Results of a new ongoing phase 1 study, presented at Transcatheter Cardiovascular Therapeutics (TCT) 2019 San Francisco, showed that as a first point-of-contact therapy for ST-elevation myocardial infarction (STEMI), a novel subcutaneous (SC) GpIIb/IIIa inhibitor, RUC-4, can achieve 80% of platelet inhibition within 15 minutes of the administration.
Half of the STEMI related mortality is reported to occur before reaching the hospital. Treatment initiation closer to the onset of symptoms predicts the mortality of myocardial infarction (MI). Inhibiting platelet aggregation has been the basis of treating and preventing an MI. Drugs, such as thienopyridine inhibitors (e.g., clopidogrel) are not rapidly acting or reliable. These drugs also do not inhibit other mechanisms at play or receptors where thrombin can act and form a thrombus. GpIIb/IIIa inhibitors interfere with the final pathway in platelet aggregation, and drugs such as abciximab and tirofiban have improved outcomes when given to STEMI patients. The one critical limitation of these drugs, however, is that they can not be delivered in pre-hospital settings. RUC-4 is designed as a SC injection that can easily be administered in a pre-hospital setting.
This is a randomized, interventional, triple blinded, phase 1, dose-escalation clinical study with an estimated enrollment of 70 subjects randomized into either RUC-4 or placebo group. The included subjects are 18-75 years old healthy adults and adults with stable coronary heart disease. Subjects with history of prior stroke or any clinically significant disease that can potentially jeopardize the safety of the subjects or impact the validity of the results were excluded from the study. The study started in February 2019 and it is estimated to be completed by January 2020.
[perfectpullquote align=”full” bordertop=”false” cite=”” link=”” color=”” class=”” size=””]“Nothing is more simple, easy and effective than a subcutaneous injection that can be administered by even EMS. The dose of RUC-4 is less than half an mL and within 15 minutes, more than 80% platelet inhibition can be achieved. The threshold of 80% platelet inhibition decreases periprocedural MI. We are excited to see Phase 2 that can show an increase in TIMI2, and TIMI3 flow will be significant when randomized to this drug and placebo. The GpIIb/IIIa inhibitors also disaggregate platelets, inhibit thrombin final pathway, and act on platelet-rich early thrombus. It locks the receptor in an inactive conformation.”-Dr.Dean J. Kereiakes, M.D., FACC, FSCAI[/perfectpullquote]
In an interview with Dr C. Michael Gibson at TCT 2019, the Principal Investigator Dr Dean J. Kerekias, who is the Medical Director of The Christ Hospital Heart and Vascular Center and The Christ Hospital Research Institute and Professor of Clinical Medicine at The Ohio State University, said,” The dose of RUC-4 is less than half an mL and within 15 minutes, more than 80% platelet inhibition can be achieved. The GpIIb/IIIa inhibitors also disaggregate platelets, inhibit thrombin final pathway, and act on platelet-rich early thrombus. It locks the receptor in an inactive conformation.”
This study has promising potential and it paves the way for revolutionizing the management of STEMI and the approach towards platelet disaggregation. We are hoping that the anticipated presentation entitled, “First Human Use of a Novel Subcutaneous Platelet GPIIb/IIIa Inhibitor (RUC-4) Designed for STEMI Point of Care Treatment,” at TCT 2019 will provide us with more insight into the dynamics of this development.
To watch the complete interview of Dr. Dean Kereiakes and Dr. C. Michael Gibson, click here.