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fentanyl citrate (OX20 / Rapinyl / EN 3267)

✓ Approved

Kyowa Kirin Co., Ltd. · 小分子 · 小分子

什么是 fentanyl citrate？

fentanyl citrate 是一种小分子，由Kyowa Kirin Co., Ltd.研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)、Sublingual (SL)/Oral Transmucosal、Topical。

药物档案

商品名OX20, Rapinyl, EN 3267
公司Kyowa Kirin Co., Ltd.
药物类别小分子
给药途径Oral (PO), Sublingual (SL)/Oral Transmucosal, Topical
状态Approved
来源： ClinicalTrials.gov, Kyowa Kirin Co., Ltd.

治疗适应症

fentanyl citrate 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
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Cancer pain✓ Approved

相关研究文献

PubMedJournal of pediatric and adolescent gynecology2026-06-13

Adolescent Experiences with Procedural Sedation for Intrauterine Device Placement: A Pilot Study.

Bryant Ellen E, Stancil Stephani S, Priebe Anne-Marie AM, Nos Andrea A et al.

This study examines adolescent experiences with intrauterine device (IUD) insertion under conscious sedation. We conducted a prospective pilot study of 11-21-year-olds who chose conscious sedation for their IUD insertion. Participants completed pre-procedure surveys (e.g., demographics, anticipated pain, reproductive history) and post-procedure surveys (e.g., pain during insertion and overall experience). Providers completed a survey on the day of IUD insertion with sedation type, complications, and reason for sedation. In 16 youth (16.1 ± 1.8 years), 14 received moderate sedation (intravenous midazolam and fentanyl) and 2 received light sedation (nitrous oxide). The most reported "worst part" was procedural cramps (n=5, 31%). The "best part" was sedation effects (n=7, 44%). All patients who received light sedation remembered the insertion compared to 2 of 14 (14%) patients who received moderate sedation. Patients reported an average satisfaction score of 83 on a 100-point visual analogue scale, with no difference between sedation types. Adolescents were highly satisfied with procedural sedation for IUD insertion. Fewer participants remembered the procedure when they received moderate compared to light sedation. IUDs are effective as reversible contraception and menstrual management. The pelvic exam and pain may discourage use of the IUD, but sedation offers an alternate experience. Examining patient experiences will help clinicians counsel future patients on their anticipated experience and provides evidence-based rationale for modification and expansion of this service.

PMID 42285392
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PubMedNeurotoxicology2026-06-13

Combined exposure to 6PPD and 6PPD-Q induced neurotoxic responses in zebrafish and SH-SY5Y cells: evidence from neurotransmitter disruption, oxidative damage, and apoptosis.

Wang Ziwei Z, Wang Shutao S, Li Wanlun W, Wang Xingyu X et al.

The rubber antioxidant N-(1,3-dimethylbutyl)-N'-phenyl-p-phenylenediamine (6PPD) and its quinone derivative (6PPD-Q) are coexisting environmental contaminants with documented neurobehavioral effects. However, the neurotoxic consequences arising from their combined exposure remain unclear. In this study, adult zebrafish and SH-SY5Y cells were used to investigate the neurotoxic effects associated with co-exposure to 6PPD and 6PPD-Q. In zebrafish, 100μg/L 6PPD+100μg/L 6PPD-Q increased time spent and distance traveled in the non-reward area of the T-maze after 28 d exposure, accompanied by pathological damage in brain tissue, including reduced neuronal density, decreased Nissl bodies, and apoptosis. 6PPD-Q exacerbated oxidative damage and the decreased levels of neurotransmitters induced by 6PPD. Metabolomics implicated disruptions in neuroactive ligand-receptor interaction and citrate cycle. Transcriptomic analysis further identified dysregulation in oxidative stress, cell death, and nervous system processes related pathways, such as Peroxisome, Axon guidance, and PI3K-Akt pathway. In SH-SY5Y cells, co-exposure reduced cell viability and produced predominantly synergistic effects across concentration combinations tested. 6PPD-Q aggravated mitochondrial damage and enhanced the protein expression levels related to apoptosis induced by 6PPD, including caspase-3 and bax/bcl-2. Moreover, co-exposure inhibited the PI3K-AKT pathway, which might exacerbate neurotransmitter disturbance and apoptosis. The findings enrich the understanding of neurological health risks linked to 6PPD and 6PPD-Q, highlighting the importance of preventive strategies to mitigate the exposure risks.

