Glpg1690 CAS No.:1628260-79-6

Introduction:

Glpg1690 is a novel small molecule that has shown promising results in the treatment of a variety of pulmonary diseases, including idiopathic pulmonary fibrosis (IPF), scleroderma-associated interstitial lung disease (SSc-ILD), and other fibrotic diseases. It has been developed by Galapagos, a biotechnology company based in Belgium, and is currently in Phase 2 clinical trials.

What is Glpg1690?

Glpg1690 is a selective autotaxin (ATX) inhibitor, which means it targets the enzyme that produces lysophosphatidic acid (LPA). LPA is known to be involved in fibrosis and inflammation, and by inhibiting ATX, Glpg1690 may reduce the production of LPA and therefore decrease the fibrotic response in the lungs.

Benefits and Features:

1. High efficacy: In preclinical studies, Glpg1690 has shown high potency and selectivity in inhibiting ATX, leading to a significant reduction in lung fibrosis and inflammation.

2. Good safety profile: Glpg1690 has been well-tolerated in clinical trials, with no reported serious adverse events.

3. Potential for multiple indications: Because fibrosis and inflammation are common features of many pulmonary diseases, Glpg1690 has the potential to be effective in treating a wide range of conditions.

4. Convenient dosing: Glpg1690 can be administered orally, making it a convenient and noninvasive treatment option for patients.

Mechanism of Action:

Glpg1690 works by inhibiting the enzyme autotaxin, which produces lysophosphatidic acid (LPA). LPA is known to be involved in a range of processes, including fibrosis and inflammation, and by reducing its production, Glpg1690 may help alleviate these symptoms.

Clinical Trials:

Glpg1690 is currently in Phase 2 clinical trials for the treatment of idiopathic pulmonary fibrosis and scleroderma-associated interstitial lung disease. These trials are designed to evaluate the safety and efficacy of the drug in patients with these conditions.

Conclusion:

Glpg1690 is a promising new treatment option for a variety of pulmonary diseases. Its high potency and selectivity in inhibiting autotaxin make it a potentially effective therapy for reducing fibrosis and inflammation in the lungs. With its convenient oral dosing and good safety profile, it may offer a valuable treatment option for patients suffering from these conditions.

Chemical Structure : GLPG-1690

CAS No.: 1628260-79-6

 

 

 

 

GLPG-1690(Ziritaxestat;GLPG 1690;GLPG1690)

Catalog No.: URK-V653 Only Used For Lab.

GLPG-1690 (Ziritaxestat, GLPG1690) is a first-in-class, potent, competitive autotaxin inhibitor with Ki/IC50 of 15 nM/131 nM.

Biological Activity

GLPG-1690 (Ziritaxestat, GLPG1690) is a first-in-class, potent, competitive autotaxin inhibitor with Ki/IC50 of 15 nM/131 nM; inhibits ATX-induced LPA 18:2 production in mouse, rat, and healthy donor plasma with IC50 of 418 nM, 542 nM, and 242 nM, respectively; shows no CYP3A4 TDI and decreased hERG inhibitory activity (IC50=15 uM), and good pharmacokinetic profile for treatment idiopathic pulmonary fibrosis.
Fibrosis
Phase 2 Clinical

Physicochemical Properties

References

1. Desroy N, et al. J Med Chem. 2017 May 11;60(9):3580-3590.

URK-V653_COA

URK-V653_SDS

URK-V653_TDS

 

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