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oxcarbazepine (SPN604 / SPN 804 / oxcarbazepine ER)

✓ Approved

Aequus Pharmaceuticals, Inc. · SCN1A · 小分子

什么是 oxcarbazepine？

oxcarbazepine 是一种小分子，由Aequus Pharmaceuticals, Inc.研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名SPN604, SPN 804, oxcarbazepine ER
公司Aequus Pharmaceuticals, Inc.
药物类别小分子
分子靶点SCN1A, SCN2A, SCN3A
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Aequus Pharmaceuticals, Inc.

作用机制

分子靶点

oxcarbazepine 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

oxcarbazepine 针对 2 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Nervous system disordersPartial seizures✓ Approved
Psychiatric disordersBipolar disorderPhase III

相关研究文献

PubMedNutricion hospitalaria2026-09-07

[Management of syndrome of inappropriate antidiuretic hormone secretion in outpatients].

Fernández Jiménez Juan J

the syndrome of inappropriate antidiuretic hormone secretion (SIADH) is the most frequent cause of hyponatremia in the outpatient setting, presenting significant diagnostic and therapeutic challenges due to the difficulty of performing laboratory monitoring and poor patient compliance with fluid restriction. we report the case of an institutionalized and polymedicated 59-year-old male, with a history of congenital epilepsy, who developed moderate euvolemic hyponatremia ([Na+] 124 mEq/l) secondary to oxcarbazepine therapy. Given the risk of a progressive decline in serum sodium, treatment with oral urea (30 g/day) was initiated, achieving a controlled and progressive increase in natremia to safe limits (133 mEq/l), even before the withdrawal of the culprit drug. Following the subsequent discontinuation of oxcarbazepine by neurology, natremia fully normalized ([Na+] 138 mEq/l), allowing a successful withdrawal of urea. oral urea stands out as the only fully effective, safe, and well-tolerated medium- and long-term therapeutic strategy available for managing outpatient SIADH.

PMID 42704005
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PubMedNeurology2026-09-03

Gestational Changes in Antiseizure Medication Concentrations and the Impact of Polytherapy: A Prospective Multicenter Cohort Study in China.

Duan Yifei Y, Huang Sikai S, Sha Leihao L, Fu Yutong Y et al.

Pregnancy alters the pharmacokinetics of antiseizure medications (ASMs). The aim of this study was to quantify gestational changes in ASM concentrations and identify independent covariates among women with epilepsy in China. In this prospective, multicenter observational cohort study in China, women with epilepsy aged 18-45 years were enrolled and followed longitudinally. Steady-state trough ASM concentrations were measured, with concentration-to-dose (C/D) ratio as the primary pharmacokinetic parameter. Linear mixed-effects models with model averaging were used to evaluate the independent effects of gestational age, concomitant ASMs, and demographic covariates on ASM C/D ratios. A total of 947 women were included and contributed 1,638 samples between 2019 and 2025, including 1,187 samples collected during nonpregnant periods (821 women, mean age 29.31 ± 8.38 years) and 451 during pregnancy (228 women, mean age 28.67 ± 4.30 years), with 64.3% receiving polytherapy. Lamotrigine exhibited the greatest gestational effect, with C/D ratios declining by 28.8% (β = -0.339; 95% CI -0.508 to -0.339; p < 0.001), 54.3% (β = -0.784; 95% CI -0.938 to -0.629; p < 0.001), and 63.2% (β = -1.001; 95% CI -1.192 to -0.809; p < 0.001) in the first, second, and third trimesters, respectively, reaching a nadir of -65.8% at 32 weeks. Levetiracetam declined by 26.2% (β = -0.303; 95% CI -0.446 to -0.160; p < 0.001), 40.1% (β = -0.512; 95% CI -0.645 to -0.379; p < 0.001), and 31.0% (β = -0.371; 95% CI -0.525 to -0.217; p < 0.001), reaching a nadir of -35.5% at 24 weeks. The metabolite of oxcarbazepine declined by 23.1% (β = -0.262; 95% CI -0.373 to -0.152; p < 0.001), 32.6% (β = -0.394; 95% CI -0.489 to -0.299; p < 0.001), and 44.3% (β = -0.585; 95% CI -0.695 to -0.475; p < 0.001). Lacosamide significantly decreased in the second trimester (-10.8%; β = -0.207; 95% CI -0.399 to -0.014; p = 0.035). Perampanel showed an increasing trend but was limited by sample and polytherapy. Concomitant ASMs primarily shifted baseline C/D ratios without altering gestational changes, and several drug-drug interactions were identified. Higher body weight was associated with lower C/D ratios for most ASMs, except for perampanel. Interindividual variability remained the dominant factor determining C/D ratios over measured covariates. Pregnancy was the primary driver of declining C/D ratios, and concomitant ASMs and body weight acted as secondary modifiers. These findings support individual therapeutic drug monitoring. ChiCTR2100046318 (Chinese Clinical Trial Registry, chictr.org.cn).

