One molecule, multiple therapeutic targets

EHP-101: Designed for targeted mechanism of action

The unique, fully synthetic novel molecule formulated in EHP-101 (VCE-004.8) has been rationally designed to be a dual peroxisome proliferator-activated receptor gamma (PPARγ) modulator and cannabinoid type 2 (CB2) receptor agonist that also activates the hypoxia inducible factor (HIF) pathway. PPARγ and CB2 are preclinically validated therapeutic targets, supported by scientific literature, for the development of novel drugs modulating inflammatory responses for the treatment of multiple sclerosis (MS) as well as for the treatment of systemic sclerosis (SSc), a severe form of scleroderma.  Effects on the HIF pathway also provide potential additional benefits to MS and SSc patients, as the HIF pathway modulates the immune response that favors both neuroprotection and myelin regeneration in MS as well as prevents collagen deposition around blood vessels and reduces vascular damage in SSc.

Furthermore, evidence shows these validated receptors may be beneficial in preventing neuroinflammation and demyelination in the CNS, and fibrogenesis in the periphery. Based on these activities, EHP is initially developing this proprietary new drug candidate for multiple sclerosis and systemic sclerosis. A summary of the effects of the novel molecule in EHP-101 on systemic sclerosis and multiple sclerosis are shown here:

In preclinical studies, EHP-101 demonstrated potential disease-modifying benefits relating to prevention of demyelination and stimulation of remyelination in multiple sclerosis. In SSc models, similar disease-modifying benefits were seen, both in reducing inflammation and fibrosis, as well as promoting the protection and regeneration of the vasculature, which is important in SSc.

Data from our large Phase 1 (104 healthy volunteers) randomized, double-blind, placebo-controlled study of EHP-101 demonstrated favorable safety and tolerability profiles. Mainly mild adverse events were observed with increasing doses, providing EHP with flexibility in setting the dosing of patients in future clinical studies.