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ART26.12, a novel fatty acid-binding protein 5 inhibitor, shows efficacy in multiple preclinical neuropathy models
W G Warren1, M Osborn1, A David-Pereira2
1Artelo Biosciences Ltd., Alderley Park, Alderley Edge, Cheshire, UK.
Background:
Painful 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.
Methods:
In 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.
Results:
ART26.12 (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.
Conclusion:
Overall, 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 Statement:
This 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.
Insights
ART26.12, a fatty acid-binding protein 5 inhibitor, effectively prevents and treats peripheral neuropathy in preclinical models. This novel therapeutic shows promise for managing neuropathic pain with a favorable safety profile.
Area of Science:
- Neuroscience
- Pharmacology
- Pain Research
Background:
- Peripheral neuropathy is a debilitating condition with diverse causes, including diabetes, chemotherapy, and cancer.
- Current treatments for neuropathic pain are limited, necessitating the development of novel therapeutic agents.
- Fatty acid-binding protein 5 (FABP5) is implicated in inflammatory pain pathways.
Purpose of the Study:
- To evaluate the efficacy of ART26.12, a novel FABP5 inhibitor, in preclinical models of peripheral neuropathy.
- To determine if ART26.12 can prevent and treat neuropathic pain across different etiologies.
- To assess the safety and therapeutic potential of ART26.12 for pain management.
Main Methods:
- ART26.12 was orally administered in multiple established preclinical models of peripheral neuropathy.
- Paclitaxel-induced peripheral neuropathy (PIPN) and streptozotocin-induced diabetic neuropathy models were utilized.
- Breast cancer-induced bone pain model was employed to assess pain reversal.
- Mechanical allodynia and cold sensitivity were measured using von Frey filaments and a cold plate test, respectively.
Main Results:
- ART26.12 reversed mechanical allodynia in paclitaxel-induced peripheral neuropathy models in male and female rats.
- ART26.12 demonstrated preventative effects against PIPN induction in female rats and protected body weight.
- The compound reversed mechanical allodynia in established diabetic neuropathy and cancer-induced bone pain models.
- ART26.12 showed rapid and sustained reversal of mechanical allodynia in cancer pain models.
Conclusions:
- ART26.12 demonstrates significant efficacy in preventing and treating various preclinical models of peripheral neuropathy.
- The compound exhibits a favorable safety profile, supporting its continued development.
- ART26.12 represents a promising therapeutic candidate for managing neuropathic pain and improving patient outcomes.
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