更新于：2024-11-21

PC/GluT(Metabomed)

更新于：2024-11-21

概要

研发状态

概要

基本信息

药物类型

未知

别名-

靶点

GLUT1 x PC

作用机制

GLUT1调节剂(葡萄糖转运蛋白调节剂)、PC调节剂(pyruvate carboxylase modulators)

治疗领域-

在研适应症-

非在研适应症-

原研机构

Metabomed Ltd.初创企业

在研机构

Metabomed Ltd.初创企业

非在研机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 PC/GluT(Metabomed) 相关的临床结果

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100 项与 PC/GluT(Metabomed) 相关的转化医学

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100 项与 PC/GluT(Metabomed) 相关的专利（医药）

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项与 PC/GluT(Metabomed) 相关的文献（医药）

2022-05-01·The FASEB Journal2区 · 生物学

Phosphatidylserine enhances anti‐inflammatory effects of reconstituted HDL in macrophages via distinct intracellular pathways

2区 · 生物学

Article

作者: Poupel, Lucie ; Huby, Thierry ; Tubeuf, Emilie ; Frisdal, Eric ; Patel, Mili ; Lesnik, Philippe ; Guerin, Maryse ; Guillas, Isabelle ; Rye, Kerry‐Anne ; Le Goff, Wilfried ; Darabi, Maryam ; Dahik, Veronica D. ; Kontush, Anatol ; Gautier, Emmanuel L. ; Lhomme, Marie

Phosphatidylserine (PS) is a minor phospholipid constituent of high-density lipoprotein (HDL) that exhibits potent anti-inflammatory activity. It remains indeterminate whether PS incorporation can enhance anti-inflammatory effects of reconstituted HDL (rHDL). Human macrophages were treated with rHDL containing phosphatidylcholine alone (PC-rHDL) or PC and PS (PC/PS-rHDL). Interleukin (IL)-6 secretion and expression was more strongly inhibited by PC/PS-rHDL than PC-rHDL in both tumor necrosis factor (TNF)-α- and lipopolysaccharide (LPS)-stimulated macrophages. siRNA experiments revealed that the enhanced anti-inflammatory effects of PC/PS-rHDL required scavenger receptor class B type I (SR-BI). Furthermore, PC/PS-rHDL induced a greater increase in Akt1/2/3 phosphorylation than PC-rHDL. In addition, PC/PS but not PC-rHDL decreased the abundance of plasma membrane lipid rafts and p38 mitogen-activated protein kinase (p38 MAPK) phosphorylation. Finally, when these rHDL formulations were administered to dyslipidemic low-density lipoprotein (LDL)-receptor knockout mice fed a high-cholesterol diet, circulating IL-6 levels were significantly reduced only in PC/PS-rHDL-treated mice. In parallel, enhanced Akt1/2/3 phosphorylation by PC/PS-rHDL was observed in the mouse aortic tissue using immunohistochemistry. We concluded that the incorporation of PS into rHDLs enhanced their anti-inflammatory activity by modulating Akt1/2/3- and p38 MAPK-mediated signaling through SR-BI in stimulated macrophages. These data identify PS as a potent anti-inflammatory component capable of enhancing therapeutic potential of rHDL-based therapy.

2016-04-15·Cancer Research and Treatment2区 · 医学

Tolerability and Outcomes of First-Line Pemetrexed-Cisplatin Followed by Gefitinib Maintenance Therapy Versus Gefitinib Monotherapy in Korean Patients with Advanced Nonsquamous Non-small Cell Lung Cancer: A <i>Post Hoc</i> Descriptive Subgroup Analysis of a Randomized, Phase 3 Trial

2区 · 医学

Article

作者: Wang, Xin ; Park, Keunchil ; Ahn, Myung-Ju ; Shin, Sang Won ; Orlando, Mauro ; Kang, Jin Hyoung ; Cho, Eun Kyung ; Kim, Dong-Wan ; Kim, Joo-Hang ; Kim, Jong Seok

PURPOSEWe recently reported on a randomized, open-label, phase 3 trial comparing pemetrexed-cisplatin chemotherapy followed by gefitinib maintenance therapy (PC/G) with gefitinib monotherapy in patients with non-small cell lung cancer (NSCLC). Here, we report on a post hoc subgroup analysis of that study assessing the demographics and disposition of the Korean patient subgroup, and comparing the tolerability of PC/G and gefitinib monotherapy and the tumor response with respect to epidermal growth factor receptor (EGFR) status.MATERIALS AND METHODSPatients, who were ≥ 18 years, chemonaïve, Korean, light ex-smokers/never-smokers with advanced NSCLC, were randomly assigned (1:1) to PC/G or gefitinib monotherapy. Treatment-emergent adverse events (TEAEs) were graded, and tumor response was measured as change in lesion sum from baseline at best response. The study was registered with ClinicalTrials. gov, NCT01017874.RESULTSOverall, 111 Korean patients were treated (PC/G, 51; gefitinib, 60). Between-arm characteristics were balanced and similar to those of the overall population. Treatment discontinuations due to adverse events were low (PC/G: 1, 2.0%; gefitinib: 7, 11.7%). Overall, 92 patients (82.9%) reported ≥ 1 TEAE (PC/G, 44; gefitinib, 48); few patients (PC/G, 16; gefitinib, 7) reported severe TEAEs; the most frequent was neutropenia (PC/G arm) and elevated alanine aminotransferase (gefitinib arm). The lesion sum was decreased by PC/G treatment in most patients, regardless of EGFR mutation status, while gefitinib monotherapy reduced the lesion sum in EGFR-positive patients but had no effect in EGFR-negative patients.CONCLUSIONOur results confirm that both PC/G and gefitinib were well tolerated in Korean patients, regardless of EGFR status; however, patients with EGFR wild-type NSCLC may not benefit from gefitinib monotherapy.

100 项与 PC/GluT(Metabomed) 相关的药物交易

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