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Everolimus - DOAJ

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Last Updated: 07 September 2022

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Asphericity of Somatostatin Receptor Expression in Neuroendocrine Tumors: An Innovative Predictor of Outcome in Everolimus Treatment?

BACKGROUP - In patients with gastroenteropancreatic neuroendocrine tumors, the mTOR inhibitor everolimus is associated with a significant rise in progression-free survival. This paper examined the relative asphericity of pretherapeutic somatostatin receptor imaging as the first imaging-based prognostic marker for PFS. All 30 patients had metachronous or progressive liver metastases, according to the study. Median PFS was 6. 7 months for ASP > 12. 9% vs. 14. 4 months for ASP u2264 12. 9% compared to 14. 4 months for ASP 00269 12. 9%. Conclusion : Pretherapeutic ASP of SSR positive lesions has independently forecast the PFS for treatment with everolimus in GEP-NET. ASP can perform risk-benefit analysis before patient admission to treatment.

Source link: https://doi.org/10.3390/diagnostics10090732


Everolimus Nanoformulation in Biological Nanoparticles Increases Drug Responsiveness in Resistant and Low-Responsive Breast Cancer Cell Lines

We have produced a new Eve nanoformulation that uses H-ferritin nanocages to enhance Eve's efficiency. To raise Eve's efficiency, we have created a new Eve nanoformulation that uses H-ferritin nanocages to increase its subcellular delivery. Breast cancer cells overexpressing TfR-1 were successfully detected by H-Ferritin, demonstrating fast nanocage internalization. In vitro efficacy in sensitive and resistant breast cancer cells, HEve has been tested and compared to Eve. In vitro, Nanoformulated Eve exhibited remarkable antiproliferative activity, making even impermeable cell lines sensitive to Eve. In a panel of Eve-sensitive or resistant breast cancer cell lines, our results show that optimizing Eve subcellular delivery, thanks to nanoformulation, results in its improved antitumor activity.

Source link: https://doi.org/10.3390/pharmaceutics11080384


Palbociclib Plus Fulvestrant or Everolimus Plus Exemestane for Pretreated Advanced Breast Cancer with Lobular Histotype in ER+/HER2− Patients: A Propensity Score-Matched Analysis of a Multicenter Retrospective Patient Series †

In patients with metastatic breast cancer, Cyclin-dependent kinase 4/6 inhibitors in combination with endocrine therapy have demonstrated significant safety and tolerability, but the correct sequence of ET has yet to be established. When receiving second line CDK4/6i, it is not clear if patients with lobular breast carcinomas derive the same benefits. This retrospective review compared the efficacy of palbociclib plus exemestane as second-line ET for hormone-resistant metastatic LBC. PFS was found to be significantly longer for patients treated with EVE u2013EXE than PALBO U2013FUL, according to the propensity score report.

Source link: https://doi.org/10.3390/jpm10040291


Therapeutic Response of CCKBR-Positive Tumors to Combinatory Treatment with Everolimus and the Radiolabeled Minigastrin Analogue [ 177 Lu]Lu-PP-F11N

Everolimus' inhibition of the mammalian target of rapamycin complex 1 by everolimus has been shown to increase the tumor uptake of radiolabeled min. . . . trins. In combination with RAD001, the N-terminal DOTA-conjugated gastrin analogue PP-F11N was used to determine treatment efficiency in the human A431/CCKBR xenograft nude mouse model. After undergoing radiation therapy with RAD001 and [177 Lu]Lu-PP-F11N did not show significant adverse effects, the histological examination of kidney and stomach dissected was not revealed. In conclusion, our analysis results indicate that mTORC1 inhibition may have the ability to enhance the therapeutic efficacy of radiolabeled min. . . . trin analogues in CCKBR-positive cancers.

Source link: https://doi.org/10.3390/pharmaceutics13122156


Achromobacter denitrificans pneumonia in a kidney transplant recipient – dose-dependent decrease of phagocytic activity as a potential mechanism for everolimus pulmonary toxicity

Increased risk of pulmonary toxicity have been reported by a Mammalian target of rapamycin inhibitors inclusive regimens, but the underlying mechanism hasn't been elucidated so far. When compared to the control group's control healthy person, the ability of phagocytosis and oxidative burst generation against A. denitrificans and Escherichia coli was dramatically reduced on EVR therapy, and it was significantly improved after 3 weeks of EVR absence. Our results indicate that dose-dependent reduction of neutrophil/monocyte phagocytic production and oxidative burst formation could be a potential cause of EVR respiratory toxication.

Source link: https://doi.org/10.5114/ceji.2021.108762


Machine learning algorithms to estimate everolimus exposure trained on simulated and patient pharmacokinetic profiles

Abstract Everolimus is an immunosuppressant with a slim therapeutic index and high between-u2010patient variation. The best indicator of exposition is the area under the concentration versus time line, but measuring it requires taking multiple blood samples. XGBoost was first trialled on 508 patient interdose AUCs using MAP_u2010BE, and then on 500 u201310,000 robust interdose PK profiles simulated using previously published population PK results. The AUC's estimate, according to an external database of 114 complete U2010PK profiles, was impressive and marginally higher than MAPu2010BE. The ML algorithm's results were not improved by using more profiles, which did not improve the ML algorithm's results. Compared to patient data alone, the contribution of mixing patient and simulated profiles was significant only when they were in balanced numbers, with 500 for each compared to placebo data alone.

Source link: https://doi.org/10.1002/psp4.12810


A predictive model involving serum uric acid, C-reactive protein, diabetes, hypercholesteremia, multiple lesions for restenosis risk in everolimus-eluting stent-treated coronary heart disease patients

Hundreds of patients with coronary heart disease underwent percutaneous coronary intervention with EES were included in this study, along with its predictive factors. ResultsInt-stent restenosis status was assessed 1 year after PCI with EES, 20 patients recovered in-stent restenosis within 1 year, while 215 patients did not experience in-stent restenosis, resulting in a 1-year restnosis rate of 8. 5%, which translated in a 1-year post-PCI with EES. Conclusion: Based on these independent risk factors, the in-stent restenosis risk prediction system, which included diabetes mellitus, hypercholesteremia, SUA, HsCRP, and patients with two target lesions, can help to identify in-stent restenosis risk in patients with CHD who underwent post-PCI with EES.

Source link: https://doi.org/10.3389/fcvm.2022.857922


A comparative study of combination treatments in metastatic 4t1 cells: everolimus and 5- fluorouracil versus lithium chloride and 5-fluorouracil

In 4T1 metastatic breast cancer cells and compared to placebo and each other, the effects of 5-fluorouracil alone with everolimus or lithium chloride were investigated in the present study. The results indicated that the combination of 5FU-LiCl and apoptosis significantly more cells cytotoxicity and apoptosis were both significantly more than EVE-5FU, but that these findings could be used in clinical trials, pointing to a clinical possibility for both types of metastatic breast cancer.

Source link: https://doi.org/10.3897/pharmacia.69.e85358

* 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