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lidocaine hydrochloride (3268 / lignocaine, Anesiva / ALGRX 3268)

✓ Approved

Marathon Pharmaceuticals · SCN9A · 小分子

什么是 lidocaine hydrochloride？

lidocaine hydrochloride 是一种小分子，由Marathon Pharmaceuticals研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)、Intradermal Injection。

药物档案

商品名3268, lignocaine, Anesiva, ALGRX 3268
公司Marathon Pharmaceuticals
药物类别小分子
分子靶点SCN9A
给药途径Injectable (Others), Intradermal Injection
状态Approved
来源： ClinicalTrials.gov, Marathon Pharmaceuticals

作用机制

分子靶点

lidocaine hydrochloride 作用于 1 个分子靶点：

SCN9Asodium voltage-gated channel alpha subunit 9 (SFNP, GEFSP7)
需要更深入的分析？Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

lidocaine hydrochloride 针对 2 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Nervous system disordersAnaesthesia✓ Approved
Nervous system disordersSensory loss✓ Approved

相关研究文献

PubMedOrganic letters2026-07-27

Divergent Access to Chiral Pyrrolidinone-Fused 4H-Pyrans and Pyridines Via Organocatalytic Asymmetric Decarboxylative Addition-Annulation of β-Keto Acids with 2,3-Dioxopyrrolidines.

Li Tianxing T, He Tianyu T, Meng Weiyue W, Jin Hui H et al.

We disclose an unprecedented organocatalytic asymmetric decarboxylative Michael addition of β-keto acids to 2,3-dioxopyrrolidines, enabling the efficient assembly of chiral pyrrolidinone-fused [3,4-b]-4H-pyrans and [3,4-b]-pyridines. The reaction affords chiral pyrrolidinone-tethered 1,5-dicarbonyl intermediates in high yields with excellent regio- and enantioselectivities. Acid-promoted intramolecular cyclization of these adducts provides enantioenriched pyrrolidinone-fused [3,4-b]-4H-pyrans without erosion of enantiopurity, whereas cyclocondensation with hydroxylamine hydrochloride delivers diverse pyrrolidinone-fused [3,4-b]-pyridines. Notably, this protocol is compatible with a one-pot tandem process and gram-scale synthesis.

PMID 42504541
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PubMedToxins2026-07-27

Enhanced Protection Against Toxicity of Nemopilema nomurai Venom Using a PEG-EGCG/Tetracycline Hydrochloride Micellar Nanocomplex.

Li Jie J, Hu Yanan Y, Qian Yunfeng Y, Luo Sai S et al.

Jellyfish stings are the most common type of marine life injuries. However, at present, the treatment measures against jellyfish stings are mostly empirical and supportive, with uncertain therapeutic outcomes, and there is a lack of specific antidotes based on the toxic mechanism of jellyfish venom in clinical practice. In our previous study, polyphenol epigallocatechin-3-gallate (EGCG) was found to neutralize the toxicity of jellyfish Nemopilema nomurai venom (NnV) in vivo and in vitro. Herein we further demonstrated that EGCG exerted its antagonistic effect against NnV through inhibiting the oxidative stress, pro-apoptotic proteins, and systemic inflammatory responses. Subsequently, we constructed a polyethylene glycol (PEG)-EGCG/tetracycline hydrochloride (HTC) co-loaded micellar nanocomplex in order to enhance the stability and bioavailability of EGCG in vivo, which successfully integrated the membrane-repair function of PEG, the enzyme inhibitory effect of HTC and the antioxidant properties of EGCG. Notably, this micellar nanocomplex demonstrated significant protective effects against both functional damage and pathological alterations in a non-lethal NnV-envenomed mouse model. When administered 1 h after NnV envenomation, EGCG (40 mg/kg), HTC and PEG-EGCG (containing 40 mg/kg EGCG) only partially improved abnormal blood biochemical indicators and moderately alleviated histopathologic damage, and PEG-EGCG/HTC containing merely 8 mg/kg EGCG completely mitigated the toxic reactions in envenomed mice. In the preventive regimen, the administration of EGCG, HTC or PEG-EGCG 30 min before exposure showed no significant improvement in abnormal blood biochemical indicators and histopathologic damage, while PEG-EGCG/HTC could still significantly improve the functional impairments and histopathologic damage of the heart and liver in NnV-envenomed mice. These findings suggest the clinical translational potential of PEG-EGCG/HTC against jellyfish envenomation.

