VX-702

2 years -80 in solvent

Administered via p.o.

VX-702 is currently in Phase II clinical trial in patients with rheumatoid arthritis.

4 - 20 nM [1], 4 - 20 nM [1], 4 - 20 nM [1], 4 - 20 nM [1], 4 - 20 nM [1], 4 - 20 nM [1]

The half-life of VX-702 is 16 to 20 hours, with a median clearance of 3.75 L/h and a volume of distribution of 73 L/kg. Both AUC and Cmax values are dose proportional for VX-702, which is predominantly cleared renally. [2] VX-702 (at a dose of 0.1 mg/kg twice daily) has an equivalent effect as that of methotrexate (0.1 mg/kg). In addition, VX-702 (5 mg/kg twice daily) also has an equivalent effect as prednisolone (10 mg/kg once daily), as measured by percentage inhibition of wrist joint erosion and inflammation score. [3] VX-702 selectively inhibits activation of p38 MAPK after ischemia with no effects on ERKs and JNKs. The MI/AAR ratio is significantly reduced in the 50 mg/kg group compared with the 5 mg/kg and vehicle groups.[4]

VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β.

VX-702 is a highly selective, orally active inhibitor of p38 MAPK