PMID 42685297
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PubMedCureus2026-09-02

Movement-Provoked Paroxysmal Neuralgia Following Longitudinally Extensive Transverse Myelitis in Neuromyelitis Optica Spectrum Disorder: A Presumed Ephaptic Spinal Cord Phenomenon.

Philips Angela A, Sosa De La Cruz Johan J, Ungerer Robert R, Betha Prudvi Tarun PT

Neuromyelitis optica spectrum disorder (NMOSD) is an autoimmune astrocytopathy frequently complicated by neuropathic pain. Paroxysmal symptoms likely arise from ephaptic transmission within demyelinated spinal cord tracts and are underdescribed when presenting as isolated sensory phenomena, unlike the well-characterized tonic spasms. We report a 76-year-old woman with aquaporin-4 (AQP4) antibody-positive NMOSD recovering from her first disease flare, which initially manifested as longitudinally extensive transverse myelitis (LETM). Weeks later, she developed sudden, excruciating, movement-provoked paroxysmal burning pain in the lower extremities. Episodes lasted 4-8 seconds and occurred approximately 20 times daily. Serial neurologic examinations revealed no new deficits suggestive of relapse, and repeat MRI was deferred as relapse was considered clinically unlikely. Symptoms were refractory to gabapentin but improved dramatically within 24 hours of initiating oxcarbazepine 300 mg twice daily. The clinical phenotype and rapid response to sodium channel blockade support a sodium channel-mediated mechanism, most likely ephaptic transmission, rather than trigger-independent ectopic firing, which remains sparsely described in the literature. Recognition of this phenomenon is crucial to avoid misclassification as relapse, unnecessary imaging, and unwarranted escalation of immunotherapy.

PMID 42683220
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PubMedPain medicine case reports2026-09-01

Long-Term Tapentadol Use for Neuropathic Pain in a Hemodialysis Patient with End-stage Renal Disease: A Case Report.

Shepherd Mattison M, Bruketta Morgan M

Tapentadol is generally not recommended in patients with end-stage renal disease on hemodialysis due to concerns about metabolite accumulation and limited safety data. Evidence in this population is scarce, with no major trials to date. A 58-year-old man with end-stage renal disease on hemodialysis developed ischemic monomelic neuropathy after fistula surgery. Previous opioids and tramadol were ineffective; pregabalin, gabapentin, and oxcarbazepine caused intolerable side effects. Due to ongoing citalopram therapy, serotonin-norepinephrine reuptake inhibitor changes were avoided. Tapentadol 75 mg three times daily was started and continued for 20 months, resulting in sustained pain control without observed adverse effects or clinical signs suggestive of drug accumulation; pharmacokinetic drug accumulation could not be assessed because blood and urine drug levels were unavailable. This case suggests long-term tapentadol may be a safe and effective pain management option in selected patients with end-stage renal disease on hemodialysis, though further study is needed.

PMID 42679080
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PubMedEpilepsy research2026-08-28

Risk factors for adverse maternal‑neonatal outcomes in pregnant women with epilepsy and the impact of different anti-seizure medications exposures on neonatal birth weight.

