INS1007 – AN INVESTIGATIONAL, NOVEL ORAL REVERSIBLE INHIBITOR OF DPP1

INS1007 is an investigational, novel oral reversible inhibitor of dipeptidyl peptidase 1 (DPP1). DPP1 is an enzyme that catalyzes the activation of neutrophil serine proteases, which play a key role in the pathology of chronic inflammatory lung diseases such as non-cystic fibrosis (non-CF) bronchiectasis.1,2

Non-CF bronchiectasis is a rare, progressive pulmonary disorder.

About Non-CF Bronchiectasis

Non-CF bronchiectasis is a rare, progressive pulmonary disorder in which the bronchi become permanently dilated due to chronic inflammation and infection.2 Neutrophils play a key role in the pathologic inflammatory process.2 Symptoms include chronic cough, excessive sputum production, shortness of breath, and repeated respiratory infections, which can worsen the underlying condition.3 There is currently no cure for non-CF bronchiectasis.

INS1007 – An Investigational, Novel Oral Reversible Inhibitor of DPP1

INS1007 is an investigational, small molecule, oral reversible inhibitor of DPP1, an enzyme responsible for activating neutrophil serine proteases in neutrophils when they are formed in the bone marrow.1

INS1007 – An Investigational, Novel Oral Reversible Inhibitor of DPP1

Neutrophils are the most common type of white blood cell and play an essential role in pathogen destruction and inflammatory mediation.1 Neutrophils contain three neutrophil serine proteases, neutrophil elastase, proteinase 3, and cathepsin G, that have been implicated in a variety of inflammatory diseases. In chronic inflammatory lung diseases, such as non-CF bronchiectasis, neutrophils accumulate in the airways and result in excessive active neutrophil serine proteases that cause lung destruction and inflammation.1,2

References

1Korkmaz B, Horwitze MS, Jenne DE, Gauthier F. Neutrophil elastase, proteinase 3, and cathepsin G as therapeutic targets in human disease. Pharmacol Rev. 2010;62(4):726759.

2Stockley R, De Soyza A, Gunawardena K, et al. Phase II study of a neutrophil elastase inhibitor (AZD9668) in patients with bronchiectasis. Respir Med. 2013;107(4):524533.

3Neves PC, Guerra M, Ponce P, Miranda J, Vouga L. Non-cystic fibrosis bronchiectasis. Interact CardioVasc Thorac Surg. 2012;13(6):619-625.