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fenofibrate (Triglide)

✓ Approved

SkyePharma PLC · PPARA · 小分子

什么是 fenofibrate？

fenofibrate 是一种小分子，由SkyePharma PLC研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Triglide
公司SkyePharma PLC
药物类别小分子
分子靶点PPARA
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, SkyePharma PLC

作用机制

分子靶点

fenofibrate 作用于 1 个分子靶点：

PPARAperoxisome proliferator activated receptor alpha (NR1C1, PPAR-alpha)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

fenofibrate 针对 2 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Metabolism and nutrition disordersHypertriglyceridaemia✓ Approved
Metabolism and nutrition disordersDyslipidaemia✓ Approved

相关研究文献

PubMedCancer letters2026-10-23

Fenofibrate enhances systemic antitumor efficacy of high- and low-dose radiotherapy plus PD-1 blockade through CD8+ T-cell metabolic reprogramming and LDRT tumor conditioning.

Wang Meidan M, Wang Liqun L, Sagar, Rao Xi X et al.

Radiotherapy (RT) combined with PD-1/PD-L1 blockade can induce systemic antitumor responses, but robust control of distant lesions remains uncommon. We identified a quadruple regimen combining immunogenic hypofractionated RT (hRT; 8 Gy × 3) to the primary tumor, low-dose RT (LDRT; 3 Gy × 3) to the secondary tumor, anti-PD-1 (αPD-1), and fenofibrate (FFB), a clinically approved PPARα agonist, that enhanced antitumor efficacy in two bilateral tumor models. Only this regimen substantially improved secondary-tumor control, eradicating LDRT-treated secondary tumors in all mice in the immunologically cold C51 model and inducing prolonged control in the aggressive, αPD-1-poorly responsive B16-CD133 model. This effect required CD8+ T cells. Tumor-specific CD8+ TILs showed enhanced effector function, reduced exhaustion, increased mitochondrial fitness, and a shift toward mitochondrial fatty acid oxidation (FAO), with scRNA-seq supporting PPARα/FAO-associated remodeling, including upregulation of Cpt1a, encoding the FAO enzyme CPT1A, in effector-associated, proliferative, and clonally expanded subsets. Both antitumor efficacy and T-cell metabolic remodeling were reversed by the CPT1 inhibitor etomoxir. By contrast, LDRT impaired tumor-cell mitochondrial fitness, while FFB shifted tumor cells from FAO toward glycolytic reliance and induced only slight apoptosis. Consistently, in vivo data argued against direct LDRT-mediated tumor-cell debulking. The quadruple regimen increased vascular MECA-79 expression, while LDRT enhanced endothelial ICAM-1/VCAM-1 and tumor-cell CXCL9/CXCL10 expression in secondary tumors, consistent with local conditioning favoring T-cell recruitment. These findings highlight FFB as a clinically tractable metabolic modulator and link FFB-enhanced hRT/LDRT/αPD-1-induced systemic antitumor efficacy to metabolic reprogramming of tumor-specific CD8+ TILs and conditioning of the LDRT-treated tumor microenvironment.

PMID 42913876
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PubMedRSC advances2026-10-23

LC-MS/MS-based metabolomics and PK/PD correlation analysis reveal the mechanism of hyperlipidemia treatment with Gastrodia elata fine powder.

Xie Weiwei W, Liu Meijuan M, Li Jiajun J, Zhang Yuqian Y et al.

Gastrodia elata Blume is used as both a food and a traditional medicine in East Asia. This study evaluated the lipid-lowering effects of G. elata fine powder (GFP) and the associated metabolic responses in Sprague-Dawley rats with high-fat diet (HFD)-induced hyperlipidemia. Thirty-five rats were assigned to seven groups: a normal-diet control, an untreated HFD model, three GFP groups (150, 300, or 500 mg kg-1 per administration, three times daily), and two positive-control groups receiving simvastatin or fenofibrate. Following a 6 week modeling period and a 2 week intervention, serum biochemical parameters, liver histology, and serum, urinary, and fecal metabolic profiles were assessed using biochemical assays, histological examination, and untargeted liquid chromatography-high-resolution mass spectrometry. A separate cohort of six hyperlipidemic rats received gastrodin (25 mg kg-1) for pharmacokinetic/pharmacodynamic (PK/PD) analysis. Compared with the untreated HFD group, medium- and high-dose GFP improved serum lipid profiles, reduced serum aminotransferase activities, and ameliorated hepatic histopathological changes. Metabolomic profiling revealed 14 urinary, 8 fecal, and 16 serum metabolites whose HFD-associated alterations shifted toward normal-control levels following high-dose GFP treatment. The associated pathways included phenylalanine metabolism, taurine and hypotaurine metabolism, and the tricarboxylic acid cycle. Gastrodin exhibited a biphasic plasma concentration-time profile, whereas responses of five endogenous metabolic markers lagged behind systemic drug exposure. These findings support the short-term lipid-lowering activity of GFP in HFD-fed rats and its association with changes in amino acid, bile-acid-related, and energy metabolism.

