Bavdegalutamide (ARV-110) is an oral protein degrader that specifically binds to AR and mediates its degradation. Bavdegalutamide can degrade clinically relevant mutant AR proteins, maintain activity in a high androgen environment, and has an acceptable safety profile.

Bavdegalutamide (ARV-110) completely degrades AR in all cell lines tested, with an observed 50% degradation concentration (DC50) of < 1 nM. [3]

METHODS: The mean plasma concentration-time profiles of Bavdegalutamide (ARV-110) were measured in rats and mice after intravenous administration of Bavdegalutamide (2 mg/kg, intravenous injection) and (5 mg/kg, oral administration) using the developed LC-MS/MS method.
RESULTS: In rats, after intravenous injection of Bavdegalutamide, the calculated total clearance (CL) value was 413.6 ± 31.7 mL/h/kg, and the steady-state (VSS) value (5775 ± 320 mL/kg) indicated that ARV-110 was well distributed in tissues; after oral administration, the peak plasma concentration (Cmax) value was 110.5 ± 9.2 ng/mL, at 5.5 ± 1.9 hours, and the oral bioavailability of ARV-110 in rats was moderate (23.8%); after intravenous administration in mice, the CL value of ARV-110 was lower than the hepatic blood flow rate of mice (90 mL/min/kg), and Bavdegalutamide showed a relatively large VSS value (2366 ± 402.2 mL/kg), indicating that the drug was mainly confined to tissues; after oral administration, the Cmax value was 612.0 ± 88.38 ng/mL. [2]
METHODS: Bavdegalutamide (1 mg/kg, orally, once a day) was used to treat xenograft model mice, and the degree of AR degradation and tumor growth in the mice were observed.
RESULTS: With over 90% AR degradation in mice, Bavdegalutamide achieved significant inhibition of tumor growth and AR signaling in both intact and castrated conditions. [3]