北京若生智能科技有限公司
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carbamazepine (Carbella / Carnexiv)

✓ Approved

Ligand Pharmaceuticals · SCN1A · 小分子

什么是 carbamazepine？

carbamazepine 是一种小分子，由Ligand Pharmaceuticals研发。该药已获批，用于治疗相关适应症，给药途径：Injectable (Others)、Intravenous (IV)。

药物档案

商品名Carbella, Carnexiv
公司Ligand Pharmaceuticals
药物类别小分子
分子靶点SCN1A, SCN2A, SCN3A
给药途径Injectable (Others), Intravenous (IV)
状态Approved
来源： ClinicalTrials.gov, Ligand Pharmaceuticals

作用机制

分子靶点

carbamazepine 作用于 3 个分子靶点：

SCN1Asodium voltage-gated channel alpha subunit 1 (DEE6B, FEB3)
SCN2Asodium voltage-gated channel alpha subunit 2 (Na(v)1.2, BFNIS)
SCN3Asodium voltage-gated channel alpha subunit 3 (Nav1.3, NAC3)
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

carbamazepine 针对 1 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Nervous system disordersGeneralised tonic-clonic seizure✓ Approved

相关研究文献

PubMedDrug design, development and therapy2026-10-26

Physiologically Based Pharmacokinetic Modeling to Predict Drug-Drug Interactions of Aficamten in the Chinese Population.

Wang Ziyang Z, Wu Xiaofei X, Jia Ranran R, Wang Hongyun H

Aficamten is a next-generation cardiac myosin inhibitor (CMI) developed for the treatment of obstructive hypertrophic cardiomyopathy (oHCM). Although extensive clinical pharmacology studies have been conducted in Caucasian populations, limited information is available regarding drug-drug interaction (DDI) risks in the Chinese population. Given the contribution of multiple cytochrome P450 (CYP) enzymes to aficamten metabolism and inter-ethnic differences in CYP-mediated metabolic capacity, it is important to characterize DDI risks and associated changes in aficamten exposure in Chinese subjects. A whole-body physiologically-based pharmacokinetic (PBPK) model of aficamten was developed using clinical data from Caucasian subjects and extrapolated to the Chinese population. The PBPK model was subsequently applied to compare aficamten exposure between Chinese and Caucasian populations and to predict DDIs in Chinese subjects. Ethnic sensitivity analysis indicated that the key PK parameters of aficamten (AUC0-∞, Cmax, and T1/2) were comparable between Caucasian and Chinese populations. Overall, the predicted DDI magnitudes in the Chinese population were generally consistent with the corresponding Caucasian DDI simulations. Specifically, the model predicted that co-administration with the broad-spectrum CYP inhibitors amiodarone and fluconazole increased the AUC0-∞ of aficamten by 1.43- and 2.27-fold, respectively, whereas the strong inducers carbamazepine and rifampicin decreased its exposure by 35% and 71%, respectively. Notably, under the simulated fluconazole or amiodarone co-administration scenarios, the predicted AUC0-∞ of CYP2D6 intermediate metabolizers (IMs) was 2.22-fold and 1.50-fold higher than that in CYP2D6 normal metabolizers (NMs), respectively. The PBPK model predicted substantial changes in aficamten exposure with broad-spectrum CYP inhibitors (eg, amiodarone, fluconazole) and strong CYP inducers (eg, carbamazepine, rifampicin), and identified CYP2D6 IMs receiving fluconazole or amiodarone as potentially sensitive scenarios. These model-based findings provide quantitative information for DDI risk assessment in Chinese subjects but require clinical confirmation.

PMID 42928782
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PubMedBioMed research international2026-10-25

Controlled-Release Nanoparticles for the Treatment of Childhood Refractory Epilepsy in Latin America.

López-Goerne Tessy T, Santamaria Abel A, Gonzalez-Bondani Antonela A, Valiente Rafael R et al.

