frunexian (EP-7041 Intravenous) / eXIthera Pharma, Haisco - LARVOL DELTA

Pharmacokinetics, pharmacodynamics, and safety of frunexian in healthy Chinese volunteer adults: A randomized dose-escalation phase I study. (PubMed, Clin Transl Sci) - "The purpose of this study was to evaluate the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of frunexian (formerly known as EP-7041 and HSK36273) injection, a small molecule inhibitor of activated coagulation factor XI (FXIa), in healthy Chinese adult volunteers...The correlations between PK and PD biomarkers (aPTT/baseline and FXI clotting activity/baseline) were described by the two Emax models, with the EC50 values of 8940 and 1300 ng/mL, respectively. Frunexian exhibits good safety and PK/PD properties, suggesting it is a promising candidate for anticoagulant drug."

Journal • P1 data • PK/PD data

COVID-19 ThromboprophylaXIs Study of Novel FXIa Inhibitor Frunexian (EP-7041) in ICU Patients (clinicaltrials.gov) - P2 | N=0 | Withdrawn | Sponsor: eXIthera Pharmaceuticals | N=90 ➔ 0 | Not yet recruiting ➔ Withdrawn

Enrollment change • Trial withdrawal • Critical care • Infectious Disease • Novel Coronavirus Disease • Thrombocytopenia

COVID-19 ThromboprophylaXIs Study of Novel FXIa Inhibitor Frunexian (EP-7041) in ICU Patients (clinicaltrials.gov) - P2 | N=90 | Not yet recruiting | Sponsor: eXIthera Pharmaceuticals | Trial completion date: Dec 2024 ➔ May 2025 | Trial primary completion date: Dec 2023 ➔ May 2024

Trial completion date • Trial primary completion date • Critical care • Infectious Disease • Novel Coronavirus Disease • Thrombocytopenia

A Study of Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Multiple Ascending Dosed of HSK36273 in Healthy Volunteers (clinicaltrials.gov) - P1 | N=54 | Completed | Sponsor: Haisco Pharmaceutical Group Co., Ltd.

New P1 trial

COVID-19 ThromboprophylaXIs Study of Novel FXIa Inhibitor Frunexian (EP-7041) in ICU Patients (clinicaltrials.gov) - P2 | N=90 | Not yet recruiting | Sponsor: eXIthera Pharmaceuticals | Trial completion date: Dec 2023 ➔ Dec 2024 | Trial primary completion date: Dec 2022 ➔ Dec 2023

Trial completion date • Trial primary completion date • Critical care • Infectious Disease • Novel Coronavirus Disease • Thrombocytopenia

EP-7041 for Treatment of Thromboprophylaxis in Patients Managed in Intensive Care Settings for COVID-19 Syndrome (clinicaltrials.gov) - P2; N=90; Not yet recruiting; Sponsor: eXIthera Pharmaceuticals

Clinical • New P2 trial • Critical care • Infectious Disease • Novel Coronavirus Disease • Thrombocytopenia

eXIthera Pharmaceuticals Announces FDA Acceptance of IND Application for Phase 2 Trial of EP-7041 for Thrombosis Prevention in COVID-19 Patients (PRNewswire) - "eXIthera Pharmaceuticals...announced the U.S. Food and Drug Administration (FDA) has accepted its Investigational New Drug (IND) application to initiate a Phase 2 clinical trial for EP-7041...The IND application indicates EP-7041 is an investigational treatment for COVID-19...The Phase 2 trial is a multicenter, prospective, open-label study that will first evaluate the safety and tolerability of two dose levels of EP-7041 in thirty COVID-19 patients admitted to an Intensive Care Unit (ICU)."

IND • Infectious Disease • Novel Coronavirus Disease

Will eXIthera provide the anticoagulant solution in corona patients? [Google translation] (The Marker) - "Shares of Clal Biotechnology (+ 0.29% 204.4 ) rose 6% after eXIthera (45%) was approved by the US Food and Drug Administration (FDA) to begin the first phase of the second phase of the clinical trial on EP-7041 - anticoagulant Which inhibits factor XI in corona patients hospitalized in intensive care units....In the first part of the trial, two doses of the drug will be given, each to 15 patients. If the safety assessment at the end of this section confirms the safety of the high dose, the second part of the trial will begin, and it will be given to 40 patients..."

Trial status

EP-7041, a Factor XIa Inhibitor as a Potential Antithrombotic Strategy in Extracorporeal Membrane Oxygenation: A Brief Report. (PubMed, Crit Care Explor) - "Selective inhibition of the contact pathway of coagulation could reduce bleeding risk, and because factor XI is linked with the inflammatory and complement systems, it can also be viewed as a biologically plausible target for the prevention of abnormal thrombosis during extracorporeal membrane oxygenation. We introduce initial information on EP-7041, a parenteral, potent, and selective, small-molecule activated factor XIa inhibitor with pharmacodynamic and pharmacokinetic characteristics that appear well suited for use in a critical care environment."

Journal • Cardiovascular • Critical care • Hematological Disorders • Thrombosis

eXIthera Announces Publication of EP-7041 Data Demonstrating Safe Antithrombotic Activity in ECMO (PRNewswire) - "eXIthera Pharmaceuticals...today announced the publication of data in Critical Care Explorations. The publication describes the pharmacodynamic, pharmacokinetic and safety profile of EP-7041...as seen in multiple preclinical studies and a Phase 1 study. The manuscript, titled 'EP-7041, a Factor XIa Inhibitor as a Potential Antithrombotic Strategy in Extracorporeal Membrane Oxygenation: A Brief Report,'...'We look forward to continuing our studies of EP-7041 in the ECMO setting and sharing additional efficacy data comparing EP-7041 to UFH.'...The data were initially presented during a virtual poster session at the International Society on Thrombosis and Haemostasis (ISTH) 2020 Congress in July 2020. The abstract (number PB0166) can be found online..."

Clinical data • PK/PD data • Cardiovascular • Venous Thromboembolism

[VIRTUAL] Anticoagulation with the Novel, Small-molecule Factor XIa (fXIa) Antagonist, EP-7041, Prevents Oxygenator Clotting but Conserves Hemostasis in a Canine Extracorporeal Circulation (ECMO) Model (ISTH 2020) - "Compared with heparin, anticoagulation with EP-7041, a short-acting, potent and selective, small-molecule Factor XIa antagonist, prevents oxygenator clotting but maintains hemostasis in a canine ECMO model."

Anesthesia • Cardiovascular • Hematological Disorders • Respiratory Diseases • Thrombosis • F2