Acetylcysteine lysinate(Acetylcysteine lysinate)

概要

基本信息

药物类型

小分子化药

别名

L-Lysine-N-acetyl-L-cysteinate、N-acetylcysteine lysinate、Nacystelyn

靶点-

作用机制

溶菌剂

治疗领域

遗传病与畸形消化系统疾病呼吸系统疾病+ [2]

在研适应症-

非在研适应症

寻常痤疮囊性纤维化慢性阻塞性肺疾病

原研机构

Galephar Research, Inc.

在研机构-

非在研机构

Galephar Research, Inc.

Laboratoires S.M.B. SA

最高研发阶段终止临床3期

首次获批日期-

最高研发阶段(中国)-

特殊审评孤儿药 (欧盟)

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结构

分子式C5H9NO3S

InChIKeyPWKSKIMOESPYIA-BYPYZUCNSA-N

CAS号616-91-1

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关联

3

项与 Acetylcysteine lysinate 相关的临床试验

EUCTR2020-005270-10-BG / Not yet recruiting临床2期

A randomized, partially blinded, parallel study to evaluate the effects of nacystelyn in combination with isotretinoin in the treatment of recalcitrant acne vulgaris.

开始日期2021-08-18

申办/合作机构-

EUCTR2019-001160-29-BE / Not yet recruiting临床2期

A single blind, placebo controlled, three period, chronic dosing (6 weeks), multicentre, exploratory study to evaluate the effects of Nacystelyn (20 mg BID and 40 mg BID) on Functional Respiratory Imaging (FRI) parameters in subjects with moderate to severe COPD

开始日期2019-06-24

申办/合作机构-

EUCTR2010-018454-13-DE / Not yet recruitingN/A

A Phase III, Multicentre, Randomised, Placebo-Controlled, Double Blind Study of the Incidence of Recurring Pulmonary Exacerbations in Cystic Fibrosis Patients using Two Different Doses of Inhaled Nacystelyn®

开始日期2010-08-31

申办/合作机构

Laboratoires S.M.B. SA

100 项与 Acetylcysteine lysinate 相关的临床结果

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100 项与 Acetylcysteine lysinate 相关的转化医学

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100 项与 Acetylcysteine lysinate 相关的专利（医药）

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48

项与 Acetylcysteine lysinate 相关的文献（医药）

2019-08-01·Clinical Pharmacology in Drug Development

Pharmacokinetic Properties of Ibuprofen (IBU) From the Fixed‐Dose Combination IBU/Caffeine (400/100 mg; FDC) in Comparison With 400 mg IBU as Acid or Lysinate Under Fasted and Fed Conditions—Data From 2 Single‐Center, Single‐Dose, Randomized Crossover Studies in Healthy Volunteers

Article

作者: Weiser, Thomas ; Schepers, Cornelia ; Mück, Tobias ; Lange, Robert

AbstractRapid onset of analgesic action is linked with rapid absorption of analgesics (high maximum concentration [Cmax] and short time to maximum concentration [tmax]). After overnight fasting, ibuprofen lysinate reaches higher peak plasma levels (Cmax) earlier than ibuprofen acid (tmax) with comparable exposure (area under the plasma concentration–time curve [AUC]); however, subjects usually take ibuprofen with or within a short time of a meal. Therefore, pharmacokinetic (PK) studies under fed conditions may better characterize properties under real‐life conditions. We investigated a new fixed‐dose combination (FDC) of ibuprofen acid 400 mg and caffeine 100 mg in 2 single‐dose, randomized, crossover PK studies in healthy subjects (both N = 36). The FDC was compared with ibuprofen 400 mg as acid and as lysinate after an overnight fast in Study 1, and with ibuprofen lysinate after a meal in Study 2. After fasting, results for ibuprofen in the FDC were comparable with those from ibuprofen acid alone. Caffeine did not affect the Cmax, tmax, and AUC. As expected, a higher Cmax and shorter tmax were observed with ibuprofen lysinates vs the FDC. Compared with administration after fasting, Cmax and tmax for ibuprofen lysinate administered postprandially were markedly different, while with FDC, these parameters were less sensitive to food intake. Taken after a meal, ibuprofen in the FDC reached tmax earlier than ibuprofen lysinate (median 1.25 vs 1.63 hours), and Cmax was approximately 13% higher, with comparable AUC, suggesting that the profile of ibuprofen was in favor of the FDC compared with ibuprofen lysinate. Thus, under real‐life conditions, ibuprofen lysinate had no PK advantage over the FDC. All preparations were well tolerated.

