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

✓ Approved

Marathon Pharmaceuticals · SCN9A · Small Molecule

What is lidocaine hydrochloride?

lidocaine hydrochloride is a small molecule developed by Marathon Pharmaceuticals. It is approved for therapeutic indications via injectable (others) or intradermal injection.

Drug Profile

Brand Names3268, lignocaine, Anesiva, ALGRX 3268
CompanyMarathon Pharmaceuticals
Drug ClassSmall Molecule
Molecular TargetSCN9A
RouteInjectable (Others), Intradermal Injection
StatusApproved
Sources: ClinicalTrials.gov, Marathon Pharmaceuticals

Mechanism of Action

Molecular Targets

lidocaine hydrochloride acts on 1 molecular target:

SCN9Asodium voltage-gated channel alpha subunit 9 (SFNP, GEFSP7)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

lidocaine hydrochloride is developed for 2 unique indications across 1 therapeutic area.

Therapeutic AreaConditionPhase
Nervous system disordersAnaesthesia✓ Approved
Nervous system disordersSensory loss✓ Approved

Related Research Articles

PubMedAAPS PharmSciTech2026-10-17

Vilazodone Hydrochloride-Loaded Nanostructured Lipid Carrier In Situ Gel for Intranasal Nose-to-Brain Antidepressant Delivery.

Shah Khushi K, Palva Rajeshkumar S RS, Patel Mitali M, Saiyed Musaratafrin M et al.

The Oral delivery of vilazodone hydrochloride (VLZ), a serotonin partial agonist-reuptake inhibitor for major depressive disorder, suffers from extensive hepatic first-pass metabolism, food-dependent absorption, and poor blood-brain barrier (BBB) penetration, limiting its central therapeutic impact. Here, VLZ-loaded nanostructured lipid carriers (NLCs) were engineered and embedded within a Poloxamer 407/188-chitosan thermosensitive in situ gel to enable direct nose-to-brain delivery. The NLCs were fabricated by combined high-shear and high-pressure homogenisation and optimised through central composite design, yielding a batch with particle size 24.74 ± 2.23 nm, polydispersity index 0.248 ± 0.012, and entrapment efficiency 91.37 ± 4.56%. The lyophilised NLCs were incorporated into an in situ gel with a physiologically appropriate gelation temperature of 34°C and gelation time of 42 s. Fourier Transform Infrared FTIR spectroscopy confirmed complete drug encapsulation, evidenced by disappearance of the diagnostic nitrile (C≡N) absorption band, while DSC and XRPD verified conversion of VLZ to an amorphous state within the lipid matrix. Drug release followed Korsmeyer-Peppas kinetics, sustained over 24 h, and the formulation remained stable under refrigerated storage. In Swiss albino mice, the intranasal NLC-in situ gel (1 mg/kg) produced a profound antidepressant-like effect relative to oral pure drug (10 mg/kg) across open field, tail suspension, and sucrose preference tests, consistent with enhanced nose-to-brain delivery via the olfactory and trigeminal pathways. Hence this nanocarrier-hydrogel strategy offers a promising, non-invasive route to enhanced CNS delivery of antidepressants.

PMID 42888351
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PubMedMedicine2026-10-17

Efficacy and safety of imeglimin hydrochloride for metabolic dysfunction-associated steatotic liver disease with type 2 diabetes: Single-center, single-arm phase 2 (IMELD study).

Yamada Hiroki H, Ida Yoshiyuki Y, Kaji Shiori S, Nagai Yoshitaka Y et al.

Imeglimin, a novel oral antidiabetic agent classified as a glimin, was developed for the treatment of type 2 diabetes (T2D). This single-center, single-arm interventional study evaluated the efficacy and safety of 24-week imeglimin treatment in patients with metabolic dysfunction-associated steatotic liver disease (MASLD) and T2D. Patients with MASLD and T2D were treated with imeglimin 1000 mg twice daily for 24 weeks. The primary endpoint was reduction in alanine aminotransferase (ALT) levels from baseline. Secondary endpoints included changes in metabolic parameters (including hemoglobin A1c, homeostatic model assessment of β-cell function, and homeostatic model assessment of insulin resistance), liver-related parameters (including aspartate aminotransferase [AST], gamma-glutamyl transpeptidase, hepatic fat, and fibrosis markers), and body composition. Twenty-five patients were included in the final analysis. As a primary outcome, the median ALT level was significantly reduced, from 56.00 (47.00-75.00) U/L at baseline to 34.00 (29.00-51.00) U/L at 24 weeks (P < .001). AST level and hemoglobin A1c value were also significantly reduced. The fibrosis-4 index showed a significant reduction at 12 weeks. By contrast, no significant changes were observed for gamma-glutamyl transpeptidase, homeostatic model assessment of β-cell function, homeostatic model assessment of insulin resistance, hepatic fat content parameters, other fibrosis-related parameters (excluding fibrosis-4 index), and body composition. All adverse events were grade 1, and no patients discontinued treatment due to adverse events. Imeglimin treatment was associated with improvements in serum ALT and AST levels after 24 weeks in patients with MASLD and T2D. These findings provide preliminary evidence of the potential clinical utility of imeglimin in this population and warrant confirmation in larger randomized controlled studies.