PMID 42506698
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PubMedAnalytical chemistry2026-07-27

A Selective, Class-Specific Aptamer for Fentanyl Analog Screening.

Wang Linlin L, Castro Gabriel G, Alkhamis Obtin O, Gangireddy Madhu Sudhana Reddy MSR et al.

Fentanyl and its analogs pose considerable dangers to public health and safety, and the development of simple tests that can detect these harmful substances accurately and rapidly could control their currently unchecked spread and thereby safeguard lives. Here, we use systematic evolution of ligands by exponential enrichment (SELEX) to isolate an aptamer that displays a rare blend of high affinity and broad cross-reactivity to 139 fentanyl analogs, alongside excellent specificity against nontarget interferents, including cutting agents, adulterants, and other drugs of abuse. We demonstrate the utility of this aptamer by developing a single-step colorimetric dye-displacement assay that can detect diverse fentanyl analogs within seconds with a simple mix-and-read format. The analog coverage of our assay rivals that of commercial immunoassay-based fentanyl tests while offering better specificity against substances that commonly trigger false positives in those tests, such as diphenhydramine, lidocaine, and methamphetamine. Our findings indicate that aptamers may be fundamentally better suited for achieving broad but specific detection of structurally related classes of molecules relative to other commonly used receptors, such as antibodies, due to their excellent and controllable binding properties, among other benefits, including low cost and high stability.

PMID 42503635
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PubMedAnalytical methods : advancing methods and applications2026-07-27

Smartphone-based fluorescence sensing platform for tetracycline determination based on a high quantum yield europium metal-organic framework with a dual-ligand strategy.

Cheng Shuang S, Song Jintian J, Wen Yue Y, Xu Yijia Y et al.

Ultrasensitive and visual detection of tetracyclines (TCs) is of great significance to public health and environmental safety. Herein, we synthesized a dual-ligand europium metal-organic framework (Eu-phen-MOF) via a one-step solvothermal method for the fluorescence detection of TCs. Compared with the Eu-MOF without 1,10-phenanthroline, Eu-phen-MOF exhibits superior stability, lower LOD and higher quantum yield. It delivers superior TC sensing performance and anti-interference, enabling high-accuracy detection with limits of 152.0 nmol L-1, 249.4 nmol L-1, 171.0 nmol L-1 and 277.7 nmol L-1 for tetracycline (TC), oxytetracycline (OTC), doxycycline hydrochloride (DOX), and chlortetracycline (CTC), respectively. Eu-phen-MOF was used for the quantitative detection of TC, OTC, DOX, and CTC in real samples (milk, eggs, and river water) and recoveries ranging from 94.64% to 105.37% were achieved. Finally, a portable fluorescence sensing platform integrating a smartphone and the Eu-phen-MOF fluorescent hydrogel was constructed, enabling convenient, rapid, and low-cost detection of TCs. This work not only highlights the significance of the dual-ligand strategy for fabricating an efficient TC sensor, but also develops a rapid and visual method for TC detection.

PMID 42504902
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PubMedDentistry journal2026-07-27

Local Anaesthetic Systemic Toxicity in Dental and Oral and Maxillofacial Surgery: Safe Dosing, Combination Agents, and Emergency Management-A Narrative Review.

