In Vitro: BGB-8035 is nontoxicin HEK293 and Ramos cells (IC50 > 10 μM, both).
In Vivo: BGB-8035 (7.5, 15, 30 mg/kg; PO; twice daily; 16 days) demonstrates dose-dependent antitumor activity. BGB-8035 (1, 3, 10, 30 mg/kg; PO; BID; 13 days) inhibits arthritis as measured by clinical scores in a dose-dependent manner in the Lewis rats aged 8-9 weeks with CIA model and prevents the CIA model-associated body weight loss. Pharmacokinetic Parameters of BGB-8035 in Rats and Dogs.