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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 ...
Imatinib use may cause lightening/depigmentation or darkening/repigmentation of hair (as is the case with some other tyrosine kinase inhibitors) and/or skin as well as hyperpigmentation of the gingiva. The median onset of hair color change is 4 weeks after initiation of therapy (but may occur over a year after initiation), is dose-dependent ...
Nilotinib is a selective Bcr-Abl kinase inhibitor. [13] [18] Nilotinib is 10-30 fold more potent than imatinib in inhibiting activity of the Bcr-Abl tyrosine kinase and proliferation of Bcr-Abl expressing cells. [12] [18] [20] [21] The drug effectively inhibits the auto phosphorylation of Bcr-Abl on Tyr-177 that is involved in CML pathogenesis ...
Inhibitors of tyrosine kinase are mainly used against some specific forms of cancer. Subcategories. This category has the following 2 subcategories, out of 2 total. ...
IDRX-42 (formerly M4205) is a highly selective small molecule KIT inhibitor compound developed for the treatment of gastrointestinal stromal tumors. [1] [2] [3] The compound was originally discovered by the German company Merck [4] and later out-licensed to IDRX. In November 2024, promising anti-tumor data from ongoing Phase 1/1B studies were ...
Ibrutinib, sold under the brand name Imbruvica among others, is a small molecule drug that inhibits B-cell proliferation and survival by irreversibly binding the protein Bruton's tyrosine kinase (BTK). Blocking BTK inhibits the B-cell receptor pathway, which is often aberrantly active in B cell cancers.
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.
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