Delving into the Latest Updates on Dexanabinol with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Dexanabinone, Sinnabidol

+ [4]

Target

NMDA receptor

Mechanism

NMDA receptor antagonists(Glutamate [NMDA] receptor antagonists)

Therapeutic Areas

Nervous System DiseasesOther Diseases

Active Indication

Brain Injuries, Traumatic

Inactive Indication

Advanced cancerAdvanced Malignant Solid NeoplasmBrain Cancer+ [5]

Originator Organization

e-Therapeutics Plc

Active Organization

Erasmus MC

Inactive Organization

e-Therapeutics PlcPHARMOS, a.s.

W World Corp.

Drug Highest PhasePhase 3

First Approval Date-

RegulationOrphan Drug (US)

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Structure

Molecular FormulaC25H38O3

InChIKeySSQJFGMEZBFMNV-PMACEKPBSA-N

CAS Registry112924-45-5

This study is a trial of dexanabinol in patients with advanced tumours. The purposes of the protocol are to study different doses of the study drug to determine the maximum safe dose of the drug given in combination with standard chemotherapies and to further understand the safety of the study drug and to measure any reduction in size of patients' cancer tumour(s).
Dexanabinol is a synthetic cannabinoid which has previously undergone clinical trials for traumatic brain injury (TBI) and in subjects undergoing coronary artery bypass surgery. Currently dexanabinol is under investigation for potential anti-tumour activity in patients with advanced tumours.

Start Date01 Apr 2015

Sponsor / Collaborator

e-Therapeutics Plc

NCT02054754 / CompletedPhase 1

Assessment of Safety, Tolerability and Pharmacokinetics of Single Doses of Oral Dexanabinol in Healthy Subjects

The purpose of this study is to test the safety and observe the pharmacokinetics (distribution and elimination of the drug) of the compound dexanabinol (ETS2101) in healthy male subjects following a single oral dose.

Start Date01 Jan 2014

Sponsor / Collaborator

e-Therapeutics Plc

NCT01654497 / CompletedPhase 1IIT

A Phase I, Sequential Cohort, Open-Label, Dose-escalation Study of the Safety and CNS Pharmacokinetics of Dexanabinol in Patients With Brain Cancer

The purpose of this study is to try to determine the maximum safe dose of dexanabinol that can be administered to people with brain cancer. Other purposes of this study are to:
find out what effects (good and bad) dexanabinol has;
see how much drug gets into the body by collecting blood and cerebrospinal fluid for use in pharmacokinetic (PK) studies;
learn more about how dexanabinol might affect the growth of cancer cells;
look at biomarkers (biochemical features that can be used to measure the progress of disease or the effects of a drug).

Start Date01 Jun 2012

Sponsor / Collaborator

University of California San Diego

[+1]

100 Clinical Results associated with Dexanabinol

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100 Translational Medicine associated with Dexanabinol

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100 Patents (Medical) associated with Dexanabinol

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94

Literatures (Medical) associated with Dexanabinol

01 Sep 2022·Journal of Forensic Sciences

Oral fluid analysis to monitor recent exposure to synthetic cannabinoids in a high‐risk subpopulation

Article

Author: Cecchi, Rossana ; Dagoli, Sara ; Pascali, Jennifer P. ; Antonioni, Maina ; Anzillotti, Luca ; Affini, Giuseppe Fertonato ; Facetti, Olivia ; Cantarelli, Barbara ; Calò, Luca

AbstractAmong novel psychoactive substances, synthetic cannabinoid receptor agonists (SCRA) seem to have the widest diffusion in the population with no limitation to any particular demographic group. Information on drug consumption relies mostly on anonymized surveys and less on clinical or analytical data; notwithstanding, the huge efforts constantly made to enroll subjects to gather epidemiological data. In the present study, we collected 66 oral fluid samples from volunteers in a drug rehabilitation center in 2019 and early 2020. A liquid chromatography–mass spectrometry method previously developed and validated by our Unit was applied to detect SCRA (n = 10) in oral fluid. 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). Concentrations were in the range < LOQ −0.36 ng/ml. Synthetic cannabinoids consumption had not been declared by any volunteer. This study enabled for the unprecedent detection of synthetic cannabinoids use in the territory of Parma (Italy) in a high‐risk subpopulation. 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.

01 Aug 2022·Journal of Gastrointestinal SurgeryQ3 · MEDICINE

Predicting Novel Drug Candidates for Pancreatic Neuroendocrine Tumors via Gene Signature Comparison and Connectivity Mapping

Q3 · MEDICINE

Article

Author: Du, Shunda ; Cloyd, Jordan M ; Mao, Yilei ; Xu, Gang ; Pawlik, Timothy M ; Xiao, Yao

INTRODUCTIONThere is a paucity of effective treatment options for advanced pancreatic neuroendocrine tumors (pNETs). Genome-wide analyses may allow for potential drugs to be identified based on differentially expressed genes (DEGs).METHODSOligo microarray data of RNA expression profiling of pNETs and normal pancreas tissues were downloaded from the Gene Expression Omnibus. Functional and pathway enrichment information of the DEGs was obtained using the Gene Ontology and Kyoto Encyclopedia of Genes and Genomes databases. Corresponding homologous proteins were analyzed and potential therapeutic drugs for pNETs were identified using the Connectivity Map and Drug-Gene Interaction Database.RESULTSAssessment of raw data from 12,610 pNET genes demonstrated that 1082 and 380 genes were upregulated and downregulated, respectively, compared with normal pancreas tissue. Upregulated pathways were associated with nitrogen metabolism (i.e., GABAergic synapse, and graft-versus-host disease), whereas downregulated pathways included C-type leptin receptor signaling pathway, pertussis and AMPK signaling pathway. In particular, the protein-protein interaction analysis revealed 10 upregulated hub genes (DYNLL1, GNB5, GNB2, GNG4, GNAI2, GNAI1, HIST2H2BE, NUP107, NUP133, and SNAP25) and 10 downregulated hub genes (CXCL8, F2, CXCL2, GCG, SST, INS, GALR3, CCL20, ADRA2B, and CXCL6). Using the Drug-Gene Interaction Database, candidate drugs for pNETs treatment included 3 EGFR inhibitors (canertinib, erlotinib, WZ-4-145), as well as other cell-signaling pathway inhibitors such as AG-592, acarbose, lonidamine, azacytidine, rottlerin, and HU-211.CONCLUSIONUsing 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.

