INS1009 is an investigational, sustained-release, inhaled treprostinil prodrug that has the potential to address some of the current limitations of existing inhaled prostanoid therapies for Pulmonary Arterial Hypertension (PAH).
PAH is a serious, progressive rare disease affecting approximately 100,000 patients globally, including approximately 25,000 treated patients in the United States.1-3 PAH ultimately leads to heart failure, and the disease has a 15% one-year mortality rate.4
INS1009: An Investigational Inhaled Prostanoid Treatment for PAH
Insmed has applied its unique drug design expertise to develop an inhalation suspension of the product hexadecyl-treprostinil, contained within approximately 100 nanometer particles. Once deposited in the lung, lung esterases convert the prodrug into the active drug treprostinil, as shown through in vitro and in vivo animal studies.5
INS1009: A Unique Inhaled Prostanoid Treatment
The goal is to develop a treatment that enables 24-hour dosing. If achieved, it may offer patients a more convenient dosing regimen over current inhaled products which must be dosed four times or more per day.6,7
This pro-drug suspension formulation was designed to optimize treprostinil’s retention within the nanoparticles and will be investigated as a once daily nebulization.8
1Yang X, Mardekian J, Sanders KN, Mychaskiw MA, Thomas J. Prevalence of pulmonary arterial hypertension in patients with connective tissue diseases: a systematic review of the literature. Clinical Rheumatology 2013 Oct;32(10):1519-31.
2Peacock AJ, Murphy NF, McMurray JJV, et al. An epidemiological study of pulmonary arterial hypertension. Eur Respir J 2007;30:104–9
3Humbert M, Sitbon O, Chaouat A, Bertocchi M, Habib G, Gressin V, Yaici A, Weitzenblum E, Cordier JF, Chabot F, Dromer C, Pison C, Reynaud-
Gaubert M, Haloun A, Laurent M, Hachulla E, Simonneau. Pulmonary arterial hypertension in France: results from a national registry. ; Am J Respir
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4Kane GC, Maradit-Kremers H, Slusser JP, Scott CG, Frantz RP, McGoon MD. Integration of clinical and hemodynamic parameters in the prediction of long-term survival in patients with pulmonary arterial hypertension. Chest. 2011;139(6):1285-1293.
5F Leifer, D Omiatek, V Malinin, J Ong, Z Li, P Klecha, RW Chapman, D Salvail, C-E Laurent, WR Perkins. Prolonged Activity of Inhaled Treprostinil Prodrug Nanoparticles in a Rat Model of Pulmonary Arterial Hypertension. European Respiratory Society (ERS) International Congress. September 6-10, 2014, 2356.
6Tyvaso (treprostinil) [package insert]. Research Triangle Park, NC: United Therapeutics Corp; 2014.
7Ventavis (iloprost) [package insert]. South San Francisco, CA: Actelion Pharmaceuticals US, Inc; 2013.
8Data on file.