EHP-102 / Emerald Health Pharmaceuticals - LARVOL DELTA

Investigation in the cannabigerol derivative VCE-003.2 as a disease-modifying agent in a mouse model of experimental synucleinopathy. (PubMed, Behav Brain Funct) - "Our study broadens the neuroprotective potential of VCE-003.2, previously described against mitochondrial dysfunction, oxidative stress, glial reactivity and neuroinflammation in PD. We now demonstrate its efficacy against another key pathogenic event in PD as α-synuclein dysregulation. Furthermore, our investigation sheds light on the molecular mechanisms underlying VCE-003.2 revealing its role in regulating interferon signaling. These findings, together with a favorable ADMET profile, enhance the preclinical interest of VCE-003.2 towards its future clinical development in PD."

Journal • Preclinical • CNS Disorders • Inflammation • Metabolic Disorders • Movement Disorders • Parkinson's Disease

The Cannabigerol Derivative VCE-003.2 Exerts Therapeutic Effects in 6-Hydroxydopamine-Lesioned Mice: Comparison with The Classic Dopaminergic Replacement Therapy. (PubMed, Brain Sci) - "(4) Our results confirmed again the therapeutic profile of VCE-003.2 in experimental PD and revealed a different and more relevant effect, as a disease modifier, compared to the classic symptom-alleviating L-DOPA treatment. This reinforces the interest in VCE-003.2 for a future clinical development in this disease."

Journal • Preclinical • CNS Disorders • Movement Disorders • Parkinson's Disease

Emerald Health Pharmaceuticals Strengthens Global Patent Portfolio with New International Patents (GlobeNewswire) - "The Company’s patents consist of composition-of-matter patents as well as formulation and method-of-use patents, including for its lead product candidates EHP-101 and EHP-102 for the treatment of the Company’s initial disease targets - multiple sclerosis, systemic sclerosis, Huntington’s disease, Parkinson’s disease - and others. The issued patents have potential patent terms in a range from 2030 to 2037, not including any patent term adjustments, patent term extensions or disclaimers.....'Expanding our intellectual property portfolio is a vital goal alongside our efforts to validate our drug candidates in the clinic, so securing these new patents is an important value-adding step as we continue to enroll patients in our Phase 2a clinical study of EHP-101 for systemic sclerosis, with interim results expected in the second half of 2022, and prepare to enroll patients in our Phase 2a for certain relapsing forms of multiple sclerosis.'"

Enrollment status • P2 data • Patent • CNS Disorders • Huntington's Disease • Immunology • Multiple Sclerosis • Parkinson's Disease • Systemic Sclerosis

Neuroprotection with the Cannabidiol Quinone Derivative VCE-004.8 (EHP-101) against 6-Hydroxydopamine in Cell and Murine Models of Parkinson's Disease. (PubMed, Molecules) - "The 3-hydroxyquinone derivative of the non-psychotrophic phytocannabinoid cannabigerol, so-called VCE-003.2, and some other derivatives have been recently investigated for neuroprotective properties in experimental models of Parkinson's disease (PD) in mice. The treatment with T0070907 alone only caused a partial reversal, whereas SR144528 alone had no effect, indicating a major contribution of PPAR-γ receptors in the cytoprotective effect of VCE-004.8 at 10 µM. In summary, our data confirmed the neuroprotective potential of VCE-004.8 in 6-OHDA-lesioned mice, and in vitro studies confirmed a greater relevance for PPAR-γ receptors rather than CB receptors in these effects."

Journal • Preclinical • CNS Disorders • Metabolic Disorders • Movement Disorders • Parkinson's Disease • CD68 • GFAP

[VIRTUAL] Emerald Health Pharmaceuticals (BIO 2021) - "EHP has two lead product candidates in development, initially targeting 4 diseases: EHP-101 in Phase 2 for multiple sclerosis (MS) and system sclerosis (SSc), and EHP-102 in preclinical development for Parkinson's disease (PD) and Huntington's disease (HD). EHP has a highly experienced, expert management team, and globally recognized clinical and scientific advisors."

CNS Disorders • Fibrosis • Huntington's Disease • Immunology • Movement Disorders • Multiple Sclerosis • Parkinson's Disease

Aggressiveness and Metastatic Potential of Breast Cancer Cells Co-Cultured with Preadipocytes and Exposed to an Environmental Pollutant Dioxin: An in Vitro and in Vivo Zebrafish Study. (PubMed, Environ Health Perspect) - "The results of our study using BC cell lines co-cultured with preadipocytes and a POP and an in vivo zebrafish model of metastasis suggest that the interactions between BC cells and their microenvironment could affect their invasive or metastatic potential. https://doi.org/10.1289/EHP7102."

