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Sunitinib - Europe PMC

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Last Updated: 18 July 2022

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Targeting the Akt/PI3K/mTOR signaling pathway for complete eradication of keloid disease by sunitinib.

Sunitinib, an oral small-molecule inhibitor of certain tyrosine kinase receptors, has shown significant therapeutic benefits in renal cell carcinoma and gastrointestinal stromal tumors. However, it has never been tested to see if keloid therapy is safe for keloids management. This research also aims to investigate the possibility of sunitinib as a keloid treatment. Moreover, a keloid explant culture model was successfully established and used to determine sunitinib's therapeutic effectiveness on nude mouse nude mice. Sunitinib was found to cause complete degeneration of keloid explant fragments in nude mice, resulting in greater therapeutic effectiveness than the most commonly used intralesional drug triamcinolone acetonide. Sunitinib blocks keloid formation in the absence of a standardized Akt/PI3K/mTOR pathway, thus making it more readily available as a monotherapy or mixed therapy for the safe treatment of keloid disease.

Source link: https://europepmc.org/article/MED/35802302


CircME1 promotes aerobic glycolysis and sunitinib resistance of clear cell renal cell carcinoma through cis-regulation of ME1.

Circular RNAs play vital roles in cellular cell carcinoma occurrences. Herein, we found circUNE1, which aids in ccRCC sunitinib resistance development. circME1 interacted with U1 snRNP at the promoter of its parent gene ME1, thus increasing aerobic glycolysis of ccRCC and promoting its malignant phenotype.

Source link: https://europepmc.org/article/MED/35798876


Optimizing the Sunitinib for cardio-toxicity and thyro-toxicity by scaffold hopping approach.

Sunitinib is a potent anti-cancer scaffold that also acts as a VEGFR-2 inhibitor. The current study seeks to optimize the Sunitinib's cardio-toxicity and thyrotoxicity by scaffold hopping using the admetSAR server. The optimization library of the optimized compounds was further screened by the molecular docking research, and results were confirmed by MD simulation and DFT analysis for VEGFR-2 inhibition. The highest affinity to VEGFR-2 receptor was seen in compounds 163, 432 with minimal cardiotoxicity and thyrotoxicity.

Source link: https://europepmc.org/article/MED/35791431


Hematologic toxicities of sunitinib in patients with gastrointestinal stromal tumors: a systematic review and meta-analysis.

Patients with imatinib-resistant gastrointestinal stromal tumors have a major survival benefit. However, the prevalence and risk of sunitinib-induced hematologic abnormalities in such a population are often ignored, and have not been well described. In patients with GIST, this meta-analysis was carried out to determine the overall incidence and risk of hematologic diseases due to sunitinib. The overall incidences of all-grade anemia, neutropenia, and thrombocytopenia in patients with GIST were 26. 2%, 41. 8%, and 36. 4%, respectively. There were 4. 7 percent for anemia, 7. 3 for neutropenia, and 5. 0% for thrombocytopenia at high-grade functions. Sunitinib was compared to placebo arms in an elevated risk of high-grade neutropenia with a RR of 10. 39. Conclusions Sunitinib has a relatively high incidence of hematologic disorders as well as a significant risk of high-grade neutropenia in patients with GIST.

Source link: https://europepmc.org/article/MED/35780257


Sunitinib Reduced the Migration of Ectopic Endometrial Cells via p-VEGFR-PI3K-AKT-YBX1-Snail Signaling Pathway.

The patient's ectopic endometrial cells were divided into two groups: the control group and the sunitinib group. In the cell of EMs, our team used Co-IP and protein spectrum assay to filtrate differential proteins between the two groups, and then, our analysis found a signaling pathway, p-VEGFR-PI3K-Snail. The result was as expected, with p-VEGFR, PI3K, AKT, YBX1, and snail measured in the control group and VEGFR+sunitinib group; then, the results were as expected. We found sunitinib reduced the number of heterotopic foci and reduced the number of heterotopic foci, YBX1, and snail by immunofluorescence in the EMs mouse model. sunitinib decreased the migration of ectopic endometrial cells as a result of the p-VEGFR-PI3K-Snail signaling pathway in both in vitro and in vivo experiments. Sunitinib, according to this report, is a potential target drug for EMs therapy.

Source link: https://europepmc.org/article/MED/35837295


Ocular delivery of sunitinib-loaded nanoparticles doped in tragacanthic acid hydrogel in treatment of diabetic retinopathy in rats.

Objection Diabetic retinopathy is a common microvascular complication of diabetes mellitus. Streptozotocin-induced DR in rats, and the rats were administered intravitreously a single dose of 20 b5L sunitinib solution, sunitinib-loaded nanoparticles in hydrogel, and bevacizumab solution. In the retina, a vascular endothelial growth factor concentration was measured. The results The results of the 20 u00b5L of sunitinib with a concentration of 25 u00b5g/mL was very efficient in DR without any changes in the retina or other side effects, according to the study. PGS/gelatin nanoparticles embedded in the injectable hydrogel and sunitinib's PGS/gelatin nanoparticles were as effective as bevacizumab in limiting DR. Although the sunitinib treatment improved VEGF production and neovascularization in the retina compared to the negative control group, it was not as effective as the nanoparticles. Conclusions The Sunitinib nanoparticles coated in TA hydrogel may be a safe substitute for bevacizumab in the treatment of DR.

Source link: https://europepmc.org/article/MED/35723593


Cost-effectiveness analysis of nivolumab plus cabozantinib versus sunitinib as first-line therapy in advanced renal cell carcinoma.

From a U. S. payer perspective, Aim: To determine the cost-effectiveness of first-line therapy for advanced renal cell carcinoma with nivolumab plus cabozantinib versus sunitinib. Conclusion: From a U. S. payer's viewpoint, first-line nivolumab plus cabozantinib for advanced renal cell carcinoma is not cost-effective.

Source link: https://europepmc.org/article/MED/35754404

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions