Soleton (zaltoprofen) / Nippon Chemiphar, Zeria Pharma - LARVOL DELTA

Synthesis, Thermal Stability, and Ionic Conductivity of Phenyl-Extended Viologen Ditriflate Salts: Tailoring Properties via Oxyethylene Chain Length. (PubMed, ACS Omega) - "The salts, which contain terminal oxyethylene chains of varying lengths ((CH2CH2O) n , n = 1, 2, 3, 4, 5, and 7), are named PEOn-OTF...Amorphous samples with long oxyethylene terminal chains display the highest direct current conductivity (σdc ∼ 10-3.5 S·cm-1 at 110 °C), which is of merit for organic media, but lower than that reported for trifluoromethylsulfonylimide (TFSI) analogues. Our detailed study of relaxations hints at the existence of strong correlations between morphology, dielectric response, and ion transport dynamics, which will be further explored in the near future."

Journal

Fragment-based discovery of TopBP1 inhibitors integrated with AI-driven molecular docking. (PubMed, Magn Reson Lett) - "Herein, we employ a fragment-based screening approach to identify four small-molecule ligands against the TopBP1 BRCT7-8 domain: adamantane acetic acid (ADA), zaltoprofen, diclofenac sodium, and quinine...Our NMR screening nominates orthosteric inhibitors, as well as quinine, a potential allosteric inhibitor. It shall also facilitate following structure-based design of more potent allosteric and orthosteric inhibitors of TopBP1."

Journal • Oncology • BACH1 • BRIP1 • TOPBP1

Optimizing Green Synthesis of Silver Nanoparticles with Peppermint Oil Nanoemulsion Using Response Surface Methodology: An Effective Antimicrobial, Antifungal, and Antioxidant Approach. (PubMed, Curr Pharm Des) - "Employing PEON, RSM effectively improved the green synthesis of bioactive, stable AgNPs. These results exhibit the potential of an environmentally friendly strategy for upcoming advancements in food safety and pharmaceuticals."

Journal

Zaltoprofen and its novel analogues exhibit dual targeting of COX-2 and PPAR-γ, providing a strategy to alleviate lipopolysaccharide - induced acute lung injury. (PubMed, Biochem Pharmacol) - "The present study also examined the effect and the cellular and molecular mechanisms of ZPF, M2 and the novel analogues on LPS-induced ALI in vitro and in vivo, through the dual targets of COX-2 and PPAR-γ. The findings of this study suggest that the STSBPT strategy could assist as a probable multi-target medicinal drug screening strategy, and ZPF, its main metabolite M2 and its novel analogues could serve as potential therapeutic agents for the treatment of acute lung injury, through the both COX-2 and PPAR-γ molecular signalling targets."

Journal • Acute Lung Injury • Inflammation • Pain • Respiratory Diseases

Development, in vitro and in vivo evaluation of film forming solutions for transdermal drug delivery of Zaltoprofen. (PubMed, J Biomater Sci Polym Ed) - "In addition, significantly elevated (ANOVA, p < 0.001) analgesic effect was noted in the hot plate test in rats treated with F13 compared to the standard for 12 h proving the superior efficacy of F13. Thus, PFFS by virtue of "in situ evaporative metamorphosis" induced supersaturation can be an attractive platform to deliver ZAL transdermally."

Journal • Preclinical • Pain

Anti-tumor effect of zartoprofen, a non-steroidal anti-inflammatory drug, targeting PPARγ (peroxisome proliferator-activated receptor gamma) on chondrosarcoma. (ASCOBT 2024) - "Zaltoprofen suppressed tumor progression by inhibiting cell proliferation, migration, and invasion with induction of PPARγ expression in chondrosarcoma cells. The suppressing effect on tumor progression by zaltoprofen was also observed in vivo. Zaltoprofen induced PPARγ expression and MMP2 downregulation in clinical specimens with expected antitumor effects."