2019-01-01·Chemico-Biological Interactions2区 · 医学

The soluble curcumin derivative NDS27 inhibits superoxide anion production by neutrophils and acts as substrate and reversible inhibitor of myeloperoxidase

2区 · 医学

Article

作者: Obinger, Christian ; Franck, Thierry ; Prévost, Martine ; Van Antwerpen, Pierre ; Furtmüller, Paul G ; Mouithys-Mickalad, Ange ; Serteyn, Didier ; Zouaoui Boudjeltia, Karim ; Soubhye, Jalal ; Aldib, Iyas ; Neven, Philippe

A water-soluble curcumin lysinate incorporated into hydroxypropyl-β-cyclodextrin (NDS27) has been developed and shown anti-inflammatory properties but no comparative study has been made in parallel with its parent molecule, curcumin on polymorphonuclear neutrophils (PMNs) and myeloperoxidase (MPO) involved in inflammation. The effect of NDS27, its excipients (hydroxypropyl-β-cyclodextrin and lysine), curcumin lysinate and curcumin were compared on the release of superoxide anion by PMNs using a chemiluminescence assay and on the enzymatic activity of MPO. It was shown that curcumin and NDS27 exhibit similar inhibition activities on superoxide anion release by stimulated PMNs but also on MPO peroxidase and halogenation activities. The action mechanism of curcumin and NDS27 on the MPO activity was refined by stopped-flow and docking analyses. We demonstrate that both curcumin and NDS27 are reversible inhibitors of MPO by acting as excellent electron donors for redox intermediate Compound I (∼10⁷ M^-1 s^-1) but not for Compound II (∼10³ M^-1 s^-1) in the peroxidase cycle of the enzyme, thereby trapping the enzyme in the Compound II state. Docking calculations show that curcumin is able to enter the enzymatic pocket of MPO and bind to the heme cavity by π-stacking and formation of hydrogen bonds involving substituents from both aromatic rings. Hydroxypropyl-β-cyclodextrin is too bulky to enter MPO channel leading to the binding site suggesting a full release of curcumin from the cyclodextrin thereby allowing its full access to the active site of MPO. In conclusion, the hydroxypropyl-β-cyclodextrin of NDS27 enhances curcumin solubilization without affecting its antioxidant capacity and inhibitory activity on MPO.

2015-11-01·Int. Journal of Clinical Pharmacology and Therapeutics4区 · 医学

Ibuprofen lysinate, quicker and less variable: relative bioavailability compared to ibuprofen base in a pediatric suspension dosage form

4区 · 医学

Article

作者: Yaira Mathison ; Ignasi Gich ; Maria R Ballester ; Xavier Font ; Maite Tarré ; Rosa M Antonijoan ; Jimena Coimbra ; Montse Puntes ; Joan Martínez ; Juan Manuel Ferrero-Cafiero

OBJECTIVESTo assess and compare the bioavailability of ibuprofen enantiomers (R and S) of two different pediatric suspensions: the first one with ibuprofen lysinate (Algidrin® Pediátrico, FARDI S.A., Barcelona, Spain) and the second one with ibuprofen base (Dalsy®, Abbott Laboratories S.A., Madrid, Spain).METHODSA randomized, open-label, single-dose, balanced, crossover study under fasting conditions was performed at the CIM-Sant Pau. 24 healthy volunteers received a single dose of ibuprofen lysinate (AlgidrinÂ® PediÃ¡trico, FARDI S.A.) and ibuprofen base (Dalsy®, Abbott Laboratories S.A.) equivalent to 400 mg of ibuprofen. 18 blood samples were drawn and ibuprofen enantiomer plasma concentrations were determined using an enantioselective analytical method. An analysis of variance (ANOVA) model was used, and the 90% confidence intervals (CI) were calculated; further analyses were made regarding rate of absorption and variability.RESULTSThe pharmacokinetic parameters (Algidrin® Pediátrico vs. Dalsy® (Mean±SD)) were: S-enantiomer: Cmax=22.39±5.33 vs. 19.97±3.19 μg/mL; AUC0t=74.83±16.69 vs. 74.64±14.80 μg×h/mL, and AUC0∞=77.46±19.33 vs. 76.98±17.13 μg×h/mL; and for R-enantiomer: Cmax=21.74±3.76 vs. 15.20±2.03 μg/mL; AUC0t=57.55±10.17 vs. 46.13±9.61 μg×h/mL, and AUC0∞ value was 58.49±10.57 vs. 47.03±10.02 μg×h/mL. The tmax (Median) for S-enantiomer (active) were: 0.5 vs. 1.33 hours (p=0.001) and for R-enantiomer: 0.5 vs. 1.0 hours (p=0.004). Ibuprofen pharmacokinetic values may vary under fed state and in pediatric population.CONCLUSIONSWhile S-ibuprofen shows a similar bioavailability for AUC0t, AUC0∞, and Cmax, R-ibuprofen shows suprabioavailability for the lysinate formulation. The rate of absorption of the ibuprofen lysinate suspension is quicker and less variable than that of the ibuprofen base reference suspension and it exhibits a shorter tmax, which is of particular interest for achieving a rapid and homogeneous analgesic and antipyretic effect.

100 项与 Acetylcysteine lysinate 相关的药物交易

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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
寻常痤疮	临床3期	保加利亚	Laboratoires S.M.B. SA	2021-08-10
慢性阻塞性肺疾病	临床3期	比利时	Laboratoires S.M.B. SA	2019-07-14
囊性纤维化	临床3期	-	Galephar Research, Inc.	-
囊性纤维化	临床3期	欧盟	-	-
囊性纤维化	临床3期	-	Laboratoires S.M.B. SA	-