- |||||||||| Preclinical, Journal: Four functional genotoxic marker genes (Bax, Btg2, Ccng1, and Cdkn1a) discriminate genotoxic hepatocarcinogens from non-genotoxic hepatocarcinogens and non-genotoxic non-hepatocarcinogens in rat public toxicogenomics data, Open TG-GATEs. (Pubmed Central) - Dec 20, 2024
The present results unequivocally demonstrate the availability of four genotoxic marker genes ((Bax, Btg2, Ccng1, and Cdkn1a) and PCA in discriminating GTHCs from NGTHCs and NGTNHCs in Open TG-GATEs. These findings strongly support our recommendation that future rat liver in vivo toxicogenomics tests prioritize these four genotoxic marker genes, as they have proven to be highly effective in discriminating between different types of hepatocarcinogens.
- |||||||||| Journal: Decatungstate-Photocatalyzed Transformations of 2-Bromo-3,3,3-trifluoropropene for Selective Synthesis of Z/E-?-CF3-Enones. (Pubmed Central) - Dec 2, 2024
The hydroacylated products, i.e., ?,?-Br,CF3-ketones, can be applied as highly functionalized synthetic building blocks for the selective synthesis of (Z/E)-?-CF3-enones. Utilizing this methodology, a broad range of commercially available aromatic and aliphatic aldehydes as well as numerous complex aldehydes, such as lily aldehyde, cyclamen aldehyde, citronellal, vanillin, and aldehydes containing bioactive moieties, including ibuprofen, gemfibrozil, naproxen, flurbiprofen, oleic acid, and aspirin, may be proficiently employed in this transformative process.
- |||||||||| gemfibrozil / Generic mfg., ibuprofen / Generic mfg., naproxen / Generic mfg.
Journal: Direct catalytic photodecarboxylative amination of carboxylic acids with diazirines for divergent access to nitrogen-containing compounds. (Pubmed Central) - Oct 25, 2024 The substrate scope includes broad functional group tolerance, such as ketones, esters, olefins, and alcohols, along with the late-stage amination of naproxen, ibuprofen, gemfibrozil, and gibberellic acid. Synthetic applications leverage the versatility of the intermediate diaziridines and include the regioselective preparation of a suite of 1H-indazoles, 2H-indazoles, and fluoroquinolones.
- |||||||||| Parmodia (pemafibrate) / Kowa
Review, Journal: Hypertriglyceridemia Therapy: Past, Present and Future Perspectives. (Pubmed Central) - Sep 14, 2024 Pemafibrate is a new PPAR-?-selective drug considered for therapy, and clinical trials are ongoing. Apart from this class of drugs, new therapies have emerged with different mechanisms of action to reduce triglycerides and the risk of cardiovascular diseases.
- |||||||||| probenecid / Generic mfg., indomethacin / Generic mfg., gemfibrozil / Generic mfg.
Journal: Isothiourea-Catalysed Acylative Kinetic Resolution of Tertiary Pyrazolone Alcohols. (Pubmed Central) - Aug 23, 2024 The application of this KR method to tertiary alcohols derived from a natural product (geraniol), alongside pharmaceutically relevant drug compounds (indomethacin, gemfibrozil and probenecid), with high efficiency (s > 100) is also described. The key structural motif leading to excellent selectivity in this KR process has been probed through computation, with an NC=O
- |||||||||| olanzapine / Generic mfg.
Acute Pancreatitis Secondary to Olanzapine-Induced Hypertriglyceridemia: A Case Report (Exhibit Hall E) - Aug 20, 2024 - Abstract #ACG2024ACG_638; Patient was also advised to discontinue cocaine and dulaglutide...Despite these associations, olanzapine's role in pancreatitis can be complex, influenced by patient-specific factors like pre-existing hypertriglyceridemia. Discontinuation often resolves pancreatitis without recurrence, emphasizing careful monitoring and tailored management in affected individuals.