Childhood refractory epilepsy (CRE) remains a major therapeutic challenge in Latin America, where limited access to specialized care, persistent treatment gaps, and high rates of pharmacoresistance contribute to poor clinical outcomes. This review examines the potential of sol-gel-derived silica and titania nanoparticles as controlled-release platforms for antiepileptic drug (AED) delivery, with particular emphasis on localized nanoreservoirs designed to improve drug retention at the epileptogenic focus while reducing systemic exposure. We summarize preclinical evidence for sol-gel matrices loaded with conventional AEDs, including carbamazepine, valproic acid, phenytoin, and topiramate, highlighting their physicochemical properties, controlled-release behavior, biocompatibility, and potential to enhance therapeutic efficacy. Particular attention is given to experimental strategies developed in murine temporal lobe epilepsy models, together with emerging approaches for targeted and minimally invasive brain delivery. We further discuss the translational pathway of these technologies, including regulatory considerations, Good Manufacturing Practice (GMP) requirements, pediatric clinical evaluation, and implementation challenges in resource-constrained healthcare systems. By integrating materials science, experimental nanomedicine, and the socioeconomic realities of epilepsy care in Latin America, this review identifies the opportunities and remaining barriers for translating sol-gel nanotechnology into clinically applicable therapies for CRE.

PMID 42927454
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PubMedChemosphere2026-10-25

Persistent pharmaceuticals and their transformation Products: From persistence mechanisms to AI-assisted integrated treatment for safe water reuse.

Shomar Basem B, Domingo Jose L JL

This review examines the physicochemical mechanisms governing pharmaceutical persistence, the formation of transformation products (TPs), and the effectiveness and limitations of conventional and advanced treatment technologies for water reuse, focusing on carbamazepine, diclofenac, iodinated contrast media, metformin, and selected antibiotics, which persist through wastewater treatment. The review follows one chain of reasoning: persistence drivers determine which TPs form, which compartments and exposure pathways are reached, and which treatment barriers can act. Conventional activated sludge often provides incomplete removal, whereas integrated trains combining biological processes, adsorption, ozonation, UV/H2O2, membranes, and other advanced oxidation technologies can improve control, although energy demand, membrane fouling, residuals, and TP formation remain constraints. Pilot- and full-scale studies report average abatement of about 80% or more with ozonation or activated carbon, but behavior differs among compounds, and evidence for complete multi-barrier trains is limited. Unlike reviews addressing occurrence, individual technologies, or TPs separately, this review links the drivers of persistence to the selection and sequencing of treatment barriers, and extends the assessment to groundwater migration, soil-plant and food-chain transfer, and antimicrobial-resistance pathways within a common water-reuse framework. This supports adaptive treatment design targeting parent compounds, TPs, and cross-compartment risks. HRMS, non-target screening, and AI/ML-assisted optimization support adaptive monitoring and control. However, identifying a TP does not demonstrate risk, so effect-based methods are needed, and AI/ML applications are mainly predictive and validated on small datasets. Safe and sustainable water reuse likely requires multi-barrier treatment, source control, continuous monitoring, TP assessment, and integrated risk management.

PMID 42925613
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PubMedMedEdPORTAL : the journal of teaching and learning resources2026-10-23

Acute-on-Chronic Carbamazepine Overdose: A Toxicology Simulation Case for Fourth-Year Medical Students.

Leung Lauren L, Senthil Krithika K, Kothmann John J, Bui Johnny J et al.

Carbamazepine is an antiepileptic medication used to treat seizures, trigeminal neuralgia, and bipolar disorder. Although carbamazepine overdose occurs frequently, it receives limited attention in undergraduate medical curricula. Multimodal, experiential learning provides a safe, structured learning environment. We developed a simulation of carbamazepine overdose to address this educational gap. Fourth-year medical students enrolled in a toxicology course completed a pretest and a Likert-scale questionnaire assessing confidence in managing carbamazepine overdose. Students received a 30-minute lecture and participated in a 15-minute simulation involving a 26-year-old patient with an intentional carbamazepine overdose followed by a 15-minute debrief. Critical actions included obtaining a focused history, neurological assessment, and carbamazepine level; administering multidose activated charcoal; and requesting toxicology and psychiatric consultation. Required equipment included a high-fidelity manikin, IV supplies, and standard pharmaceuticals. We evaluated students with a critical actions checklist and posttest. Students then completed additional Likert-scale questionnaires assessing workshop reactions, confidence, and intent to change practice. Forty-nine students participated across 10 sessions. Mean pretest and posttest scores were 67% (SD = 19) and 98% (SD = 5), respectively, with significant improvement (Wilcoxon W = 0.0, P < .001). All groups completed the critical actions checklist. Median confidence scores for identifying clinical manifestations, ordering and interpreting diagnostic studies, and initiating treatment increased from 3's and 4's to 5 across all domains (Mann-Whitney U P < .001). Students rated the workshop favorably and most reported intent to change practice. Experiential learning is an effective pedagogical technique to teach carbamazepine overdose.

