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topiramate (USL255 / Qudexy XR)

✓ Approved

Upsher-Smith Laboratories, LLC. · GRIA1 · 小分子

什么是 topiramate？

topiramate 是一种小分子，由Upsher-Smith Laboratories, LLC.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USL255, Qudexy XR
公司Upsher-Smith Laboratories, LLC.
药物类别小分子
分子靶点GRIA1, SCN5A
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Upsher-Smith Laboratories, LLC.

作用机制

分子靶点

topiramate 作用于 2 个分子靶点：

GRIA1glutamate ionotropic receptor AMPA type subunit 1 (GLUR1, HBGR1)
SCN5Asodium voltage-gated channel alpha subunit 5 (CMD1E, SSS1)
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

topiramate 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
Surgical and medical proceduresMigraine prophylaxis✓ Approved

相关研究文献

PubMedBMC pregnancy and childbirth2026-10-27

Prenatal antiseizure medication exposure and offspring structural and neurodevelopmental outcomes: an umbrella review of systematic reviews and meta-analyses.

Li Yulong Y, Fu Yutong Y, Duan Yifei Y, Shi Fanfan F et al.

Review-level evidence on prenatal antiseizure medication (ASM) exposure is difficult to interpret because outcome domains are often synthesized separately, primary studies overlap, and comparator frameworks and certainty vary. We aimed to calibrate evidence across structural and neurodevelopmental outcomes. We conducted an anchor-based umbrella review of systematic reviews and meta-analyses (PROSPERO: CRD420251142541), searching four databases through December 31, 2025. One prespecified anchor review represented each drug-outcome-comparator question; overlapping reviews were not combined into second-order pooled estimates. AMSTAR 2, corrected covered area, GRADE, and directional umbrella-credibility classes were applied, with NS assigned when the 95% confidence interval included the null. Fourteen reviews were included: nine structural and five neurodevelopmental. All had Low or Critically Low AMSTAR 2 confidence, and ASD/ADHD review overlap was very high (CCA, 28.1%). Valproate showed the most consistent retained pattern, including Class I credibility for combined major congenital anomalies and the most credible retained neurodevelopmental signal for autism spectrum disorder (adjusted hazard ratio, 3.10; 95% CI, 2.24-4.28; Low certainty; Class II). Topiramate showed an oral-cleft signal with Low certainty and Class III credibility. The lamotrigine estimate for major congenital anomalies was NS, whereas the orofacial-cleft estimate excluded the null but had Very Low certainty (OR, 1.42; 95% CI, 1.05-1.92; Class IV). Other retained neurodevelopmental anchors had Very Low certainty and were Class IV or NS; no independent pairwise neurodevelopmental anchor was available for carbamazepine, oxcarbazepine, topiramate, or levetiracetam. Review-level evidence was most consistent for valproate and aligned with its established structural and neurodevelopmental risks. NS or Very Low-certainty findings for non-valproate ASMs should not be interpreted as evidence of no risk. Comparative safety requires individualized risk-benefit assessment rather than binary safety classifications.

PMID 42934576
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PubMedNutrients2026-10-27

Emerging Therapeutic Strategies for Child and Adolescent Obesity: A Narrative Review.

Oliaro Tomaso T, Amianto Federico F

Childhood obesity is a chronic, multifactorial disease requiring attention to biological, behavioral, psychological, family, and socioeconomic factors. This narrative review examined the integration of lifestyle, family-based, psychological, and pharmacological approaches, focusing on treatment engagement, eating disorders, attention-deficit/hyperactivity disorder (ADHD), and treatment durability. A single search interface covering PubMed/MEDLINE, Scopus, and Web of Science (the University of Turin library discovery platform) was used to identify studies published primarily from 2010 to August 2026. Pediatric trials, observational studies, systematic reviews, meta-analyses, guidelines, and public-health reports were prioritized. Intensive family-based, multicomponent behavioral treatment remains the best-supported foundation of care, although psychological outcomes are infrequently assessed. Psychiatric comorbidity is heterogeneous; loss-of-control eating, emotional symptoms, ADHD, and executive-function difficulties may impair engagement in selected patients, and untreated ADHD has been associated with a slower BMI response to weight management. Professionally supervised obesity treatment containing a dietary component did not, on average, worsen eating psychopathology and reduced several related symptoms. Family participation improved outcomes, whereas logistical, socioeconomic, and psychological barriers reduced attendance. Across randomized trials, adding anti-obesity medication to behavioral treatment produced an additional, although on average modest, reduction in BMI. Semaglutide, liraglutide, and phentermine/topiramate produced larger numerical reductions than older agents in separate trials, but heterogeneity and the absence of head-to-head comparisons preclude formal ranking. Gastrointestinal adverse events were frequent with glucagon-like peptide-1 (GLP-1) receptor agonists. Pediatric trials and real-world evidence indicate partial weight regain after discontinuation, while prescribing remains limited and unequal. Pediatric obesity care should be phenotype-informed, multidisciplinary, and longitudinal. Pharmacotherapy can enhance BMI reduction but should complement rather than replace behavioral, psychological, and family care. Outcomes should extend beyond BMI to metabolic, psychological, functional, and long-term measures.

PMID 42943020
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PubMedPharmaceutics2026-10-27

Progress in Anti-Obesity Drug Development: A Pharmacodynamics Perspective.

Ahmad Ishtiaque I, Azmi Sarfuddin S, Albabtain Monirah A MA, Mustafa Mohammad M et al.

