Press releases

• This data opens the way to BAPAIs for the treatment of cardiovascular diseases

• Larger Phase II clinical trial launched in the United States

Quantum Genomics (Alternext - FR0011648971 - ALQGC), a biopharmaceutical company with the mission of developing new therapies for unmet medical needs in the field of cardiovascular diseases, today announced that its drug candidate QGC001 showed efficacy in patients with mild to moderate arterial hypertension, according to the results of a Phase IIa pilot study.

The results of this study were presented at the Congress of the European Society of Hypertension on June 18 by its principal investigator, Prof Michel Azizi, Director of the Clinical Investigation Center and Head of the Arterial Hypertension Unit at Georges Pompidou European Hospital, Paris.

QGC001 is the first molecule of a new class of antihypertensive agents called BAPAIs (Brain Aminopeptidase A Inhibitors). It is a prodrug that allows EC33, a specific selective aminopeptidase A inhibitor, to be released in the brain preventing the production of angiotensin III in the brain.

Lionel Ségard, Chairman & CEO of Quantum Genomics, says:

"We are excited to present these positive results, which are fully in line with our expectations. They constitute a major milestone in our strategy and show that aminopeptidase A inhibitors in the brain have an antihypertensive effect and, as such, constitute a new class of promising drugs that open the door to new treatments for high blood pressure. They validate our continuing clinical development, in particular the launch of a larger Phase II trial on hypertensive patients with higher cardiovascular risks, which will start in the autumn in the United States.”

This Phase IIa was planned as a multicentric, randomized, double-blind, crossover study, administered over two periods of four weeks each. The main goal was to assess in 34 patients suffering from Grade I or II arterial hypertension (systolic pressure 40 ≤ 179 mmHg, diastolic pressure 90 ≤ 109 mmHg) the effect on blood pressure of QGC001 administered orally at a dose of 250 mg twice a day for one week, then a dose of 500 mg twice a day for three weeks, compared to placebo. Another goal was to assess the safety and tolerance of QGC001 and its effects on the plasma levels of hormones involved in cardiovascular regulation.

Multivariate data analysis demonstrated the effects of initial blood pressure level (p=0.01) and treatment by QGC001 (p=0.06) on lowering ambulatory systolic blood pressure.

The study also showed, despite the small sample size, that QGC001 led to a decrease in ambulatory systolic blood pressure (primary evaluation criterion) of 2.7 mmHg (p=0.16) and in-office systolic blood pressure of 4.7 mm Hg (0=0.15), as compared with placebo where no decrease in blood pressure was observed.

Bruno Besse, Chief Medical Officer of Quantum Genomics, says:

 "Remarkably, the study also showed that QGC001 had the greatest antihypertensive effect in patients with the highest blood pressure. This seems to confirm our hypothesis that QGC001 could be particularly effective in patients with complicated hypertension, which will be the subject of a larger Phase II trial that will be launched in the United States."

The goal of this study was to demonstrate in humans the proof-of-concept obtained in animals and to help define future clinical trials.

The conclusions of the study are fully consistent with the experimental results in animals. No effect was found in normotensive rats but a decrease in blood pressure was revealed in hypertensive rats (SHR and DOCA-salt) in which aminopeptidase A is hyperactive as compared to normotensive animals, in the same way as in Phase I in humans, QGC001 led to no decrease in blood pressure in healthy normotensive volunteers.

The clinical trial also showed no change in plasma hormone concentrations such as active renin, aldosterone, cortisol, adrenocorticotropic hormone and apelin in either the QGC001 group or placebo, confirming that QGC001's action mechanism is not mediated by renin or aldosterone.

The good tolerance observed on renal function as well as on blood electrolytes, such as sodium and potassium, is particularly important from the perspective of the potential use of QGC001 in the treatment of heart failure, an indication for which Quantum Genomics is currently carrying out a pan-European Phase II clinical study.

In general, QGC001's tolerance profile is consistent with observations in the Phase I clinical trials.

Following FDA (Food and Drug Administration) guidance, Quantum Genomics is preparing a larger Phase II study to be launched in autumn 2017 in the United States. Called NEW-HOPE, this study will cover 250 hypertensive patients with higher cardiovascular risks.

More details of this study will be provided at the KOL (Key Opinion Leaders) & Investor Day, to be held on June 27 in New York, USA.

Quantum Genomics will host, today at 6:00pm CET, a conference call followed by a question-and-answer session to discuss these phase IIa results for the drug candidate QGC001.

QGC001, Quantum Genomics' lead Brain Aminopeptidase A Inhibitor (BAPAI) candidate, is a first-in-class standalone treatment for hypertension. Functionally, QGC001 is a prodrug of EC33, a selective and specific inhibitor of Aminopeptidase A that prevents the production of Angiotensin III in the brain.

Due to its unique action mechanism, QGC001 is an improved therapeutic approach which interferes with mechanisms involved in the genesis and control of high blood pressure in hypertensive patients, especially in those who exhibit a particular hormonal profile characterized by a low renin and a high vasopressin concentration (Low Renin High Vasopressin (LRHV) profile).