Fang Chun C, Yang Heqin H, Yang Yongmei Y

To investigate the risk factors for adverse maternal‑neonatal outcomes in pregnant women with epilepsy and to analyze the effects of different anti-seizure medications (ASMs) on neonatal birth weight, thereby providing clinical evidence for the management of epilepsy during pregnancy. A total of 218 pregnant women with epilepsy who delivered at our hospital between January 2021 and December 2025 were enrolled. Demographic data, epilepsy‑related clinical characteristics, ASM regimens, pregnancy complications, and maternal‑neonatal outcomes were collected. Patients were divided into an adverse outcome group (n = 74) and a favorable outcome group (n = 144) based on the occurrence of adverse maternal‑neonatal outcomes (including preterm birth, low birth weight, fetal distress, and neonatal malformations). Logistic regression analysis was performed to identify independent risk factors for adverse outcomes. Among patients receiving monotherapy (n = 131, 60.09%), they were categorized into lamotrigine, levetiracetam, carbamazepine, oxcarbazepine, and valproate groups according to ASM exposure during pregnancy; a separate polytherapy group (n = 87, 39.91%) was also included. Analysis of variance (ANOVA) was used to compare neonatal birth weight across groups. Multivariate logistic regression showed that uncontrolled epilepsy before and during pregnancy (presence of seizures within six months before pregnancy: OR=4.300, P < 0.001; any seizure during pregnancy: OR=3.661, P < 0.001; increased seizure frequency during pregnancy: OR=3.781, P < 0.001), focal epilepsy (OR=2.245, P = 0.005), polytherapy (OR=2.046, P = 0.014), and gestational hypertension (OR=2.764, P = 0.008) were independent risk factors for adverse maternal‑neonatal outcomes. Regarding neonatal birth weight, the monotherapy group had a significantly higher mean birth weight (3170 ± 452 g) than the polytherapy group (2963 ± 501 g, P = 0.002). Among monotherapy regimens, the valproate group had the lowest mean birth weight (2805.50 ± 395.53 g), which was significantly lower than that of the lamotrigine group (3273.51 ± 429.49 g, P = 0.012) and the levetiracetam group (3236.51 ± 407.47 g, P = 0.023). No significant differences were observed among the lamotrigine, levetiracetam, carbamazepine, and oxcarbazepine groups (ANOVA: F=3.822, P = 0.006). Uncontrolled epilepsy before and during pregnancy, polytherapy, focal epilepsy, and gestational hypertension are independent risk factors for adverse maternal‑neonatal outcomes in pregnant women with epilepsy. Different ASMs have differential effects on neonatal birth weight; valproate and polytherapy are associated with significantly lower birth weight. Physicians should counsel women with epilepsy that achieving at least six months of seizure freedom before conception is associated with improved maternal-neonatal outcomes. Lamotrigine or levetiracetam monotherapy should be prioritized whenever possible, and close monitoring should be maintained throughout pregnancy.

PMID 42659781
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PubMedBMJ supportive & palliative care2026-08-26

Sodium channel blocker rotation for refractory neuropathic pain.

Huguet Max M, Curtin John J, Broderick Marianne M, Howard Paul P

To investigate the efficacy and safety of sodium channel blocker (SCB) rotation and/or combined use for neuropathic pain where the initial SCB is ineffective or poorly tolerated. A retrospective chart review of SCB rotation in a single palliative care centre. We reviewed the notes of those receiving two or more SCBs for pain. All clinical notes and medication administration records were examined to ascertain efficacy and tolerability. We found 45 examples of SCB rotation in 32 patients. Most (81%) had metastatic cancer. All had tried multiple other analgesics. Most (29/45) were rotated for persistent pain; the remainder for poor tolerability (11/45) or to change the route (5/45), for example, an SCB that could not be given parenterally when the oral route was lost. SCB rotation appeared helpful for the majority (69%). Switches appeared effective in both directions between lacosamide and oxcarbazepine; thus, neither SCB appeared 'superior'. A minority (7/32) received two SCBs together having had insufficient analgesia from SCB monotherapy; dual SCB therapy was well tolerated and appeared effective in 6/7. Rotation appeared effective and well tolerated for neuropathic pain where an initial SCB was ineffective or poorly tolerated. Further, in those with the most analgesic-refractory pains, we found preliminary evidence that combining SCBs with different characteristics might be beneficial, for example, combining slow channel inactivators with fast channel inactivators. Thus, we believe that SCBs should not be considered a homogenous analgesic class and that further research into both SCB rotation and dual SCB therapy is justified.

PMID 42648885
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