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

Action

inhibitors

Mechanism

COX-2 inhibitors(Cyclooxygenase-2 inhibitors)

Therapeutic Areas

Immune System DiseasesSkin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Osteoarthritis, HipPrimary osteoarthritis of knee NOSRheumatoid Arthritis

Originator Organization

Novartis Pharma AG

Active Organization-

Inactive Organization

Novartis AG

License Organization-

Drug Highest PhasePendingPhase 3

First Approval Date-

Regulation-

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Structure/Sequence

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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404

Literatures (Medical) associated with Lumiracoxib

01 Feb 2025·Journal of Pharmaceutical Sciences

Enzymatic hydrolysis of acyl glucuronide metabolites in human liver microsomes correlates to the risk of idiosyncratic drug toxicity

Article

Author: Ikuta, Hiroyuki ; Yabuuchi, Yusuke ; Hashimoto, Yu ; Iwaki, Masahiro ; Shimada, Hiroaki ; Kawase, Atsushi ; Matzno, Sumio

Acyl glucuronide (AG) is a reactive metabolite that causes idiosyncratic drug toxicity (IDT). Although the instability of AG is used to predict the IDT risk of novel drug candidates, it sometimes overestimates the IDT risk. We investigated whether the rate of enzymatic AG hydrolysis in human liver microsomes (HLM) can predict the risk of IDT. We used 16 drugs classified into three categories in terms of IDT risk: drugs withdrawn from the market owing to severe IDT (withdrawn, WDN) and drugs still being on the market, regardless of IDT risk (warning, WA) or not (safe, SA). AG was incubated with HLM, and the resulting parent drugs for AG hydrolysis were quantified using HPLC. The rate of enzymatic AG hydrolysis in the HLM of WDN was higher than that in WA and SA, and no difference was observed between WA and SA. We categorized WA and SA as commercially available (CA) drugs and performed a logistic regression analysis. The rate of enzymatic AG hydrolysis in HLM significantly distinguished WDN drugs from CA drugs, with an estimated classification value of 0.189 nmol/min/mg protein. In conclusion, the rate of enzymatic AG hydrolysis in HLM may be useful for predicting the risk in drug development.

28 Jan 2025·Environmental Science & Technology

Read-Across of Biotransformation Potential between Activated Sludge and the Terrestrial Environment: Toward Making It Practical and Plausible

Article

Author: Coll, Claudia ; Hafner, Jasmin ; Zhang, Kunyang ; Fenner, Kathrin ; Screpanti, Claudio

Recent emphasis on the development of safe-and-sustainable-by-design chemicals highlights the need for methods facilitating the early assessment of persistence. Activated sludge experiments have been proposed as a time- and resource-efficient way to predict half-lives in simulation studies. Here, this persistence "read-across" approach was developed to be more broadly and robustly applicable. We evaluated 21 previously used reference plant protection products (PPPs) for their broader applicability in calibrating regression and classification models for predicting half-lives in soil (DT50_OECD307) and water-sediment systems (DT50_OECD308) based on their half-life in sludge and the organic carbon-water partition coefficient K_OC as predictors. The calibrated regression models showed satisfactory predictions of DT50_OECD307 for another 22 test PPPs. Performance was less satisfying for the prediction of DT50_OECD308 for 46 active pharmaceutical ingredients (APIs), suggesting a need for expanding the set of calibration substances and more experimental K_OC values. The classification models mostly correctly classified persistent and non-persistent test compounds for both PPPs and APIs, which is relevant for early-stage screening of persistence. Transformation products of the reference compounds in activated sludge samples were consistent with the reported degradation pathways in soil, particularly with respect to major aerobic, enzyme-catalyzed transformation reactions. Overall, "reading across" biotransformation in environmental compartments such as soils or sediments from experiments with activated sludge outperformed three widely used in silico approaches for estimating half-lives and hence has immediate potential to support early assessment of biodegradability when aiming to develop chemicals that are safe and sustainable by design.

