α-Tocopherolquinone(α-Tocopherolquinone) - 药物靶点：PTP1B_专利_临床

概要

基本信息

药物类型

小分子化药

别名

alpha-tocopherol quinone、alpha-Tocopherolquinone、alpha-Tocopheroquinone

+ [8]

靶点

PTP1B

作用方式

抑制剂

作用机制

PTP1B抑制剂(蛋白酪氨酸磷酸酶-1B抑制剂)

治疗领域

神经系统疾病遗传病与畸形内分泌与代谢疾病+ [2]

在研适应症-

非在研适应症

Friedreich共济失调遗传性线粒体呼吸链疾病神经肌肉疾病+ [1]

原研机构

Edison Pharmaceuticals, Inc.

在研机构-

非在研机构

Endo International Plc

Penwest Pharmaceuticals Co.

Edison Pharmaceuticals, Inc.

权益机构-

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评孤儿药 (美国)

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结构/序列

分子式C29H50O3

InChIKeyLTVDFSLWFKLJDQ-IEOSBIPESA-N

CAS号7559-04-8

关联

4

项与 α-Tocopherolquinone 相关的临床试验

JPRN-UMIN000028386

/ Completed临床3期IIT

Efficacy and Safety of A0001 for Anterior Capsule Staining: Phase III Investigator-initiated Multicenter Clinical Trial - Efficacy and Safety of A0001 for Anterior Capsule Staining

开始日期2017-09-15

申办/合作机构-

NCT01074359

/ Terminated临床2期

A Phase 2a, Double Blind, Randomized, Placebo-controlled, 28 Day, Two-arm, Parallel Group Study of A0001 in Patients With the A3243G Mitochondrial DNA Point Mutation and Evidence of Impaired Mitochondrial Function

This is a phase 2a, double-blind, placebo-controlled, single-center study. Twenty-one patients who qualify for the study will be randomly assigned to either active drug or placebo. The study will take place at Newcastle University. Patients will have a 66% chance of getting active drug. Patients will be required to take study treatment orally twice a day for 28 days. A baseline visit will occur within 21 days of screening visit. All patients will be followed for 1 week after completion of study or early withdrawal from the study.

开始日期2010-02-01

申办/合作机构

Penwest Pharmaceuticals Co.

EUCTR2009-014263-40-GB

/ Not yet recruitingN/A

A Phase 2a, Double Blind, Randomized, Placebo-controlled, 28 day, Two-arm, Parallel Group Study of A0001 in Patients with the A3243G Mitochondrial DNA Point Mutation and Evidence of Impaired Mitochondrial Function - MEL01. A0001 in Patients with A3243G Mitochondrial DNA Mutation

开始日期2009-12-14

申办/合作机构

Penwest Pharmaceuticals Co.

100 项与 α-Tocopherolquinone 相关的临床结果

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100 项与 α-Tocopherolquinone 相关的转化医学

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100 项与 α-Tocopherolquinone 相关的专利（医药）

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584

项与 α-Tocopherolquinone 相关的文献（医药）

2025-10-18·NATURAL PRODUCT RESEARCH

Chemical constituents of Coccoloba peltata Schott leaves and their cytotoxic activities

Article

作者: Hamed, Abdelaaty ; Fumiko Yamaguchi, Lydia ; Syrovets, Tatiana ; Ziegler, David ; El Gaafary, Menna ; Kato, Massuo Jorge ; Salih, Layth M. ; Stammler, Hans Georg

Chromatographic fractionation of CH₂Cl₂:MeOH (1:1) extract of Coccoloba peltata Schott cultivated in Egypt afforded four compounds, lupeol acetate (1), ent-13-epi-manoyl oxide (2), 5-methoxymethyl-7,8-dimethyltocol (3), and α-tocopherol quinone (4). The planar structures of the isolated compounds were concluded based on HRESIMS and NMR spectroscopy. X-ray crystallography of 2 is reported herein for the first time and its unambiguous absolute configuration was deduced from anomalous dispersion. To the best of our knowledge, this is the first known report on the isolation of compounds 1-4 from this species. Among the isolated compounds, only compound 4 showed a moderate level of cytotoxic activity against six cancer cell lines out of seven cell lines tested.