PMID 42285362
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PubMedSchizophrenia research2026-06-13

Energy metabolism dysregulation in schizophrenia with non-thyroidal illness syndrome: Roles of citric acid and Tyrosol-4-sulfate.

Chen Junhao J, Dong Yeqing Y, Li Yanzhe Y, Liu Nannan N et al.

Non-Thyroidal Illness Syndrome (NTIS) is frequently observed in schizophrenia and is traditionally regarded as a peripheral endocrine disturbance. However, whether NTIS reflects a distinct metabolic phenotype linked to central energy dysregulation in schizophrenia remains unclear. We hypothesized that NTIS in schizophrenia reflects a distinct metabolic state characterized by disrupted energy metabolism, which may be linked to specific symptom dimensions. A total of 185 patients with schizophrenia were enrolled and classified into NTIS and non-NTIS groups based on standard thyroid hormone criteria. Untargeted metabolomic profiling was performed using ultra-high-performance liquid chromatography high-resolution mass spectrometry. Differential metabolites were identified using Orthogonal-Partial-Least Squares-Discriminant-Analysis and Receiver Operating Characteristic curve analysis, followed by pathway enrichment analyses and regression analyses to examine associations with clinical symptoms. A total of 29 differential metabolites were screened (Variable Importance in Projection > 2, P - correction < 0.05), primarily related to amino acids and organic acids. Pathway enrichment analysis revealed significant perturbations in 10 metabolic pathways, with the TCA cycle (citrate cycle) (impact = 0.261, P < 0.0001). Two metabolites, Citric acid (AUC = 0.701, P < 0.05) and Tyrosol-4-sulfate (AUC = 0.703, P < 0.05) demonstrated good discriminative performance for NTIS status. These 2 metabolites were positively associated with the Visuospatial/Constructional dimension and negatively associated with positive symptoms in the NTIS group. Schizophrenia patients with NTIS display a distinct metabolic phenotype marked by TCA cycle dysregulation. Citric acid and tyrosol-4-sulfate may serve as metabolic indicators linking thyroid dysfunction to cognitive, psychotic symptoms.

PMID 42284951
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PubMedbioRxiv : the preprint server for biology2026-06-12

Uncovering phenotypic diversity and cell-type-specific prefrontal cortex calcium dynamics in rat fentanyl self-administration.

Whitebirch Alexander C AC, Panh Shawn S, Tripathi Loveleen L, Garcia Aaron F AF et al.

The proliferation of the potent synthetic opioid fentanyl has exacerbated the ongoing crisis of substance use disorder and associated overdose deaths, yet the neurobiological mechanisms that underlie individual vulnerability to addiction and relapse remain poorly understood, particularly in the context of fentanyl use. The prefrontal cortex (PFC) has been identified as a key brain structure important for cognitive functions impacted in addiction, including inhibitory control of behavior and association of drug experience with specific cues, contexts, or actions. Although the heterogenous neuronal composition of the PFC complicates attribution of addiction-related behavioral regulation to specific cortical cell types and circuits, application of cell-type-specific methods in translationally relevant rodent models have begun to elucidate the key neural substrates of opioid addiction. We used an intermittent access fentanyl self-administration (IntA SA) model to characterize individual variation and sex differences in addiction vulnerability in male and female rats. Longitudinal wireless fiber photometry recording was used to track calcium activity patterns in intratelencephalic (IT) neurons of the prelimbic cortex across acquisition of self-administration, escalation of fentanyl intake, extinction training, and cue-induced reinstatement of fentanyl seeking. We found that our fentanyl IntA SA paradigm produces distinct low- and high-risk addiction severity phenotypes and that female rats exhibited a greater propensity for high-risk classification, which was characterized by abundant and consistent fentanyl intake, robust responsiveness to conditioned and discriminative fentanyl-associated cues, and high levels of fentanyl-seeking during periods of drug unavailability, extinction training, and a cue-induced reinstatement test. Fiber photometry recordings revealed dynamic encoding of fentanyl-associated stimuli by prelimbic IT neurons across the IntA SA paradigm with event-related calcium transients observed in association with lever presses, fentanyl infusions, and presentation of conditioned and discriminative cues. Our data indicate that fentanyl IntA SA is a translationally relevant paradigm that enables investigation of phenotypic diversity and the role of sex in fentanyl addiction. Longitudinal cell-type-selective calcium recordings revealed dynamic representation of fentanyl-associated stimuli by IT neurons of the prelimbic cortex consistent with a role for this cortical subpopulation in addiction-related behaviors.

