Drug Database
FE

fentanyl citrate (OX20 / Rapinyl / EN 3267)

✓ Approved

Kyowa Kirin Co., Ltd. · Small Molecule · Small Molecule

What is fentanyl citrate?

fentanyl citrate is a small molecule developed by Kyowa Kirin Co., Ltd.. It is approved for therapeutic indications via oral (po) or sublingual (sl)/oral transmucosal or topical.

Drug Profile

Brand NamesOX20, Rapinyl, EN 3267
CompanyKyowa Kirin Co., Ltd.
Drug ClassSmall Molecule
RouteOral (PO), Sublingual (SL)/Oral Transmucosal, Topical
StatusApproved
Sources: ClinicalTrials.gov, Kyowa Kirin Co., Ltd.

Therapeutic Indications

fentanyl citrate is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Neoplasms benign, malignant and unspecified (incl cysts and polyps)Cancer pain✓ Approved

Related Research Articles

PubMedJournal of clinical apheresis2026-10-15

Apheresis in Children of Weight Under 7 kg-A Single Center Experience.

Rungsiprakarn Phassawan P, Wilson Bryan E BE, Rintoul Natalie E NE, Wild K Taylor KT et al.

Although apheresis techniques in children are well established, published experience with very low-weight children is limited. We reviewed 68 procedures performed in 19 children weighing less than 7 kg, including hematopoietic progenitor and T-cell collections and plasmapheresis. With significant modifications of standard techniques, all but one procedure was successfully and safely completed without serious citrate toxicity. Access was a major challenge. For plasmapheresis, the mean plasma volume removed was 1.2 × total plasma volume, but the mean total blood processed was 1.74 × total blood volume (TBV). For collections, the mean number of whole blood volumes processed was 4.1 × TBV. For T cell collections, the median CD3+ yield was 243.6 × 106/kg. For HPC collections, the median CD34+ cell yield was 14.8 × 106/kg. Mean durations for collections and plasmapheresis were 247.00 and 120.67 min, respectively. Of the CBC parameters, only platelet count was significantly lower after collections.

PMID 42875967
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PubMedPharmacological reports : PR2026-10-15

GLS2 reshapes glycolytic metabolism and bioenergetic homeostasis in glioblastoma cells.

De Los Santos-Jiménez Juan J, Campos-Sandoval José A JA, Sudderth Jessica J, Zacharias Lauren G LG et al.

Glioblastoma (GBM) exhibits extensive metabolic reprogramming, including glucose and glutamine (Gln) addiction, with Gln being converted into glutamate by glutaminase, encoded by the GLS and GLS2 genes. GLS2 acts as a context-dependent tumor suppressor, although the underlying mechanisms remain poorly understood. GLS2 is silenced in GBM, and we previously showed that its re-expression modulates pyruvate dehydrogenase (PDH) activity and tricarboxylic acid cycle (TCAC) metabolism, suggesting a distinct metabolic rewiring associated with its tumor-suppressive function. LN229 and T98G GBM cell lines were used as experimental models. Metabolomic profiling by liquid chromatography-mass spectrometry was performed to compare changes in central metabolic pathways following GLS2 or GLS overexpression. Glutaminase and PDH enzymatic activities were measured, and Western blotting was performed to assess GLS, GLS2, and PDHA1 protein levels and PDHA1 phosphorylation. A Seahorse analyzer was employed to quantify real-time ATP production derived from glycolysis and oxidative phosphorylation. Overexpression of GLS2, but not GLS, in LN229 cells caused the accumulation of TCAC-related metabolites, except for citrate, whose depletion is attributed to GLS2's effect on PDH phosphorylation, causing reduced PDH activity. This was accompanied by decreased levels of several acyl-carnitines. Furthermore, GLS2 induced the accumulation of glucose/fructose, while reducing levels of glucose-6-phosphate and pentose-phosphates, consistent with altered glycolysis. GLS2 also diminished the ATP/AMP ratio, confirmed by a reduced ATP synthesis rate, particularly glycolytic ATP, whereas mitochondrial ATP production remained unaltered. GLS2 exerts an isoenzyme-specific effect on Gln and glucose metabolism in GBM, likely modulating the glycolysis/pentose-phosphate pathway (PPP)-TCAC-axis.

PMID 42875721
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PubMedDrugs2026-10-15

Metformin Lowers Fasting Hyperglycemia by Increasing Glucose Clearance in People with Moderately Controlled Type 2 Diabetes.

Kahl Sabine S, LaMoia Traci E TE, Jonuscheit Marc M, Heilmann Geronimo G et al.

Metformin is the most frequently prescribed antidiabetic drug worldwide; however, the mechanism by which it lowers blood glucose remains incompletely understood. The objective of this study was to examine the effects of metformin on whole-body and specifically on hepatic glucose and energy metabolism in type 2 diabetes. This open repeated-measures pilot study examined this question using Positional Isotopomer NMR Tracer Analysis (PINTA) to assess rates of endogenous glucose production (VEGP), hepatic pyruvate carboxylase flux (VPC), and citrate synthase (VCS) flux in 16 men with moderately controlled type 2 diabetes (T2D; BMI 30 ± 3 kg/m2, HbA1c 8.4 ± 1.4%) undergoing two examination days with (M+; 1 g twice daily) and without metformin (M-) treatment. Hepatic ATP and glycogen concentrations were quantified by 31P/13C magnetic resonance spectroscopy. M+ reduced fasting glycemia by 18%, which could mostly be attributed to a 24% increase in rates of whole-body glucose clearance. Surprisingly, these changes were accompanied by a 58% increase in VPC and a 34% increase in VCS, due to a 26% increase in plasma glucagon concentrations. The increase in VPC was offset by reductions in the contributions of glycerol conversion to glucose resulting in no change in VEGP. Metformin decreased hepatic ATP content by 16% and increased plasma GDF-15 concentrations, but did not alter rates of net hepatic glycogenolysis. Metformin treatment in male individuals of European ancestry with moderately controlled T2D decreases blood glucose concentrations by increasing rates of whole-body glucose clearance. Metformin further inhibits glycerol-derived gluconeogenesis, which is consistent with complex IV, not complex I, being the molecular target of metformin action. ClinicalTrials.gov ( https://clinicaltrials.gov/ ): NCT04088851.

