Delving into the Latest Updates on Lumiracoxib with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

2-((2-chloro-6-fluorophenyl)amino)-5-methylbenzeneacetic acid, Joicela, Lumiracoxib (USAN/INN)

+ [4]

Target

COX-2

Mechanism

COX-2 inhibitors(Cyclooxygenase-2 inhibitors)

Therapeutic Areas-

Active Indication-

Inactive Indication-

Originator Organization

Novartis Pharma AG

Active Organization-

Inactive Organization

Novartis AG

Drug Highest PhasePendingPhase 3

First Approval Date-

Regulation-

Structure

Molecular FormulaC15H13ClFNO2

InChIKeyKHPKQFYUPIUARC-UHFFFAOYSA-N

CAS Registry220991-20-8

The purpose of this study is to determine whether the use of lumiracoxib in this particular population is associated with a decrease in glomerular filtration rate (GFR) compared to diclofenac; and to compare the magnitude of such impairment, if any, associated with use of lumiracoxib and diclofenac.

Start Date01 Jan 2012

Sponsor / Collaborator-

NCT00419796 / CompletedPhase 4

A 4-Week, Multicentre, Randomized, Double-Blind, Placebo Controlled, Double Dummy, Parallel Group Study, to Assess the Effect of Lumiracoxib 100 mg o.d. and Ibuprofen 600 mg t.i.d on 24-Hour Blood Pressure Profile and on Urinary Excretions of Eicosanoids, in Osteoarthritis Patients With Controlled Hypertension

This randomized study will compare the effect of lumiracoxib, ibuprofen and placebo on 24-hour blood pressure profile and on urinary excretions of eicosanoids in controlled hypertensive patients who have osteoarthritis.

Start Date01 Nov 2006

Sponsor / Collaborator

Novartis AG

NCT00333567 / CompletedPhase 4

A Multicenter, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study to Compare Efficacy of a Single Dose of Lumiracoxib 400 mg Given Pre-Emptively Versus Post-Operatively, in Reducing Pain Associated With Ambulatory Arthroscopic Knee Surgery

This study is designed to investigate the efficacy and safety of a single daily dose of 400 mg lumiracoxib given pre-emptively versus post-operatively in terms of efficacy in reducing pain associated with ambulatory arthroscopic knee surgery

Start Date01 Aug 2006

Sponsor / Collaborator

Novartis AG

100 Clinical Results associated with Lumiracoxib

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100 Translational Medicine associated with Lumiracoxib

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100 Patents (Medical) associated with Lumiracoxib

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257

Literatures (Medical) associated with Lumiracoxib

31 Dec 2024·Annals of Medicine

Efficacy and safety of simple analgesics for acute treatment of episodic tension-type headache in adults: a network meta-analysis

Review

Author: Tian, Jinhui ; Xie, Runsheng ; Li, Jiahui ; Jing, Yuyu ; Xu, Feilong ; Cai, Yefeng ; Li, Hui ; Wang, Yangyang ; Chen, Wenjia

OBJECTIVETension-type headache is the most common type of primary headache and results in a huge socioeconomic burden. This network meta-analysis (NMA) aimed to compare the efficacy and safety of simple analgesics for the treatment of episodic tension-type headache (ETTH) in adults.METHODSWe searched the Cochrane Library, PubMed, Web of Science, Embase, Chinese BioMedical Literature database and International Clinical Trials Registry Platform databases for eligible randomized clinical trials reporting the efficacy and/or safety of simple analgesics. A Bayesian NMA was performed to compare relative efficacy and safety. The surface under the cumulative ranking curve (SUCRA) was calculated to rank interventions. PROSPERO registration number: CRD42018090554.RESULTSWe highlighted six studies including 3507 patients. For the 2 h pain-free rate, the SUCRA ranking was ibuprofen > diclofenac-K > ketoprofen > acetaminophen > naproxen > placebo. All drugs except naproxen reported a higher 2 h pain-free rate than placebo, with a risk ratio (RR) of 2.86 (95% credible interval, CrI: 1.62-5.42) for ibuprofen and 2.61 (1.53-4.88) for diclofenac-K. For adverse events rate, the SUCRA ranking was: metamizol > diclofenac-K > ibuprofen > lumiracoxib > placebo > aspirin > acetaminophen > naproxen > ketoprofen. The adverse event rates of all analgesics were no higher than those of placebo, except for ketoprofen. Moreover, all drugs were superior to placebo in the global assessment of efficacy. In particular, the RR of lumiracoxib was 2.47 (1.57-4.57). Global heterogeneity I² between the studies was low.CONCLUSIONSSimple analgesics are considered more effective and safe as a placebo for ETTH in adults. Our results suggest that ibuprofen and diclofenac-K may be the two best treatment options for patients with ETTH from a comprehensive point of view (both high-quality evidence).

