etrinabdione (EHP-101) / Emerald Health Pharmaceuticals, Aphios, Emerald Health Research - LARVOL DELTA

CLAUDIA: Evaluation of Safety, Tolerability and Preliminary Efficacy of Etrinabdione in Patients With Peripheral Arterial Disease (clinicaltrials.gov) - P2 | N=30 | Not yet recruiting | Sponsor: VivaCell Biotechnology España

New P2 trial • Cardiovascular • Peripheral Arterial Disease • ESM1 • IL17A • IL18 • IL6 • TNFA • VEGFA

Etrinabdione (VCE-004.8), a B55α activator, promotes angiogenesis and arteriogenesis in critical limb ischemia. (PubMed, J Transl Med) - "The findings presented in this study indicate that Etrinabdione holds promise in mitigating endothelial cell damage and senescence, while concurrently fostering arteriogenesis and angiogenesis. These observations position Etrinabdione as a compelling candidate for the treatment of PAD, and potentially other cardiovascular disorders."

Biomarker • Journal • Cardiovascular • Fibrosis • Immunology • Inflammation • Peripheral Arterial Disease • AMPK • CAV1 • HIF1A • NOS3 • PPP2R2A • SIRT1

Neuroprotective effects of VCE-004.8 in a rat model of neonatal stroke. (PubMed, Eur J Pharmacol) - "These data suggest that this drug could be effective for the treatment of stroke in newborns."

IO biomarker • Journal • Preclinical • Cardiovascular • CNS Disorders • Hematological Disorders • Inflammation • Vascular Neurology • PPARG • TLR4 • TNFA

Evaluation of Safety, Tolerability and Preliminary Efficacy of EHP-101 in Diffuse Cutaneous Systemic Sclerosis (clinicaltrials.gov) - P2a | N=36 | Suspended | Sponsor: Emerald Health Pharmaceuticals | Recruiting ➔ Suspended

Trial suspension • Fibrosis • Immunology • Scleroderma • Systemic Sclerosis

Neuroprotection by the cannabidiol aminoquinone VCE-004.8 in experimental ischemic stroke in mice. (PubMed, Neurochem Int) - "Our data show that VCE-004.8 is a promising drug candidate for treating ischemic brain injury. Since VCE-004.8 has been shown to be safe in the clinical setting, the possibility of repurposing its use as a delayed treatment option for ischemic stroke adds substantial translational value to our findings."

Journal • Preclinical • Cardiovascular • CNS Disorders • Immunology • Inflammation • Ischemic stroke • Multiple Sclerosis • Vascular Neurology • MMP9 • PPARG

Emerald Health Pharmaceuticals Receives Safety Review Committee Approval to Proceed to Final Cohorts of EHP-101 Phase 2a Systemic Sclerosis Trial (GlobeNewswire) - "Emerald Health Pharmaceuticals...has received a positive safety review following a pre-specified interim analysis by the Safety Review Committee ('SRC') of its Phase 2a study of EHP-101 for systemic sclerosis ('SSc'). The SRC has recommended that the trial continue without modification. EHP expects to report interim results from the study in early 2023."

DSMB • P2a data • Immunology • Systemic Sclerosis

Evaluation of Safety, Tolerability and Preliminary Efficacy of EHP-101 in Relapsing Forms of Multiple Sclerosis (clinicaltrials.gov) - P2a | N=50 | Suspended | Sponsor: Emerald Health Pharmaceuticals | Recruiting ➔ Suspended

Trial suspension • CNS Disorders • Multiple Sclerosis • NEFL

A Study to Evaluate the Safety, Tolerability and Preliminary Efficacy of EHP-101 in Patients with Relapsing Forms of Multiple Sclerosis (RMS) Estudio para evaluar la seguridad, la tolerabilidad y la eficacia preliminar de EHP-101 en pacientes con formas recidivantes de esclerosis múltiple (EMR) (clinicaltrialsregister.eu) - P2 | N=50 | Ongoing | Sponsor: Emerald Health Pharmaceuticals Inc.

New P2 trial • CNS Disorders • Multiple Sclerosis

Emerald Health Pharmaceuticals Completes Enrollment of First Two Cohorts of Phase II Systemic Sclerosis Trial (GlobeNewswire) - "Emerald Health Pharmaceuticals Inc...has completed enrolling the first two cohorts of nine patients each of its Phase II clinical study of the Company’s lead product candidate, EHP-101, an oral formulation of a patented new molecule....After completing drug dosing and monitoring for each patient as per the study protocol, EHP expects to report interim results from the study in early 2023."