- |||||||||| Opdivo (nivolumab) / BMS
IMMUNE CHECKPOINT INHIBITOR-INDUCED SARCOIDOSIS IN A PATIENT WITH HIGH-GRADE UROTHELIAL CARCINOMA (Convention Center Exhibit Hall: Rapid Fire Area 4B) - Jul 31, 2024 - Abstract #CHEST2024CHEST_1659; He completed 4 cycles of neoadjuvant chemotherapy (Cisplatin/Gemfibrozil) followed by a cystoprostatectomy with creation of neobladder. Our report aims to provide awareness and highlights an important irAE of ICIs, given their increasingly widespread utility, as prompt recognition and biopsy is necessary to distinguish it from malignancy progression and make proper treatment decisions.
- |||||||||| Review, Journal: Occurrence of pharmaceuticals in Latin America: case study on hazard assessment and prioritization in Costa Rica. (Pubmed Central) - Jul 16, 2024
The prioritization approach (which included the Frequency of Appearance (FoA), the Frequency of PNEC exceedance (FoE), and the Extent of predicted no-effect concentration (PNEC) exceedance (EoE)), showed a critical list of nine pharmaceuticals: caffeine, diphenhydramine, acetaminophen, lovastatin, gemfibrozil, ciprofloxacin, ibuprofen, doxycycline and norfloxacin. These compounds should be taken into account as a first concern during the implementation of environmental policies related to pharmaceutical products in the region.
- |||||||||| gemfibrozil / Generic mfg.
Preclinical, Journal, IO biomarker: Gemfibrozil-Platinum(IV) Precursors for New Enhanced-Starvation and Chemotherapy In Vitro and In Vivo. (Pubmed Central) - Apr 18, 2024 In vivo, GP showed superior antitumor activity in A2780 tumor-bearing mice with no observable tissue damage. Mechanistic studies suggested that highly selective chemotherapy could be due to the new enhanced starvation effect: blocking vasculature formation via inhibiting the CYP2C8/EETs pathway and VEGFR2, NF-?B, and COX-2 expression and cholesterol efflux and degradation acceleration via increasing ABCA1 and PPAR?.
- |||||||||| dexamethasone / Generic mfg., gemfibrozil / Generic mfg.
MANAGEMENT OF SEVERE HYPERTRIGLYCERIDAEMIA IN PREGNANCY: REPORT OF TWO CASES () - Mar 17, 2024 - Abstract #ICEEDEC2024ICE_EDEC_1136; Hypoglycaemia was avoided with the use of high-volume dextrose-containing fluids, and the use of dexamethasone for foetal lung maturation (which might worsen hypertriglyceridaemia) was not precluded in either case. The latter is especially relevant, as patients with hypertriglyceridaemia are at increased risk of preterm delivery.
- |||||||||| Journal: Pharmaceuticals, hazard and ecotoxicity in surface and wastewater in a tropical dairy production area in Latin America. (Pubmed Central) - Feb 6, 2024
Six pharmaceuticals were considered either of high (albendazole, lovastatin and caffeine) or intermediate estimated hazard (ciprofloxacin, acetaminophen and ketoprofen) based on the HQ approach, while 26% of the samples were considered of high estimated hazard according to the cumulative ?HQ approach...Seven out of these compounds showed high estimated risk (risperidone, diphenhydramine, trimethoprim, fluoxetine, ofloxacin, caffeine and ibuprofen), while three (gemfibrozil, ciprofloxacin and cephalexin) exhibited intermediate estimated risk...Despite being nontoxic for D. magna or V. fischeri, frequent inhibition (>20%) of GI in L. sativa was determined in 34% of surface water samples; such findings raise concern on the apparent inceptive environmental pollution and risk within the area. According to the pharmaceutical content patterns in both kinds of studied matrices, no clear evidence of significant contamination in surface water due to livestock activities could be retrieved, suggesting a main role of urban influence.
- |||||||||| gemfibrozil / Generic mfg., naproxen / Generic mfg., adapalene / Generic mfg.
