更新于：2024-11-01

Artelo Biosciences Ltd.

子公司|

United Kingdom

子公司|

United Kingdom

更新于：2024-11-01

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项与 Artelo Biosciences Ltd. 相关的临床试验

EUCTR2020-000464-27-NO / Unknown status临床1/2期

A Phase 1/2 Trial of the Synthetic Cannabinoid ART27.13 in Patients with Cancer Anorexia and Weight Loss - ART27.13 in Patients with Cancer Anorexia and Weight Loss

开始日期2023-10-03

申办/合作机构

Artelo Biosciences Ltd.

100 项与 Artelo Biosciences Ltd. 相关的临床结果

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0 项与 Artelo Biosciences Ltd. 相关的专利（医药）

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项与 Artelo Biosciences Ltd. 相关的文献（医药）

2024-10-01·Toxicology and Applied Pharmacology

Potential safety implications of fatty acid-binding protein inhibition

Review

作者: Yates, Andrew ; O'Sullivan, Saoirse E ; Warren, William G ; Duffy, Paul ; Warren, William G. ; Osborn, Myles ; O'Sullivan, Saoirse E.

Fatty acid-binding proteins (FABPs) are small intracellular proteins that regulate fatty acid metabolism, transport, and signalling. There are ten known human isoforms, many of which are upregulated and involved in clinical pathologies. As such, FABP inhibition may be beneficial in disease states such as cancer, and those involving the cardiovascular system, metabolism, immunity, and cognition. Recently, a potent, selective FABP5 inhibitor (ART26.12), with 90-fold selectivity to FABP3 and 20-fold selectivity to FABP7, was found to be remarkably benign, with a no-observed-adverse-effect level of 1000 mg/kg in rats and dogs, showing no genotoxicity, cardiovascular, central, or respiratory toxicity. To understand the potential implication of FABP inhibition more fully, this review systematically assessed literature investigating genetic knockout, knockdown, and pharmacological inhibition of FABP3, FABP4, FABP5, or FABP7. Analysis of the literature revealed that animals bred not to express FABPs showed the most biological effects, suggesting key roles of these proteins during development. FABP ablation sometimes exacerbated symptoms of disease models, particularly those linked to metabolism, inflammatory and immune responses, cardiac contractility, neurogenesis, and cognition. However, FABP inhibition (genetic silencing or pharmacological) had a positive effect in many more disease conditions. Several polymorphisms of each FABP gene have also been linked to pathological conditions, but it was unclear how several polymorphisms affected protein function. Overall, analysis of the literature to date suggests that pharmacological inhibition of FABPs in adults is of low risk.

European Journal of Pain

ART26.12, a novel fatty acid‐binding protein 5 inhibitor, shows efficacy in multiple preclinical neuropathy models

Article

作者: Xue, Wenwen ; Osborn, M. ; OSullivan, S. E. ; Yates, A. ; Warren, W. G. ; Tsantoulas, C. ; David‐Pereira, A.

AbstractBackgroundPainful neuropathy is a pathological condition caused by numerous factors including diabetes, chemotherapy or cancer. ART26.12 is a novel fatty acid‐binding protein 5 inhibitor, which our group showed could prevent and treat persistent pain in a preclinical model of oxaliplatin‐induced peripheral neuropathy.MethodsIn the current study, the efficacy of orally dosed ART26.12 was tested in multiple neuropathy models of different aetiology. Paw withdrawal threshold to von Frey monofilaments and latency to escape a cold plate were used as measurements of mechanical and cold sensitivity.ResultsART26.12 (25 and 50 mg/kg BID), dosed prior to the induction of paclitaxel‐induced peripheral neuropathy (PIPN), reversed mechanical allodynia induced by paclitaxel in both male and female rats, and ART26.12 (50 mg/kg BID) prevented the induction of PIPN in female rats. ART26.12 (50 mg/kg BID) also had a protective effect on body weight in the PIPN model. ART26.12 (25 and 100 mg/kg BID) reversed mechanical allodynia when treating established streptozotocin‐induced diabetic neuropathy in male rats. In a model of breast cancer‐induced bone pain in female rats, ART26.12 (100 mg/kg BID) reversed mechanical allodynia within 1 h of dosing. In the same model, ART26.12 (25 mg/kg BID) reversed mechanical allodynia from day 4 of treatment.ConclusionOverall, these preclinical data suggest that ART26.12 is a safe and efficacious therapeutic drug for continued development towards the prevention and treatment of peripheral neuropathy.Significance StatementThis work now shows that ART26.12, a novel and selective inhibitor of FABP5, can prevent and treat multiple preclinical models of peripheral neuropathy. Given its excellent safety profile, further work is warranted to develop ART26.12 as a potential therapeutic tool for pain management.

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100 项与 Artelo Biosciences Ltd. 相关的转化医学

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