PMID 42875657
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PubMedRSC advances2026-10-14

Assessment and development of decontamination strategies for fentanyl and fentanyl analogues.

Bazley Mikaela M MM, Robertson Avril A B AAB, Blanchfield Joanne T JT

Over the past decade, fentanyl and fentanyl analogues have pervaded the illicit drug market and are encountered with growing frequency by law enforcement, HazMat and other first-responder groups. Several studies have addressed the removal of fentanyl from surfaces. However, significantly fewer have focussed efforts on the chemical breakdown of this class of pharmaceuticals. This work presents a new approach to assessing fentanyl decontamination efficacy involving upscaling the reaction between fentanyl (∼15 mg) and the decontaminant, and fractionation of the reaction mixture by medium pressure liquid chromatography (MPLC). This method allowed the identification of surfactant-formulated sodium dichloroisocyanurate as a decontaminant that achieves molecular destruction of fentanyl, rather than simply conversion to the N-oxide of the compound achieved by most recommended degradation methods. The upscaled decontamination assessment approach developed and described herein represents an important reform in decontamination methodology by providing a wider lens through which to assess decontamination efficacy.

PMID 42871932
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PubMedAmerican journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists2026-10-14

Implementing a Multidisciplinary Fentanyl Patch Verification Workflow Across a 12-Hospital Health System.

Zamora Francis F, Krichbaum Michelle M, Singh Devada Franco DF, Wolowich William W

To describe the development, implementation, and early experience of a multidisciplinary opioid stewardship workflow designed to improve the safety of transdermal fentanyl ordering across a 12-hospital health system. A systemwide gap analysis and baseline medication use evaluation (MUE) identified inconsistent documentation of opioid tolerance, variable Prescription Drug Monitoring Program (PDMP) review, and missed opportunities to assess fentanyl patch appropriateness before dispensing. A multidisciplinary team implemented a two-step electronic workflow across 12 hospitals that paired prescriber clinical decision support with mandatory pharmacist verification, centralized fentanyl patch dispensing, standardized education, and longitudinal MUE. In the baseline sample, 12 of 36 orders did not meet institutional criteria: 11 were for acute pain in opioid-naive patients and 1 had no documented pain indication. A later postimplementation review evaluated 135 orders; 125 (92.6%) met institutional ordering criteria and 10 (7.4%) did not. Eight documented pharmacist interventions were identified; 5 recommendations were accepted, resulting in discontinuation of the fentanyl patch and conversion to a short-acting opioid, while 3 recommendations were not accepted. Embedding prescriber decision support and mandatory pharmacist review within the medication-use process created a reproducible fentanyl patch safety workflow across a large integrated health system. The experience supports a stewardship model that combines governance, electronic decision support, pharmacist verification, and iterative process improvement.

PMID 42874078
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PubMedJournal of the Chinese Medical Association : JCMA2026-10-14

A safe and efficient analgesic approach for percutaneous transluminal angioplasty: Fentanyl plus targeted local anesthesia.

Huang Hsuan-Chiao HC, Hsu Chiann-Yi CY, Kang Ming-Yuan MY

Stenosis is a common complication of arteriovenous access (AV), for which percutaneous transluminal angioplasty (PTA) is a well-established intervention. Nevertheless, balloon dilation commonly induces pain. Common analgesic approaches during PTA encompass moderate intravenous sedation and analgesia, brachial plexus block, and local infiltrative anesthesia, each with its own limitations. A need currently exists for a safe, simple, and effective analgesic approach during PTA. This retrospective observational study was conducted between January 2020 and July 2022 at a single tertiary medical center. Patients with AV access dysfunction undergoing PTA were included. Patients were allocated into two groups based on the analgesia approach: one group received intraluminal fentanyl injection alone, and the other a combination of intraluminal fentanyl and local lidocaine infiltration at the stenotic site. Data regarding AV access type, lesion locations, 11-point Numerical Rating Scale (NRS) scores and procedural complications were collected. Comparative analysis between groups was conducted using appropriate statistical methods, and significance was set at p < 0.05. A total of 120 patients (mean age, 62.9±11.8 years; 65% male) were included in the study: 34 in the fentanyl-only group (Group A) and 86 in the fentanyl combined with lidocaine group (Group B). Group A had a higher proportion of male patients compared to Group B (79.4% vs. 59.3%, p = 0.037). No significant differences were found in balloon size, inflation pressure, fluoroscope time, or procedural complications between groups. The primary outcome, procedural pain, was significantly lower in Group B as compared to Group A (NRS score 2.3 ± 0.9 vs. 5.1 ± 2.2, p < 0.001), and this analgesic advantage remained after adjusting for gender and age. Our study findings suggest that administering a combination of intraluminal fentanyl and a direct lidocaine injection in patients undergoing percutaneous transluminal angioplasty is both an efficient and safe analgesic procedure for PTA.

PMID 42870325
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