PMID 42888537
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PubMedInternational archives of allergy and immunology2026-10-16

Optimizing emergency management of anaphylaxis in dentistry: a systematic review of current practices.

Li Huamin H, Zhong Siyu S, Yu Zhujun Z, Ma Beibei B et al.

This review characterizes anaphylaxis in dental practice, including patient demographics, clinical presentations, implicated allergens, diagnostic approaches and emergency management, to provide actionable guidance for safer dentistry. A systematic search was conducted across PubMed/Medline, Embase, and Web of Science for case reports of dental-related anaphylaxis published between 2000 and 2025. Fifty-five cases from 44 studies were analyzed. Patients were predominantly male (63.64%), with a median age of 43 years. Most anaphylaxis (76.36%) occurred within 30 minutes, primarily during oral/maxillofacial surgery, endodontic treatments, and extractions. Dental materials (34.55%, mainly formaldehyde) were the leading triggers, followed by combined anesthesia (18.18%), antibiotics (10.91%), chlorhexidine (9.09%) and lidocaine (5.45%). Prior exposure was notable for dental materials (36.84%) and lidocaine (100%). Initial presentation patterns were trigger-specific: cutaneous symptoms dominated for dental materials and lidocaine; hypotension for combined anesthesia and antibiotics; and gastrointestinal distress for chlorhexidine. Alarmingly, epinephrine was administered in only 56.36% of cases, with the recommended intramuscular route utilized in merely 7.72%. Diagnosis relied primarily on skin prick and sIgE testing, supplemented by drug provocation. Anaphylaxis remains a persistent risk in dentistry. Enhancing dentist training, standardizing allergen testing, and increasing vigilance for atypical symptoms are critical to mitigating risks and improving patient outcomes.

PMID 42886610
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PubMedMolecules (Basel, Switzerland)2026-10-16

A Robust AQbD-Based RP-HPLC Method for Simultaneous Quantification of Acyclovir and Doxepin Hydrochloride in Bulk and Topical Cream Formulation.

Kumar Akshay A, Kumar Mohit M, Saini Abhishek A, Agrawal Mohit M et al.

The present study describes the development and validation of a simple, rapid, and reliable RP-HPLC method for the simultaneous estimation of acyclovir and doxepin hydrochloride in bulk and topical cream formulation using an Analytical Quality by Design (AQbD) approach. The combination of acyclovir, an antiviral agent, and doxepin, an antipruritic and anti-inflammatory drug, offers a combined topical approach for the management of herpes-associated skin conditions. The method development was guided by a predefined Analytical Target Profile (ATP), followed by systematic risk assessment to identify critical quality attributes (CQAs) and critical method parameters (CMPs). The central composite design (CCD) was employed to optimize key chromatographic variables, including mobile phase composition and flow rate. The chromatographic separation was achieved on a C18 column using an isocratic mobile phase of acetonitrile and water (40:60 v/v) at a flow rate of 1.0 mL/min, with UV detection at 240 nm. The retention times were found to be 2.58 min for acyclovir and 4.64 min for doxepin hydrochloride, indicating efficient separation with good peak symmetry. The method was validated according to ICH Q2(R2) guidelines and demonstrated excellent linearity over the concentration ranges of 2-10 µg/mL (acyclovir) and 12-28 µg/mL (doxepin hydrochloride), with correlation coefficients greater than 0.997. The method exhibited high precision (%RSD < 2%), accuracy (recovery within 99-101%), and good sensitivity with low LOD and LOQ values. The robustness studies confirmed the reliability of the method under small, deliberate variations in chromatographic conditions. The developed cream formulation showed uniform drug content and satisfactory in vitro drug release, with a sustained release profile reaching approximately 96% over 24 h. In conclusion, the proposed AQbD-based RP-HPLC method is suitable for routine quantitative analysis and quality control of acyclovir and doxepin hydrochloride in combined topical formulations.

