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ibuprofen + arginine (Spedifen / Zafen / Espedifen)

✓ Approved

Zambon · PTGS1 · Small Molecule

What is ibuprofen + arginine?

ibuprofen + arginine is a small molecule developed by Zambon. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesSpedifen, Zafen, Espedifen
CompanyZambon
Drug ClassSmall Molecule
Molecular TargetPTGS1, PTGS2
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Zambon

Mechanism of Action

Molecular Targets

ibuprofen + arginine acts on 2 molecular targets:

PTGS1prostaglandin-endoperoxide synthase 1 (COX3, PCOX1)
PTGS2prostaglandin-endoperoxide synthase 2 (GRIPGHS, hCox-2)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

ibuprofen + arginine is developed for 2 unique indications across 2 therapeutic areas.

Therapeutic AreaConditionPhase
Gastrointestinal disordersAbdominal pain✓ Approved
Hepatobiliary disordersHepatitis✓ Approved

Related Research Articles

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NSAID-Induced Acute Interstitial Nephritis Concurrent With IgA Vasculitis: A Case-Based Systematic Review.

Caputo Carmela C, Sessa Concetto C, Serio Vittorio V, Baciga Federica F et al.

Overlap between acute interstitial nephritis (AIN) and glomerulonephritis is uncommon and diagnostically challenging. We present the first pediatric case of clinically diagnosed immunoglobulin A vasculitis nephritis (IgAV-N) concurrent with nonsteroidal anti-inflammatory drug (NSAID)-induced AIN. A 14-year-old boy was hospitalized for recurrent gastroenteritis, purpura, and arthralgia treated with ibuprofen. After 5 days, he developed stage 3 acute kidney injury, subnephrotic proteinuria, hypertension, and oligoanuria. Kidney biopsy showed mild to moderate interstitial inflammation with tubulitis; immunofluorescence was negative for glomerular IgA, with nonspecific tubular C3 staining. After NSAID discontinuation, 10 dialysis sessions, and corticosteroids, kidney function recovered completely within 3 months. To support the clinical lesson highlighted by our case, we conducted a systematic review of biopsy-confirmed AIN-glomerulonephritis overlap. PubMed, Scopus, Web of Science, and Google Scholar were searched for biopsy-confirmed AIN with concurrent glomerulonephritis. Clinical features, etiologies, treatments, and outcomes were extracted. Systematic review identified 8 studies (12 patients). Drug-related AIN predominated (9 of 12), followed by infection (2 of 12) and autoimmune disease (1 of 12). Nephrotic-range proteinuria was described in 6, hematuria in 8, and hypersensitivity findings in 7 of the 12 patients. Complete recovery occurred in 7 and partial recovery in 3 patients, and dialysis was required in 2 of the 12 patients. NSAID-induced AIN concurrent with IgA vasculitis nephritis should be suspected in atypical acute kidney injury.

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Targeting CARM1 impairs DNA damage repair and attenuates B-cell acute lymphoblastic leukemia progression.

Liao Peiyun P, Qiu Yingqi Y, Li Meifang M, Hu Rong R et al.

B-cell acute lymphoblastic leukemia (B-ALL) is a prevalent hematological malignancy, posing difficulties in identifying efficacious treatment strategies for refractory and recurrent patients. Our research revealed that coactivator-associated arginine methyltransferase 1 (CARM1) was highly expressed in B-ALL and associated with unfavorable prognostic outcomes. Down-regulation and inhibition of CARM1 effectively suppressed proliferation and colony formation of B-ALL, while also inducing apoptosis and cell cycle arrest. Mechanistically, inhibition or down-regulation of CARM1 reduced PARP1 level and contributed to double-strand breaks (DSBs) accumulation. Inhibition of CARM1 and PARP1 synergistically supressed B-ALL development. Significantly, the inhibition of CARM1 was found to promote memory differentiation and reduce the exhaustion of CD19-CAR-T cells. Taken together, CARM1 inhibition not only suppressed B-ALL but also enhanced the durability of CAR-T cells against B-ALL, which provides novel insights into the tumor suppression and immune regulation of CARM1 inhibition on cancer therapy.

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Molecular origins of ion mobility differences between the peptide standards GRGDS and SDGRG.

Geue Niklas N, Prabhu Gurpur Rakesh D GRD, Ivanov Mikhail M, Jarvet Jüri J et al.

The reversed-sequence pentapeptides GRGDS and SDGRG are widely used ion mobility spectrometry (IMS) standards as they exhibit distinct gas-phase mobilities despite their identical mass and composition. Here, we investigate the molecular origins of their differing charge-state-dependent conformations using ion mobility mass spectrometry, cryogenic gas-phase infrared spectroscopy, NMR spectroscopy, molecular dynamics simulations, and density functional theory calculations. In aqueous solution, both peptides populate highly flexible conformational ensembles with only minor differences in compactness. Upon desolvation, the peptides collapse into distinct gas-phase structures stabilized by intramolecular hydrogen bonding. For the doubly protonated species, GRGDS adopts a compact cyclic "C-like" fold, whereas SDGRG forms a more extended "S-like" conformation driven by coulombic repulsion between the protonated N-terminus and the arginine side chain. The singly charged ions show a more compact conformation for SDGRG compared to GRGDS, and a combination of different protomers and conformers appears to be present. Crown ether complexation and terminal glycine extensions of the doubly protonated species reduce the differences in IMS, in agreement with contributions from charge-charge interactions in defining the gas-phase folds. These findings provide molecular-level insight into a widely used IMS standard system and contribute to our fundamental understanding of structural rearrangements in peptides upon transfer to the gas phase.

