Posted on 04/07/2022 3:35:34 PM PDT by ConservativeMind
A research team led by Prof. Liu Qingsong and Liu Jing from the Hefei Institutes of Physical Science (HFIPS) of the Chinese Academy of Sciences (CAS) has recently found that nintedanib, a multikinase inhibitor of the receptor tyrosine kinase FGFR/VEGFR/PDGFR, could be used in the treatment of drug-resistant gastrointestinal stromal tumors (GISTs). Results were published in Molecular Oncology.
GISTs are mesenchymal tumors that usually occur in the gastrointestinal tract. Nearly 85% of GISTs bear oncogenic mutations in mast/stem cell growth factor receptor (KIT). As the first-line therapy, imatinib has significantly improves GIST patient survival. However, most patients eventually experience disease progression due to KIT secondary mutations. Besides, activation of alternative signaling pathways may also lead to drug resistance.
Although several second- and third-generation KIT kinase inhibitors could overcome some of the KIT mutations conferring resistance, the low clinical responses and narrow safety window have limited their broad application. Therefore, there is still an urgent need for effective drugs to overcome the problem.
In this study, through high-throughput screening, the research team found that nintedanib, which has been approved for the treatment of idiopathic pulmonary fibrosis and non-small-cell lung cancer, exhibited strong inhibitory effects against a panel of primary gain-of function mutations and secondary drug resistance mutations of KIT kinase, especially the T670I mutation.
In vitro experiments showed that nintedanib significantly inhibited the proliferation of GIST cell lines and human primary GIST cells through the KIT signaling pathway.
In addition, they found that nintedanib overcame resistance mediated by extracellular signal–regulated kinase reactivation caused by upregations of fibroblast growth factor activity. In vivo antitumor efficacy has also been observed in several xenograft GIST models.
This study provides evidence for the repurposing of nintedanib as a new therapy to improve the treatment of GIST patients with de novo or acquired resistance to imatinib.
(Excerpt) Read more at medicalxpress.com ...
This drug company should be bought out, quadruple the drug prices and make a fortune. We should be able to buy a few senators votes for protection and live like kings.
I was more of a sega fan
Who the heck chooses these wacky drug names?! Is there some sort of protocol big pharma follows? And then every drug has at least two names . . .
There's some pattern to the generic names. For example, the "ib" at the end of "imatinib" stands for "inhibitor", as I recall. Imatinib inhibits the effect of one of the human growth factors.
The reason every drug ends up having two names is because the initial developer wants to take best advantage of patent protection. Until the patent on a drug expires, only the developing company can market it. After the patent expires, the developer hopes to maintain an advantage by having the public remember the brand name rather than the generic name.
Imatinib, the generic name, was developed by Novartis and sold under their brand name Gleevec. The Novartis patent ran out a couple of years ago. Hopefully the $300 per pill price has come down.
I’m waiting for super nintedanib, or even nintedanib 64!
Curcumin/Turmeric works wonders to prevent colon and gi cancers. Lot less expensive. Tastier. Add some to your chili recipe. Its like spicy orange umami.
This is some dangerous **** including gastrointestinal perforations. My pulmonary doctor (VA) pushed this on me. I told him to pound sand, I wasn’t going to take it under any circumstances. https://www.ofevhcp.com/
My 6 month appointments for the last three years have suddenly turned into an appointment a year from now. Does that make any sense. I see how that works. I think he fully intended to knock me off.
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