Enrollment status • P2a data • Immunology • Systemic Sclerosis

Emerald Health Pharmaceuticals Reports Data Showing Novel Drug Candidate is First-in-class B55α/PP2A Activator (GlobeNewswire) - "Emerald Health Pharmaceuticals Inc...today announced the publication of a scientific article in the peer-reviewed Journal of Neuroinflammation highlighting additional data supporting the unique mechanism of action of EHP-101, the company’s first-in-class drug candidate for the treatment of systemic sclerosis (SSc) and multiple sclerosis (MS)....The publication demonstrates that VCE-004.8, the active pharmaceutical ingredient of EHP-101, is a highly specific activator of the B55a subunit of the protein phosphatase, thus activating the hypoxia-inducible factor (HIF) pathway. This first-in-class activator of the HIF pathway via modulation of B55a provides a new mechanism to treat diseases where vascular integrity is compromised. Therefore, these findings support the use of EHP-101 for the treatment of SSc and MS, and illustrate the potential of VCE-004.8 for acute disorders including traumatic brain injury and stroke."

Preclinical • Immunology • Multiple Sclerosis • Scleroderma • Systemic Sclerosis

Evaluation of Safety, Tolerability and Preliminary Efficacy of EHP-101 in Diffuse Cutaneous Systemic Sclerosis (clinicaltrials.gov) - P2a | N=36 | Recruiting | Sponsor: Emerald Health Pharmaceuticals | Trial completion date: Sep 2022 ➔ Oct 2024 | Trial primary completion date: Jun 2022 ➔ Jul 2024

Trial completion date • Trial primary completion date • Fibrosis • Immunology • Scleroderma • Systemic Sclerosis

A cannabidiol aminoquinone derivative activates the PP2A/B55α/HIF pathway and shows protective effects in a murine model of traumatic brain injury. (PubMed, J Neuroinflammation) - "This study provides new insight about the mechanism of action of VCE-004.8 regulating the PP2A/B55α/PHD2/HIF pathway. Furthermore, we show the potential efficacy for TBI treatment by preventing BBB disruption, enhancing angiogenesis, and ameliorating neuroinflammation and neurodegeneration after brain injury."

Journal • Preclinical • CNS Disorders • Fibrosis • Immunology • Inflammation • Multiple Sclerosis • Scleroderma • Systemic Sclerosis • Vascular Neurology • CD31 • PECAM1 • PPARG • PPP2R2A • TJP1 • VCAM1

Emerald Health Pharmaceuticals Adds Leading Rheumatologist to Distinguished Systemic Sclerosis Clinical Advisory Board (GlobeNewswire) - "'Dr. Furst’s extensive expertise in the research and treatment of systemic sclerosis and clinical trial design will be invaluable as we assess Phase 2a clinical trial results of our EHP-101 drug candidate, starting with preliminary data in 2022, and plan the next phase of our SSc clinical program'...In addition...Clinical Advisory Board includes John Varga, MD...Janet Pope, MD, who are all internationally-respected rheumatologists who have shown leadership in advancing research and clinical development related to scleroderma."

Media quote • Scleroderma • Systemic Sclerosis

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

Evaluation of Safety, Tolerability and Preliminary Efficacy of EHP-101 in Relapsing Forms of Multiple Sclerosis (clinicaltrials.gov) - P2a; N=50; Recruiting; Sponsor: Emerald Health Pharmaceuticals; Not yet recruiting ➔ Recruiting; Phase classification: P2 ➔ P2a; Trial completion date: Sep 2023 ➔ Apr 2024; Trial primary completion date: Jun 2023 ➔ Dec 2023

Enrollment open • Phase classification • Trial completion date • Trial primary completion date • CNS Disorders • Multiple Sclerosis • MRI

Emerald Health Pharmaceuticals Receives IND Clearance to Begin Phase 2 Clinical Trial of EHP-101 for Relapsing Forms of Multiple Sclerosis (GlobeNewswire) - "Emerald Health Pharmaceuticals Inc...has received clearance of its Investigational New Drug (IND) application by the U.S. Food and Drug Administration (FDA) to begin enrolling patients in its Phase 2a clinical trial of EHP-101 for certain relapsing forms of multiple sclerosis (RMS), specifically relapsing-remitting MS (RRMS) and active secondary progressive MS (SPMS)....The international Phase 2a, open-label, multicenter dose-finding study in patients with RMS will evaluate the safety, tolerability, and preliminary efficacy of the Company’s lead product candidate, EHP-101. The study is designed to enroll 50 patients who suffer from RMS in approximately 30 study centers in the US, the EU, and Australia. Patients will receive escalating doses administered once or twice daily and will be evaluated over a treatment duration of 24 weeks."

