Firibastat - First-in-class - hypertension as monotherapy

FIRIBASTAT, A FIRST-IN-CLASS DRUG CANDIDATE FOR RESISTANT HYPERTENSION

The firibastat (originally named QGC001) product is the first BAPAI candidate-drug selected by Quantum Genomics. The firibastat product is a prodrug that delivers in the brain the EC33 product, a selective and specific inhibitor of Aminopeptidase A, thus preventing the production of Angiontensin III in the brain.

Due to its unique action mechanism, firibastat represents an alternative therapeutic approach which can interfere with the mechanisms involved in the genesis and control of blood pressure in hypertensive patients, especially those with a particular hormonal profile, characterized by a low renin concentration and a high vasopressin concentration (Low Renin High Vasopressin (LRHV) profile).

Firibastat and its therapeutic use are strongly protected by several families of patents ensuring an industrial protection until 2033 without taking into consideration the potential additional protection certificates.

Several preclinical studies and two clinical studies have been conducted already using firibastat to assess its pharmacokinetic, pharmacodynamic, safety and tolerance parameters in animals and humans. In 2014, Quantum Genomics intends to pursue the clinical development of firibastat by initiating a Phase IIa study to evaluate its effectiveness in hypertensive patients.

The Phase IIa clinical trials for high blood pressure (firibastat program) were completed in April 2016 and the company presented positive results in June 2017 at the European Society of Hypertension congress.

The resulting data showed positive signals over several parameters of the study, particularly on the main indicator (primary endpoint), the drop in daytime systolic blood pressure measured as ambulatory pressure in hypertensive patients.

Quantum Genomics launched a Phase IIb study in Q4 2017 in the United States. This study, named NEW-HOPE, covered 256 hypertensive patients at high cardiovascular risk.

Phase IIb results published last November demonstrate that firibastat has highly significant anti-hypertensive efficacy in patients at high cardiovascular risk whose hypertension is generally difficult to treat.

In accordance with these results, Quantum Genomics is preparing to launch a Phase III trial studying the effectiveness of firibastat as a treatment for resistant hypertension, thus paving the way for marketing authorisation. The complications of hypertension are particularly severe, and the disease is responsible for 9.4 million deaths worldwide each year[1].

In order to design and implement this trial, Quantum Genomics has set up a scientific steering committee composed of recognised European and American experts in high blood pressure:

– Keith C. Ferdinand: Cardiologist, Professor of Medicine at the Tulane School of Medicine, and Past President of the National Forum for Heart Disease and Stroke Prevention (New Orleans, USA).

– Georges Bakris: Nephrologist, Professor of Medicine & Director of the University of Chicago Medicine’s Comprehensive Hypertension Centre, and Past President of the American Society of Hypertension (Chicago, USA).

– William B. White: Professor of Medicine at the University of Connecticut School of Medicine, Chief of the Calhoun Cardiology Centre’s Division of Hypertension and Clinical Pharmacology, and Past President of the American Society of Hypertension (Farmington, USA).

– Jacques Blacher: Cardiologist, Professor at the Paris Descartes University, Head of the Diagnosis and Therapeutics Centre at the Hôtel Dieu University Hospital (AP-HP, Paris), and Past President of the French Society of Hypertension (Paris, France).

– Alexandre Persu: Head of the Hypertension Clinic at the Catholic University of Louvain (Department of Cardiology, Cliniques Universitaires Saint-Luc, Brussels). Secretary of the Belgian Hypertension Committee and Chairman of the working group “Hypertension and the kidney” of the European Hypertension Society (Brussels, Belgium).

The steering committee will work closely with Quantum Genomics’ scientific team to define the design of the Phase III trial, in particular its methodology, target population and evaluation criteria, and will be involved in discussions with the EMA (European Medicines Agency) and FDA (Food and Drug Administration). It will also be directly involved in the clinical trial’s conduct.

[1] WHO (World Health Organisation) – A Global Brief on Hypertension: Silent Killer, Global Public Health Crisis (2013).