Background/Objectives: Obesity is a chronic, multifactorial condition driven by complex neuroendocrine and metabolic pathways that limit the long-term success of lifestyle interventions. Pharmacotherapy has advanced from early monoaminergic agents to incretin-based and multi-receptor agonists with substantially improved efficacy. This review aims to provide pharmacodynamics-focused synthesis of current and emerging anti-obesity medications, emphasizing mechanistic targets, receptor interactions, and translational implications. Methods: We conducted a narrative review integrating Phase I-III clinical trials, mechanistic pharmacology data (receptor affinity, potency, and signaling bias), and regulatory summaries for FDA-approved and selected emerging, investigational, repurposed, or regionally approved anti-obesity agents. Inclusion focused on clinical relevance, pharmacodynamic novelty, and weight-loss efficacy. Results: Approved anti-obesity medications act through diverse pathways, including the inhibition of fat absorption (orlistat), the modulation of central appetite circuits (phentermine/topiramate, naltrexone/bupropion), and incretin-based mechanisms (liraglutide, semaglutide, tirzepatide, and the oral GLP-1 receptor agonists semaglutide 25 mg and the nonpeptide orforglipron). GLP-1 receptor agonists achieve approximately 6-15% weight loss, while dual glucose-dependent insulinotropic polypeptide/GLP-1 receptor agonists such as tirzepatide reach 15-20%. Emerging agents-including triple agonists (retatrutide), glucagon-based co-agonists, amylin analogs with Phase III efficacy data, earlier-stage growth differentiation factor 15 (GDF15) pathway agonists, and peripherally restricted cannabinoid-1 receptor inverse agonists-demonstrate enhanced metabolic effects and potential improvements in lean-mass preservation. Obesity-related alterations in pharmacokinetics and pharmacodynamics highlight the need for individualized dosing strategies. Conclusions: Clinical efficacy and tolerability cannot be inferred from receptor identity alone. They emerge from relative receptor potency and efficacy, exposure, tissue access, receptor trafficking, and mechanism-linked adverse effects. Dual and triple agonists can broaden efficacy, but receptor balance and standardized comparative pharmacology remain essential for rational development and individualized dosing.

PMID 42942813
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PubMedCurrent atherosclerosis reports2026-10-26

Strategies for Managing Obesity and Cardiometabolic Risk in Young Children: Current Evidence and Future Directions.

Salama Mostafa M, Kumar Seema S

Early-onset obesity is associated with adverse cardiometabolic risk factors and early vascular changes linked to atherosclerosis, yet evidence-based treatment options for young children remain limited. The purpose of the review is to examine current evidence for lifestyle, pharmacologic, and surgical interventions for obesity management in preadolescent children, with emphasis on cardiometabolic and atherosclerotic risk. Lifestyle and familybased behavioral interventions remain first line therapy but often produce modest and variable weight reduction. Pharmacologic options for children younger than 12 years are limited, emerging data suggest selected agents, including topiramate, lisdexamfetamine, glucagon-like peptide-1 receptor agonists and metformin can improve weight status and cardiometabolic risk factors in carefully selected patients. Bariatric surgery provides durable weight loss and cardiometabolic benefit and adolescents with severe obesity, though data and younger children are sparse. Available interventions may improve cardiometabolic risk profiles when appropriately applied early in life, but high-quality long-term data and preadolescent children are needed.

PMID 42932074
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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.

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PubMedFrontiers in cell and developmental biology2026-10-25

A zebrafish model of NEXMIF-related encephalopathy identified drivers of hyperlocomotion and provides a scalable platform for drug discovery.

Bernal-Bermúdez Beatriz B, Martínez-Morcillo Francisco J FJ, Fuentes-Martínez Inmaculada I, Martínez-López Alicia A et al.

X-linked Intellectual Disability type 98 (XLID-98) is a neurodevelopmental disorder with a broad phenotypic spectrum caused by pathogenic variants in the neurite extension and migration factor (NEXMIF) gene, formerly known as KIAA2022, KIDLIA, or XPN (OMIM 300524). To investigate the pathogenic mechanisms of XLID-98, a double knock-out zebrafish model (nexmifa/b -/-) was generated using CRISPR/Cas9 technology. Mutant larvae displayed limited morphological abnormalities, the most notable being an increase in total body length. They also exhibited a significant hyperlocomotor phenotype in the visual-startle OFF assay, which was attenuated by treatment with sodium valproate (VPA) and topiramate, thereby supporting the pharmacological validity of the model. Transcriptomic analysis of larval heads at seven dpf revealed 414 differentially expressed genes enriched in mitogen-activated protein kinase (MAPK) signaling, cell adhesion, and sodium transport pathways. Functional analyses demonstrated that simultaneous CRISPR/Cas9-mediated disruption of the upregulated genes entpd3 (ectonucleoside triphosphate diphosphohydrolase 3) and ddx43 (DEAD-box helicase 43) exacerbated the hyperlocomotor phenotype, suggesting that these genes may participate in a compensatory response, whereas reduced kbtbd7 (kelch repeat and BTB domain-containing protein 7) activity may contribute to phenotype severity. A targeted screen of 87 natural compounds identified kahweol acetate, veratridine, and rauwolscine as potent inducers of entpd3. However, despite robust transcriptional activation, rauwolscine failed to improve behavioral outcomes, suggesting that modulation of a single molecular target may be insufficient for phenotypic rescue. Collectively, these findings establish the first zebrafish model of NEXMIF-related encephalopathy, identify entpd3, ddx43, and kbtbd7 as candidate modulators of this behavioral phenotype, and provide a scalable platform for targeted therapeutic discovery in XLID-98.

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