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naproxen (naproxen, Verex / naproxen, Biovail)

✓ Approved

Bausch Health Companies Inc. · PTGS1 · Small Molecule

What is naproxen?

naproxen is a small molecule developed by Bausch Health Companies Inc.. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand Namesnaproxen, Verex, naproxen, Biovail
CompanyBausch Health Companies Inc.
Drug ClassSmall Molecule
Molecular TargetPTGS1, PTGS2
RouteOral (PO)
StatusApproved

Mechanism of Action

Molecular Targets

naproxen acts on 2 molecular targets:

PTGS1prostaglandin-endoperoxide synthase 1 (COX3, PCOX1)
PTGS2prostaglandin-endoperoxide synthase 2 (GRIPGHS, hCox-2)
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Therapeutic Indications

naproxen is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Musculoskeletal and connective tissue disordersMusculoskeletal pain✓ Approved

Related Research Articles

PubMedJournal of colloid and interface science2026-11-10

Defect-driven Electron transfer activation of persulfate over N-doped graphene aerogels for naproxen degradation.

Liu Yu Y, Zhao Ying Y, Wang Jun J, Shen Yi Y et al.

Defect-driven catalysis has emerged as a promising paradigm for persulfate activation, yet the precise role of carbon defects relative to nitrogen dopants remains poorly understood. Herein, we synthesized nitrogen-doped graphene aerogels (NGA) with systematically tailored defect densities and nitrogen configurations via controlled pyrolysis temperatures and durations. Using naproxen (NPX) as a model pollutant, we demonstrate that the defect-engineered catalysts activate both peroxymonosulfate (PMS) and peroxydisulfate (PDS) effectively through an electron-transfer process (ETP), as verified by quenching experiments, electron paramagnetic resonance (EPR) spectroscopy, electrochemical analysis, and in-situ Raman spectroscopy. Quantitative structure-activity relationship analyses revealed that in-plane lattice disruptions (vacancies and topological defects), rather than edge sites, oxygenated functionalities, or graphitic nitrogen, serve as the primary active sites governing catalytic kinetics. Notably, PMS activation showed a stronger association with localized sp3-hybridized defective domains, whereas PDS activation exhibited a greater dependence on overall defect density, revealing distinct oxidant-dependent site preferences arising from their molecular asymmetry and electrophilicity. The optimized catalyst demonstrated excellent stability, broad pH adaptability in the PMS system (pH 3-11), resistance to real water matrices, and effective detoxification. This work resolves the ambiguity regarding active sites in nitrogen-doped carbocatalysts and provides a mechanistic framework for rational catalyst design.

PubMedJournal of chromatography. A2026-11-08

One-pot synthesis of an amphoteric polydopamine-silica sorbent for solid-phase extraction of pharmaceuticals from water and urine.

