Nintedanib esylate Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Nintedanib esylate is a potent, oral triple angiokinase inhibitor developed by Boehringer Ingelheim that targets proangiogenic and pro-fibrotic pathways mediated by the vascular endothelial growth factor receptor, fibroblast growth factor receptor and plateletderived growth factor receptor families, as well as Src and Flt-3 kinases. It was approved for the treatment of idiopathic pulmonary fibrosis (IPF), a condition in which the lungs become progressively scarred over time, by the US FDA in October 2014 and by the EMA in January 2015. The FDA granted nintedanib esylate fast-track, priority review, orphan product, and breakthrough designations. The drug was also approved by the EMA in November 2014 for treatment of non-small cell lung cancer in combination with docetaxel after first-line chemotherapy.

Chemische Eigenschaften

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.

Verwenden

Nintedanib Esylate is the salt form of Nintedanib, which is angiokinase inhibitor and is used in the treatment of idiopathic pulmonary fibrosis. Also inhibits the process blood vessel formation which may be used to assist in cancer therapy.

Definition

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.

Properties and Applications

Nintedanib esylate (NE) is used in the treatment of idiopathic pulmonary fibrosis (IPF) and in diverse cancers, including nonsmall cell lung cancer (NSCLC). NE has a pH-dependent solubility profile with low aqueous solubility under neutral pH and increased solubility at acidic pH. The oral bioavailability of NE is 4.7% because it is a P-gp substrate and also undergoes first-pass metabolism in the liver by esterases. However, the administration of NE along with food increases the area under the curve (AUC) and maximum concentration (Cmax) when the drug is taken with food; hence, it has a positive food effect[1].

Nintedanib esylate Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte

Nintedanib esylate Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Firmenname	Telefon	E-Mail	Land	Produktkatalog	Edge Rate
Cangzhou Kangrui Pharma Tech Co. Ltd.,	+86-18632776803 +86-13833998158	cangzhoukangrui@126.com	China	733	58
Hebei Yanxi Chemical Co., Ltd.	+8617531190177	peter@yan-xi.com	China	5858	58
HangZhou RunYan Pharma Technology Co.,LTD.	+8618882027439	sales2@runyanpharma.com	China	302	58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.	+86-18600796368 +86-18600796368	sales@sjar-tech.com	China	375	58
Shanghai Daken Advanced Materials Co.,Ltd	+86-371-66670886	info@dakenam.com	China	18648	58
Beijing Cooperate Pharmaceutical Co.,Ltd	010-60279497	sales01@cooperate-pharm.com	CHINA	1803	55
Shanghai Bojing Chemical Co.,Ltd.	+86-86-02137122233 +8613795318958	bj1@bj-chem.com	China	299	55
Henan Tianfu Chemical Co.,Ltd.	+86-0371-55170693 +86-19937530512	info@tianfuchem.com	China	21639	55
Hangzhou FandaChem Co.,Ltd.	008657128800458; +8615858145714	fandachem@gmail.com	China	9218	55
Nanjing ChemLin Chemical Industry Co., Ltd.	025-83697070	product@chemlin.com.cn	CHINA	3009	60

656247-18-6()Verwandte Suche:

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• (3Z)-2,3-Dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-1H-indole-6-carboxylic acid methyl ester ethanesulfonate
• BIBF 1120 esylate
• BIBF-1120 esylate
• BIBF1120/nintedanib ethanesulfonate salt
• Trinidad Neeb esylate
• Intedanib ethanesulfonate
• Nintedanib ethanesulfonate salt
• Trinidad Neeb ethanesulfonate
• Nintedanib(ethanesulfonic acid)
• BIBF1120 ethanesulfonate salt
• (Z)-Methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene
• 1H-Indole-6-carboxylic acid,2,3-dihydro-3-[[[4-[methyl[(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]-phenylmethylene]-2-oxo-, methylester, (3Z)-, ethanesulfonate (1:1)
• 1H-Indole-6-carboxylic acid, 2,3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-, methyl ester, (3Z)-, ethanesulfonate (1:1)
• Nintedanib (Ofev)
• (Z)-methyl 3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate
• BIBF 1120 BIBF-1120
• BIBF1120; BIBF 1120 BIBF-1120; NINTEDANIB ESYLATE. NINTEDANIB ETHANESULFONATE SALT; INTEDANIB; BRAND NAME OFEV. VARGATEF.
• Brand name OFEV. Vargatef.
• Nintedanib esylate. Nintedanib ethanesulfonate salt
• Nintedanib Ethanesulfonate (Intedanib Ethanesulfonate)
• Nintedani
• NSC 116056
• Nintedanib ethanesulfonate
• Nintedanib esylate
• 6-Benzofuranpropanenitrile,β-oxo-
• methyl (Z)-3-(((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)(phenyl)methylene)-2-oxoindoline-6-carboxylate ethanesulfonate
• Intedanib|||BIBF 1120 (esylate)|||Nintedanib Ethanesulfonate Salt|||BIBF 1120
• Buprenorphine Impurity 24
• 656247-18-6
• 1217052-38-5
• C31H33N5O4C2H6O3S
• C33H39N5O7S
• API