Table 2.
Potential therapeutic utility of peripherally restricted compounds targeting the CB1 receptor directly or indirectly.
| Peripherally Restricted CB1 Antagonists |
Peripherally Restricted CB1 Agonists | Peripherally Restricted FAAH Inhibitors |
|
|---|---|---|---|
| Preclinical research | Obesity [81,82,83,86] Type 2 diabetes [85,105] Prader–Willi syndrome [88] Chronic kidney disease [101] Diabetic nephropathy [93] Alcoholic liver steatosis [94] Alcoholism [99,100] Non-alcoholic liver steatosis [96] Obesity-related liver steatosis [95] Liver fibrosis [102] Pulmonary fibrogenesis [97,98] Skin fibrosis [103] |
Inflammatory pain [106,107] Neuropathic pain [107,108] Bone cancer pain [109] Chemotherapy-induced pain [110] Migraine and medication overuse headache [111] Spasticity in multiple sclerosis [112] Gastrointestinal motility in colitis [42,43] Anticipatory nausea [113] Cardiac disease [114] |
Neuropathic pain [115] Chemotherapy-induced neuropathy [116] Inflammatory pain [115,117,118] Diabetic neuropathy [119] Visceral pain [115] Migraine [120,121] Anticipatory nausea [113] Cystitis [122] Bladder overactivity [123] Gastric lesions [118] |
| Clinical research | INV-101 in Prader–Willi syndrome (PWS) and non-alcoholic steatohepatitis (NCT04531150) (Inversago Pharma) TM38837 in healthy subjects [104] (7TM Pharma) GFB-024 in diabetic nephropathy (Goldfinch Bio, NCT04880291) |
AZD1940 in capsaicin-induced pain [124] and post-operative pain [125] ART27.13 (previously AZD1940) in Cancer anorexia (EudraCT NUMBER:2020-000464-27) (Artelo Biosciences) |
URB937 is in the early stages of clinical development (Exxel Pharma) |