BIBF 1202 is the carboxylate metabolite of BIBF 1120 which inhibits VEGFR2 kinase with an IC50 of 62 nM. IC50: 62 nM (VEGFR2)[1]
The major metabolic pathway for BIBF 1120 is methyl ester cleavage to BIBF 1202. Subsequently, the free carboxyl group of BIBF 1202 is glucuronidated to 1-O-acylglucuronide[2].
[1]. Hilberg F, et al. BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumorefficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. [2]. Stopfer P, et al. Pharmacokinetics and metabolism of BIBF 1120 after oral dosing to healthy male volunteers. Xenobiotica. 2011 Apr;41(4):297-311.