PMID 42883330
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PubMedTurkish journal of anaesthesiology and reanimation2026-10-16

Comparison of Postoperative Analgesic Efficacy Between Opioid-free Anaesthesia Using Intravenous Magnesium, Lidocaine, and Erector Spinae Plane Block, and Opioid-based Anaesthesia in Laparoscopic Abdominal Surgeries: A Randomised Controlled Trial.

Vj Jerfiha J, Vaithiyalingam Ezhilrajan E, Johny Pradeesh P

Opioid-based anaesthesia is a standard practice in laparoscopic surgeries. However, it is associated with adverse effects that can limit its use. To address these issues, opioid-free anaesthesia has been introduced as an alternative. This study aims to compare the analgesic efficacy of opioid-free anaesthesia, incorporating magnesium, lidocaine, and an erector spinae plane block (ESPB), with traditional opioid-based anaesthesia during laparoscopic procedures. Seventy patients aged 18-60 years undergoing laparoscopic surgery were randomly divided into two groups of 35 each. Opioid-free group received opioid-free anaesthesia, which included an intravenous (IV) bolus of 2 g magnesium, a continuous lidocaine infusion at 1.5 mg kg-1 hr-1, and a bilateral ESPB with 25 mL of 0.25% bupivacaine. Opioid-based group received opioid-based anaesthesia with an IV dose of 2 μg kg-1 fentanyl. Postoperative pain and the need for rescue analgesia were assessed for 24 h. Perioperative haemodynamic parameters were recorded, and the incidence of postoperative complications, including sedation, nausea, vomiting, and shivering, was monitored for 24 h. Pain scores were significantly lower in the opioid-free group compared to the opioid-based group at 0 h (P < 0.001), 2 h (P < 0.001), and 4 h (P=0.005) postoperatively. The opioid-based group required rescue analgesia more frequently (P < 0.001). Additionally, the incidence of postoperative complications was significantly lower in the opioid-free group than in the opioid-based group (P < 0.001). Haemodynamic parameters were similar between the two groups. Opioid-free anaesthesia provides superior postoperative analgesia and reduces the incidence of postoperative complications compared with opioid-based anaesthesia for laparoscopic surgery.

PMID 42885412
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PubMedInternational journal of molecular sciences2026-10-16

Intraosseous Lidocaine Trigger Point Injection for Vertebrogenic Pain: From Molecular Principles to Clinical Applications: A Narrative Review.

Al-Zamil Mustafa M, Shnayder Natalia A NA, Petrova Marina M MM, Naprienko Margarita V MV et al.

Intraosseous lidocaine trigger point injection (LTPI) has been utilized for an extended period in the management of chronic vertebrogenic pain; yet, its molecular mechanisms and clinical efficacy require critical appraisal. This narrative review highlights the milestones of osteoreception and elucidates the molecular mechanisms driving intraosseous receptor irritation and its pivotal role in chronic pain development. Pathological vertebral bone remodeling triggers a receptor activator of nuclear factor-kappa B ligand/osteoprotegerin (RANKL/OPG) imbalance, accelerating hyperactive osteoclastogenesis. Enhanced osteoclastic vacuolar-type H+-ATPase (V-ATPase) expression drives microenvironment acidity and intraosseous hypertension, persistently stimulating acid-sensing ion channel 3 (ASIC3) and purinergic P2X2/3 receptors on intraosseous afferents. Concurrently, upregulated nerve growth factor (NGF) binds to tropomyosin receptor kinase A (TrkA), driving peripheral sensitization via transient receptor potential vanilloid 1 (TRPV1) phosphorylation. The available clinical studies investigating intraosseous LTPI for vertebrogenic pain are scarce and heterogeneous, focusing primarily on low back pain, cervicalgia, and residual chronic pain after degenerative lumbar spinal stenosis decompression surgery. The reviewed data provide preliminary signals of potential benefit, observing a statistically significant analgesic effect of intraosseous LTPI within the studied cohorts. In two trials comparing it to intramuscular LTPI, one of which utilized a randomized controlled design, the intraosseous approach was reported to provide more pronounced short-term pain relief. However, these trials are limited by small sample sizes, heterogeneous designs, and a lack of active long-term safety monitoring. Nevertheless, although current data provide promising but still limited insights, future double-blinded, multicenter randomized controlled trials are required to comprehensively establish the clinical efficacy, safety profile, and prolonged effect of intraosseous LTPI in the treatment of vertebrogenic pain.

PMID 42884176
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