Alshatti Laila L, Rashad Mohamed M, Alhendal Abdullah A

A polydopamine-silica (PDA-SiO2) hybrid sorbent was fabricated via a one-pot, base-catalyzed sol-gel condensation and oxidative polymerization strategy, employing dodecyltrimethylammonium bromide (DTAB) as a cationic surface texture-directing agent. Following thorough sequential washing to ensure complete DTAB removal, the final sorbent - comprising an APTES-grafted silica core (providing protonatable amine binding sites) enveloped by a conformal polydopamine shell (5-10 nm, offering π-π stacking, cation-π, and hydrogen bonding interaction pathways)-was systematically evaluated for the simultaneous preconcentration of acidic (naproxen, mefenamic acid) and basic (amitriptyline, tamoxifen) pharmaceuticals from tap water and simulated biological matrices. Material characterization by SEM, TEM, FT-IR, XPS, BET, and zeta potential confirmed a non-porous, solid-core architecture with an amphoteric surface charge profile (pHpzc = 5.98), which is substantially higher than that of unmodified silica (pHpzc ≈ 2-3), confirming successful APTES and PDA functionalization. Under optimized conditions (pH 7.0, 5.0% (w/v) NaCl, 10.0 mL sample volume), simultaneous quantitative retention of all four analytes was achieved. A pH-responsive sequential elution protocol - 0.1% formic acid in methanol for basic drugs, followed by 2% NH4OH in methanol for acidic drugs - delivered class-selective desorption with recoveries of 89-98% across both tap water and synthetic urine matrices. The method exhibited excellent linearity over 1.0-500 µg L-1 (R2 ≥ 0.9982), limits of detection of 0.1-0.3 µg L-1, and a theoretical enrichment factor of 20 (10.0 mL → 0.5 mL), with experimentally confirmed values of 18.2-19.6 across all analytes, and maintained quantitative performance (recovery >91%) over five of six consecutive extraction-regeneration cycles, with a marginal decline to 86-88% observed only in the sixth cycle. Validated in spiked tap water (92-98 %, RSD < 5%) and synthetic urine (89-97 %, RSD < 5 %), the method demonstrated robust anti-matrix interference capability.

PubMedACS omega2026-11-06

pH-Responsive Delivery of Nonsteroidal Anti-Inflammatory Drugs by ZIF‑8 Metal-Organic Frameworks for Cancer Treatment.

di Nicola Nicola N, Di Vito Nolfi Mauro M, Vetrano Alice A, Esposito Jennifer J et al.

Nonsteroidal anti-inflammatory drugs (NSAIDs) have attracted increasing attention as potential anticancer agents due to their ability to inhibit cyclooxygenase-mediated inflammatory pathways involved in tumor progression. However, their clinical use in oncology remains limited by poor tumor selectivity and systemic toxicity. In this work, we investigate zeolitic imidazolate framework-8 (ZIF-8) nanoparticles as pH-responsive carriers for the delivery of different NSAIDs with potential anticancer activity. A loading strategy based on the conversion of the drugs into their sodium salts, followed by ultrasound-assisted encapsulation, was developed to preserve the structural integrity of the MOF while achieving efficient drug incorporation. Structural and textural characterization by XRPD, SEM, ATR-MIR spectroscopy, and nitrogen physisorption confirmed the formation of ZIF-8 nanoparticles with an average size of about 150 nm and the successful encapsulation of the drugs within the porous framework. High-performance liquid chromatography revealed drug-loading efficiencies exceeding 80% for selected formulations. Release studies demonstrated a pronounced pH-dependent behavior, with significantly faster drug release under mildly acidic conditions that mimic the tumor microenvironment. The biological activity of selected formulations was evaluated in prostate-derived cell models (BPH, LNCaP, and DU145), revealing enhanced cytotoxicity toward cancer cells under acidic conditions compared to physiological pH. In particular, naproxen@ZIF-8 showed a marked reduction in DU145 cell viability at low concentrations and under mildly acidic conditions. These results highlight the potential of ZIF-8 as a versatile nanoplatform for the controlled and tumor-responsive delivery of anti-inflammatory drugs with an anticancer activity.

PubMedFuture medicinal chemistry2026-11-05

Design, synthesis, and in vitro evaluation of novel 2-(5,8-dimethyl-2-naphthyl) propanoic acid derivatives as selective COX-2 inhibitors.

Tripathi Nancy N, Kotiyal Akhilesh A, Chouhan Deepak D, Bhardwaj Nivedita N et al.

