Inhibitors

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

A JAK2 inhibitor: Fedratinib

Fedratinib is a JAK2 inhibitor approved for treating adult patients with intermediate-2 or high-risk primary or secondary myelofibrosis.

Jan 19,2024  Inhibitors

Erdafitinib can be used to treat urothelial cancer

Erdafitinib, also known as JNJ-42756493, is a first-in-class pan-fibroblast growth factor receptor (FGFR) kinase inhibitor discovered by Astex Pharmaceuticals and Janssen.

Jan 19,2024  Inhibitors

Belumosudil: Synthesis and Description

Belumosudil is an orally active Rho-associated coiled-coil-containing protein kinase-2 (ROCK2) inhibitor recently approved for chronic graft-versus-host disease (cGVHD) after failure of two prior line

Jan 17,2024  Inhibitors

How is Difamilast synthesised?

Difamilast is synthesised in two steps by chemical reaction using the monobenzylated protocatechuic acid ethyl ester as a raw material.

Jan 17,2024  Inhibitors

Voclosporin: Synthesis and Description

Voclosporin is a calcineurin inhibitor immunosuppressant that received its first approval by the USFDA for the treatment of active lupus nephritis, making it the first oral therapy approved in the US

Jan 17,2024  Inhibitors

Abrocitinib: Synthesis and Application

Abrocitinib is synthesised using ketoester as a raw material by chemical reaction. Abrocitinib is an orally available small-molecule Janus Kinase 1 (JAK1) inhibitor developed by Pfizer and approved i

Jan 16,2024  Inhibitors

Odevixibat: Synthesis and Application

Odevixibat is synthesised in two steps by chemical reaction using enfumafungin as a raw material.

Jan 16,2024  Inhibitors

How is Atogepant synthesised?

Atogepant was synthesised from the late-stage amide coupling of two highly complex fragments (Carboxylic Acid Fragment and Spirocyclic Motif Fragment).

Jan 15,2024  Inhibitors

The synthesis method of Upadacitinib hemihydrate

Upadacitinib, a once-daily orally administered selective JAK1 inhibitor developed by AbbVie, was approved for the treatment of moderate to severe RA.

Jan 11,2024  Inhibitors

How to synthesize Solriamfetol?

Solriamfetol is a selective dopamine and norepinephrine reuptake inhibitor.

Jan 9,2024  Inhibitors
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