GAL-021(GAL-021) - _专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点-

作用机制

一氧化氮供体

治疗领域

呼吸系统疾病

在研适应症-

非在研适应症

呼吸功能不全

原研机构

Galleon Pharmaceuticals, Inc.

在研机构-

非在研机构

Galleon Pharmaceuticals, Inc.

最高研发阶段无进展临床1期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构

分子式C11H22N6O

InChIKeyFJNLCHNQVJVCPY-UHFFFAOYSA-N

CAS号1380341-99-0

关联

3

项与 GAL-021 相关的临床试验

NL-OMON41554 / CompletedN/A

A Double Blind, Ascending Multiple Dose Study to Evaluate the Safety and Tolerability of GAL-021 in Healthy Volunteers. - An Ascending Multiple Dose Study of GAL-021.

开始日期2013-10-01

申办/合作机构

Galleon Pharmaceuticals, Inc.

NL-OMON23830 / RecruitingN/A

A Two-Part, Double Blinded, Placebo Controlled, Crossover, Re-peated Stepped Infusion Dose Study of Respiratory Pharmacodynamics of GAL-021 and Opioids.

开始日期2012-11-05

申办/合作机构-

NL-OMON37240 / CompletedN/A

A Two-Part, Double Blinded, Placebo Controlled, Crossover Repeated Stepped Infusion Dose Study of Respiratory Pharmacodynamics of GAL- 021 and Opioids (Protocol - GAL-021-104). - A two-part study of the effects of GAL-021 and opioids.

开始日期2012-10-29

申办/合作机构

Galleon Pharmaceuticals, Inc.

100 项与 GAL-021 相关的临床结果

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100 项与 GAL-021 相关的转化医学

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100 项与 GAL-021 相关的专利（医药）

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17

项与 GAL-021 相关的文献（医药）

2024-02-27·Cureus

A Single Ascending-Dose Study of the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of the Novel Respiratory Stimulant ENA-001

Article

作者: Colucci, Robert ; Pergolizzi, Joseph ; Miller, Thomas L ; Raffa, Robert B ; Diana, Frank J ; Gould, Errol ; Mathews, Jeanette

Background ENA-001 (formerly known as GAL-021) is a novel, first-in-class respiratory stimulant. Pharmacokinetic and pharmacodynamic properties, plus safety and tolerability, were assessed in a randomized, single-center study of healthy volunteers. Methodology This four-period study was designed to test continuous two-hour intravenous infusion regimens of ENA-001 at doses of 0.96, 1.44, and 1.92 mg/kg/hour versus placebo. Each participant received four infusions with a seven-day minimum washout between them: one infusion each of the three doses of ENA-001 and one placebo. Pharmacokinetic and pharmacodynamic parameters were assessed and adverse events were recorded. Results A total of 17 participants completed the study. ENA-001 was generally safe and well tolerated over the dose range studied (0.96 to 1.92 mg/kg/hour). ENA-001 was able to drive hyperventilation in a dose-dependent manner in healthy participants. Increases in ventilation due to ENA-001 were not associated with like-magnitude blood pressure response. ENA-001-stimulated decreases in ETCO₂ were associated with small, statistically significant, increases in SpO₂ levels. Hyperventilation occurred in two participants at the highest dose level, leading to study discontinuation. The terminal half-life of ENA-001 was 6.33 hours. Conclusions The respiratory stimulant ENA-001 demonstrated well-behaved pharmacokinetics following the two-hour infusion. Mean peak plasma concentrations and the mean total systemic exposure values were approximately dose-proportional in the dose range studied.

2023-08-02·Biomedicines

Modulating Hyperpolarization-Activated Cation Currents through Small Molecule Perturbations: Magnitude and Gating Control.

Review

作者: Chen, Cheng-Shih ; Wu, Sheng-Nan ; So, Edmund Cheung

The hyperpolarization-activated cation current (I_h) exhibits a slowly activating time course of the current (I_h) when the cell membrane is hyperpolarized for an extended duration. It is involved in generating electrical activity in various excitable cells. Numerous structurally distinct compounds or herbal drugs have the potential to impact both the magnitude and gating kinetics of this current. Brivaracetam, a chemical analog of levetiracetam known to be a ligand for synaptic vesicle protein 2A, could directly suppress the I_h magnitude. Carisbamate, an anticonvulsant agent, not only inhibited the I_h amplitude but also reduced the strength of voltage-dependent hysteresis (Hys_(V)) associated with I_h. Cilobradine, similar to ivabradine, inhibited the amplitude of I_h; however, it also suppressed the amplitude of delayed-rectifier K⁺ currents. Dexmedetomidine, an agonist of α2-adrenergic receptor, exerted a depressant action on I_h in a concentration-dependent fashion. Suppression of I_h amplitude was observed when GAL-021, a breathing control modulator, was present at a concentration exceeding 30 μM. Lutein, one of the few xanthophyll carotenoids, was able to suppress the I_h amplitude as well as to depress Hys_(V)'s strength of I_h. Pirfenidone, a pyridine derivative known to be an anti-fibrotic agent, depressed the I_h magnitude in a concentration- and voltage-dependent fashion. Tramadol, a synthetic centrally active analgesic, was shown to reduce the I_h magnitude, independent of its interaction with opioid receptors. Various herbal drugs, including ent-kaurane-type diterpenoids from Croton tonkinensis, Ganoderma triterpenoids, honokiol, and pterostilbene, demonstrated efficacy in reducing the magnitude of I_h. Conversely, oxaliplatin, a platinum-based chemotherapeutic compound, was observed to effectively increase the I_h amplitude. Collectively, the regulatory effects of these compounds or herbal drugs on cellular function can be partly attributed to their perturbations on I_h.

2021-12-01·BMC Pharmacology and Toxicology4区 · 医学

Depressive effectiveness of vigabatrin (γ-vinyl-GABA), an antiepileptic drug, in intermediate-conductance calcium-activated potassium channels in human glioma cells

4区 · 医学

ArticleOA

作者: Huang, Huai-Ying Ingrid ; Hung, Te-Yu ; Huang, Chin-Wei ; Wu, Sheng-Nan

AbstractBackgroundVigabatrin (VGB) is an approved non-traditional antiepileptic drug that has been revealed to have potential for treating brain tumors; however, its effect on ionic channels in glioma cells remains largely unclear.MethodsWith the aid of patch-clamp technology, we investigated the effects of VGB on various ionic currents in the glioblastoma multiforme cell line 13–06-MG.ResultsIn cell-attached configuration, VGB concentration-dependently reduced the activity of intermediate-conductance Ca2+-activated K+ (IKCa) channels, while DCEBIO (5,6-dichloro-1-ethyl-1,3-dihydro-2H-benzimidazol-2-one) counteracted the VGB-induced inhibition of IKCa channels. However, the activity of neither large-conductance Ca2+-activated (BKCa) nor inwardly rectifying K+ (KIR) channels were affected by the presence of VGB in human 13–06-MG cells. However, in the continued presence of VGB, the addition of GAL-021 or BaCl2 effectively suppressed BKCa and KIR channels.ConclusionsThe inhibitory effect of VGB on IKCa channels demonstrated in the current study could be an important underlying mechanism of VGB-induced antineoplastic (e.g., anti-glioma) actions.

100 项与 GAL-021 相关的药物交易

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