2025-10-18·NATURAL PRODUCT RESEARCH

A new lignan from Laggera crispata (Vahl) Hepper & J. R. I. Wood

Article

作者: Chen, Xiao-Li ; Wu, Ji-Chun ; Tian, Ming-Ming

A new lignan, 9'-O-angelyllariciresinol (1), and 20 known compounds (2-21) were isolated from the petroleum ether fraction of Laggera crispata (Vahl) Hepper & J. R. I. Wood. Their structures were identified by spectral analysis (NMR, IR, UV, and MS). Activity screening showed that compound 5 exhibited significant inhibitory effect on Staphylococcus aureus, while compound 2 exhibited significant inhibitory effect against liver cancer cell line HepG2.

2025-07-01·Transplant Infectious Disease

Does Switching From Trimethoprim/Sulfamethoxazole to Atovaquone Result in Less Hyperkalemia? A Single‐Center Retrospective Analysis in Heart Transplant Patients

Article

作者: Nnani, Daryl ; Sims, Daniel ; Bazarbachi, Abdulhamid ; Shin, Jooyoung ; Novakovic, Marko ; Chavez, Patricia ; Gjelaj, Christiana ; Saeed, Omar ; Madan, Shivank ; Murthy, Sandhya ; Jorde, Ulrich ; Marsela, Enklajd ; Rochlani, Yogita ; Vukelic, Sasa ; Patel, Snehal R.

ABSTRACT:

Background:

Trimethoprim/sulfamethoxazole (TMP/SMX) is commonly used after orthotopic heart transplant (OHT) for opportunistic infection (OI) prophylaxis, but its contribution to hyperkalemia is uncertain. Whether switching to atovaquone (ATQ), which has a narrower antimicrobial spectrum, affects infection risk and improves hyperkalemia has not been investigated. This study evaluated whether transitioning from TMP/SMX to ATQ in the setting of post‐OHT hyperkalemia is beneficial in lowering risk of recurrent hyperkalemia while maintaining OI prophylaxis efficacy.

Methods:

A single‐center retrospective review of OHT patients (January 2011–April 2022) compared those maintained on TMP/SMX with those switched to ATQ due to side effects, specifically hyperkalemia. The primary endpoint was the resolution of hyperkalemia, and the secondary endpoint was the combined infection rate.

Results:

Among 321 OHT recipients, 76% were switched to ATQ. Patients switched to ATQ had higher rates of severe and recurrent hyperkalemia and experienced numerically higher overall infection rates compared to TMP/SMX patients (27% vs. 52%; p < 0.001). However, in a Poisson regression model adjusted for immortal time bias, the incidence rate ratio (IRR) for infections with ATQ versus TMP/SMX was 1.32 (95% CI: 0.93–1.86; p = 0.119). Multivariable analyses excluding chronic kidney disease patients confirmed TMP/SMX's association with lower hyperkalemia rates (initial/recurrent). Age and diabetes independently predicted initial hyperkalemia.

Conclusions:

Transitioning from TMP/SMX to ATQ did not decrease hyperkalemia rates and was associated with a numerically higher incidence of infections, though this difference was not statistically significant. Hyperkalemia is likely multifactorial and often unresolved by switching from TMP/SMX. image

100 项与 α-Tocopherolquinone 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB14094

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
神经肌肉疾病	临床2期	英国	Penwest Pharmaceuticals Co.	2010-02-01
呼吸功能不全	临床2期	英国	Penwest Pharmaceuticals Co.	2010-02-01
Friedreich共济失调	临床2期	美国	Penwest Pharmaceuticals Co.	2009-12-01
遗传性线粒体呼吸链疾病	临床2期	-	Edison Pharmaceuticals, Inc.	-
遗传性线粒体呼吸链疾病	临床2期	-	Endo International Plc	-