| Hazard Information | Back Directory | [Description]
GDC0276, also known as RG7893, is a selective, reversible, orally bioavailable small-molecule sodium channel blocker that is selective for Nav1.7, which is expressed primarily on peripheral nociceptor C-fiber neurons and is required for pain sensing in humans. | [Uses]
GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects[1]. | [in vivo]
GDC-0276 (oral adminstration; 0.5-5 mg/kg) shows enrichment of 14C with observed specific activities of 22.6 μCi/mg. GDC-0276 is not detected in urine; however, metabolites in urine were enriched in 14C with observed specific activities of 19.6 μCi/mg[3]. | Animal Model: | Six drug-na?ve beagle dogs Group 1 four dogs (n=2 per sex) and Group 2 2 BDC dogs (n=2 male)[3] | | Dosage: | 0.5, 1, 2, 3, 4, 5 mg/kg | | Administration: | Oral adminstration | | Result: | Showed mean specific activities of 12.2 μCi/mg (a 24% enrichment) (n=4 animals) and 23.5 μCi/mg (a 139% enrichment) (n=2 animals) for Groups 1 and 2, respectively. |
| [IC 50]
Nav1.7 | [References]
[1] Rothenberg ME, et al. Safety, Tolerability, and Pharmacokinetics of GDC-0276, a Novel NaV1.7 Inhibitor, in a First-in-Human, Single- and Multiple-Dose Study i DOI:10.1007/s40261-019-00807-3
[2] Steven J. McKerrall, et al. Nav1.7 inhibitors for the treatment of chronic pain. Bioorganic & Medicinal Chemistry Letters (2018)
[3] Takahashi RH,et al.Unequal Absorption of Radiolabeled and Nonradiolabeled Drug from the Oral Dose Leads to Incorrect Estimates of Drug Absorption and Circulating Metabolites in a Mass Balance Study.Drug Metab Lett. 2019;13(1):37-44. DOI:10.2174/1872312813666181129162237 |
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