跳至主要内容

Six Directions of Chemical Synthesis Drug Research and Development

As an important part of the development of the pharmaceutical industry, chemically synthesized drugs are the main source of drug candidates, as well as a high-input, high-output and high-efficiency work. The main directions for chemical synthesis drug research and development are as follows.

Medicilon can undertake the synthesis of special reagents, intermediates and molecular fragments, preparation of standard products, synthesis design and preparation of impurities or metabolites, synthesis of stable isotope internal standards and synthesis of tritiated compounds.

Research and Develop New Chemical Entity Drugs

New Chemical Entities (NCE) drugs refer to newly discovered drugs with new chemical structures, creating “NCE” new drugs. The research and development of breakthrough new drugs is guided by the latest medical theories, based on the principles of modern new drug design, and uses structure-activity relationships, analytical methods, and computer-aided drug design to synthesize a batch of new compounds, from which lead compounds with the expected activity are screened. Then the structure is optimized and modified, and the research finds the NCE that can finally be developed into a breakthrough new drug. As a series of products of various major categories of chemically synthesized drugs are successively marketed, the speed of discovering new drug monomer compounds is slowing down, and research and development costs are getting higher and higher. Among the new products on the market in recent years, anti-infective drugs, cardiovascular drugs, central nervous system drugs and anti-cancer drugs dominate.

Medicilon provides new drug research and development outsourcing services, and has established a company in Shanghai that integrates compound synthesis, compound activity screening, structural biology, pharmacodynamic evaluation, pharmacokinetic evaluation, toxicological evaluation, formulation research and new drug registration. A comprehensive technical service platform of international standards, and has been recognized by the international drug administration.

Create  “Me-Too” New Drug-Research and Development of Imitation New Drugs

The imitative innovation of new drugs (Me-too) refers to the use of the research results of the mechanism of action and structure-activity relationship of known drugs, without infringing on the patents of others, to carry out molecular modifications based on the analysis of the chemical structure of the known drugs. Design and synthesize the drug’s derivatives, structural analogs and structure-related compounds, and through systematic pharmacological research, a new drug research and development method for the purpose of generating new drugs, and the new drugs produced are compared with known drugs. It has the characteristics of high activity or similar activity. Because the research and development funds and risks of the new compound (NCE) are very high, most companies have chosen the “Me-too” drug research and development path. The main methods of the Me-too strategy in the research and development of new drugs include the application of bioelectronic isostere replacement, prodrug design, and chiral drug research.

Further Research and Development of Known Drugs

Extensive new drug research and development is a common way to modify or transform known drugs (including the effective ingredients of medicinal plants), and create new drugs with stronger specificity, higher efficacy or better safety. Continue research on existing drugs (drugs with expired patents of individual companies) and make more ideal derivatives or precursors (such as better physical and chemical properties, higher bioavailability, or targeting, etc.). Pay attention to.

Pharmaceutics Research and Development of Existing Drugs

The development of new formulations is to carry out pharmacy research and development on the basis of affirmative curative effect, such as the application of new pharmaceutical excipients or new formulation technologies, research and development aimed at improving the quality of treatment, especially new formulations with improved bioavailability, or design, The development of new dosage forms and compound preparations, etc., can not only be easier to approve, but also help extend the patent protection period of the original product. It is a new product research and development work with low investment, low risk, and possibly excellent economic benefits. In recent years It has been valued by all pharmaceutical companies, and some have achieved great success.

Research on New Uses of Existing Drugs

Development of drugs with new indications The discovery of new uses of drugs is actually the discovery of new indications for the treatment of certain drugs in addition to the original treatment of conventional diseases. New use of drugs is an important direction of new drug research and development, and it is also a very active field in current clinical pharmacy with rapid development. New uses of drugs are generally found in the pharmacological research phase of drugs (including clinical and non-clinical), and even some new indications for drug treatment are directly based on the information feedback of doctors or patients. The study of drug pharmacological mechanisms is the fundamental way to discover new uses of drugs. one.

To Circumvent Patented Processes

Applying modern new technology to research the production process of products to avoid patent technology “Avoiding patent technology” means that the production process of chemical raw materials is included in the production process of pharmaceuticals, avoiding the production process routes listed in the patent scope of the original research enterprise, and adopting Innovative processes other than patents produce the same APIs. For example, the research and development of the domestically produced “Tamiflu” or “Military Coover” has adopted a method of avoiding patented technology. Although “Junkeaowei” is an imitation of “Tamiflu”, it has adopted the strategy of “imitation first and then invented” and innovated in production process and dosage form, thus obtaining independent intellectual property rights. “Junkeowei” has also become the world’s first approved non-azide route to produce oseltamivir phosphate.

At present, chemically synthesized drugs are still relatively effective, commonly used, and a large number of important therapeutic drugs. They are also the subject of drug research and development of major pharmaceutical research and development companies, and they have good development prospects.

标签：

评论

发表评论

此博客中的热门博文

What is preclinical testing?

In the process of  preclinical testing  of a compound or biological agent into a drug, the compound involved must go through the testing phase. First, we need to identify potential targets that can treat the disease. Then, a variety of compounds or preparations are screened out. Any compound that has shown potential as a drug for the treatment of this disease needs to be tested for toxicity before clinical testing to reduce the possibility of injury. preclinical testing What is the basis of preclinical testing? According to US Food and Drug Administration (FDA) regulations, a series of tests are required before a new drug is approved for use. In the first stage, basic research determines a hypothetical target for the treatment of a certain disease, and then screens small molecules or biological compounds to discover any substance with the potential to treat the disease. Then, a  preclinical research  phase followed, before which, as described above, the potential toxicity of the compou
发表评论
阅读全文

Inventory of the three major in vitro pharmacokinetic research methods

  The metabolic properties of a compound are an essential factor in whether or not it can be used as a drug in the clinical setting, so pharmacokinetic studies of newly synthesized compounds are required in drug development. In vitro incubation with liver microsomes, recombinant CYP450 enzyme lines, and in vitro incubation with hepatocytes are some of the more common in vitro drug metabolism methods. 1. In vitro incubation method with liver microsomes The metabolic stability and metabolic phenotypes of candidate compounds in different species of liver microsomes are good predictors of the metabolic properties of compounds in vivo. They are practical tools for evaluating candidate compounds in the pre-development phase of drug development. Liver microsomes include rat liver microsomes, human liver microsomes, canine liver microsomes, monkey liver microsomes, and mouse liver microsomes. In in vitro incubation of the liver, microsomes are the "gold standard" for in vitro d
发表评论
阅读全文

Novel Parkinson’s Therapies Possible with New Mouse Model

Parkinson's disease (PD) is a neurodegenerative disorder that is marked by the accumulation of the protein, α-synuclein (αS), into clumps known as Lewy bodies, which diminish neural health. Now, researchers from Brigham and Women's Hospital (BWH) report the development of a mouse model to induce PD-like αS aggregation, leading to resting tremor and abnormal movement control. The mouse responds to L-DOPA, similarly to patients with PD. The team's study (“Abrogating Native α-Synuclein Tetramers in Mice Causes a L-DOPA-Responsive Motor Syndrome Closely Resembling Parkinson’s Disease”) on the use of this transgenic mouse model appears in  Neuron . “α-Synuclein (αS) regulates vesicle exocytosis but forms insoluble deposits in PD. Developing disease-modifying therapies requires animal models that reproduce cardinal features of PD. We recently described a previously unrecognized physiological form of αS, α-helical tetramers, and showed that familial PD-causing missense mutati
发表评论
阅读全文