HMG-CoA Reductase Inhibitors (Statins) Custom Development

BOC Sciences can provide development and manufacturing services for statin Featured APIs. Statins, also known as hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitors, are the most widely used and effective lipid-lowering drugs in the world. With the increase of cardiovascular and cerebrovascular diseases year by year, statins have become an indispensable part of the treatment and prevention of such diseases. Recently, the therapeutic use of statins has been increasingly recognized recently, so its economic impact on the pharmaceutical market is huge. We can provide you with the synthesis and industrial production of statin specialty APIs and key intermediates, and accelerate product launch, greatly improving your competitiveness in the industry.

What are Hydroxymethylglutaryl-CoA Reductase Inhibitors (Statins)?

Hydroxymethylglutaryl-CoA reductase inhibitors are drugs that lower cholesterol levels by inhibiting the enzyme HMG-CoA reductase. HMG-CoA reductase is involved in the production of cholesterol in the liver. By inhibiting this enzyme, the amount of cholesterol produced in the body can be reduced, thereby lowering blood cholesterol levels. Among them, statins are the most commonly used HMG-CoA reductase inhibitors.

HMG-CoA Reductase Inhibitors (Statins) Custom Development Fig. 1. Chemical structures of the statins.^[2]

Statins inhibit the rate-limiting enzyme in the process of cholesterol synthesis in the body, while promoting the metabolism of low-density lipoprotein (LDL) and increasing high-density lipoprotein (HDL-C). The molecular structures of several common statins are shown in Fig 1. According to the chemical structure, the mechanism of action of statins can be divided into three parts. The first part is an analog of the target enzyme substrate (HMGCoA). The second part is covalent to the substrate analog. The complex hydrophobic ring structure that connects and participates in the binding of statins to reductases. The third part is the side groups on the rings, which define the solubility properties of the drugs as well as many of their pharmacokinetic properties.^[1]

Our Statin Development Services

HMG-CoA Reductase Inhibitors (Statins) Custom Development

BOC Sciences is a leading supplier of research chemicals and pharmaceutical intermediates, including statins. We provide a series of services related to statin drug development, including custom synthesis of statin drugs and their intermediates, production process development and optimization, characterization and purity analysis services, and formulation development. Our statin development services include but are not limited to the following:

Catalytic Synthesis

We employ green and sustainable biocatalytic methods to prepare statins and are able to implement different biocatalytic pathways on an industrial scale for the stereoselective preparation of side chains (with stereocenters) of superstatins. The types of biocatalysts we use include nitrilases, ketoreductases and aldolases,etc.

Fermentative Synthesis

In addition to biocatalytic synthesis, we can also use microbial fermentation to prepare fermentation-derived statins. The microorganisms we use are mainly divided into two types of mold groups: Aspergillus and Penicillium, and the methods involved are submerged fermentation and solid-state fermentation.

Consistency Evaluation

Our consistency evaluation service mainly includes pharmaceutical equivalence and bioequivalence evaluation. The former is to evaluate whether the active ingredients, dosage, route of administration, and dosage form of the drug are consistent with the original drug and meet the drug quality standards; the latter verify that the absorption and metabolism of generic drug preparations in the body are consistent with the original drug.

BOC Sciences has extensive capabilities in the development of statins and can provide customized solutions to meet the specific needs of clients in the pharmaceutical industry. We can provide statin drug preclinical and clinical research contract research services according to customer project needs. Regulatory and registration support for statin drug development in different regions is also available at BOC Sciences. If you are interested in our custom development services, please contact us immediately.

References

Srinivasa, K. et al. An Overview of Statins as Hypolipidemic Drugs. International Journal of Pharmaceutical Sciences and Drug Research. 2011.
Hoyos, P. et al. Biocatalyzed Synthesis of Statins: A Sustainable Strategy for the Preparation of Valuable Drugs. Catalysts. 2019.

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