dexanabinol (ETS2101) / Tangram Therapeutics, Ceska Lekarnicka - LARVOL DELTA

Cannabis Medicine 2.0: Nanotechnology-Based Delivery Systems for Synthetic and Chemically Modified Cannabinoids for Enhanced Therapeutic Performance. (PubMed, Nanomaterials (Basel)) - "This comprehensive review explores the advancements in nanoformulation strategies to enhance the therapeutic efficacy and safety of synthetic cannabinoids and related compounds, such as CB13, rimonabant, and HU-211, which have been studied in a range of preclinical models addressing conditions such as neuropathic pain, depression, and cancer. The provided summary of research concerning either chemical modifications of existing cannabinoids or the creation of new compounds that interact with cannabinoid receptors, followed by the development of nanoformulations for these agents, allows for the identification of new research directions and future perspectives for Cannabis-based medicine. In conclusion, the combination of nanotechnology and cannabinoid pharmacology holds promise for delivering more effective and safer therapeutic solutions for a broad spectrum of medical conditions, making this an exciting area of research with profound implications for the healthcare and..."

Journal • Review • CNS Disorders • Depression • Neuralgia • Oncology • Pain • Psychiatry

Integrative bioinformatics analysis for identifying the mitochondrial-related gene signature associated with immune infiltration in premature ovarian insufficiency. (PubMed, BMC Med) - "Our results highlight the crosstalk between mitochondrial function and the immune response in the development of POI. The identification of MitoDEGs could lead to reliable biomarkers for the early diagnosis, monitoring, and personalized treatment of POI."

Gene Signature • Journal • Immunology • Metabolic Disorders • Women's Health • CFTR • CPT1A • MRPL51

Cannabinoids Used for Medical Purposes in Children and Adolescents: A Systematic Review and Meta-Analysis. (PubMed, JAMA Pediatr) - "Interventions included purified cannabidiol (11 [47.8%]), nabilone (4 [17.4%]), tetrahydrocannabinol (3 [13.0%]), cannabis herbal extract (3 [13.0%]), and dexanabinol (2 [8.7%]). In this systematic review and meta-analysis, cannabinoids used for medical purposes in children and adolescents in RCTs were associated with an increased risk of adverse events. The findings suggest that long-term safety studies, including those exploring cannabinoid-related drug interactions and tools that improve adverse event reporting, are needed."

Clinical • Journal • Retrospective data • Review • Chemotherapy-Induced Nausea and Vomiting • CNS Disorders • Epilepsy

Efficacy of N-Methyl-D-Aspartate (NMDA) Receptor Antagonists in Treating Traumatic Brain Injury-Induced Brain Edema: A Systematic Review and Meta-analysis of Animal Studies. (PubMed, Neurocrit Care) - "Sixteen studies were included, with the predominant drugs being ifenprodil, MK-801, magnesium, and HU-211. Overall, NMDA antagonists exhibit promising efficacy in the treatment of traumatic brain injury. Notably, our systematic review consistently demonstrated a significant reduction in brain edema with compounds including HU-211 and NPS 150."

Journal • Retrospective data • Review • CNS Disorders • Vascular Neurology

Neuroprotective and neuroregenerative drugs after severe traumatic brain injury : A narrative review from a clinical perspective. (PubMed, Wien Klin Wochenschr) - "Some pharmacologic attempts that appeared very promising in experimental settings have had disappointing clinical results (progesterone, cyclosporine A, ronopterin, erythropoietin, dexanabinol)...Some medications appear to be beneficial: N‑methyl-D-aspartate receptor (NMDA) antagonists (esketamine, amantadine, Mg++) reduce excitotoxicity and statins and cerebrolysin are known to counteract neuroinflammation. By supporting the impaired mitochondrial energy supply, oxidative processes are inhibited and neuroregenerative processes, such as neurogenesis, angiogenesis and synaptogenesis are promoted by citicoline and cerebrolysin. First clinical evidence shows an improvement in cognitive and thymopsychic outcomes, underlined by own clinical experience combining different therapeutic approaches. Accordingly, adjuvant treatment with neuroprotective substances appears to be a promising option, although more randomized prospective studies are still needed."

