BIBF1120 (Vargatef, Nintedanib) is an oxindole-based, orally-available triple kinase inhibitor targeting the angiogenesis factors VEGF, PDGF, and FGF. It inhibits VEGFR, PDGFR, and FGFR at potency ranges of 13-34, 59-65, and 37-108 nM. [1] Kinase panel studies show that it also inhibits Flt-3, Lck, Lyn, and Src at 26, 16, 195, and 156 nM, respectively. BIBF1120 also inhibits cell proliferation in MAPK and Akt signaling pathways at EC50s of 10-80 nM.

Continuous oral QD dosing of BIBF1120 displayed antitumor activity in a number of tumor cell lines (FaDu, Caki-1, HT-29, SKOV-3, Calu-6, PAC-120, and GS-9L.

BIBF-1120 is being explored as a treatment for idiopathic pulmonary fibrosis and has shown promise in the delay of lung fibrosis progression. [2]