- |||||||||| simvastatin / Generic mfg., fluvastatin / Generic mfg.
Journal: Simvastatin and fluvastatin attenuate trauma-induced cell death and catabolism in human cartilage. (Pubmed Central) - Sep 29, 2022 However, while long-term administration of statins for 4 weeks impaired chondrogenic redifferentiation, addition of simvastatin at low concentrations for 1 week exhibited a slightly promoting effect. In conclusion, our data imply that simvastatin and fluvastatin are suitable in terms of initial harm reduction after cartilage trauma.
- |||||||||| fluvastatin / Generic mfg.
Journal: SARS-CoV-2 disrupts respiratory vascular barriers by suppressing Claudin-5 expression. (Pubmed Central) - Sep 29, 2022 CLDN5 overexpression or Fluvastatin treatment rescued the SARS-CoV-2-induced respiratory endothelial barrier disruption. We concluded that the down-regulation of CLDN5 expression is a pivotal mechanism for SARS-CoV-2-induced endothelial barrier disruption in respiratory organs and that inducing CLDN5 expression is a therapeutic strategy against COVID-19.
- |||||||||| Journal: Lipid-lowering drugs. (Pubmed Central) - Sep 20, 2022
We concluded that the down-regulation of CLDN5 expression is a pivotal mechanism for SARS-CoV-2-induced endothelial barrier disruption in respiratory organs and that inducing CLDN5 expression is a therapeutic strategy against COVID-19. No abstract available
- |||||||||| Journal: Systems assessment of statins hazard: Integrating in silico prediction, developmental toxicity profile and transcriptomics in zebrafish. (Pubmed Central) - Sep 10, 2022
72 h LC values for lovastatin, simvastatin, fluvastatin, atorvastatin, rosuvastatin, and pravastatin were 0.01 μM, 0.04 μM, 1.93 μM, 37.28 μM, 79.29 μM, and 2170 μM, respectively...Finally, the ecotoxicity profile of statins was predicted by in silico method, and statins were high or moderate risk to aquatic organisms. We provide a systems toxicology strategy to explore the toxicity of statins and illustrate the potential mechanisms of action.
- |||||||||| Livalo (pitavastatin) / Kowa, Eli Lilly
Journal: Is The Protein-Mediated Uptake Of Drugs By OATPs A Real Phenomenon Or An Artifact? (Pubmed Central) - Sep 3, 2022 In contrast, this was not the case for OATP1B1-mediated uptake of pitavastatin and passive uptake of cerivastatin, suggesting that the PMUE is a real phenomenon for these drugs...Future experiments on PMUE must take into consideration such NSB. In addition, mechanisms other than PMUE need to be explored to explain the underprediction of in vivo OATP-mediated hepatic drug CL from in vitro uptake studies.
- |||||||||| Paxlovid (nirmatrelvir and ritonavir) / Pfizer
Review, Journal: Cholesterol-lowering drugs for high-risk hypercholesterolemia patients with COVID-19 while on Paxlovid™ therapy. (Pubmed Central) - Aug 10, 2022 Since an abrupt withdrawal of statin use may cause serious negative rebound effects on the cardiovascular system, it is essential to continue statin treatment also during the 5-day Paxlovid treatment period. During Paxlovid treatment, simvastatin and lovastatin need to be substituted with another statin, such as pravastatin or fluvastatin, while a reduction of the dose of atorvastatin and rosuvastatin is recommended.
- |||||||||| fluvastatin / Generic mfg.
C3-arylation of indole using organobismuthin reagent | Poster Board #2166 (Hall F2 (McCormick Place Convention Center)) - Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_12999; This motif can be found in a large variety of bioactive molecules such as Fluvastatine 1 that targets the HMG-CoA receptor to lower the LDL cholesterol and compound 2 which was identified as a potential treatment against the uterine fibroid and targets progesterone receptors (Figure 1a)...Herein, we report our results on the C3-arylation of indoles using pentavalent organobismuth compounds. The reaction, which is based on the work of Barton,5 uses catalytic amounts of copper(II) trifluoroacetate, operates under simple conditions and shows excellent substrate and bismuth scope (Figure 1b).