PMID 42910039
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PubMedChemSusChem2026-10-23

Direct α-C(sp3)─H Alkylation and Arylation of Ethers Enabled by Carbon Nitride/Nickel Metallaphotoredox Catalysis.

de Vries Ibáñez Miguel M MM, Husy Nathan G G NGG, Inico Elisabetta E, Karaca Kaan K et al.

The direct functionalization of α-C(sp3)─H bonds offers a powerful strategy for converting abundant feedstocks and complex molecules into value-added products, yet sustainable catalytic platforms that avoid precious-metal photocatalysts remain underdeveloped. Here, we report a metallaphotoredox system that combines recyclable carbon nitride nanosheets with nickel catalysis for the direct α-C(sp3)─H cross-coupling of ethers, amides, and benzylic substrates under visible light. The method operates at mild temperature in air and enables both α-C(sp3)─C(sp2) and α-C(sp3)─C(sp3) bond formation using aryl and alkyl halides, including challenging ether donors such as THF, 2-MeTHF, 1,4-dioxane, and DME. Broad functional group tolerance is demonstrated across electronically diverse aryl halides, while late-stage alkylation of pharmaceutically relevant molecules including loratadine, caffeine, and fenofibrate highlights the utility of the platform for molecular diversification. The carbon nitride photocatalyst is readily recovered and reused over five cycles without loss of activity, and the process is further translated to continuous flow, providing accelerated reaction kinetics and reduced photocatalyst loading. Mechanistic studies combining Stern-Volmer analysis, radical trapping, cyclic voltammetry, NMR spectroscopy, and DFT calculations support a dual catalytic cycle in which photoexcited carbon nitride promotes oxidative generation of α-heteroatom-stabilized radicals, while nickel mediates radical capture, cross-coupling, and product-forming reductive elimination. This work establishes carbon nitride as an earth-abundant, recyclable alternative to noble-metal photocatalysts for metallaphotoredox C─H functionalization and expands the scope of heterogeneous photocatalysis to direct α-C(sp3)─H cross-coupling.

PMID 42912554
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PubMedCureus2026-10-19

Reduction in Rheumatoid Factor and Matrix Metalloproteinase-3 With Successful Glucocorticoid Withdrawal After Initiation of Pemafibrate in a Patient With Rheumatoid Arthritis and Hypertriglyceridemia: A Case Report.

