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Review, Journal: Critical Analysis of Thrombocytopenia Associated With Glycoprotein IIb/IIIa Inhibitors and Potential Role of Zalunfiban, a Novel Small Molecule Glycoprotein Inhibitor, in Understanding the Mechanism(s). (Pubmed Central) - Dec 8, 2023
Thrombocytopenia is a rare but serious complication of the intravenous glycoprotein IIb/IIIa (GPIIb/IIIa; integrin ?IIb?3) receptor inhibitors (GPIs), abciximab, eptifibatide, and tirofiban...It is unclear whether the antibody binding depends on the conformational change and whether the drug contributes directly to the epitope. Zalunfiban, a second-generation subcutaneous small molecule GPI, does not induce the conformational changes; therefore, data from studies of zalunfiban will provide information on the contribution of the conformational changes to the development of GPI-associated thrombocytopenia.
- |||||||||| zalanfiban (RUC-4) / CeleCor, selatogrel (ACT-246475) / Idorsia
Journal: Comparison of the effects of the GPIIb-IIIa antagonist Zalunfiban and the P2Y12 antagonist Selatogrel on Platelet Aggregation. (Pubmed Central) - Aug 10, 2023
An example is the antithrombotic treatment of acute coronary syndrome (ACS), in particular ST-elevated myocardial infarction (STEMI) patients who are in need for rapid acting strong antithrombotic therapy despite the use of aspirin and oral P2Y12-inhibitors...Zalunfiban also had greater inhibition of MA in response to TRAP at the Cmax dose. These data suggest that zalunfiban may provide greater protection in reducing thrombus formation than selatogrel, especially since thrombin is an early, key primary agonist in the pathophysiology of thrombotic events.
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In vitro comparison of platelet aggregation between zalunfiban and selatogrel in healthy donors (Station 9) - May 13, 2023 - Abstract #ESC2023ESC_5086;
Whole blood from healthy donors not taking aspirin (N=10) was anticoagulated with 3.2% TSC and 100 ?M PPACK...Conclusion Selatogrel is a potent inhibitor of ADP-induced platelet aggregation, but has low impact on TRAP-induced platelet aggregation, whereas zalunfiban is a potent inhibitor of both ADP and TRAP-induced platelet aggregation. The difference between the drugs needs to be considered in light of the known generation of thrombin at the site of vascular injury within seconds.
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Review, Journal: Dual Antiplatelet Therapy with Parenteral P2Y Inhibitors: Rationale, Evidence, and Future Directions. (Pubmed Central) - Apr 27, 2023
The difference between the drugs needs to be considered in light of the known generation of thrombin at the site of vascular injury within seconds. Dual antiplatelet therapy (DAPT), consisting of the combination of aspirin and an inhibitor of the platelet P2Y receptor for ADP, remains among the most investigated treatments in cardiovascular medicine...The latter have been shown to be extremely suitable in drug-na
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Trial primary completion date: CELEBRATE: A Phase 3 Study of Zalunfiban in Subjects With ST-elevation MI (clinicaltrials.gov) - Feb 10, 2023
P3, N=2499, Recruiting,
The CELEBRATE trial will assess whether a single prehospital subcutaneous injection of zalunfiban in addition to standard-of-care in patients with STEMI with intent to undergo primary PCI will result in improved clinical outcome. Trial primary completion date: Dec 2023 --> Dec 2024
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Journal: Parenteral Antiplatelet Drugs in ST-Elevation Myocardial Infarction: Current Status and Future Directions. (Pubmed Central) - Sep 11, 2022
Novel parenteral antiplatelet drugs, such as cangrelor, selatogrel, and zalunfiban, have been recently developed to achieve rapid, potent antiplatelet effects while preserving hemostasis. We provide a description of currently available parenteral antiplatelet agents and of those in clinical development for prehospital administration in STEMI patients.
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Phase classification, Enrollment change, Trial completion date, Trial primary completion date: CELEBRATE: A Phase 3 Study of Zalunfiban in Subjects With ST-elevation MI (clinicaltrials.gov) - May 18, 2022
P3, N=2499, Recruiting,
We provide a description of currently available parenteral antiplatelet agents and of those in clinical development for prehospital administration in STEMI patients. Phase classification: P2b --> P3 | N=1668 --> 2499 | Trial completion date: Jun 2023 --> Dec 2024 | Trial primary completion date: Mar 2023 --> Dec 2023
- |||||||||| zalanfiban (RUC-4) / CeleCor
[VIRTUAL] Assessing the Pharmacodynamics of RUC-4 (Zalunfiban), a Novel αIIbβ3 Antagonist, Using VerifyNow Assays in Patients with ST-Segment Elevation Myocardial Infarction (STEMI) Treated with Aspirin and Ticagrelor (Room 4) - Jun 9, 2021 - Abstract #ISTH2021ISTH_2713;
Over the next 3 hours, as RUC-4’s blood concentration decreased (Table) and ticagrelor’s effects increased, the ADP assay remained inhibited, the Base assay returned to pre-treatment levels, and the iso-TRAP assay returned toward pre-treatment levels, but not as completely as with the Base assay, reflecting modest inhibition of the iso-TRAP assay by ticagrelor. Conclusions : Combining VerifyNow assays provides important information: 1) the Base assay is best suited for measuring the isolated effect of RUC-4 after co-therapy with ticagrelor, and 2) when the Base assay returns to baseline, the ADP assay provides an accurate assessment of the ticagrelor effect.
- |||||||||| zalanfiban (RUC-4) / CeleCor
Enrollment open: CELEBRATE: A Phase 3 Study of Zalunfiban in Subjects With ST-elevation MI (clinicaltrials.gov) - May 12, 2021
P2b, N=1668, Recruiting,
Conclusions : Combining VerifyNow assays provides important information: 1) the Base assay is best suited for measuring the isolated effect of RUC-4 after co-therapy with ticagrelor, and 2) when the Base assay returns to baseline, the ADP assay provides an accurate assessment of the ticagrelor effect. Not yet recruiting --> Recruiting
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