- |||||||||| Review, Journal: Pathobiology of the Klotho Antiaging Protein and Therapeutic Considerations. (Pubmed Central) - Jul 30, 2022
In preclinical work, antidiabetic drugs (metformin, GLP-1-based, GABA, PPAR-γ agonists) also enhanced Klotho...Notably, exercise and sport activity increased Klotho. This review addresses molecular, physiological and therapeutic aspects of Klotho.
- |||||||||| metformin / Generic mfg., aspirin / Generic mfg., fluvastatin / Generic mfg.
Journal, Heterogeneity: The molecular heterogeneity of the precancerous breast affects drug efficacy. (Pubmed Central) - Jul 27, 2022 However, the nonspecific inhibitors, aspirin and metformin, were equally ineffective in inhibiting proliferation across the progression model. Our data provides proof-of-principle that in the prevention domain, treatment with agents developed to target specific pathways, will need to consider the molecular heterogeneity of the precancerous breast in order to achieve maximum efficacy.
- |||||||||| Journal: A practical strategy to develop isoform-selective near-infrared fluorescent probes for human cytochrome P450 enzymes. (Pubmed Central) - Jul 20, 2022
Using our double-filtering approach, probes S9 and S10 were successfully developed for the real-time and selective detection of CYP2C9 and CYP2J2, respectively, to facilitate high-throughput screening and assessment of CYP2C9-mediated clinical drug interaction risks and CYP2J2-associated disease diagnosis. These observations suggest that our strategy could be used to develop the isoform-specific probes for CYPs.
- |||||||||| nafamostat / Generic mfg.
Journal: Identification of nafamostat mesylate as a selective stimulator of NK cell IFN-γ production via metabolism-related compound library screening. (Pubmed Central) - Jun 22, 2022 Our data showed that eight compounds (nafamostat mesylate (NM), loganin, fluvastatin sodium, atorvastatin calcium, lovastatin, simvastatin, rosuvastatin calcium, and pitavastatin calcium) and three compounds (NM, elesclomol, and simvastatin) increased the proportions of NK cells and CD3 T cells that expressed IFN-γ among PBMCs cultured with IL-12 and IL-15, respectively...However, NM showed no effect on NK cell cytotoxicity. Collectively, our study identifies NM as a selective stimulator of IFN-γ production by NK cells, providing a new strategy for the prevention and treatment of infection or cancer in select populations.
- |||||||||| fluvastatin / Generic mfg.
Journal: Therapeutic effect of fluvastatin on medication-related osteonecrosis of the jaw. (Pubmed Central) - Jun 11, 2022 Collectively, our study identifies NM as a selective stimulator of IFN-γ production by NK cells, providing a new strategy for the prevention and treatment of infection or cancer in select populations. This study suggests that a single topical administration of fluvastatin may be a novel treatment for medication-related osteonecrosis of the jaw.
- |||||||||| Livalo (pitavastatin) / Kowa, Eli Lilly
Biomarker, Journal: Combining familial hypercholesterolemia and statin genetic studies as a strategy for the implementation of pharmacogenomics. A multidisciplinary approach. (Pubmed Central) - Jun 4, 2022 Of these 221 patients, 66.5% were carriers of actionable variants in any of the studied pharmacogenomic pathways: 46.6% of patients in one pathway, 19.0% in two pathways, and 0.9% in three pathways. 45.7% of patients could have a response to atorvastatin different from that of the reference population, 45.7% for simvastatin and lovastatin, 29.0% for fluvastatin, and 6.7% patients for pitavastatin.This implementation approach facilitates the incorporation of pharmacogenomic studies in clinical care practice, it does not add complexity nor additional steps to laboratory processes, and improves the pharmacotherapeutic process of patients.
- |||||||||| atorvastatin / Generic mfg., fluvastatin / Generic mfg.