01 Jan 2025·Microvascular Research

The role of the cyclooxygenase-2 pathway in tissue ischemia and revascularization following skeletal muscle injury induced by bothropic snake venom

Article

Author: Moreira, Vanessa ; Han, Sang Won ; Correia, Melissa Rodrigues ; Escalante, Teresa

Bothrops asper venom (Bav) contains metalloproteinases that disrupt the microvascular system, impairing muscle tissue regeneration after injury. This study investigated the impact of the cyclooxygenase-2 (COX-2) pathway on vascular injury and revascularization in muscle injuries induced by Bav. Mice were injected with Bav into the gastrocnemius muscle and treated with lumiracoxib, a selective COX-2 inhibitor, 30 min, 2 days, and 6 days post-Bav injection. Muscle tissue was analyzed at 24 h, 7 days, and 21 days post-injection. A decrease in COX-2 expression at 24 h post-Bav injection indicated significant necrosis and tissue loss. Both Bav injection and lumiracoxib treatment influenced the decrease of prostaglandin (PG)D₂ and PGE₂ production. Seven and 21 days post-Bav injections, COX-2 expression increased, along with PGDs levels unaffected by lumiracoxib, indicating that the other isoform COX-1 pathway could contribute to the release of PGs. Bav/lumiracoxib treated animals presented exacerbated limb ischemia, implying that COX-2-derived prostaglandins preserve vessel integrity. CD31, an angiogenesis marker, initially (24 h) decreased post-Bav injection but increased at 7 and 21 days in Bav/lumiracoxib mice, suggesting a down-modulatory role for COX-2-derived prostaglandins in early angiogenesis and tissue regeneration. Vascular endothelial growth factor (VEGF) production rose 7 days post-Bav injection, supporting its role in angiogenesis. Previous treatment with lumiracoxib promoted release of VEGF levels 21 days post-Bav injury showing that the inhibition of COX-2 pathway in the early stage of revascularization stimulates the neovascularization regulated by elevated release of VEGF. Similarly, metalloproteinases (MMPs), such as MMP-9, MMP-10, and MMP-13, crucial for vascular remodeling, were elevated 21 days after Bav/lumiracoxib treatment. In conclusion, the COX-2 pathway is essential to decrease the high grade of ischemia caused by acute injury induced by Bav. However, the decrease of activity in the COX-2 pathway in the first stages of revascularization contributes to the elevated production of key pro-angiogenic mediators that up-regulate the restoration of microvasculature and blood flow in muscle tissue injured by botropic venoms.

1

News (Medical) associated with Lumiracoxib

19 Oct 2005

·www.biospace.com

Companies Debate Arthritis Drug Safety At FDA; Whistleblower To Air New Pain Drug Analysis

The maker of Celebrex and Bextra says the two prescription painkillers are safe, even as an official of another company that makes a similar drug says he believes all drugs in the same class may pose heart or stroke problems. Merck & Co., pulled Vioxx from the market after a long-term trial indicated that users of the popular pill could have a variety of problems from stroke to irregular heartbeat to heart attack. Officials of Pfizer Inc. told a joint meeting of two Food and Drug Administration (news - web sites) advisory committees on Wednesday that they believe the company’s Celebrex and Bextra remain safe and effective treatments for chronic pain. When Merck withdrew Vioxx on Sept. 30 the company acted because it feared some problem with the drug itself was leading to the strokes and heart trouble. But Dr. Ned S. Braunstein, senior director of Merck Research Laboratories, told the panels that since then studies suggesting similar problems with Celebrex and Bextra have changed his mind. “The data strongly suggest it is a class effect” for all drugs of that type, Braunstein said. The drugs, designed to help people in chronic pain from conditions such as arthritis, are known as Cox-2 inhibitors. At least two other Cox-2 drugs are awaiting approval from the FDA, Arcoxia from Merck and Lumiracoxib from Novartis Pharmaceuticals. The panels planned to discuss those drugs Thursday.