New P2a trial • CNS Disorders • Immunology • Multiple Sclerosis

Emerald Health Pharmaceuticals Adds Leading Rheumatologist to Distinguished Systemic Sclerosis Clinical Advisory Board (GlobeNewswire) - "'Dr. Furst’s extensive expertise in the research and treatment of systemic sclerosis and clinical trial design will be invaluable as we assess Phase 2a clinical trial results of our EHP-101 drug candidate, starting with preliminary data in 2022, and plan the next phase of our SSc clinical program...'"

P2a data • Immunology • Scleroderma • Systemic Sclerosis

Emerald Health Pharmaceuticals’ Novel Drug Candidate Demonstrates Significant Anti-inflammatory and Anti-fibrotic Activity in Multi-organ Fibrosis Preclinical Model (GlobeNewswire) - "Emerald Health Pharmaceuticals Inc...has announced the publication of a scientific article in the peer-reviewed journal, Biomedicine & Pharmacotherapy, highlighting a new study providing additional data supporting the potential of EHP’s patented, first-in-class drug candidate, EHP-101, to treat fibrotic diseases, including cardiac fibrosis and systemic sclerosis (SSc). EHP is currently enrolling patients dosed with oral EHP-101 in a Phase IIa clinical trial for SSc (NCT04166552)...EHP-101 was shown to reduce fibrotic markers and prevent multiple organ fibrosis, including cardiac fibrosis, and reduce the infiltration of macrophages and T cells in cardiac tissue."

Enrollment status • Preclinical • Immunology • Systemic Sclerosis

EHP-101 alleviates angiotensin II-induced fibrosis and inflammation in mice. (PubMed, Biomed Pharmacother) - "EHP-101 is an oral lipidic formulation of the novel non-psychotropic cannabidiol aminoquinone VCE-004.8, which showed antifibrotic activity in murine models of systemic sclerosis induced by bleomycin...Mice infused with Ang II resulted in collagen accumulation in left ventricle, aortic, dermal, renal and pulmonary tissues; oral administration of EHP-101, Ajulemic acid and Losartan improved these phenotypes...Furthermore, EHP-101 inhibits renal, pulmonary and dermal fibrosis. EHP-101 could offer new opportunities in the treatment of cardiac fibrosis and other fibrotic diseases."

Journal • Preclinical • Fibrosis • Immunology • Inflammation • Scleroderma • Systemic Sclerosis • CCL2 • CDK1 • COL1A2 • IL1B • IL6 • TGFB1 • TOP2A

Cannabinoquinones: Synthesis and Biological Profile. (PubMed, Biomolecules) - "These studies culminated in the discovery of the aminocannabinoquinone VCE-004.8 (5), a compound under phase 2 clinical development with orphan drug status by EMA and FDA for the management of scleroderma. The synthesis and rich chemistry of these compounds will be described, summarizing their biological profile and clinical potential."

Journal • Review • Fibrosis • Immune Modulation • Immunology • Inflammation • Scleroderma • 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

Evaluation of Safety, Tolerability and Preliminary Efficacy of EHP-101 in Relapsing Forms of Multiple Sclerosis (clinicaltrials.gov) - P2; N=50; Not yet recruiting; Sponsor: Emerald Health Pharmaceuticals

Clinical • New P2 trial • CNS Disorders • Multiple Sclerosis • MRI

Evaluation of Safety, Tolerability and Preliminary Efficacy of EHP-101 in Diffuse Cutaneous Systemic Sclerosis (clinicaltrials.gov) - P2a; N=36; Recruiting; Sponsor: Emerald Health Pharmaceuticals; Trial completion date: Jul 2021 ➔ Sep 2022; Trial primary completion date: Mar 2021 ➔ Jun 2022

Clinical • Trial completion date • Trial primary completion date • Fibrosis • Immunology • Scleroderma • Systemic Sclerosis

Emerald Health Pharmaceuticals Starts Activities for Initiation of Phase 2 Clinical Study in Multiple Sclerosis (GlobeNewswire) - "Emerald Health Pharmaceuticals Inc....has initiated activities for a Phase 2 international clinical study for the treatment of patients with multiple sclerosis (MS). 'The initiation of this MS Phase 2 study is another important milestone for our lead product candidate, EHP-101,'...'We have finalized the trial design with our MS Clinical Advisory Board members...We will soon be seeking regulatory approvals to begin the study and look forward to starting clinical site initiations and enrolling multiple sclerosis patients later this year.'...The study is planned to enroll approximately 50 patients who suffer from RMS (relapsing-remitting and relapsing secondary progressive MS) in approximately 20 study centers in the United States and Australia."

Trial status • CNS Disorders • Multiple Sclerosis