Journal: Statins downregulate YAP and TAZ and exert anti-cancer effects in canine mammary tumor cells. (Pubmed Central) - May 19, 2022 Taken together, our results demonstrate for the first time that statins act upon the Hippo pathway in CMT cells to counteract several molecular and cellular hallmarks of cancer. These findings suggest that targeting the Hippo pathway with statins represents a novel and promising approach for the treatment canine mammary gland cancers.
- |||||||||| Livalo (pitavastatin) / Kowa, Eli Lilly
Preclinical, Journal: Development and validation of an HPLC method to be used for simultaneous detection and quantification of different statins after ex vivo skin diffusion studies. (Pubmed Central) - Apr 9, 2022 A novel high performance liquid chromatography (HPLC) method was developed and validated to simultaneously analyse all statins currently available globally (atorvastatin, fluvastatin, lovastatin, mevastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin)...The limit of detection (LOD) and limit of quantification (LOQ) values were found to be within the permissible criteria of ≤15% and ≤20%, respectively. Following an appropriate investigation of all the parameters for method validation, it was confirmed that the HPLC method was successfully validated and proven to be accurate to simultaneously quantify statins even in combination with other excipients used during the formulation of nano-emulsions and nano-emulgels.
- |||||||||| fluvastatin / Generic mfg.
Loss of isoprenylation significantly reduces IgE mediated mast cell activation (Exhibit Hall; P236) - Apr 8, 2022 - Abstract #IMMUNOLOGY2022IMMUNOLOGY_480; Previous findings showed repurposing of statin drugs, such as Fluvastatin, reduced allergic symptoms in vitro and in vivo...Finally, we show that FGTI-2734 can significantly reduce IgE-induced cytokine production from human skin mast cells. These data show that dual farnesyl and geranylgeranyl transferase inhibitors may be an effective therapeutic treatment for mast cell-associated diseases.
- |||||||||| fluvastatin / Generic mfg.
Journal: The Effects of Fluvastatin on Indian Hedgehog Pathway in Endochondral Ossification. (Pubmed Central) - Apr 7, 2022 This led to the promotion of cell proliferation, increase of the hypertrophic chondrocyte layer, inhibition of apoptosis, and decrease in mineralization. This study demonstrated that statins had an influence on Ihh, and that the hyperfunction of Ihh may prevent premature cell death caused by FGFR3-related chondrodysplasia through an indirect increase in the expression of PTHrP.
- |||||||||| fluvastatin / Generic mfg.
Journal, Gene Signature: Gene signature associated with resistance to fluvastatin chemoprevention for breast cancer. (Pubmed Central) - Apr 5, 2022 This study demonstrated that statins had an influence on Ihh, and that the hyperfunction of Ihh may prevent premature cell death caused by FGFR3-related chondrodysplasia through an indirect increase in the expression of PTHrP. High basal level, or restorative upregulation, in the cholesterol biosynthesis pathway genes appear to be strongly associated with resistance to statin chemoprevention for breast cancer and may serve as a biomarker to tailor statin treatment to individuals who are most likely to benefit.
- |||||||||| Livalo (pitavastatin) / Kowa, Eli Lilly
Journal: Comparative hepatic and intestinal efflux transport of statins. (Pubmed Central) - Mar 25, 2022 Based on in vitro findings and protein abundance data, we conclude that BCRP, MRP3 and P-gp have a major impact in the efflux of various statins. Together with in vitro metabolism, uptake transport and clinical data, our findings are applicable for use in comparative systems pharmacology modelling of statins.
- |||||||||| Livalo (pitavastatin) / Kowa, Eli Lilly
PK/PD data, Journal: Comparative hepatic and intestinal metabolism and pharmacodynamics of statins. (Pubmed Central) - Mar 24, 2022 Significance Statement The present comparison of the in vitro metabolic and pharmacodynamic properties of atorvastatin, fluvastatin, pitavastatin, pravastatin, rosuvastatin, and simvastatin and their metabolites using unified methodology provides a strong basis for further application. Together with in vitro drug transporter and clinical data, our findings are applicable for use in comparative systems pharmacology modelling to predict the pharmacokinetics and pharmacological effects of statins at different dosages.
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