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

Immune System DiseasesSkin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Inflammation of hip jointOsteoarthritis, HipPrimary osteoarthritis of knee NOS+ [1]

Originator Organization

Novartis Pharma AG

Active Organization-

Inactive Organization

Novartis AG

Drug Highest PhasePendingPhase 3

First Approval Date-

Regulation-

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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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258

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).

01 Oct 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 ; Tong, Yu ; Wang, Shirui ; 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).

01 Sep 2024·Exploratory Research in Clinical and Social Pharmacy

Renal effects of selective cyclooxygenase-2 inhibitor anti-inflammatory drugs: A systematic review and meta-analysis

Review

Author: Silva, Marcus Tolentino ; Rocha, João Gabriel Mendes ; Galvão, Taís Freire ; Ribeiro-Vaz, Inês ; Biase, Tayanny Margarida Menezes Almeida

BackgroundSelective cyclooxygenase-2 inhibitor anti-inflammatory drugs (coxibs) are associated with the development of adverse events, mainly gastrointestinal and cardiovascular, but renal effects are less known.ObjectiveTo assess the renal risks of coxibs compared to placebo by means of a systematic review and meta-analysis.MethodsRandomized controlled trials that assessed renal effects of coxibs (celecoxib, etoricoxib, lumiracoxib, parecoxib, and valdecoxib) were searched in PubMed, Embase, Scopus and other sources up to March 2024. Two independent reviewers performed study screening, data extraction, and risk of bias assessment. Random effect meta-analysis was employed to calculate the relative risks (RR) and 95% confidence intervals (CI) of renal effects of coxibs compared to placebo and inconsistency among studies (I ² ). Certainty of evidence was assessed using the Grading of Recommendations Assessment, Development and Evaluation approach.ResultsOut of 5284 retrieved records, 49 studies (comprising 46 reports) were included. Coxibs increased the risk of edema (RR 1.46; 95% CI 1.15, 1.86; I ² = 0%; 34 studies, 19,754 participants; moderate-certainty evidence), and celecoxib increased hypertensive or renal events (RR 1.24; 95% CI 1.08, 1.43; I ² = 0%; 2 studies, 3589 participants; moderate-certainty evidence). Etoricoxib increased the risk of hypertension (RR 1.98; 95% CI 1.14, 3.46; I ² = 34%; 13 studies, 6560 participants; moderate-certainty evidence); no difference was observed when pooling all coxibs (RR 1.26; 95% CI 0.91, 1.76; I ² = 26%; 30 studies, 16,173 participants; moderate-certainty evidence).ConclusionsCoxibs likely increase the renal adverse effects, including hypertension and edema. Awareness about the renal risks of coxibs should be increased, mainly in high-risk patient.

100 Deals associated with Lumiracoxib

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External Link

KEGG	Wiki	ATC	Drug Bank
D03714	Lumiracoxib	M01AH06	DB01283

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Inflammation of hip joint	Phase 3	DE	Novartis AG	01 Nov 2004
Inflammation of hip joint	Phase 3	GB	Novartis AG	01 Nov 2004
Osteoarthritis, Hip	Phase 3	US	Novartis AG	01 Nov 2004
Osteoarthritis, Hip	Phase 3	DE	Novartis AG	01 Nov 2004
Osteoarthritis, Hip	Phase 3	GB	Novartis AG	01 Nov 2004
Osteoarthritis, Hip	Phase 3	IT	Novartis AG	01 Nov 2004
Osteoarthritis, Hip	Phase 3	CA	Novartis AG	01 Nov 2004
Primary osteoarthritis of knee NOS	Phase 3	DE	Novartis AG	01 Sep 2003
Primary osteoarthritis of knee NOS	Phase 3	US	Novartis AG	01 Sep 2003
Primary osteoarthritis of knee NOS	Phase 3	CH	Novartis AG	01 Sep 2003

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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	digszffuel(utpbvgnigl) = eufuvjeehp pkkrdwqhud (ubbpiuhmvs )	Positive	01 Nov 2008
				Naproxen 500 mg bid	digszffuel(utpbvgnigl) = atpsthfama pkkrdwqhud (ubbpiuhmvs )
EULAR2004	Not Applicable	Rheumatoid Arthritis	1,151	Lumiracoxib 200 mg	(ofrjfxzgjx) = iybcohvgyr bejepmuiyn (sdarsaqhmg ) View more	-	09 Jun 2004
				Placebo	(ofrjfxzgjx) = srnqetctwv bejepmuiyn (sdarsaqhmg )
EULAR2004	Not Applicable	Osteoarthritis	49	Lumiracoxib 400 mg	ewuijjhonq(thnzoayboh) = eqcukzhbal qqblkhpsqq (pznvubocuc )	-	09 Jun 2004
				Lumiracoxib 800 mg	ewuijjhonq(thnzoayboh) = fsedestgbg qqblkhpsqq (pznvubocuc )
EULAR2003	Not Applicable	Osteoarthritis, Knee	62	Lumiracoxib 200 mg	(ljsedpkybj) = 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) alajtyyimy (rhuykvaazb ) View more	-	18 Jun 2003
				Lumiracoxib 400 mg
EULAR2003	Not Applicable	Osteoarthritis, Knee	364	Lumiracoxib 400 mg	(kcehbainwu) = ildqjvwngf tqqortjxxy (rmcarezwxc ) View more	-	18 Jun 2003
				Celecoxib 200 mg	(kcehbainwu) = evetgqbqgk tqqortjxxy (rmcarezwxc ) View more
EULAR2002	Not Applicable	Osteoarthritis	583	COX189 50 mg bid	-	-	12 Jun 2002
				COX189 100 mg bid
EULAR2002	Not Applicable	-	-	COX-189	odlbrgaejy(bzygclptax) = hhfyoyydek fcipxzluyf (xnmizazymo )	-	12 Jun 2002
				Naproxen	odlbrgaejy(bzygclptax) = eeavxmjgkv fcipxzluyf (xnmizazymo )
EULAR2002	Not Applicable	Osteoarthritis, Hip \| Osteoarthritis, Knee	-	COX189 50 mg b.i.d.	(vzecshthec) = aovxctxegm pjaxxrtugy (wzilkduhcv )	-	12 Jun 2002
				COX189 100 mg b.i.d.	(vzecshthec) = sywpaijyaq pjaxxrtugy (wzilkduhcv )
EULAR2002	Not Applicable	Osteoarthritis	-	COX189 200 mg	(aqpchyjwju) = cfnguhmtgq dnnezybqlh (njblondehn ) View more	Positive	12 Jun 2002
				COX189 400 mg	(aqpchyjwju) = iphfjcqgmf dnnezybqlh (njblondehn ) View more