Nintedanib esylate RC02685

Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Nintedanib esylate is an organosulfonate salt obtained by combining nintedanib with one molar equivalent of ethanesulfonic acid. A kinase inhibitor used for the treatment of idiopathic pulmonary fibrosis and cancer. It has a role as an angiogenesis inhibitor, an antineoplastic agent, a fibroblast growth factor receptor antagonist, a tyrosine kinase inhibitor and a vascular endothelial growth factor receptor antagonist. It contains a nintedanib(1+).|Nintedanib Esylate is the esylate salt form of nintedanib, an orally bioavailable, indolinone-derived inhibitor of multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs), with potential antiangiogenic, antifibrotic and antineoplastic activities. Upon administration, nintedanib selectively binds to and inhibits vascular endothelial growth factor receptor (VEGFR), fibroblast growth factor receptor (FGFR), platelet-derived growth factor receptor (PDGFR), and colony stimulating factor 1 receptor (CSF1R) tyrosine kinases, which may result in the induction of endothelial cell apoptosis, the reduction in tumor vasculature, the inhibition of tumor cell proliferation and migration, and antifibrotic activity in pulmonary fibrosis. In addition, nintedanib also binds to and inhibits members of the Src family of tyrosine kinases, including Src, Lck and Lyn, and fms-like tyrosine kinase 3 (FLT-3). VEGFR, FGFR, PDGFR and CSF1R RTKs play key roles in tumor angiogenesis, tumor cell proliferation and metastasis, as well as pulmonary fibrosis.
Nintedanib esilate is a bright yellow powder. The octanol-water partition coefficient (log Pow) for the nintedanib esilate-free base was determined to be 3.6, demonstrating the molecule's lipophilic character. Due to the ionisable groups in nintedanib esilate, the lipophilicity profile is strongly pH-dependent. At physiological pH (pH = 7.4), the apparent partition coefficient (log D) was calculated to be 3.0. The molecule is less lipophilic in the acidic pH range (log D ≤ 1 for pH < 5). Nintedanib esilate is soluble in water. A saturated solution in water was found to have a concentration of 2.8 mg/mL and exhibited an intrinsic pH of 5.7. The solubility of nintedanib esilate is strongly pH dependent, with an increased solubility at acidic pH, particularly for pH < 3. The highest solubility of nintedanib esilate in organic solvents is observed in methanol and N-methylpyrrolidone. The best solubility in pharmaceutically relevant co-solvents is observed in propylene glycol. OFEV are soft gelatin capsules containing 100 mg or 150 mg nintedanib (as nintedanib esilate) for oral administration. Excipients: Each OFEV capsule contains medium-chain triglycerides, hard fat and lecithin.
ChEBI: An organosulfonate salt obtained by combining nintedanib with one molar equivalent of ethanesulfonic acid. A kinase inhibitor used for the treatment of idiopathic pulmonary fibrosis and cancer.