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

Larotrectinib (LOXO-101)- Pharmacodynamics

Larotrectinib (VITRAKVIR) is an orally administered, small molecule, highly-selective, tropomyosin receptor kinase (TRK) inhibitor that was developed by Loxo Oncology in collaboration with Bayer AG.

Dec 13,2019  Inhibitors

AZD3759- preclinical and clinical studies

AZD3759 is a selective EGFR inhibitor that can fully penetrate the blood-brain barrier (BBB), with equal free concentrations in the blood, cerebrospinal fluid, and brain tissue.

Dec 13,2019  Inhibitors

Neratinib- pharmacology

Neratinib is an oral pan HER inhibitor that irreversibly inhibits the tyrosine kinase activity of epidermal growth factor receptors, EGFR (or HER1), HER2, and HER4.

Dec 13,2019  Inhibitors

AP26113- Pharmacodynamics

Brigatinib (AP26113) is a tyrosine kinase inhibitor with in vitro activity against a number of kinases, including ALK, ROS1, insulin-like growth factor-1 receptor (IGF-1R), FLT-3, and also epidermal g

Dec 13,2019  Inhibitors

BIBW2992 Dimaleate - Pharmacodynamics

Afatinib dimaleate (Tovok; BIBW2992; Gilotrif) is a salt form of Afatinib. Afatinib is a second-generation, orally administered, irreversible inhibitor of the ErbB family of tyrosine kinases.

Dec 13,2019  Inhibitors

Lenvatinib - pharmacodynamics

Lenvatinib (LenvimaTM) is a multitargeted receptor kinase inhibitor that inhibits the kinase activities of vascular endothelial-derived growth factor receptors.

Dec 13,2019  Inhibitors

PLX3397 (Pexidartinib)

Pexidartinib (TURALIO) is a novel, orally available small molecule tyrosine kinase inhibitor (TKI) with potent and selective activity against the colony-stimulating factor 1 (CSF1) receptor.

Dec 11,2019  Inhibitors

Medicinal Effect of Fenspiride Hydrochloride

Fenspiride hydrochloride {8-(2-phenylethyl)-1-oxa-3,8-diazaspiro[4,5]decan-2-one. HCl} with the CAS registry number 5053-08-7 is a whitish water-soluble microcrystalline solid. It is marketed in Europ

Dec 11,2019  Inhibitors

Applications of 3,3-Difluoroazetidine Hydrochloride

3,3-Difluoroazetidine hydrochloride(C3H6ClF2N) is colorless to yellow solid. 3,3-Difluoroazetidine hydrochloride can be considered as a fairly typical cyclic amine.

Dec 10,2019  Inhibitors

Biological Activity of Poziotinib (HM781-36B)

Poziotinib (HM781-36B) is a novel oral cancer cell inhibitor developed by Seoul Medical University in 2008. It is used for the treatment of breast and gastric cancer, and has targeted Small molecule i

Dec 10,2019  Inhibitors
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