Oncology • Sarcoma • Solid Tumor • CDKN1A • CEBPA • MMP2 • PPARG • TP53

Heteroatom-doped carbon dots from medicinal plants as novel biomaterials for as-use biomedical applications in comparison with synthetic drug, zaltoprofen. (PubMed, Sci Rep) - "When tested on six bacterial strains (three each for gram-positive and gram-negative), the FN-CDs displayed a halo (ZOI) between 9 and 19 mm, whereas the Z-FN-CDs displayed a clearance zone between 9 and 17 mm. The FN-CDs showed significant emission-red-shift effects and demonstrated concentration-dependent biocompatibility and viability in neuroblastoma and beta-TC6-cell lines."

Clinical • Journal • CNS Tumor • Infectious Disease • Neuroblastoma • Oncology • Solid Tumor

Effects of acidic non-steroidal anti-inflammatory drugs on human cytochrome P450 4A11 activity: Roles of carboxylic acid and a sulfur atom in potent inhibition by sulindac sulfide. (PubMed, Chem Biol Interact) - "Sulindac sulfide, ibuprofen, and flurbiprofen effectively decreased the luciferin-4A O-demethylase activity of HLMs and recombinant CYP4A11 (inhibition rates of 30-96% at an inhibitor concentration of 100 μM), while salicylic acid, aspirin, diclofenac, mefenamic acid, indomethacin, etodolac, ketoprofen, loxoprofen, S-naproxen, pranoprofen, zaltoprofen, and oxaprozin exhibited weaker inhibitory activity (inhibition rates up to 23%). The present results indicate that sulindac sulfide is a potent inhibitor of CYP4A11. These results and the molecular modeling of CYP4A11 with sulindac sulfide and its oxidized forms suggest that a sulfur atom of sulindac sulfide as well as its carboxylic acid play important roles in the inhibition of CYP4A11."

Journal

Anti-inflammatory and arthritic activity of zaltoprofen compared to piroxicam in murine models. (PubMed, Bioinformation) - "However, in the chronic inflammation model, zaltoprofen 10 mg/kg and 20 mg/kg doses of the test compound showed a significant reduction in chronic inflammation, comparable to the negative control (NaCl 10 ml/kg), although the potency was lower than the positive control (piroxicam 10 mg/kg) (P 0.05). Thus, zaltoprofen shows significant anti-inflammatory and arthritic effects in both acute and chronic models by inhibiting various inflammatory mediators."

Journal • Preclinical • Immunology • Inflammation • Inflammatory Arthritis • Rheumatology

Population Pharmacokinetic Modeling of Zaltoprofen in Healthy Adults: Exploring the Dosage Regimen. (PubMed, Pharmaceuticals (Basel)) - "Steady-state plasma exposure to zaltoprofen was significantly reduced in the group with CrCL and albumin levels of 130 mL/min and 3.5 g/dL, respectively, suggesting that dose adjustment may be necessary. This study is useful to guide precision medicine of zaltoprofen and provides scientific quantitative judgment data for its clinical applications."

Journal • PK/PD data • Inflammation • Pain • CYP2C9

A comparative study of effects of curcumin and its nanoparticles on the growth, immunity and heat stress resistance of Nile tilapia (Oreochromis niloticus). (PubMed, Sci Rep) - "Six diets were supplemented with three levels of nano-curcumin (50 (CN50), 100 (CN100), 200 (CN200) mg kg diet) or free-curcumin (50 (C50), 100 (C100), 200 (C200) mg kg diet), and the control diet was left without an additive (CON)...After the heat stress, ALT, AST, IgM, C3, C4, cortisol and glucose increased. Thus, nano-curcumin is more effective than its free-form in enhancing the resistance to heat stress, inducing innate immunity, lowering the stress indicators and promoting growth performance of Nile tilapia with the best concentration at 100 mg kg diet."