Ucer Cemal C, Wright Simon S, Khan Rabia R, Kumar Sushil S

Background/Objectives: Local anaesthetic systemic toxicity (LAST) is a rare but potentially fatal complication of dental and oral and maxillofacial surgical local anaesthesia (LA). Three amide agents are commonly used in the UK: lignocaine (lidocaine) 2% with adrenaline 1:80,000; articaine 4% with adrenaline 1:100,000 (2.2 mL cartridges); and bupivacaine 0.5%. Clinically significant discrepancies between guideline sources for maximum recommended dosages (MRDs) persist, and the additive toxicity of combined amide agents remains underappreciated. The objectives are: to provide clear, evidence-appraised MRD guidance for dental practitioners; to explain safe combination dosing using the fractional dose rule with acknowledgement of its pharmacokinetic limitations; and to outline recognition and management of LAST, including intravenous lipid emulsion (ILE) therapy, setting-stratified response, and differential diagnosis. Methods: These include the following: narrative review of MEDLINE (via PubMed), the Cochrane Library, and Embase (inception to May 2026), supplemented by key regulatory documents (British National Formulary (BNF) 91; US Food and Drug Administration (FDA) prescribing information; UK Summaries of Product Characteristics (SmPCs)); major guideline documents (American Society of Regional Anesthesia and Pain Medicine (ASRA) 2018; Association of Anaesthetists 2021; Resuscitation Council UK 2021); systematic reviews; and peer-reviewed literature, ranked by a jurisdiction-specific UK prescribing and regulatory source hierarchy. Results: BNF 91 and the FDA both support a 7 mg/kg (500 mg) MRD for lignocaine with adrenaline; in practice, the adrenaline ceiling limits administration to 6-7 cartridges (2.2 mL) regardless of the guideline followed. The principal reasons for caution when combining amide agents are; additive systemic toxicity, more complex dose calculation, absence of proven clinical benefit for concurrent mixing, unnecessary drug exposure, and incremental hypersensitivity risk-not metabolic pathway differences. The fractional dose rule is a pharmacologically justified safety heuristic with acknowledged pharmacokinetic limitations. ILE is a specific rescue therapy for severe or cardiovascular LAST; airway support and oxygenation remain the primary interventions. Patient-specific factors substantially lower the effective toxic threshold. Conclusions: Safe LA administration in oral surgery requires systematic MRD calculation, application of the fractional dose rule for combined-agent appointments, attention to patient-specific risk factors, setting-appropriate emergency preparedness, and structured differential diagnosis to distinguish LAST from more common dental emergencies.

PMID 42505765
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PubMedMicrobiology spectrum2026-07-27

Mocravimod as a repurposing drug against clinical isolates of Staphylococcus aureus by targeting cell membrane.

Tang Yuanyuan Y, Xia Yuqing Y, Huang Xuancheng X, Yu Zhijian Z et al.

Staphylococcus aureus infections, particularly those caused by multidrug-resistant strains and associated with biofilm formation, pose a major therapeutic challenge in clinical practice. The objective of this study was to evaluate the antibacterial and antibiofilm activity of mocravimod (KRP-203), an FDA-approved S1P receptor modulator, against clinical S. aureus isolates and to explore its underlying mechanism of action. The antibacterial activity of KRP-203 was assessed against methicillin-susceptible S. aureus (MSSA) and methicillin-resistant S. aureus (MRSA) using MIC determination, time-kill assays, and biofilm inhibition models. KRP-203 exhibited strong bactericidal activity against planktonic MSSA and MRSA, with MIC values ranging 6.25-50μM. Time-kill assays demonstrated rapid bacterial eradication at 8× MIC within 2 h, showing superior killing kinetics compared with vancomycin. At sub-inhibitory concentrations, KRP-203 inhibited biofilm formation by up to 70% and reduced viable bacterial counts in mature biofilms by >2.5 logs. To elucidate the antibacterial mechanism, whole-genome sequencing and quantitative proteomic analyses were performed. These analyses revealed mutations in membrane-associated genes, including glnQ and BCAT, and significant alterations in proteins related to membrane integrity and redox regulation. Consistently, functional assays confirmed that KRP-203 disrupts bacterial cell membrane, as evidenced by dose-dependent membrane depolarization, increased permeability, and direct binding to cardiolipin and phosphatidylglycerol. Molecular docking further predicted a favorable interaction between KRP-203 and GlnQ. In conclusion, KRP-203 demonstrated notable antibacterial and antibiofilm activity against S. aureus, likely through membrane integrity disruption. While these findings highlight its potential as a repurposed antibacterial agent, further studies are required to fully elucidate its molecular targets, optimize antibacterial efficacy, and evaluate its in vivo safety profile. Antibiotic resistance and the formation of biofilms, which protect bacteria from medications and immunological responses, present the significant challenges for the clinical treatment of Staphylococcus aureus infections. This study reveals mocravimod hydrochloride (KRP-203), a clinically approved drug initially intended to treat leukemia, as a viable new candidate against S. aureus infection. KRP-203 quickly kills both drug-susceptible and resistant S. aureus, including difficult-to-treat biofilm-associated cells. Its membrane-disrupting activity quickly kills drug-resistant bacteria while also destroying biofilm formations, presenting a dual action rarely accomplished by conventional antibiotics. Critically, KRP-203's established safety profile in human studies may hasten its repurposing as a new weapon against biofilm-associated infections, providing possible solutions for chronic and drug-resistant S. aureus infections where existing treatments commonly fail.

PMID 42505145
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