01 Apr 2022·Journal of Obstetrics and Gynaecology Canada

Guideline No. 425a: Cannabis Use Throughout Women’s Lifespans – Part 1: Fertility, Contraception, Menopause, and Pelvic Pain

Review

Author: Tanguay, Robert L ; Gabrys, Robert L ; Graves, Lisa E ; Allen, Victoria M ; Robert, Magali ; Turner, Suzanne D ; Dama, Sumeet ; Cook, Jocelynn L ; Green, Courtney R

OBJECTIVETo provide health care providers with the best evidence on cannabis use with respect to women's health. Areas of focus include general patterns of cannabis use as well as safety of use; care for women who use cannabis; stigma; screening, brief intervention, and referral to treatment; impact on hormonal regulation; reproductive health, including contraception and fertility; sexual function; effects on perimenopausal and menopausal symptoms; and use in chronic pelvic pain syndromes.TARGET POPULATIONThe target population includes all women currently using or contemplating using cannabis.OUTCOMESOpen, evidence-informed dialogue about cannabis use, which will lead to improvement in patient care.BENEFITS, HARMS, AND COSTSExploring cannabis use through a trauma-informed approach provides the health care provider and patient with an opportunity to build a strong, collaborative, therapeutic alliance. This alliance empowers women to make informed choices about their own care. It also allows for the diagnosis and possible treatment of cannabis use disorders. Use should not be stigmatized, as stigma leads to poor "partnered care" (i.e., the partnership between the patient and care provider). Multiple side effects of cannabis use may be mistaken for other disorders. Currently, use of cannabis to treat women's health issues is not covered by public funding; as a result, individual users must pay the direct cost. The indirect costs of cannabis use are unknown. Thus, health care providers and patients must understand the role of cannabis in women's health issues, so that women can make knowledgeable decisions.EVIDENCEPubMed, EMBASE, and grey literature were searched to identify studies of "cannabis use and effect on infertility, contraception, perimenopause and menopausal symptoms, and pelvic pain" published between January 1, 2018 and February 18, 2021. All clinical trials, observational studies, reviews (including systematic reviews and meta-analyses), guidelines, and conference consensus statements were included. Publications were screened for relevance. The search terms were developed using the Medical Subject Headings (MeSH) terms and keywords (and variants), including cannabis, cannabinoids, marijuana, dexanabinol, dronabinol, tetrahydrocannabinol; the specific terms to capture women's health were estrogen, estradiol, medroxyprogesterone acetate, vaginal contraception, oral contraceptives, fertilization, amenorrhea, oligomenorrhea, pelvic pain, dysmenorrhea, endometriosis, interstitial cystitis, vulvodynia, and menopause.VALIDATION METHODSThe authors rated the quality of evidence and strength of recommendations using the Grading of Recommendations Assessment, Development and Evaluation (GRADE) approach. See online Appendix A (Tables A1 for definitions and A2 for interpretations of strong and weak recommendations).INTENDED AUDIENCEAll heath care providers who care for women.SUMMARY STATEMENTSRECOMMENDATIONS.

100 Deals associated with Dexanabinol

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Dexanabinol	-	DB06444

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Brain Injuries	Phase 3	-	e-Therapeutics Plc	-
Cognitive Dysfunction	Phase 3	-	e-Therapeutics Plc	-
Cognitive Dysfunction	Phase 3	IL	W World Corp.	-
Advanced cancer	Discovery	PL	e-Therapeutics Plc	01 Apr 2015
Advanced cancer	Discovery	ES	e-Therapeutics Plc	01 Apr 2015
Advanced cancer	Discovery	GB	e-Therapeutics Plc	01 Apr 2015
Brain Cancer	Discovery	US	e-Therapeutics Plc	01 Jun 2012
Advanced Malignant Solid Neoplasm	Discovery	GB	e-Therapeutics Plc	01 Jan 2012
Brain Injuries, Traumatic	Discovery	-	PHARMOS, a.s.	01 Jan 2001
Brain Injuries, Traumatic	Discovery	-	W World Corp.	01 Jan 2001

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01654497 (Pubmed) Manual	Phase 1	Brain Cancer	26	Dexanabinol	(sknkelhorl) = pesyedpmiz yfgkqnrdul (drimfovdmv ) View more	Positive	15 Feb 2021
NCT01489826 (CTgov)	Phase 1	Advanced Malignant Solid Neoplasm	40	Cremophor+Dexanabinol (Dexanabinol 2 mg/kg)	qvnnfpxzvt(vqepuekigo) = gilbrjmigg xfvroymycp (pwoyexiskg, lspkdyjbju - qrjbksqssb) View more	-	18 Oct 2016
NCT01489826 (CTgov)	Phase 1	Advanced Malignant Solid Neoplasm	40	Cremophor+Dexanabinol (Dexanabinol 3 mg/kg)	qvnnfpxzvt(vqepuekigo) = fhznpdrbti xfvroymycp (pwoyexiskg, njzeegtfpr - jkpkgobgta) View more	-	18 Oct 2016