更新于：2024-11-21

PPAR (Autobahn Therapeutics)

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-

作用机制-

治疗领域-

在研适应症-

非在研适应症-

原研机构

Autobahn Therapeutics, Inc.初创企业

在研机构-

非在研机构

Autobahn Therapeutics, Inc.初创企业

最高研发阶段终止临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 PPAR (Autobahn Therapeutics) 相关的临床结果

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100 项与 PPAR (Autobahn Therapeutics) 相关的转化医学

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100 项与 PPAR (Autobahn Therapeutics) 相关的专利（医药）

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项与 PPAR (Autobahn Therapeutics) 相关的文献（医药）

2003-09-01·Gut1区 · 医学

Potential role for peroxisome proliferator activated receptor (PPAR) in preventing colon cancer

1区 · 医学

Article

作者: Michalik, L. ; Bennett, A. J. ; Morris, T. ; Wahli, W. ; Hawkey, C. J. ; Bell, D. R. ; Smith, J. A. ; Jackson, L. ; Anderton, K. ; Watson, S. A.

BACKGROUNDPeroxisome proliferator activated receptors (PPARs) are nuclear hormone receptors involved in genetic control of many cellular processes. PPAR and PPAR have been implicated in colonic malignancy. Here we provide three lines of evidence suggesting an inhibitory role for PPAR in colorectal cancer development.METHODSLevels of PPAR mRNA and protein in human colorectal cancers were compared with matched non-malignant mucosa using RNAse protection and western blotting. APC(Min)/+ mice were randomised to receive the PPAR activator methylclofenapate 25 mg/kg or vehicle for up to 16 weeks, and small and large intestinal polyps were quantified by image analysis. The effect of methylclofenapate on serum stimulated mitogenesis (thymidine incorporation), linear cell growth, and annexin V and propidium iodide staining were assessed in human colonic epithelial cells.RESULTSPPAR (mRNA and protein) expression levels were significantly depressed in colorectal cancer compared with matched non-malignant tissue. Methylclofenapate reduced polyp area in the small intestine from 18.7 mm(2) (median (interquartile range 11.1, 26.8)) to 9.90 (4.88, 13.21) mm(2) (p=0.003) and in the colon from 9.15 (6.31, 10.5) mm(2) to 3.71 (2.71, 5.99) mm(2) (p=0.009). Methylclofenapate significantly reduced thymidine incorporation and linear cell growth with no effect on annexin V or propidium iodide staining.CONCLUSIONSPPAR may inhibit colorectal tumour progression, possibly via inhibition of proliferation, and may be an important therapeutic target.

2003-03-01·The Journal of Clinical Pharmacology3区 · 医学

Randomized, Double‐Blind, Placebo‐Controlled Comparison of the Analgesic Efficacy of Oxycodone 10 mg/Acetaminophen 325 mg versus Controlled‐Release Oxycodone 20 mg in Postsurgical Pain

3区 · 医学

Article

作者: Arnold R. Gammaitoni ; Scott Bulloch ; Thomas Schlagheck ; Bradley S. Galer ; Frank Caruso ; Tina Ma ; Peter Lacouture

This randomized, controlled trial compared the analgesic efficacy and safety of the new oxycodone 10‐mg/acetaminophen 325‐mg formulation (Percocet®) for the treatment of acute pain following oral surgery with double the dose of oxycodone alone (controlled‐release [CR] oxycodone 20 mg [OxyContin®]). A total of 150 male and female patients with ≥ 2 full or partial bone‐impacted mandibular molars, at least moderate persistent pain, and moderate trauma received a single dose of combination agent, CR oxycodone, or placebo following oral surgery and rated pain intensity and pain relief over the next 6 hours. The intent‐to‐treat population comprised 141 patients (55 on combination agent, 56 on oxycodone, and 30 on placebo). Combination agent and CR oxycodone were significantly superior to placebo for all efficacy measures. Combination agent was statistically superior to CR oxycodone in four of five outcome measures of pain intensity and pain relief (PPID, PPAR, SPID, and SPRID). It also provided a faster onset and 24% reduction in the number of patients reporting treatment‐related adverse events compared with twice the dose of opioid alone. This new formulation offers the combination of two analgesic drugs with complementary mechanisms of action, which results in enhanced analgesia, an “opioid‐sparing” effect, and an improved side effect and safety profile.

Pharmaceuticals3区 · 医学

Effects of Selective Peroxisome Proliferator Activated Receptor Agonists on Corneal Epithelial Wound Healing

3区 · 医学

ArticleOA

作者: Shimizu, Akira ; Nakano, Yuji ; Takahashi, Hiroshi ; Tobita, Yutaro ; Arima, Takeshi ; Uchiyama, Masaaki

The effects of each subtype-selective peroxisome proliferator activated receptor (PPAR) agonist (α, β/δ, γ) on corneal epithelial wound healing were investigated using a rat corneal alkali burn model. After the alkali burn, each PPAR agonist or vehicle ophthalmic solution was instilled topically onto the rat’s cornea. Corneal epithelial healing processes were evaluated by fluorescein staining. Pathological analyses and real-time reverse transcription polymerase chain reactions were performed to evaluate Ki67 (proliferative maker) expression and inflammatory findings. The area of the corneal epithelial defect at 12 h and 24 h after the alkali burn was significantly smaller in each PPAR group than in the vehicle group. Ki67 mRNA expression was increased in the PPARβ/δ group, whereas mRNA expressions of inflammatory cytokines were suppressed in all of the PPAR agonist groups. Nuclear factor kappa B (NF-κB) was the most suppressed in the PPARγ group. The accelerated corneal epithelial healing effects of each PPAR ligand were thought to be related to the promotion of proliferative capacity and inhibition of inflammation.

100 项与 PPAR (Autobahn Therapeutics) 相关的药物交易

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