Journal • Review • CNS Disorders • Critical care • Inflammation • Vascular Neurology

Effect of drug therapy on nerve repair of moderate-severe traumatic brain injury: A network meta-analysis. (PubMed, Front Pharmacol) - " We included 30 randomized controlled trials that included 13 interventions (TXA, EPO, progesterone, progesterone + vitamin D, atorvastatin, beta-blocker therapy, Bradycor, Enoxaparin, Tracoprodi, dexanabinol, selenium, simvastatin, and placebo). Among these, the progesterone + vitamin D had not only a higher proportion of patients with good recovery and moderate disability but also a lower proportion of patients with severe disability and mortality. However, whether this intervention can be used for clinical promotion still needs further exploration."

Retrospective data • Review • CNS Disorders • Vascular Neurology

Identifying Drug Candidates for Pancreatic Neuroendocrine Tumors Based on Differently Expressed Genes (IHPBA 2022) - "Drug candidates targeted against pNET were identified based on differentially expressed genes. Available genetic atlas data may help identify agents with therapeutic efficacy to treat pNET patients using a more targeted approach."

Endocrine Cancer • Graft versus Host Disease • Immunology • Infectious Disease • Neuroendocrine Tumor • Oncology • Pancreatic Cancer • Pertussis • Respiratory Diseases • Solid Tumor • CCL20 • CXCL8 • GNG4 • LEP • LEPR

Oral fluid analysis to monitor recent exposure to synthetic cannabinoids in a high-risk subpopulation. (PubMed, J Forensic Sci) - "Results proved the presence of synthetic cannabinoids at a positivity rate of almost 20%, with detection frequency HU211(5/13) > UR144/JWH122 (3/13) > JWH019/JWH081/AM2201 (1/13). The identified SCRA proved the persistence into the market of the "first-generation" JWH family into the Italian territory and the marketing of relatively new ones (AM-2201). Public health consequences represented by NPS consumption are still scarce; therefore, further studies are needed to understand the real diffusion in the population."

Journal

Predicting Novel Drug Candidates for Pancreatic Neuroendocrine Tumors via Gene Signature Comparison and Connectivity Mapping. (PubMed, J Gastrointest Surg) - "Using available genetic atlas data, potential drug candidates for treatment of pNETs were identified based on differentially expressed genes. These results may help focus efforts on identifying targeted agents with therapeutic efficacy to treat patients with pNETs."

Journal • Endocrine Cancer • Graft versus Host Disease • Immunology • Infectious Disease • Neuroendocrine Tumor • Oncology • Pancreatic Cancer • Pertussis • Respiratory Diseases • Solid Tumor • CCL20 • CXCL8 • GNG4 • LEP • LEPR

Directive clinique n 425a : Le cannabis aux différentes périodes de la vie des femmes - Partie 1 : Fertilité, contraception, ménopause et douleur pelvienne. (PubMed, J Obstet Gynaecol Can) - "Les termes de recherche ont été définis à l'aide des termes MeSH (Medical Subject Headings) et mots clés (et variantes) suivants : cannabis, cannabinoids, marijuana, dexanabinol, dronabinol et tetrahydrocannabinol. PROFESSIONNELS CONCERNéS: Tous les fournisseurs de soins de santé qui prodiguent des soins aux femmes. DÉCLARATIONS SOMMAIRES: RECOMMANDATIONS."

Clinical guideline • Endometriosis • Gynecology • Infertility • Interstitial Cystitis • Musculoskeletal Pain • Pain • Women's Health

Guideline No. 425a: Cannabis Use Throughout Women's Lifespans - Part 1: Fertility, Contraception, Menopause, and Pelvic Pain. (PubMed, J Obstet Gynaecol Can) - "RECOMMENDATIONS."

Clinical guideline • Endometriosis • Gynecology • Infertility • Interstitial Cystitis • Mood Disorders • Musculoskeletal Pain • Pain • Sexual Disorders • Substance Abuse • Women's Health

Deficiency of autism-related Scn2a gene in mice disrupts sleep patterns and circadian rhythms. (PubMed, Neurobiol Dis) - "Performing a transcriptome-based compound discovery, we identified dexanabinol (HU-211), a putative glutamate receptor modulator, that can partially reverse the sleep disturbance in mice. Overall, our study reveals possible molecular and cellular mechanisms underlying Scn2a deficiency-related sleep disturbances, which may inform the development of potential pharmacogenetic interventions for the affected individuals."