Journal • Preclinical • Breast Cancer • Oncology • Solid Tumor

Emerald Health Pharmaceuticals Demonstrates Potential Disease-Modifying Activity of Novel Product Candidate with Multi-Modal Mechanism of Action in Parkinson’s Disease (GlobeNewswire) - "Emerald Health...has published a scientific article in the peer-reviewed journal, Molecular and Cellular Neuroscience, highlighting data supporting the potential of EHP’s drug product candidate, EHP-102, to treat Parkinson’s disease (PD)...The results of the study demonstrated that oral administration of EHP-102 in 6-OH-dopamine-lesioned mice, a validated Parkinson’s disease model...The published scientific paper is titled, 'Neuroprotection with the cannabigerol quinone derivative VCE-003.2 and its analogs CBGA-Q and CBGA-Q-Salt in Parkinson’s disease using 6-hydroxydopamine-lesioned mice.'...EHP is currently advancing the formulation and manufacturing of EHP-102 in preparation for nonclinical studies required to advance to clinical development in both PD and HD."

Preclinical • CNS Disorders • Huntington's Disease • Parkinson's Disease

Neuroprotection with the cannabigerol quinone derivative VCE-003.2 and its analogs CBGA-Q and CBGA-Q-Salt in Parkinson's disease using 6-hydroxydopamine-lesioned mice. (PubMed, Mol Cell Neurosci) - "Additional phytocannabinoid derivatives, CBGA-Q and CBGA-Q-Salt, also afforded neuroprotection in 6-OHDA-lesioned mice, but their effects were lower compared to VCE-003.2, in particular in the case of CBG-Q-Salt. In vitro studies confirmed the relevance of PPAR-γ receptors for these effects."

Journal • CNS Disorders • Metabolic Disorders • Movement Disorders • Parkinson's Disease • CD68 • GFAP

Emerald Health Pharmaceuticals to Open a New Financing Round Under its Regulation A+ Offering (GlobeNewswire) - "Emerald Health Pharmaceuticals Inc. (EHP)...will open a new financing round under its Regulation A ('Reg A') offering on December 7, 2020 following demand from existing and new investors to purchase shares....The Company has also advanced preclinical work for EHP-102, its novel, patented synthetic cannabigerol (CBG) derivative being developed to treat Huntington’s disease...Additional proceeds from this offering will be used to continue advancing its Phase 2 clinical programs, including the initiation of EHP’s planned Phase 2 study for multiple sclerosis and to continue the preclinical development of EHP-102."

Financing • CNS Disorders • Huntington's Disease

Emerald Health Pharmaceuticals Announces Closing Date For its Current Regulation A+ Offering Round (GlobeNewswire) - "Emerald Health Pharmaceuticals Inc....has announced a closing date for its current Regulation A ('Reg A') offering round following the strong demand for its capital raise to date....Proceeds from this offering are being used primarily to complete EHP’s current Phase 2a clinical study of EHP-101 in systemic sclerosis, initiate preparations for EHP’s planned Phase 2 study for multiple sclerosis and continue preclinical development of EHP-102 for the treatment of Huntington’s and Parkinson’s disease."

Financing • CNS Disorders • Huntington's Disease • Immunology • Multiple Sclerosis • Parkinson's Disease • Systemic Sclerosis

Emerald Health Pharmaceuticals Renews Regulation A Offering and Provides Mid-Year Corporate Update (GlobeNewswire) - "Emerald Health Pharmaceuticals Inc. (EHP)...is now accepting investments under its Regulation A ('Reg A') offering. As of June, EHP had raised more than $22 million under its Reg A offering....The Company has also advanced preclinical work for EHP-102....Demonstrated and published the anti-inflammatory and neuroprotective activity and the potential to stop the damage to nerves that produce dopamine (the main issue in PD) in PD models; Demonstrated and published the potential to promote the regeneration of nerve cells and protect against neuroinflammation and neurodegeneration in HD models."

Financing • Preclinical • CNS Disorders • Huntington's Disease • Parkinson's Disease

A Systematic Review of Minor Phytocannabinoids with Promising Neuroprotective Potential. (PubMed, Br J Pharmacol) - "Limited mechanistic data showed CBG, VCE.003, VCE.003.2 and Δ -THCA mediated some of their effects through PPARy, but no other receptors were probed. Further studies with these phytocannabinoids, and their combinations, are warranted across a range of neurodegenerative disorders."

Journal • Review • Alzheimer's Disease • CNS Disorders • Epilepsy • Gene Therapies • Huntington's Disease • Movement Disorders • Parkinson's Disease

EMA grants orphan status to EHP-102 for treatment of Huntington’s (Huntington’s Disease News) - “The European Medicines Agency (EMA) granted orphan designation to Emerald Health Pharmaceuticals’ (EHP) EHP-102 for the treatment of Huntington’s disease.”

Orphan drug

Emerald Health Pharmaceuticals granted Orphan Designation in Europe for Huntington’s disease (GlobeNewswire) - "Emerald Health Pharmaceuticals Inc. (EHP)...announced today that the European Medicines Agency (EMA) has granted Orphan Designation for its product candidate, EHP-102, for the treatment of Huntington’s disease (HD)."