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PubMedMaterials today. Bio2026-08-29

Thiol-mediated ROS-responsive hydrogel with arginine-driven NO cascade for colitis treatment.

Liu Shuang S, Zhao Zhongming Z, Wang Ziyi Z, Pi Xianghe X et al.

Developing integrated, drug-free therapeutic platforms that simultaneously address oxidative stress, immune dysregulation, and gut microbiota dysbiosis remains a significant challenge in UC management. Although hydrogels offer localized delivery advantages, their clinical versatility is frequently hindered by a reliance on exogenous drug encapsulation. To overcome this limitation, we developed a multifunctional, ROS-responsive hydrogel (ODCAS) that functions as an inherently bioactive platform. The ODCAS network is constructed via dynamic Schiff base crosslinking between ODex and thiolated arginine chitosan, further reinforced by ROS-triggered disulfide bonds leveraging. This sophisticated architecture undergoes ROS-responsive programmed degradation, driving in situ NO generation to trigger a therapeutic cascade. Specifically, the TPA-derived thiol moieties facilitate inflammation-targeted mucoadhesion via disulfide exchange with the mucosal layer, while simultaneously providing potent, direct ROS scavenging (72.21 ± 2.47% DPPH· radical scavenging). Furthermore, the metabolic byproducts of the hydrogel network provide prebiotic support to restore microbial equilibrium. In a DSS-induced murine colitis model, oral administration of ODCAS significantly attenuated disease severity, reducing the DAI by 52.08%, downregulating pro-inflammatory cytokines, and restoring both intestinal barrier integrity and microbial homeostasis. These findings highlight the ODCAS hydrogel as a robust, ROS-responsive biomaterial platform that orchestrates disulfide-mediated anchoring and an arginine-driven NO cascade for the effective management of chronic inflammatory diseases.

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CRISPR-Cas9 mediated adiA knockout in Hafnia paralvei: Implications for agmatine production and acid stress survival in a fermented dairy matrix.

Casado Angel A, Wellner Sandra M SM, Quirós Alejandro A, Herrero-Fresno Ana A et al.

Agmatine, the product of the decarboxylation of arginine, catalysed by arginine decarboxylase (ADC), is a bioactive compound that functions as a neuromodulator and co-transmitter and has gained increasing attention in recent years due to its therapeutic potential, particularly for its neuroprotective properties. Members of the genus Hafnia are the main agmatine producers in dairy products. In this regard, Hafnia is considered a beneficial microorganism due to its ability to enhance cheese organoleptic properties and its emerging probiotic potential, making it relevant for functional food development, specially agmatine-enriched dairy products. This study aimed to identify the genetic basis for agmatine production in Hafnia paralvei and to assess its role in bacterial fitness. Genomic analysis of the strain H. paralvei IPLA15029 revealed the presence of two genes encoding putative ADC enzymes, adiA and speA, however, organized slightly different than those in other enterobacteria. In some bacteria, ADC exists in two forms: one involved in polyamine biosynthesis, encoded by the constitutive speA gene, and another involved in acid stress resistance, encoded by the adiA gene, which is inducible under acidic conditions. In vivo experiments under controlled pH conditions showed that agmatine accumulation occurs exclusively under acidic conditions, which also stabilize the compound by preventing its catabolism to putrescine. Gene expression analysis revealed that adiA was transcribed as a monocistronic unit, and that in these conditions, adiA is the gene responsible for agmatine production. This was confirmed by generating an adiA knockout mutant after the implementation of the CRISPR-Cas9 system, marking the first successful application of this technology in the genus Hafnia. Moreover, the adiA knockout demonstrated that the encoded arginine decarboxylase is essential for survival under severe acid stress.

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PubMedMikrochimica acta2026-08-29

Arginine-engineered gold nanoclusters for doxorubicin chemiluminescence sensing.

Cai Chuangui C, Lin Zhen Z, Yao Wensong W, Lian Shan S et al.

Arginine surface-engineered 6-aza-2-thiothymine gold nanoclusters (Arg/ATT-AuNCs) via host-guest assembly were synthesized which exhibit exceptional catalytic activity and intense photoluminescence. Arg/ATT-AuNCs enhanced the CL intensity from NaIO4-H2O2 system by 1200-fold. The CL mechanistic studies revealed that Arg/ATT-AuNCs not only accelerated decay of H2O2 to form reactive oxygen species, but also acted as efficient energy acceptors of singlet oxygen (1O2) via a CL resonance energy transfer (CRET) pathway. It was observed that doxorubicin (DOX) quenches the CL signal through an inner filter effect that disrupts the CRET process. Based on this, a straightforward, rapid, and highly sensitive biosensor has been developed for the detection of DOX in human serum samples, achieving a low detection limit of 0.029 µM. The biosensor was applied to DOX determination in human serum samples with recoveries ranging from 91.1 to 106.2%. This study not only provides a new method for the detection of DOX, but also broadens the application scope of AuNCs in the field of CL.

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