oligodendrocytes and promotes remyelination.The relaxin modulated pathways which promote remyelination include Glucocorticoid receptors, Olig 1/2 and Relaxin family receptors 1&2.
Synergy with steroids
Relaxin has shown to have synergistic effects with steroids (in models of respiratory fibrosis). This is likely to be to due the MoA of RLN and could also have a similar effect in Multiple Sclerosis. Lynflexin™ would have an even more attractive positioning, as steroids are some of the most commonly used drugs as first line therapy in MS.
Underlying the need for effective and well tolerated therapeutics to increase compliance in treating relapses in Multiple Sclerosis, prompted our investigation of the anti-inflammatory immune-modifying pregnancy hormone relaxin (RLN) as a novel pathway.
A spontaneous remission of symptoms in the later stages of pregnancy has been well characterized in subjects with MS, (Lorenzi and Ford, 2002). These remissions are thought to be due to the production of pregnancy hormones. One such pregnancy factor is RLN, a member of the relaxin peptide superfamily (Bathgate et al, 2013) which is also up regulated in the later stages of pregnancy (Goldsmith and Voskuhl, 2009). RLN is pleiotropic in nature, acting as an agonist for the glucocorticoid receptor (GCR, Dschietzig et al, 2004) and the relaxin family peptide receptors 1 and 2 (RXFP1 and RXFP2, Bathgate et al, 2013). Through these receptors RLN can modulate the immune system by suppressing cell adhesion molecules (Bani et al, 2003), increasing cyclic adenosine monophosphate (Nguyen and Dessauer, 2005), regulating differential expression of matrix metalloproteinases (Mu et al, 2010), regulating cytokine and chemokine receptor (CCR) expression (Bathgate 2013) and inhibit cell-mediated pro-inflammatory activity by stimulation of the peroxisome proliferatoractivated receptor gamma (PPARĪ³; Singh and Bennet, 2010) which has neuroprotective effects (Gray et al, 2012). Through these diverse actions, RLN could have a potential to modulate the clinical symptoms of MS, be neuroprotective and promote remyelination.
The use of glucocorticoid agonists in treating acute attacks of multiple sclerosis is well established. Relaxin, a member of the insulin super family is a pleiotropic hormone capable of influencing multiple pathways which include the glucocorticoid receptor and relaxin family peptide receptors 1 and 2. In addition to the action of relaxin on the glucocorticoid receptor, activation of the relaxin receptors have additional anti-inflammatory and immuno-modulating effects.
Our study has shown that relaxin significantly reduced the clinical signs of disease, decreased mRNA expression of pro-inflammatory cytokines and chemokine receptors. Treatment also lead to a decrease in lesion load and size and macrophage infiltration, preserved myelin and neurofilaments, reduced gliosis and promoted remyelination.
in development targetting Multipe Sclerosis, and other CNS indications. It has the potential to modulate the clinical symptoms of MS, be neuroprotective and promote remyelination.
We are proud to be pioneering innovative R&D with a neuroprotective effect and potential in Multiple Sclerosis and other disorders.
Multiple Sclerosis is our first indication. Additional indications are Chronic Traumatic Encephalopathy and Traumatic Brain Injury.
Our development products are protected by patents, know-how and technical information which provides exclusivity.
BVBiomed is a research driven company dedicated to the discovery of novel therapeutic compounds for use in treating neuro-degenerative diseases. We are currently developing two new compounds which are anti-inflammatory and auto-immune regulators and are preparing clinical trials of these therapies in treating multiple sclerosis.