PMID 42282838
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PubMedResearch square2026-06-12

Novel Swine Model of Respiratory Depression Induced by Fentanyl and Heroin Overdose.

Hatschbach Eduardo E, Raleigh Michael D MD, Vigliaturo Jennifer J, Hicks Dustin D et al.

Background This study characterized a swine model of fentanyl- and heroin-induced non-lethal apnea to support development of translational strategies for opioid overdose interventions. Methods Spontaneously breathing, isoflurane-anesthetized Hanford swine (n = 18; 4-25 kg) received intravenous fentanyl (n = 12) or heroin (n = 6) via constant rate infusion (fentanyl: 30 µg/kg/h; heroin: 1 mg/kg/h) until production of respiratory arrest (i.e., apnea), defined as the absence of spontaneous breaths for two consecutive minutes. Fentanyl-treated pigs were either sexually immature (~ 2 months) or mature (~ 4 months); heroin-treated pigs were immature; both groups included equal numbers of males and females. Results Results are presented as median (IQR) or mean ± SEM. Immature pigs required higher fentanyl doses to induce apnea compared with mature pigs, 17 (15-36) µg/kg vs 8 (7-10) µg/kg respectively, despite similar serum fentanyl concentration at apnea, which were 4 (3-7) and 6 (4-8) ng/mL respectively, consistent with a significantly faster clearance in immature pigs. No significant age-related differences were observed in norfentanyl concentrations or in its pharmacokinetic parameters. Heroin infusion resulted in apnea at 360 (290-502) µg/kg. Although serum heroin concentrations remained below the LLOQ throughout all time points, its metabolites 6-acetylmorphine (6-AM) and morphine serum concentration at apnea were 57 (44-91) and 34 (29-61) ng/mL, with 6-AM displaying faster clearance and a shorter half-life than morphine. Latency to resume spontaneous breathing was longer in immature than mature pigs that received fentanyl, and pigs exposed to heroin exhibited more severe respiratory depression, characterized by prolonged apnea and delayed or incomplete recovery, with a reduced response to naloxone compared with fentanyl. No statistically significant differences were detected between male and female pigs. Conclusion In conclusion, this reproducible model enables evaluation of opioid-induced respiratory depression and its pathophysiological consequences, supporting targeted therapeutic development.

PMID 42282039
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PubMedInternational journal of molecular sciences2026-06-12

Plasma Citrate Levels Are Inversely Associated with Estimated Muscle Mass and Strength in Liver Transplant Recipients.

Li Yakun Y, Post Adrian A, Chvatal Medina Mateo M, Doorenbos Caecilia S E CSE et al.

Reduced muscle mass and strength are highly prevalent in liver transplant recipients (LTRs). Citrate, a key intermediate of the tricarboxylic acid cycle, may adversely relate to muscle health through disturbances in mitochondrial energy metabolism and metabolic flexibility. We aimed to investigate the association of plasma citrate levels with estimated muscle mass, strength, and physical performance in LTRs. We included stable LTRs from the TransplantLines Biobank and Cohort Study at least 1 year after transplantation. Muscle mass, strength, and physical performance were assessed using the 24 h urinary creatinine excretion rate divided by height squared (creatinine excretion rate index, CERI), handgrip strength, sit-to-stand (STS) and Timed Up and Go (TUG) tests. Associations of plasma citrate with muscle-related parameters were examined using Spearman correlation and linear regression analyses. A total of 501 LTRs were included (median age 59 [49-67] years; 58.7% men) at a median of 14.0 (7.4-22.5) years post-transplantation. Spearman correlation analyses showed that plasma citrate levels were inversely correlated with CERI (ρ= -0.226, p < 0.001) and handgrip strength (ρ= -0.211, p < 0.001). Additionally, plasma citrate levels were positively correlated with STS time (ρ = 0.170, p = 0.019) and TUG time (ρ = 0.203, p = 0.006). In linear regression analyses, higher plasma citrate levels were associated with lower CERI and lower handgrip strength and with longer STS and TUG time. In multivariable linear regression analyses, plasma citrate remained independently associated with CERI (fully adjusted standardized β= -0.14, p = 0.001) and handgrip strength (fully adjusted standardized β= -0.11, p = 0.010), whereas associations with physical performance measures were no longer significant after adjustment. CERI mediated 45.8% of the association between citrate and handgrip strength. In conclusion, higher plasma citrate levels are independently associated with lower estimated muscle mass and strength in LTRs. Circulating citrate may serve as a potential biomarker of post-transplant muscle impairment risk.

PMID 42278339
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