ORAL PCSK9 INHIBITOR
Our intention is to develop a PCSK9 inhibitor in a once daily tablet for patients

All available PCSK9 treatment options in our therapeutic area are delivered by injection, but four out of five patients prefer a pill.1 That’s why Esperion is developing a small molecule oral PCSK9 inhibitor that can be taken as a tablet.

PCSK9 (proprotein convertase subtilisin/kexin type 9) is an enzyme responsible for regulating low-density lipoprotein (LDL) receptors. PCSK9 inhibitors stop LDL receptors from being broken down, increasing the number of LDL receptors present to remove cholesterol from the blood. Current approved PCSK9 inhibitors – delivered as injections – have proven to be out of reach for many patients.2,3 A tablet oral PCSK9 inhibitor would fill a key gap in non-statin treatment options for patients, between statins and shots.

DEVELOPMENT TIMELINE FOR ORAL PCSK9 INHIBITOR4

PCSK9 is a validated target for the treatment of dyslipidemia and reduction of cardiovascular risk, with demonstrated efficacy and safety in various high-risk CVD populations.5,6

References: 1. Dibonaventura, M. D., Wagner, J. S., Girman, C. J., Brodovicz, K., Zhang, Q., Qiu, Y., Pentakota, S. R., & Radican, L. (2010). Multinational Internet-based survey of patient preference for newer oral or injectable Type 2 diabetes medication. Patient preference and adherence, 4, 397–406. https://doi.org/10.2147/PPA.S14477 2. Baum SJ, Toth PP, Underberg JA, Jellinger P, Ross J, Wilemon K (2017). “PCSK9 inhibitor access barriers-issues and recommendations: Improving the access process for patients, clinicians and payers”. Clinical Cardiology. 40 (4): 243–254. doi:10.1002/clc.22713. PMC 5412679. PMID 28328015. 3. Gina Kolata, “These Cholesterol-Reducers May Save Lives. So Why Aren’t Heart Patients Getting Them?”, The New York Times, Oct. 2, 2018. Retrieved 18 December 2020. 4. Esperion Reports Preliminary Fourth Quarter 2020 Financial Results and Further Commits to Unmet Patient Needs with Oral PCSK9 Inhibitor Program [press release]. Ann Arbor, MI: Esperion Therapeutics, Inc.; January 13, 2021. 5. Sabatine MS et al. Evolocumab and Clinical Outcomes in Patients with Cardiovascular Disease. N Engl J Med 2017; 376:1713-1722. DOI: 10.1056/NEJMoa1615664. https://www.nejm.org/doi/full/10.1056/nejmoa1615664 6. Schwartz, GG et al. Alirocumab and Cardiovascular Outcomes after Acute Coronary Syndrome. N Engl J Med 2018; 379:2097-2107. DOI: 10.1056/NEJMoa1801174. https://www.nejm.org/doi/full/10.1056/NEJMoa1801174