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 T1/2 of 1.4 hours, a CL of 28 mL/min kg, and a Vss 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 T1/2 of 4.4 hours, a CL of 19 mL/min kg, and a Vss of 3.9 L/kg for male SD rats[1].
| Animal Model: | Male Wistar Hannover rats (Hep3B xenograft model)[1] |
| Dosage: | 10, 30, 100 mg/kg |
| Administration: | Gavage; for 10 days |
| Result: | Caused blood concentrations dropped below the IC90 threshold between 8 and 12 h following dosing.
Had the maximal level of inhibition of FGFR4-dependent tumor growth in the Hep3B xenograft model.
|
| Animal Model: | Male mice (C57BL/6)[1] |
| Dosage: | 1 mg/kg or 3 mg/kg (Pharmacokinetic Analysis) |
| Administration: | IV at 1 mg/kg; PO at 3 mg/kg |
| Result: | Had a T1/2 of 1.4 hours, a CL of 28 mL/minkg, and a Vss of 2.3 L/kg.
|