Selective cyclooxygenase-2 (COX-2) inhibitors are important therapeutic agents for the management of inflammatory disorders due to their reduced gastrointestinal adverse effects compared to nonselective NSAIDs. Naproxen is a widely used anti-inflammatory drug; however, its limited COX-2 selectivity necessitates the development of improved analogs with enhanced efficacy and safety profiles. Santonin, a naturally occurring sesquiterpene lactone, offers a valuable scaffold for the semi-synthesis of novel bioactive compounds. The present study aimed to design and synthesize novel 2-(5,8-dimethyl-2-naphthyl)-propanoic acid derivatives as naproxen analogs from santonin and evaluate their potential as selective COX-2 inhibitors with enhanced anti-inflammatory activity. A series of novel derivatives was designed through docking studies and semi-synthesized from santonin using molecular iodine as a catalyst. The synthesized compounds were structurally characterized and evaluated for their inhibitory activity against COX isoforms in vitro. MD simulation of the compound 12-COX-2 complex was performed to determine the stability of the protein-ligand complex. Among the synthesized derivatives, 2-(7-methoxy-5,8-dimethylnaphthalen-2-yl) propanoic acid (12) emerged as the most promising candidate. These findings demonstrate that santonin-derived naproxen analogs represent a promising class of selective COX-2 inhibitors, with 12 showing significant potential for further development as an anti-inflammatory therapeutic agent.

PubMedAmerican journal of veterinary research2026-11-04

Elimination kinetics of nonsteroidal anti-inflammatory drugs during carbon hemoperfusion in 19 dogs with toxicosis.

Her Jiwoong J, Labato Mary A MA, Langston Catherine E CE, Butty Emmanuelle M EM

To describe the elimination kinetics of NSAIDs during carbon hemoperfusion (cHP) in dogs with toxicosis, specifically the apparent elimination rate constant, half-life, and plasma reduction. 19 client-owned dogs (median age, 2.5 years; median body weight, 22 kg) with ibuprofen (n = 10), carprofen (5), or naproxen (4) toxicosis treated with cHP at 2 academic veterinary teaching hospitals from November 30, 2022, through July 7, 2024. Dogs were presented after known or suspected ingestion at median estimated maximum doses of 720, 200, and 325 mg/kg for ibuprofen, carprofen, and naproxen, respectively. The median interval from ingestion to cHP was 6.8 hours. Plasma concentrations were measured by LC-MS-MS in-serial samples collected during and, when available, after cHP. The median total plasma reduction was 58% (IQR, 51 to 80). The overall half-life during cHP was 1.3 hours (IQR, 1.1 to 1.8) by the 2-point method, concordant by regression (1.4 hours), and approximately 3.7-, 5.4-, and 52.0-fold shorter than respective therapeutic-dose half-lives. Among 5 dogs with posttreatment samples, plasma concentration rebounded after cHP in 1 naproxen-treated dog. The cHP-associated rate constant exceeded the intrinsic rate constant 11- to 40-fold in 4 of 5 dogs. Carbon hemoperfusion was associated with substantial reductions in plasma NSAID concentrations during treatment in dogs with severe ibuprofen, carprofen, or naproxen toxicosis. Most of the decline occurred early in the session. Further studies are warranted to optimize treatment protocols. Carbon hemoperfusion markedly shortened NSAID elimination half-lives in dogs with severe toxicosis, accelerating removal well beyond endogenous elimination.

PubMedThe Journal of organic chemistry2026-11-03

TfOH-Promoted C-C Cross-Coupling of Iodonium Ylides with Nucleophiles.

Zhan Shiping S, Cheng Xiang X, Chen Xingyu X, Zhang Li L et al.

2-Naphthol and coumarin represent privileged scaffolds prevalent in bioactive agents and chiral catalytic ligands such as naproxen, warfarin, and (R)-(+)-BINOL. Hybridization of these two skeletons is a powerful approach to generate unreported molecular frameworks with unique activity. We herein describe a TfOH-promoted C─C cross-coupling of 2-naphthols and other nucleophiles with coumarin-based iodonium ylides, delivering a series of novel scaffolds. This transformation requires no metal catalysts, proceeding under mild conditions with good functional group tolerance. Gram-scale synthesis and multiple postfunctionalization reactions confirm the synthetic practicability of this methodology. The obtained hybrid molecules exhibit promising potential for further exploration in organic synthesis and drug discovery.

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