Inhibitor refers to substance that can hinder the chemical reactions, biological reactions (including immune response) and biological activity. In present time, commonly used inhibitors include immunosuppressants and inhibitors. 1. Immunosuppressive agents: immunosuppressants system refers to drug that can reduce the immune response. It can selectively suppress certain steps of the immune response and immune cells. Immune response refers to the body’s response to a variety of pathogenic substances. Some reactions are favorable to the body and can enhance the body's resistance to disease; some have adverse effects on the body and can cause tissue damage or disorders of physiological functions (allergy). Therefore, patients suffering from allergic reactions being harmful to the body should be subject to the treatment of immunosuppressant to affect the related immune processes and reduce the immune response of the body. For the treatment of various autoimmune diseases and weakening the tissue incompatibility, it has been developed of a variety of immunosuppressive agents, some of which have been widely used in clinical practice. Commonly used immunosuppressants include glucocorticoids (prednisone, prednisolone, etc.), alkylating agents (nitric oxide mustard, cyclophosphamide, thiotepa, busulfan, etc.), and antimetabolites (6- mercaptopurine, azathioprine, methotrexate, etc.). The mechanism of immunosuppressants, though not entirely clear, but is characterized by the following several aspects: ① most kinds of immunosuppressants can simultaneously inhibit cellular and humoral immunity and can be used for organ transplantation and autoimmune disease. ②Its inhibitory effect is strong for the primary immune response while the inhibitory effect against secondary response is weak. ③It can simultaneously act on normal and pathological immunity, therefore, can often lead to some complications. ④These drugs often have strong with serious adverse reactions. 2. Enzyme
An irreversible EGFR/HER2 dual tyrosine kinase inhibitor: Pyrotinib Maleate
Pyrotinib, an irreversible EGFR/HER2 dual tyrosine kinase inhibitor used for treating HER2-positive breast cancer, is primarily metabolized by cytochrome P450 (CYP)3A4 isozyme.
Jan 2，2024 Inhibitors
How to synthesize Lorlatinib?
Lorlatinib is an oral small molecule inhibitor of anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (ROS1) kinase developed by Pfizer for the treatment of ALK-positive non-small cell lung cancer.
Jan 2，2024 Inhibitors
Synthesis of Ripretinib
Ripretinib was synthesized by construction of a 1,6-naphtholide involving the junction of an α-aryl ester and appropriately functionalized 4-aminopyridine.
Jan 2，2024 Inhibitors
Pralsetinib: Synthesis and Introduction
Pralsetinib (BLU-667) is synthesised using bromopyridine as a raw material by chemical reaction.
Jan 2，2024 Inhibitors
How is Pemigatinib Synthesised?
Pemigatinib is synthesised using pyrrolopyridine as a raw material, firstly by synthesis of Pemigatinib Morpholine Intermediate and then by reduction, cyclisation and other reactions.
Jan 2，2024 Inhibitors
Synthesis of Ensartinib Dihydrochloride
Ensartinib Dihydrochloride is synthesised by a three-step reaction using piperazine as a raw material and the addition of the intermediate compounds Ensartinib Amino Pyridazine and Ensartinib Carboxyl
Jan 2，2024 Inhibitors
Synthesis of Cedazuridine
Cedazuridine is synthesised using gemcitabine precursor as raw material by chemical reaction.
Dec 29，2023 Inhibitors
Synthesis of Capmatinib Dihydrocholride
Capmatinib Dihydrocholride is synthesised from a quinoline fragment and a bis-aryl fragment of capmatinib by a late cyclisation reaction.
Dec 29，2023 Inhibitors
The synthesis method of Ivosidenib
Ivosidenib is a first-in-class, oral small molecule, potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (mIDH1).
Dec 28，2023 Inhibitors
The pharmacodynamics and Synthetic method of Fruquintinib
Fruquintinib, a highly potent and selective vascular endothelial growth factor (VEGFR)-1, -2, and -3 tyrosine kinase inhibitor.
Dec 28，2023 Inhibitors