Journal

Application of sequential multimodal analgesia before and after impacted mandibular third molar extraction: Protocol for a randomized controlled trial. (PubMed, Contemp Clin Trials Commun) - "This multi-center, prospective, double-blind, randomized controlled trial aims to evaluate the efficacy and safety of sequential multimodal analgesia combined with postoperative zaltoprofen along with multiple preemptive analgesics...Two surgical extractions were performed at one-month intervals, and in a crossover design, celecoxib or tramadol/acetaminophen was administered before one extraction and placebo before the other extraction...The results of this study will provide guidance to clinicians regarding the timing and combination of oral analgesics in various oral surgeries performed under local anesthesia. KCT0005450, registered on October 7, 2020."

Journal • Anesthesia • Pain

A nonsteroidal anti-inflammatory drug, zaltoprofen, inhibits the growth of extraskeletal chondrosarcoma cells by inducing PPARγ, p21, p27, and p53. (PubMed, Cell Cycle) - "Zaltoprofen treatment inhibited tumor growth, induced tumor cell apoptosis, and was well tolerated in a mouse model of extraskeletal myxoid chondrosarcoma. Our results provide mechanistic insights into the therapeutic effect of zaltoprofen that should promote further studies on the rational use of this drug for the effective treatment of sarcomas."

Journal • Oncology • Sarcoma • Solid Tumor • CDKN1A • PPARG

Enhancement of S(+)-zaltoprofen oral bioavailability using nanostructured lipid carrier system. (PubMed, Arch Pharm Res) - "NLC-SZPF was successfully optimized using experimental designs to enhance the oral bioavailability of SZPF. Hence, NLC-SZPF could be a promising approach to overcome the poor oral bioavailability of SZPF."

Journal

Randomized placebo-controlled double-blind phase II study of zaltoprofen for patients with diffuse-type and unresectable localized tenosynovial giant cell tumors: The REALIZE study. (PubMed, Front Oncol) - "Further analysis of long-term administration of zaltoprofen should be considered in future studies. University Hospital Medical Information Network Clinical Trials Registry, identifier (UMIN000025901)."

Journal • P2 data • Cardiovascular • Giant Cell Tumor of Bone • Hematological Disorders • Hypertension • Immunology • Oncology • Orthopedics • Tenosynovial Giant Cell Tumor • PPARG

Relationships of pain-causing substances with dry skin and effects of zaltoprofen on alleviation of symptoms in arthritis model mice. (PubMed, Cutan Ocul Toxicol) - "No changes in plasma levels of corticosterone or reactive oxygen species or skin levels of glucocorticoid receptor were observed in ZLT-treated arthritis model mice. Overall, these findings suggested that patients with RA may benefit from biopharmacy to alleviate joint symptoms and nonsteroidal anti-inflammatory drugs for pain relief and alleviation of skin symptoms."

Journal • Preclinical • Dermatology • Immunology • Inflammation • Inflammatory Arthritis • Oncology • Pain • Pruritus • Rheumatoid Arthritis • Rheumatology • IL6 • TNFA • TSLP

Development of a series of flurbiprofen and zaltoprofen platinum(IV) complexes with anti-metastasis competence targeting COX-2, PD-L1 and DNA. (PubMed, Dalton Trans) - "Furthermore, inflammation in tumor tissues is restrained by the suppression of enzymes COX-2, MMP-9, NLRP3 and caspase1, which would favor the inhibition of tumor metastasis. Moreover, compound 2 boosts T-cell immunity by restraining PD-L1 expression, and further improving the density of CD3 and CD8 T cells in tumor tissues."

IO biomarker • Journal • Immunology • Inflammation • Oncology • BCL2 • CASP3 • CD8 • MMP9 • NLRP3 • TP53

Randomized, placebo-controlled, double blind, phase II study of zaltoprofen for patients with diffuse-type and unresectable localized tenosynovial giant cell tumors. (ASCO 2022) - "To our knowledge, this was the first study to evaluate the efficacy of zaltoprofen in patients with TGCT. The TGCT patients in zaltoprofen group did not have higher PER compared with those in the placebo group at week 48. Zaltoprofen appeared to improve the limb-function."