10 Jul 2024·Bioorganic & medicinal chemistry letters

Discovery of L15 as a novel Vif PROTAC degrader with antiviral activity against HIV-1.

Article

Author: Wang, Weilin ; Liu, Yuanyuan ; Zheng, Yongtang ; Huang, Qing ; Deng, Rui ; Luo, Dan ; Wang, Shirui ; Tong, Yu ; Yu, Su ; Ma, Xinyu ; Li, Rui ; Pu, Chunlan ; Luo, Ronghua ; Zhang, Hongjia ; Yang, Liumeng

Viral infectivity factor (Vif) has been recognized as a new therapeutic target for human immunodeficiency virus-1 (HIV-1) infected patients. In our previous work, we have synthesized a novel class of Vif inhibitors with 2-amino-N-(5-hydroxy-2-methoxyphenyl)-6-((4-nitrophenyl)thio)benzamide scaffold, which show obvious activity in HIV-1 infected cells and are also effective against drug-resistant strains. Proteolytic targeting chimera (PROTAC) utilizes the ubiquitin-proteasome system to degrade target proteins, which is well established in the field of cancer, but the antiviral PROTAC molecules are rarely reported. In order to explore the effectiveness of PROTAC in the antiviral area, we designed and synthesized a series of degrader of HIV-1 Vif based on 2-amino-N-(5-hydroxy-2-methoxyphenyl)-6-((4-nitrophenyl)thio)benzamide scaffold. Among them, L15 can degrade Vif protein obviously in a dose-dependent manner and shows certain antivirus activity. Meanwhile, molecular dynamics simulation indicated that the ternary complex formed by L15 Vif, and E3 ligase adopted a reasonable binding mode and maintained a stable interaction. This provided a molecular basis and prerequisite for the selective degradation of the Vif protein by L15. This study reports the HIV-1 Vif PROTAC for the first time and represents the proof-of-concept of PROTACs-based antiviral drug discovery in the field of HIV/ acquired immune deficiency syndrome (AIDS).

23 Mar 2024·Journal of Biomolecular Structure and Dynamics

Molecular insights in repurposing selective COX-2 inhibitor celecoxib against matrix metalloproteinases in potentiating delayed wound healing: a molecular docking and MMPB/SA based analysis of molecular dynamic simulations

Article

Author: Tallapaneni, Vyshnavi ; Karri, Veera Venkata Satyanarayana Reddy ; Jupudi, Srikanth ; Swaroop, Akey Krishna ; Mude, Lavanya

Matrix metalloproteinases (MMPs) are proteolytic enzymes that play a role in healing, including reducing inflammation, promoting fibroblast and keratinocyte migration, and modifying scar tissue. Due to their pleiotropic functions in the wound-healing process in diabetic wounds, MMPs constitute a significant cause of delayed wound closure. COX-2 inhibitors are proven to inhibit inflammation. The present study aims to repurpose celecoxib against MMP-2, MMP-8 and MMP-9 through in silico approaches, such as molecular docking, molecular dynamics, and MMPB/SA analysis. We considered five selective COX-2 inhibitors (celecoxib, etoricoxib, lumiracoxib, rofecoxib and valdecoxib) for our study against MMPs. Based on molecular docking study and hydrogen bonding pattern, celecoxib in complex with three MMPs was further analyzed using 1 µs (1000 ns) molecular dynamics simulation and MMPB/SA techniques. These studies identified that celecoxib exhibited significant binding affinity -8.8, -7.9 and -8.3 kcal/mol, respectively, against MMP-2, MMP-8 and MMP-9. Celecoxib formed hydrogen bonding and hydrophobic (π-π) interactions with crucial substrate pocket amino acids, which may be accountable for their inhibitory nature. The MMPB/SA studies showed that electrostatic and van der Waal energy terms favoured the total free binding energy component, while polar solvation terms were highly disfavored. The in silico analysis of the secondary structures showed that the celecoxib binding conformation maintains relatively stable along the simulation trajectories. These findings provide some key clues regarding the accommodation of celecoxib in the substrate binding S1' pocket and also provide structural insights and challenges in repurposing drugs as new MMP inhibitors with anti-inflammatory and anti-inflammatory wound-healing properties.Communicated by Ramaswamy H. Sarma.

