Nintedanib Esylate is the ethanesulfonate salt of Nintedanib, a small-molecule multi-target tyrosine kinase inhibitor used in pharmaceutical formulations for the treatment of idiopathic pulmonary fibrosis (IPF) and certain cancers. Nintedanib inhibits multiple receptor tyrosine kinases, including VEGFR, FGFR and PDGFR, as well as other kinases involved in angiogenesis, fibrosis and tumor progression.
Nintedanib Esylate is an important antifibrotic and antineoplastic pharmaceutical API for research, formulation development and manufacture of oral solid dosage formulations.
Nintedanib Esylate is a specialized pharmaceutical active ingredient used in the development and manufacture of medicines targeting fibrotic lung diseases and oncology indications.
The esylate salt improves the pharmaceutical properties of Nintedanib and is the form used in marketed Nintedanib capsule formulations. EMA identifies the active substance as nintedanib esylate and describes its molecular mass as 649.76 g/mol.
CAS Number: 656247-18-6
Molecular Formula: C₃₃H₃₉N₅O₇S
Molecular Weight: 649.76 g/mol
Chemical Name: Nintedanib ethanesulfonate
Salt Form: 1:1 ethanesulfonate salt
Synonym: BIBF 1120 esylate
Drug Class: Tyrosine Kinase Inhibitor
Therapeutic Class: Antifibrotic / Antineoplastic Agent
Therapeutic Area: Respiratory Diseases / Oncology
Molecule Type: Synthetic Small Molecule
Target Class: Receptor Tyrosine Kinases and Non-Receptor Tyrosine Kinases
PubChem identifies Nintedanib Esylate as CAS 656247-18-6 with molecular formula C₃₃H₃₉N₅O₇S and molecular weight approximately 649.8 g/mol.
Nintedanib is a multi-target tyrosine kinase inhibitor. It inhibits receptor tyrosine kinases involved in angiogenesis, fibrosis and cellular signaling.
Important targets include:
Through inhibition of these pathways, Nintedanib can interfere with angiogenic signaling and fibroblast-related processes.
Nintedanib Esylate API is relevant to:
Nintedanib is used therapeutically in formulations for idiopathic pulmonary fibrosis and other approved fibrosing interstitial lung diseases. Its antifibrotic activity is associated with inhibition of growth-factor receptor signaling involved in fibroblast activation and fibrosis.
Nintedanib also has applications in oncology. Its inhibition of VEGFR, FGFR and PDGFR signaling makes it relevant to research involving tumor angiogenesis and cancer-cell signaling.
Its exact approved indications depend on the regulatory jurisdiction and specific formulation.
Nintedanib Esylate is described in U.S. regulatory labeling as a greenish-yellow to bright-yellow powder. The FDA documentation identifies its empirical formula as C₃₁H₃₃N₅O₄·C₂H₆O₃S and molecular weight as 649.76 g/mol.
Nintedanib Esylate has limited aqueous solubility, although its salt form has improved aqueous properties compared with the free base. A published solubility study specifically investigated Nintedanib Esylate hemihydrate and reported that solubility varies significantly with solvent and temperature.
For CMS purposes, a useful reported value is approximately 2.8 mg/mL in water at around pH 5.7, although this is a literature/reference solubility value rather than a pharmaceutical release specification.
A controlled Nintedanib Esylate API manufacturing process may involve:
Typical Nintedanib Esylate API quality-control testing may include:
Because Nintedanib Esylate can occur in different solid forms, solid-form and water-content control can be particularly important. Research has identified Nintedanib Esylate hemihydrate as a distinct crystalline form containing approximately half a molecule of water.
Store Nintedanib Esylate API in a tightly closed container under controlled pharmaceutical storage conditions, protected from excessive moisture, heat and direct light.
The exact commercial storage condition should follow the validated stability data and applicable API specification.
| Parameter | Specification |
|---|---|
| Appearance | White crystalline powder or crystals |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.1% |
| pH (1% Solution) | 4.0 – 10.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 5.0% |
| Melting Point | >233°C (decomposition reported) |