Journal • Preclinical • Autism Spectrum Disorder • CNS Disorders • Developmental Disorders • Genetic Disorders • Psychiatry • Sleep Disorder • PER1 • PER2

Systems Pharmacology Modeling Identifies a Novel Treatment Strategy for Bortezomib-Induced Neuropathic Pain. (PubMed, Front Pharmacol) - "Dexanabinol failed to restore bortezomib-induced decreases in electrophysiological endpoints in rats, and it did not compromise bortezomib anti-cancer effects in U266 multiple myeloma cells and a murine xenograft model. Owing to its favorable safety profile in humans and preclinical efficacy, dexanabinol might represent a treatment option for bortezomib-induced neuropathic pain."

Journal • Hematological Malignancies • Multiple Myeloma • Neuralgia • Oncology • Pain • Peripheral Neuropathic Pain • TNFA

Analysis of long non-coding RNA expression profiles in disuse osteoporosis using microarray and bioinformatics. (PubMed, J Biol Regul Homeost Agents) - "Three bioactive compounds (scoulerine, kinetin riboside, dexanabinol) with potential therapeutic significance for DOP were obtained through the Connectivity Map (CMAP) analysis. Our study revealed a new mechanism for a lineage shift of bone marrow mesenchymal stem cells under microgravity, and linked the function of protein-coding mRNAs with ncRNAs, which may contribute to the development of new therapies for DOP."

Journal • CNS Disorders • Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology

Phase I dose-escalation, safety, and CNS pharmacokinetic study of dexanabinol in patients with brain cancer. (PubMed, Neurooncol Adv) - "Five of 24 efficacy-evaluable patients (21%) experienced stable disease with a median duration of 2 cycles (28-day cycle) as the best response. Dexanabinol administered weekly by intravenous infusion was safe and well-tolerated up to 28 mg/kg in brain cancer patients, but has limited antitumor activity in patients with brain cancer."

Clinical • Journal • P1 data • PK/PD data • Fatigue • Immunology • Oncology • Pruritus • Solid Tumor

Effects of cannabinoids on the development of chick embryos in ovo. (PubMed, Sci Rep) - "We have examined the effects of the synthetic cannabinoids HU 210 and HU 211, the plant-derived cannabidiol and the endogenous cannabinoid anandamide on the viability and development of chick embryos...This study shows that exposure to plant-derived or synthetic cannabinoids during early embryonal development decreases embryonal viability. Extrapolation of data across species is of course difficult, but the data would argue against the use of cannabinoids, be it recreationally or therapeutically, during pregnancy."

Journal

Solid lipid nanoparticles loading with curcumin and dexanabinol to treat major depressive disorder. (PubMed, Neural Regen Res) - "This study was approved by the Institutional Ethics Committee of Tongji Hospital of Tongji University, China (approval No. 2017-DW-020) on May 24, 2017."

Journal • CNS Disorders • Depression • Mood Disorders • Psychiatry • EGR1

Dexanabinol in Patients With Brain Cancer (clinicaltrials.gov) - P1; N=60; Active, not recruiting; Sponsor: Santosh Kesari, M.D., Ph.D.; Recruiting ➔ Active, not recruiting

Enrollment closed • Biosimilar • Oncology

A Phase 1 Study of Dexanabinol in Patients With Advanced Solid Tumours (clinicaltrials.gov) - P1; N=45; Recruiting; Sponsor: e-Therapeutics PLC; Trial primary completion date: Oct 2014 ->Jun 2015

Trial primary completion date • Biosimilar • Immunology • Inflammation • Oncology

Dexanabinol in Patients With Brain Cancer (clinicaltrials.gov) - P1; N=26; Completed; Sponsor: Santosh Kesari, M.D., Ph.D.; Active, not recruiting ➔ Completed

Trial completion • Biosimilar • Oncology • Solid Tumor