Journal: Enantioselective Intermolecular C-H Functionalization of Primary Benzylic C-H Bonds Using ((Aryl)(diazo)methyl)phosphonates. (Pubmed Central) - Jan 11, 2024 The phosphonate group is much more sterically demanding than the previously studied carboxylate ester group, leading to much higher selectivity for a primary site versus more sterically crowded positions. The effectiveness of this methodology has been demonstrated by the late-stage primary C-H functionalization of estrone, adapalene, (S)-naproxen, clofibrate, and gemfibrozil derivatives.
- |||||||||| gemfibrozil / Generic mfg.
Biomarker, Journal: Are 20-hydroxyecdysone and related genes potential biomarkers of sublethal exposure to lipid-altering contaminants? (Pubmed Central) - Nov 28, 2023 The present study aimed to (i) assess baseline levels of 20E and transcription levels of four related-genes (shade, neverland, ultraspiracle, and ecdysteroid receptor); and (ii) evaluate effects in D. magna after 21 days of exposure to fenarimol (anti-ecdysteroid) and a mixture of gemfibrozil and clofibric acid (lipid-lowering drugs) at sublethal concentrations...These results suggest that changes in transcription levels of the target genes and concentrations of 20E may not be sensitive endpoints that can be used as biomarkers of sublethal exposure to the target compounds in D. magna. Measuring multiple time points instead of a single measure as well as additional molecular endpoints obtained from transcriptomic and metabolomic studies could afford more insights on the changes occurring in exposed daphnids to lipid-altering compounds and identify efficient biomarkers of sublethal exposure.
- |||||||||| Tukysa (tucatinib) / Seagen
Journal: Creation of novel sensitive probe substrate and moderate inhibitor models for a comprehensive prediction of CYP2C8 interactions for tucatinib. (Pubmed Central) - Nov 17, 2023 To simulate a potential interaction with a moderate CYP2C8 inhibitor, two novel PBPK models representing a moderate CYP2C8 inhibitor and a sensitive CYP2C8 substrate were developed based on the existing PBPK models for gemfibrozil and rosiglitazone, respectively. The simulated population GMR of tucatinib with a moderate CYP2C8 inhibitor ranged from 1.98- to 3.08-fold, and based on these results, no dose modifications were proposed for moderate CYP2C8 inhibitors for the tucatinib label.
- |||||||||| drospirenone/ethinyl estradiol / Generic mfg., gemfibrozil / Generic mfg., spironolactone / Generic mfg.
Unveiling the Link: Hypertriglyceridemia Induced Acute Pancreatitis in a Young Female on Oral Contraceptives - A Case Report (Exhibit Hall) - Jul 29, 2023 - Abstract #ACG2023ACG_1997; Case Description/ A 24-year-old female with a history of cystic acne on spironolactone and Loryna (drospirenone and ethinyl estradiol tablets) presented to the Emergency Department with severe left flank pain rated 9/10...Management involved NPO status, an insulin drip, discontinuation of Loryna and spironolactone, and initiating Gemfibrozil and Omega 3 therapy...Further research is needed to assess the value of routine triglyceride monitoring in oral contraceptive users. Figure: CT abdomen findings
- |||||||||| Interpretable Deep Learning and MultiOme data repurposing in Alzheimer's target and drug discovery: NIA Artificial Intelligence and Machine Learning Consortium (Hall 10) - Jul 6, 2023 - Abstract #AAIC2023AAIC_8992;
Combining network-based prediction and retrospective case-control observations with 10 million individuals, we identified that usage of four drugs (ibuprofen, gemfibrozil, cholecalciferol, and ceftriaxone) is significantly associated with reduced likelihood of AD incidence, after adjusting for various confounding factors. From a translational perspective, the deep learning and network-based approaches presented here, if broadly applied would significantly catalyze effective treatment development in AD and other neurodegenerative diseases from the human genome sequencing findings.
- |||||||||| Journal, Metabolomic study: The impact of pharmaceutical pollutants on daphnids - A metabolomic approach. (Pubmed Central) - May 24, 2023
A targeted analysis of the hydrophilic profile of daphnids revealed mainly the up-regulation of metabolites following metformin, gabapentin, amoxicillin, trimethoprim and ?-estradiol. Whereas gemfibrozil, sulfamethoxazole and oestrone exposure resulted in the down-regulation of majority of metabolites.
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