Roblitinib

Roblitinib (FGF-401) is an orally active and highly selective FGFR4 inhibitor with an IC₅₀ of 1.9 nM^[1]. Roblitinib has antitumor activity^[2]. IC50 & Target: IC50: 1.9 nM (FGFR4)^[1] In Vitro: Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor (IC₅₀= 1.9 nM)^[1].
Roblitinib shows no activity FGFR1, FGFR2, FGFR3, rat FGFR4, C552A FGFR4 (all IC₅₀>10 uM)^[1].
Roblitinib inhibits HUH7 (IC₅₀=12 nM), Hep3B (IC₅₀=9 nM), JHH7 (IC₅₀=9 nM), HEPG2 (IC₅₀>10 uM), JHH (IC₅₀>10 uM)^[1].
In Vivo: Roblitinib (gavage; 10-100 mg/kg; b.i.d.; for 10 days) with the 30 mg/kg has the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model^[1].
Roblitinib causes blood concentrations dropped below the IC90 threshold level within 8 h of dosing, and controlles tumor growth to the level of stasis at the lowest dose of 10 mg/kg for 6 days^[1].
Roblitinib (iv at 1 mg/kg; po at 3 mg/kg) has a T_1/2 of 1.4 hours, a CL of 28 mL/min kg, and a V_ss of 2.3 L/kg for Male mice (C57BL/6) ^[1].
Roblitinib (iv at 0.5 mg/kg; po at 3 mg/kg) has a T_1/2 of 4.4 hours, a CL of 19 mL/min kg, and a V_ss of 3.9 L/kg for male SD rats^[1].