Suzuki Kimihiro K

Pemafibrate is a selective peroxisome proliferator-activated receptor α (PPARα) modulator (SPPARMα) used for hypertriglyceridemia. PPARα activation also suppresses nuclear factor-κB (NF-κB) signaling, a pathway central to synovial inflammation and joint destruction in rheumatoid arthritis (RA). Whether pemafibrate affects RA-related biomarkers in humans is unknown. A 51-year-old woman (height: 164 cm, body weight: 71 kg, body mass index: 26.4 kg/m²) with RA treated with methotrexate, bucillamine, iguratimod, and low-dose prednisolone (0.7 mg/day) had hypertriglyceridemia with coexisting metabolic dysfunction-associated steatotic liver disease (MASLD). Pemafibrate was started at 0.2 mg/day and increased to 0.4 mg/day after 12 weeks, while the disease-modifying antirheumatic drug (DMARD) regimen was kept unchanged throughout. Over the 20 months following the initiation of pemafibrate, rheumatoid factor (RF) and matrix metalloproteinase-3 (MMP-3) declined, and C-reactive protein (CRP) showed an overall decrease with a transient rise at month 6; prednisolone was tapered and discontinued after 17 months. The 28-joint Disease Activity Score based on C-reactive protein (CRP; DAS28-CRP), already in the remission range at baseline (1.9), remained below the remission threshold throughout. Serum triglycerides fell from 184 mg/dL to 88 mg/dL, and hepatic transaminases (aspartate aminotransferase (AST) and alanine aminotransferase (ALT)) showed a transient early increase followed by a return toward baseline, without meeting criteria for drug-induced liver injury. No adverse events attributable to pemafibrate were observed. In this patient, the introduction of pemafibrate was temporally associated with reductions in RA-related biomarkers and with successful glucocorticoid withdrawal, without any intensification of DMARD therapy. Because the baseline prednisolone dose was already low (0.7 mg/day), this withdrawal should be interpreted cautiously and should not be regarded as strong evidence of a glucocorticoid-sparing effect. Causality cannot be established from a single case; nevertheless, together with earlier clinical reports on fenofibrate, animal studies showing anti-arthritic effects of fenofibrate and bezafibrate, and preclinical evidence of PPARα-mediated NF-κB inhibition, this observation suggests that PPARα agonists merit further investigation as adjunctive agents in RA, particularly in patients with coexisting dyslipidemia or steatotic liver disease.

PMID 42894855
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PubMedInternational journal of pharmaceutics: X2026-10-18

Applicability of a miniaturized precipitation assay as an early-stage screening tool for prototype formulation development.

Mayer Sara S, Krollik Katharina K, Wagner Christian C, Lehmann Andreas A et al.

Poor aqueous solubility is a frequently faced challenge in oral drug development. Therefore, the development of predictive in vitro tools for the selection of a suitable formulation is essential. For early formulation development, such an assay ideally requires minimal resources. To address this need, we evaluated the benefits of a previously published miniaturized two-compartment precipitation assay to assess formulation effects early in drug product development. The assay was originally developed for screening compounds for their absorption behavior during preclinical stage. Six poorly soluble weakly basic compounds (albendazole, ibrutinib, itraconazole, posaconazole, ritonavir, ziprasidone; two formulations each) and one poorly soluble neutral compound (fenofibrate; three formulations) were tested under simulated fasted conditions. Formulation differences found in vitro were compared to human pharmacokinetic data obtained from literature. From a qualitative perspective, the assay correctly reflected the in vivo observations for five out of the six basic compounds, as well as for fenofibrate. Quantitatively, the assay approximated the observed in vivo formulation effects for several compounds, including itraconazole, posaconazole, ritonavir, ziprasidone and fenofibrate, whereas the effect size was overestimated for albendazole and ibrutinib, likely reflecting potential assay limitations. These findings support the use of the miniaturized precipitation assay as a fit-for-purpose screening tool for early formulation development.

PMID 42893118
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PubMedRheumatology international2026-10-17

Tocilizumab for active rheumatoid arthritis in a patient with concomitant primary biliary cholangitis: a case based review.

Šukara Goran G, Dinjar Kujundžić Petra P, Madir Anita A, Piteša Košutić Ivana I et al.

The coexistence of active rheumatoid arthritis and active primary biliary cholangitis represents a distinct therapeutic challenge. Evidence-based guidance for treatment selection in this clinical setting remains limited, and published experience with tocilizumab is restricted to isolated case reports. We report a 59-year-old woman with highly active, seropositive rheumatoid arthritis and marked cholestatic biochemical activity, in whom diagnostic evaluation revealed active primary biliary cholangitis in the absence of advanced liver fibrosis. Following multidisciplinary assessment, methotrexate and leflunomide were avoided because of active cholestatic liver disease, and treatment with subcutaneous tocilizumab was initiated in combination with ursodeoxycholic acid and fenofibrate. Tocilizumab was well tolerated and led to a progressive improvement in arthritis. In parallel, cholestatic liver parameters showed sustained improvement in the absence of hepatic adverse effects. To contextualize this observation, we performed a focused literature review and identified only two directly relevant case reports, both reporting favorable rheumatologic and hepatic outcomes during tocilizumab therapy. This case adds to the limited body of evidence suggesting that tocilizumab may represent a feasible therapeutic option for selected patients with active rheumatoid arthritis and concomitant primary biliary cholangitis.

PMID 42888283
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