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
Osteoarthritis, Hip	Phase 3	Canada	Novartis AG	01 Nov 2004
Osteoarthritis, Hip	Phase 3	Germany	Novartis AG	01 Nov 2004
Osteoarthritis, Hip	Phase 3	Italy	Novartis AG	01 Nov 2004
Osteoarthritis, Hip	Phase 3	United Kingdom	Novartis AG	01 Nov 2004
Osteoarthritis, Hip	Phase 3	United States	Novartis AG	01 Nov 2004
Rheumatoid Arthritis	Phase 3	-	Novartis AG	01 Nov 2004
Primary osteoarthritis of knee NOS	Phase 3	Germany	Novartis AG	01 Sep 2003
Primary osteoarthritis of knee NOS	Phase 3	United States	Novartis AG	01 Sep 2003
Primary osteoarthritis of knee NOS	Phase 3	Switzerland	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	lcjrwdrjnh(nxtwncjxha) = mnivlxifwn kdclyokcwv (cqmyxqayrp )	Positive	01 Nov 2008
				Naproxen 500 mg bid	lcjrwdrjnh(nxtwncjxha) = jumzilzses kdclyokcwv (cqmyxqayrp )
NCT00637949 (Pubmed \| BMC Musculoskelet Disord)	Phase 3	Osteoarthritis	309	Lumiracoxib 400 mg	ptbfzndero(yevdiwjdku) = xudhldwduw avryuygipf (xkjchhlwpx )	-	08 Sep 2008
				Rofecoxib 25 mg	ptbfzndero(yevdiwjdku) = qusyrdseye avryuygipf (xkjchhlwpx )
NCT00145301 (Pubmed \| BMC Musculoskelet Disord)	Phase 3	Osteoarthritis	-	Lumiracoxib 100 mg once daily	yngjnqdxjk(ppnlelrztn) = sosvqdadns gwyskvsajk (esejxvedon )	Positive	07 Mar 2008
				Lumiracoxib 100 mg twice daily	yngjnqdxjk(ppnlelrztn) = vvlmqhjaws gwyskvsajk (esejxvedon )
NCT00348491 (Pubmed \| J Pain)	Phase 4	Pain	-	Lumiracoxib 400 mg	(wbmgmcsxrs) = kbdegffkhj vsuyvnccnw (eauxppxoso )	-	01 Jan 2008
				Celecoxib 400 mg	(wbmgmcsxrs) = pngnbnuwjz vsuyvnccnw (eauxppxoso )
NCT00267215 (Pubmed \| Arthritis Res Ther)	Phase 3	Osteoarthritis, Knee	364	Lumiracoxib 400 mg/day	bxnpspqdez(ounlybdqdi) = The overall incidence of adverse events was similar across treatment groups. pcuoernxkj (vpynqonmri )	Positive	01 Jan 2006
				Placebo
EULAR2004	Not Applicable	Osteoarthritis	49	Lumiracoxib 400 mg	bxmjsxsepp(vbvbwwcclw) = wywbdonyve cnwkjhmmzh (urqqjlzlxe )	-	09 Jun 2004
				Lumiracoxib 800 mg	bxmjsxsepp(vbvbwwcclw) = uldxxdkxpw cnwkjhmmzh (urqqjlzlxe )
EULAR2004	Not Applicable	Rheumatoid Arthritis	1,151	Lumiracoxib 200 mg	(xhglbsimhh) = mivymjwzpo qcvajreeao (muzbjkemmz ) View more	-	09 Jun 2004
				Placebo	(xhglbsimhh) = edghskwicr qcvajreeao (muzbjkemmz )
EULAR2003	Not Applicable	Osteoarthritis, Knee	62	Lumiracoxib 200 mg	(iqdkxhrmic) = 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) wvvcgrxgla (xbdgbccpor ) View more	-	18 Jun 2003
				Lumiracoxib 400 mg
EULAR2003	Not Applicable	Osteoarthritis, Knee	364	Lumiracoxib 400 mg	(zfxjhunldv) = snzsapqpwb vghpgjbqtb (dgmzxtlhth ) View more	-	18 Jun 2003
				Celecoxib 200 mg	(zfxjhunldv) = svlouorduz vghpgjbqtb (dgmzxtlhth ) View more
EULAR2002	Not Applicable	Osteoarthritis, Hip \| Osteoarthritis, Knee	-	COX189 50 mg b.i.d.	(rguxdfpove) = reizosarox qudyzvwviw (xexhgoorfs )	-	12 Jun 2002
				COX189 100 mg b.i.d.	(rguxdfpove) = vlmjqtdoxc qudyzvwviw (xexhgoorfs )