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A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases. Tyrosine kinases are enzymes responsible for the activation of many proteins by signal transduction cascades. The proteins are activated by adding a phosphate group to the protein (phosphorylation), a step that TKIs inhibit. TKIs are typically used as ...
Sorafenib is a small molecule inhibitor of many tyrosine kinase receptors such as VEGFR-2. Side effects are in most cases mild to moderate such as rash, hand-foot skin reaction, diarrhea and dermatitis, and occur in about 33-38% patients using sorafenib. Other side effects are mild hypertension, leukopenia and bleeding. Uncommon side effects ...
Axitinib, sold under the brand name Inlyta, is a small molecule tyrosine kinase inhibitor developed by Pfizer.It has been shown to significantly inhibit growth of breast cancer in animal models [4] and has shown partial responses in clinical trials with renal cell carcinoma (RCC) [5] and several other tumour types.
Ibrutinib is a potent, irreversible inhibitor of Bruton's tyrosine kinase (BTK). The acrylamide group of ibrutinib forms a covalent bond with the cysteine residue C481 in the BTK active site, leading to sustained inhibition of BTK enzymatic activity. BTK is an important signalling molecule of the B-cell antigen receptor (BCR) pathway, which ...
c-Met inhibitors are a class of small molecules that inhibit the enzymatic activity of the c-Met tyrosine kinase, the receptor of hepatocyte growth factor/scatter factor (HGF/SF). These inhibitors may have therapeutic application in the treatment of various types of cancers.
Remibrutinib is a small molecule drug that acts as a Bruton's tyrosine kinase (BTK) inhibitor. It is in development for the treatment of chronic spontaneous urticaria. [1] [2] In November 2023, Novartis announced that the compound "demonstrated clinically meaningful and statistically significant reduction in urticaria activity vs placebo" in a Phase III trial.
Gefitinib is a tyrosine kinase inhibitor that targets the epidermal growth factor receptor, inducing favorable outcomes in patients with non-small cell lung cancers. A common, widespread cancer, non-small cell lung cancer is the cause of death in more people than breast, colorectal, and prostate cancer together. [ 15 ]
Mobocertinib is a small molecule tyrosine kinase inhibitor structurally similar to osimertinib (differs only by the presence of an additional isopropyl ester group). [9] Its molecular target is epidermal growth factor receptor (EGFR) bearing mutations in the exon 20 region.
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