100 Deals associated with Lumiracoxib

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External Link

KEGG	Wiki	ATC	Drug Bank
D03714	Lumiracoxib	M01AH06	DB01283

R&D Status

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00170898 (Pubmed \| Int J Clin Pract)	Phase 4	Musculoskeletal Pain	406	Lumiracoxib 400 mg qd	rffuppedms(vfrqbwbffr) = mkqkerlzub haahjavbrj (huumhoqehz )	Positive	01 Nov 2008
				Naproxen 500 mg bid	rffuppedms(vfrqbwbffr) = mrbvrqdyjt haahjavbrj (huumhoqehz )
EULAR2004	Not Applicable	Rheumatoid Arthritis	1,151	Lumiracoxib 200 mg	(ekvobjpxuy) = xltpgqpojy ndbpyojxbk (uhaxsgydtx ) View more	-	09 Jun 2004
				Placebo	(ekvobjpxuy) = oyzirestxd ndbpyojxbk (uhaxsgydtx )
EULAR2004	Not Applicable	Osteoarthritis	49	Lumiracoxib 400 mg	lyowuntewd(zsgphbqeof) = zvabxizpdq bvekytaazr (fchdyculik )	-	09 Jun 2004
				Lumiracoxib 800 mg	lyowuntewd(zsgphbqeof) = yyqkxqzdtf bvekytaazr (fchdyculik )
EULAR2003	Not Applicable	Osteoarthritis, Knee	364	Lumiracoxib 400 mg	(nwxofsmaze) = ljzmxbufsk bhuvuioqzu (uhvrploqcu ) View more	-	18 Jun 2003
				Celecoxib 200 mg	(nwxofsmaze) = sbftbgvkti bhuvuioqzu (uhvrploqcu ) View more
EULAR2003	Not Applicable	Osteoarthritis, Knee	62	Lumiracoxib 200 mg	(sdfnhxekrp) = Normalized (dose and weight) apparent plasma clearance of lumiracoxib was similar in both males and females and in older (≥65 years) and younger patients (<65 years) smfdfprhqk (nwximnvfxf ) View more	-	18 Jun 2003
				Lumiracoxib 400 mg
EULAR2002	Not Applicable	Osteoarthritis	-	COX189 200 mg	(apsssjaqiu) = wnircndsrx rjgxbeenuf (ujpjmkxomh ) View more	Positive	12 Jun 2002
				COX189 400 mg	(apsssjaqiu) = wlpoxiknwu rjgxbeenuf (ujpjmkxomh ) View more
EULAR2002	Not Applicable	Osteoarthritis	583	COX189 50 mg bid	-	-	12 Jun 2002
				COX189 100 mg bid
EULAR2002	Not Applicable	-	-	COX-189	lglcskbgio(amisklibmj) = epvqjonkod wasbntqmqi (wtlwqfomhy )	-	12 Jun 2002
				Naproxen	lglcskbgio(amisklibmj) = kdlhwtpppz wasbntqmqi (wtlwqfomhy )
EULAR2002	Not Applicable	Osteoarthritis, Hip \| Osteoarthritis, Knee	-	COX189 50 mg b.i.d.	(bmrjfisxqf) = iviaeyyevu xucsbwvmbn (iutmfuomed )	-	12 Jun 2002
				COX189 100 mg b.i.d.	(bmrjfisxqf) = eobypwhywx xucsbwvmbn (iutmfuomed )