Orphan drug

Development of An Oral Treatment with the PPAR-γ-Acting Cannabinoid VCE-003.2 Against the Inflammation-Driven Neuronal Deterioration in Experimental Parkinson's Disease. (PubMed, Molecules) - "The analysis using qPCR in the striatum of proinflammatory mediators, such as tumor necrosis factor-α, interleukin-1β, inducible nitric oxide synthase, and cyclooxygenase-2, showed that the marked elevations provoked by the LPS lesion tended to be, in general, attenuated by VCE-003.2 treatment, with the greatest effects normally found with the highest dose of 20 mg/kg. In summary, our data confirm the neuroprotective potential of an oral formulation of VCE-003.2 against neuronal injury in an in vivo model of PD based on neuroinflammation, and this study opens the possibility to further the development of oral VCE-003.2 in the clinic."

Journal

Cannabinoid derivatives show therapeutic potential in mouse model, but EHP-102 still superior (Huntington’s Disease News) - “In a mouse model of Huntington’s disease, all three compounds reduced clinical symptoms and neuronal loss. They all also inhibited the production of proinflammatory cytokines — a type of immune signalling molecules that promote inflammatory processes. However, when compared with the other two cannabigerol-acid derivatives, EHP-102 showed significantly better effects on multiple clinical parameters.”

Preclinical

Neuroprotective effects of the cannabigerol quinone derivative VCE-003.2 in SOD1 transgenic mice, an experimental model of amyotrophic lateral sclerosis. (PubMed, Biochem Pharmacol) - "Lastly, VCE-003.2 attenuated the LPS-induced generation of TNF-α and IL-1β in cultured astrocytes obtained from SOD1 transgenic newborns, an effect also produced by rosiglitazone, then indicating a probable PPAR-γ activation as responsible of its neuroprotective effects. In summary, our results showed benefits with VCE-003.2 in SOD1 transgenic mice supporting PPAR-γ as an additional neuroprotective target available for cannabinoids in ALS. Such benefits would need to be validated in other ALS models prior to be translated to the clinical level."

Journal • Preclinical

Emerald Health Pharmaceuticals Demonstrates Neuroprotective Activity of Novel Cannabigerol Derivatives in Huntington’s and Parkinson’s Disease Models (GlobeNewswire, Emerald Health Pharmaceuticals) - EHP-102 and other novel cannabigerol derivatives from Emerald Health Pharmaceuticals demonstrate therapeutic potential in validated animal models . SAN DIEGO, CA, July 02, 2019 (GLOBE NEWSWIRE) -- Emerald Health Pharmaceuticals Inc (EHP or the Company), a clinical-stage company developing medicines based on cannabinoid science, presented preclinical data for its drug product candidate, EHP-102, an oral formulation of a patented cannabigerol (CBG)-derived new chemical entity (NCE), as well as other novel CBG acid (CBGA) derivatives for the treatment of Huntington’s disease (HD) and Parkinson’s disease (PD) at the 29th Annual Symposium of the International Cannabinoid Research Society (ICRS) in Bethesda MD, USA.

Preclinical

Emerald Health Pharmaceuticals to Present Preclinical Data at the 29th Annual Symposium of the International Cannabinoid Research Society (GlobeNewswire, Emerald Health Pharmaceuticals) - SAN DIEGO, CA, June 19, 2019 (GLOBE NEWSWIRE) -- Emerald Health Pharmaceuticals Inc (EHP), a clinical-stage company developing medicines based on cannabinoid science, will present preclinical data on EHP-101, an oral formulation of a patented synthetic cannabidiol (CBD)-derived new chemical entity (NCE), for the treatment of multiple sclerosis (MS) and systemic scleroderma (SSc). EHP will also present preclinical data on EHP-102, an oral formulation of a patented synthetic cannabigerol (CBG)-derived NCE as well as new CBG acid (CBGA) derivatives for the treatment of Huntington’s disease (HD) and Parkinson’s disease (PD) at the 29th Annual Symposium of the International Cannabinoid Research Society. Effects of EHP-101 on inflammation and remyelination in murine models of multiple sclerosis. Its second product candidate, EHP-102, is in preclinical development and is focused on treating Huntington’s disease and Parkinson’s disease.

Preclinical

Oral administration of the cannabigerol derivative VCE-003.2 promotes subventricular zone neurogenesis and protects against mutant huntingtin-induced neurodegeneration. (PubMed, Transl Neurodegener) - "VCE-003.2 was able to increase neuroblast formation and striatal-like CTIP2-mediated neurogenesis. The cannabigerol derivative VCE-003.2 improves subventricular zone-derived neurogenesis in response to mutant huntingtin-induced neurodegeneration, and is neuroprotective by oral administration."

Journal