PMID 42910297
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PubMedEcotoxicology (London, England)2026-10-23

Behavioural impacts of ionisable and neutral pharmaceuticals on marbled crayfish (Procambarus virginalis).

Koubová Anna A, Thammatorn Worrayanee W, Kubec Jan J, Nováková Petra P et al.

Ionisable environmental pollutants, including pharmaceutical residues, can be readily bioavailable, bioaccumulative, and potentially toxic for aquatic biota. Risks to organisms arise from continuous exposure, facilitated ion entry through cell membranes and various modes of action on cell receptors. In the present study, we examined behavioural changes in marbled crayfish Procambarus virginalis exposed to environmentally relevant concentrations (EC) and lowest observed effect concentrations (LOEC) of three selected pharmaceuticals. The anticonvulsant carbamazepine (neutral compound; EC = 11.6; LOEC = 116 µg/L), the anti-inflammatory diclofenac (ionisable weak acid; EC = 31; LOEC = 310 µg/L), and the antihistamine diphenhydramine (ionisable weak base; EC = 1.4; LOEC = 95 µg/L) were selected to investigate pharmaceutical-induced behavioural alterations in crayfish following a 96-hour exposure under laboratory conditions (water pH 7.6 and temperature 22 °C). The results showed that exposure to carbamazepine stimulated locomotor activity in crayfish, while no changes were observed in crayfish exposed to diclofenac or diphenhydramine. Specifically, crayfish exposed to EC of carbamazepine displayed an increased percentage of movement activity, nearly double the distance moved, and a higher walking speed compared to the solvent control. However, the exposure to the LOEC of carbamazepine resulted only in an increase in relative movement activity. This study demonstrates that the modes of action and physicochemical properties of pharmaceuticals may significantly influence how aquatic crustaceans respond to chemical stressors. Alterations in ecologically important behavioural traits may occur even at ECs of pharmaceuticals present in aquatic environments.

PMID 42911285
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PubMedChemical research in toxicology2026-10-23

Shared and Distinct T-Cell Receptor Characteristics of CD4+ and CD8+ Drug-Specific T-Cells In Vitro Generated from Healthy Donors and Hypersensitive Patients.

Jaruthamsophon Kanoot K, Thomson Paul J PJ, Pratoomwun Jirawat J, Zhao Qing Q et al.

The initiation of T-cell-mediated drug hypersensitivity reaction requires the formation of a human leukocyte antigen (HLA)-peptide-drug-T-cell receptor (TCR) complex. While specific interactions between HLA molecules and drug antigens are well-defined, the characteristics of drug binding to the TCR are unclear. Herein, we sequenced the TCR mRNAs of T-cells that express drug-specific HLAs (including HLA-A*31:01, HLA-B*15:02, and HLA-B*13:01) and exhibit drug-specific immune responses against carbamazepine, sulfamethoxazole, and dapsone. This study included a total of 46 in vitro-generated monoclonal drug-specific (CD4+ and CD8+) T-cell clones. The T-cell clones were characterized for their drug-specific immune response, including HLA restriction properties, interferon-γ secretion, and cross-reactive responses. RNA isolated from these cells was used for TCR library preparation and subsequent long-read sequencing analyses. T-cell characterization studies showed different drug-responsiveness properties among the clones. TCR sequencing revealed wide heterogeneity among drug-specific T-cells. Only TCR Vβ (TRBV) and TCR Jβ (TRBJ) segments of CD4+ T-cell clones displayed noticeable shared characteristics. A YEQYF residue on CDR3β, which correlates with the preferential use of TRBJ2-7, was identified in 5 out of 16 CD4+ carbamazepine-specific clones. However, CD8+ drug-specific clones showed no preferential usage of TCR α/β. Sequence alignment analyses among clones with similar or different drug-responsiveness properties also showed no evidence of structure-function correlation. In summary, TCR specificity against drug antigens appears to be nonrestrictive, suggesting that the extent of possible binding and its key determinants are not rigid.

PMID 42915728
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