Peptide APIs are the active ingredient used in the production of polypeptide pharmaceutical preparations. Compared with chemical APIs and protein APIs, peptide APIs have some characteristics of both due to their molecular weight between them. Peptide APIs not only have the characteristics of good stability, high purity and controllable quality of small molecule chemical drugs, but also have the characteristics of strong specificity and high biological activity of protein drugs.
As the active ingredient of drugs, peptides API are used to prepare peptide drugs, which are often used in disease prevention, diagnosis and treatment. According to the function of peptide APIs, they can be divided into peptide vaccine, anti-tumor peptide, antiviral peptide, peptide-oriented drug, cytokine mimic peptide, antibacterial active peptide, diagnostic peptide, etc., which are mainly used for the treatment of asthma, allergy, hepatitis, AIDS, tumor, diabetes and other diseases.
But peptide drugs have a single route of administration, and cannot be taken orally. On the one hand, because peptide drugs are affected by peptidase, they are easy to be degraded, with short half-life and low stability. On the other hand, because peptide drugs are difficult to pass through the intestinal mucosa, the main route of administration is intravenous injection or drip.
There are about 100 kinds of peptides on the market around the world, mainly focusing on the treatment of chronic diseases such as anti-tumor, diabetes, immune regulation and cardiovascular diseases. The major blockbuster varieties with sales of over $1 billion are glarirelle, liraglutide, dula glucotide, octreotide, leipperaline, telipatide, exenatide and goseraline.
The stability of peptide APIs is an important factor restricting its development. In order to enhance the stability of peptide structure, researchers are committed to optimizing the stability by modifying the peptide structure and adding barriers. The transformation of peptide is to transform the peptide into a ring type, modify the amino acid skeleton, insert non-natural amino acids, replace individual amino acids, coupled with polyethylene glycol, lipid and protein structures, prolong the half-life of protein, to increase the stability of peptide, reduce the frequency of injection of peptide drugs.