Clinical • P2 data • Giant Cell Tumor of Bone • Hematological Disorders • Hypertension • Immunology • Musculoskeletal Diseases • Oncology • Tenosynovial Giant Cell Tumor • PPARG

ANTIBODY RESPONSES AND PERSISTENCE AFTER IMMUNISATION WITH A REDUCED RECOMBINANT PERTUSSIS BOOSTER DOSE AMONG ADOLESCENTS (ESPID 2022) - "Recombinant acellular pertussis (aPgen) vaccines containing 5µg of genetically detoxified Pertussis Toxin (Peon) and 5 µg Filamentous Hemagglutinin (FHA) are licensed in Singapore and Thailand... From June to August 2019, 450 adolescents with median age of 12 years were enrolled. Seroconversion rates were statistically significant higher in ap-2,5 and Tdap-2,5 than in Tdapchem group for ELISA anti-PT, after 1 month: 93% (95% CI 88-97), 94% (90-98) and 70% (63-78) respectively(P ≤ 0.05); and after 1 year: 73% (61-86), 56% (42-70) and 16% (6-26)(P ≤ 0.05). Similar findings were found for anti-FHA."

Infectious Disease • Pertussis • Respiratory Diseases • Tetanus • TFAP2A

Solvent Etching Process for Graphitic Carbon Nitride Photocatalysts Containing Platinum Cocatalyst: Effects of Water Hydrolysis on Photocatalytic Properties and Hydrogen Evolution Behaviors. (PubMed, Nanomaterials (Basel)) - "While the addition of O-functional groups positively influenced the oxidation state of the Pt cocatalyst and the hydrogen production rate, the changes to g-CN structure retarded charge transfer on its surface, inducing negative effects such as fast recombination and less oxidized Pt species. Pt/CN50 that was synthesized with the 50:50 solvent mixture exhibited the highest hydrogen production rate of 590.9 µmol gh, while the hydrogen production rates of Pt/CN0 (with pure ethanol solvent) and Pt/CN100 (with pure water solvent) were 462.7, and 367.3 µmol gh, respectively."

Journal

"Nope…. I’m just a peon🙃" (,@diane2400)

"Stfu you peon. Stay in your house." (,@King_Slayer1203)

Sustainable and efficient skin absorption behaviour of transdermal drug: The effect of the release kinetics of permeation enhancer. (PubMed, Int J Pharm) - "The lower variance of an innovative parameter permeation enhancement coefficient (C) represented the relatively sustainable and effective enhancement effect and was listed as followed: 0.20 (Zaltoprofen (ZPF)), 0.31 (Diclofenac (DCF)), 0.27 (Indomethacin (IMC)), 0.07 (Azasetron (AST)), 0.11 (Oxybutynin (OBN)) and 0.06 (Donepezil (DNP)). In conclusion, zero-order release kinetic of POCC lead to sustainable and efficient penetration enhancement efficiency on basic drug, while the Higuchi release kinetic showed opposite effect for acidic drugs. A deep understanding of release kinetics of enhancer and its enhancement efficiency may drive the ideal selection of permeation enhancers and rational optimization of transdermal patches."

Journal

"Nobody read the patient's name to the surgeon because that's a job for a peon. 35,000 hours of training and no formal training on reading the arm band." (,@TempletonPeckP1)

Clinical

RANDOMIZED PLACEBO-CONTROLLED DOUBLE BLIND PHASE II STUDY OF ZALTOPROFEN FOR PATIENT WITH DIFFUSE-TYPE AND UNRESECTABLE LOCALIZED TENOSYNOVIAL GIANT CELL TUMORS (CTOS 2021) - "This was the first study to evaluate the efficacy of zaltoprofen in patients with D-TGCT or unresectable L-TGCT. Zaltoprofen was well tolerated and there were no incidents of safety issues with zaltoprofen; however, both groups presented with a stable disease course for 48 weeks. The long-term clinical course of TGCT should be clarified."

Clinical • P2 data • Giant Cell Tumor of Bone • Hematological Disorders • Immunology • Oncology • Tenosynovial Giant Cell Tumor • PPARG