Micrograph showing an ALK positive adenocarcinoma of the lung. The ALK immunostain allows individuals with ALK rearrangements to be identified.
ALK inhibitors are anti-cancer drugs that act on tumours with variations of anaplastic lymphoma kinase (ALK) such as an EML4-ALK translocation.[1] They fall under the category of tyrosine kinase inhibitors, which work by inhibiting proteins involved in the abnormal growth of tumour cells. All the current approved ALK inhibitors function by binding to the ATP pocket of the abnormal ALK protein, blocking its access to energy and deactivating it.
A majority of ALK-rearranged NSCLC harbour the EML4-ALK fusion,[2] although as of 2020, over 92 fusion partners have been discovered in ALK+ NSCLC.[3] For each fusion partner, there can be several fusion variants depending on the position the two genes were fused at, and this may have implications on the response of the tumour and prognosis of the patient.[4]
^Nelsen R (15 January 2010). "ALK Inhibitors: Possible New Treatment for Lung Cancer". Medscape.
^Cite error: The named reference Farmer2010 was invoked but never defined (see the help page).
^Cite error: The named reference FusionCatalog was invoked but never defined (see the help page).
^Cite error: The named reference VariantPrognosis was invoked but never defined (see the help page).
brigatinib (also an inhibitor of mutated EGFR) was the latest second-generation inhibitor and was approved in April 2017 by the US FDA for ALK-positive NSCLC...
non-small cell lung cancer. It is an orally administered inhibitor of anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (ROS1), two enzymes that play a...
malignant neoplasms. It also acts as an ALK (anaplastic lymphoma kinase) and ROS1 (c-ros oncogene 1) inhibitor. Crizotinib is indicated for the treatment...
is a tyrosine kinase inhibitor that selectively and potently inhibits anaplastic lymphoma kinase (ALK). In normal physiology, ALK functions as a key step...
tyrosine kinase inhibitor (TKI), of the tropomyosin receptor kinases (TRK) A, B and C, C-ros oncogene 1 (ROS1) and anaplastic lymphoma kinase (ALK). The most...
kinase (ALK) also known as ALK tyrosine kinase receptor or CD246 (cluster of differentiation 246) is an enzyme that in humans is encoded by the ALK gene...
"Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALKInhibitor That Potently Inhibits ROS1/TRK/ALK Solvent- Front Mutations". Cancer Discovery. 8 (10):...
ALK positive lung cancer is a primary malignant lung tumor whose cells contain a characteristic abnormal configuration of DNA wherein, most frequently...
ceritinib. Those treated with ALK inhibitors who relapse can then be treated with the third-generation ALKinhibitor lorlatinib. Up to 5% with NSCLC have...
Brigatinib acts as both an anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR) inhibitor.[medical citation needed] Brigatinib could overcome...
second-generation ALKinhibitors including ceritinib, alectinib and brigatinib. Resistance to ALKinhibitors can occur with novel acquired ALK mutations or...
lung cancer (NSCLC). It blocks the activity of anaplastic lymphoma kinase (ALK). It is taken by mouth. It was developed by Chugai Pharmaceutical Co. Japan...
SU11654 (Toceranib), was also approved for cancer in dogs, and the ALKinhibitor Crizotinib also grew out of a SUGEN program. In October 2006, the company...
kinases. Work started at Sugen also contributed to the development of the ALKinhibitor crizotinib (Xalkori), FDA-approved for NSCLC in 2011. Sugen also generated...
hypertension. Dalantercept is an experimental ALK1 inhibitor. (Not to be confused with anaplastic lymphoma kinase (ALK) ) ALK4 is ACVR1B, ALK7 is ACVR1C, and ALK5...
first of these drugs to enter clinical trials and is the sole available ALKinhibitor, approved by the FDA on August 26, 2011. Thus far, it has proven its...
relevant subgroup as they can be very effectively treated with the ALKinhibitor crizotinib. Apart from cancers, CISH has also been shown to be useful...
targeted therapy. Janus kinase inhibitors, e.g. FDA approved tofacitinib ALKinhibitors, e.g. crizotinib Bcl-2 inhibitors (e.g. FDA approved venetoclax...
A protein kinase inhibitor (PKI) is a type of enzyme inhibitor that blocks the action of one or more protein kinases. Protein kinases are enzymes that...
suppressor genes. When used in combination with other drugs such as an ALK or an MEK inhibitor, ribociclib has been shown to have a synergistic effect, resulting...
recurrent disease might benefit by adding the ALKinhibitor, crizotinib, or a tyrosine kinase inhibitor, either larotrectinib or entrectinib, to surgical...
anaplastic lymphoma kinase ALK-NF1-RAS/ERK signaling pathway in flies. Pharmacological treatment using a highly-specific ALKinhibitor corrected all these defects...
ALK - Anaplastic lymphoma kinase or ALK tyrosine kinase receptor. ALK plays an important role in the development of the brain. Several ALK-inhibitor drugs...
doi:10.1056/NEJMoa061884. PMID 17167137. "ALKinhibitor crizotinib has high response rate in patients with ALK-positive NSCLC". HemOncToday. 2010-06-05...
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