Development of an original and non-infringing route of synthesis of the antihypertensive drug aliskiren

The objective is the development of an original, patentable synthesis of the antihypertensive generic drug aliskiren, class renin-angiotensin antagonist. The project result will be the process, leading to the cheap, safe and environmentally friendly production of aliskiren.

The objective of the project submitted is the development of an original patentable synthesis of the active pharmaceutical ingredient Aliskiren, a compound belonging to the group of antihypertensive drugs. The substance was chosen from the group of pharmaceuticals most attractive for pharmaceutical companies. There are several reasons for the choice of the therapeutic group mentioned. Arterial hypertension is one of the most frequent cardio-vascular disorders, is widely spread, affects approximately 25 percent of the adult population, and is often referred to as a non-infectious epidemic. Hypertension, because of complications it causes, significantly influences a population's sickness and death rate. According to estimations, up to 25 percent of deaths among those over 40 years of age are caused by high blood pressure, either directly or indirectly. High blood pressure, along with other risk factors, quickens atherosclerosis (arterial sclerosis). Their transparency decreases gradually, then, leaving blood vessel walls less flexible. Blood circulation becomes insufficient and the organs' supply of necessary nutrients is therefore shortened. On a long-term basis, uncontrolled high blood pressure leads to tissue and vital organ (e.g. brain, kidneys, eyes) damage. Based on the facts stated, it is clear that the target users of an affordable generic antihypertensive drug fall within the wide population group of middle-aged people and seniors. At present, all large pharmaceutical companies (Merck, Bristol-Meyers, Novartis, Sanofi-Aventis) strive to develop anti-hypertensive group substances and average expected turnover from sales of each of these pharmaceuticals is estimated to be 1 - 2 billion dollars a year, after these pharmaceutical are introduced to the market. Considering the high costs of the new substances’ development, the relative high cost of these medications can also be expected and prices will fall, in general, after introducing generic pharmaceuticals to the market. The development of a brand new economical synthesis, applicable for low-cost production of generic pharmaceuticals, has a high prospect of application not only in the CZECH REPUBLIC (prominent generic pharmaceutical producers like Zentiva, Farmak and Teva, formerly Galena), but also among European producers. Along with that, a technologically simpler and cheaper production process will also enable price reductions and will subsequently increase European pharmaceutical producers' competitive advantage in comparison with growing Asian competition. The solution of the proposed development project requires appropriate technical equipment and, most of all, a team of experienced and erudite research workers. Asides from organic laboratories provided with state-of-the-art equipment, there is also an above-standard analytical laboratory at RATIOCHEM’s disposal, serving as necessary support for the research team. The chief research workers are authors of five patents of generic pharmaceutical original syntheses. They are also participating as inventors in five more patents of generic pharmaceutical intermediate developments.
Project ID: 
5 026
Start date: 
Project Duration: 
Project costs: 
760 000.00€
Technological Area: 
Organic Chemistry
Market Area: 
Pharmaceuticals/fine chemicals

Raising the productivity and competitiveness of European businesses through technology. Boosting national economies on the international market, and strengthening the basis for sustainable prosperity and employment.