Nintedanib esylate
- CAS No.
- 656247-18-6
- Chemical Name:
- Nintedanib esylate
- Synonyms
- Nintedanib esylate;Nintedanib ethanesulfonate;Nintedani;NSC 116056;BIBF-1120 esylate;BIBF 1120 esylate;Nintedanib (Ofev);BIBF 1120 BIBF-1120;Trinidad Neeb esylate;Intedanib ethanesulfonate
- CBNumber:
- CB02509952
- Molecular Formula:
- C33H39N5O7S
- Molecular Weight:
- 649.76
- MOL File:
- 656247-18-6.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/4/2 13:34:07
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P305+P351+P338 | |||||||||
| NFPA 704 |
|
Nintedanib esylate Chemical Properties,Uses,Production
Description
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.
Uses
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].
References
[1] Priyanshi Patel, Mitali Patel. “Enhanced oral bioavailability of nintedanib esylate with nanostructured lipid carriers by lymphatic targeting: In vitro, cell line and in vivo evaluation.” European Journal of Pharmaceutical Sciences 159 (2021): Article 105715.
[2] Veerareddy Arava, Surendrareddy Gogireddy. “An improved process for the synthesis of nintedanib esylate.” Synthetic Communications 47 10 (2017): Pages 975-981.
[3] Esylate, Nintedanib. “Nintedanib Esylate.” Definitions 10 1 (2020).
[4] Shabari Girinath Kala, Santhivardhan Chinni. “Bioavailability enhancement of vitamin E TPGS liposomes of nintedanib esylate: formulation optimization, cytotoxicity and pharmacokinetic studies.” Drug Delivery and Translational Research 12 11 (2022): 2856–2864.
Nintedanib esylate Preparation Products And Raw materials
Raw materials
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| Basil Drugs AND Pharmaceuticals Pvt Ltd | +91-2249700250 +91-9619320820 | Mumbai, India | 108 | 58 | Inquiry |
| Beta Drugs | +91-9316590666 +91-7015991921 | Haryana, India | 34 | 58 | Inquiry |
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| SUN PHARMACEUTICAL INDUSTRIES LTD | (+91 22) 4324 4324 | New Delhi, India | 175 | 58 | Inquiry |
| A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
| Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
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