product Description
Lifitegrast is a novel small-molecule anti-inflammatory agent specifically developed for the treatment of dry eye disease (DED), a common ocular disorder characterized by insufficient tear production or poor tear film stability. Its core mechanism of action lies in inhibiting the interaction between lymphocyte function-associated antigen 1 (LFA-1) on the surface of immune cells and intercellular adhesion molecule 1 (ICAM-1) expressed on corneal and conjunctival epithelial cells. This blocking effect prevents inflammatory cell recruitment and infiltration into ocular tissues, reduces the release of pro-inflammatory mediators such as cytokines and chemokines, and thereby alleviates typical DED symptoms including dryness, foreign body sensation, burning, and photophobia.
Developed by Shire Pharmaceuticals (USA), lifitegrast was approved by the US FDA in 2016 under the trade name Xiidra. As the first LFA-1 antagonist approved for DED treatment, it offers advantages of rapid onset (with symptom relief observable within weeks) and good tolerability, with adverse reactions mostly limited to transient ocular irritation. Clinically, it effectively improves ocular inflammatory conditions, enhances tear film stability, and is applicable to both mild-to-moderate and severe DED patients, providing a new therapeutic alternative to traditional artificial tears.
Its physicochemical properties are crucial for formulation development and quality control: it is freely soluble in N,N-dimethylacetamide and tetrahydrofuran but almost insoluble in ethanol and water, which presents challenges for aqueous formulation development. The specific rotation ranges from -6° to -10° (DMSO, 20℃), and strict purity and quality standards are imposed—main peak purity ≥99.5%, isomer content ≤0.1%, single impurity ≤0.10%, residue on ignition ≤0.1%, heavy metals ≤10ppm, water content ≤2.0%, and anhydrous-based content between 98.0% and 102.0%—to ensure efficacy and safety.
For packaging, the inner layer adopts pharmaceutical low-density polyethylene bags, while the outer layer uses polyester/aluminum/polyethylene pharmaceutical composite film bags. This dual-layer packaging effectively isolates moisture, oxygen, and external contaminants, safeguarding the drug’s chemical stability during long-term storage and transportation.
product Specification
|
Item |
Unit |
Specification |
|
Appearance |
|
white to off-white ,solid |
|
Solubility |
|
freely soluble in N,N-dimethylacetamide and tetrahydrofuran but almost insoluble in ethanol and water |
|
Specific rotation |
|
-6° to -10° (DMSO, 20℃) |
|
Identification |
|
infrared spectroscopy + HPLC retention time |
|
Other impurities |
% |
≤0.10 |
|
Related Substances - Total Impurities |
% |
≤0.5 |
|
Main peak purity |
% |
≥99.5 |
|
Isomer content |
% |
≤0.1 |
|
Content |
% |
anhydrous-based content between 98.0% and 102.0% |
|
Residue on ignition |
% |
≤0.1 |
|
Water content |
|
≤2.0 |
|
Heavy metals |
ppm |
≤10 |
|
Storage |
|
the inner layer adopts pharmaceutical low-density polyethylene bags, while the outer layer uses polyester/aluminum/polyethylene pharmaceutical composite film bags |
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