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fluorouracil (Carac, microsponge)

✓ Approved

Heron Therapeutics, Inc. · TYMS · 小分子

什么是 fluorouracil？

fluorouracil 是一种小分子，由Heron Therapeutics, Inc.研发。该药已获批，用于治疗相关适应症，给药途径：Transdermal。

药物档案

商品名Carac, microsponge
公司Heron Therapeutics, Inc.
药物类别小分子
分子靶点TYMS
给药途径Transdermal
状态Approved
来源： ClinicalTrials.gov, Heron Therapeutics, Inc.

作用机制

分子靶点

fluorouracil 作用于 1 个分子靶点：

TYMSthymidylate synthetase (DKCD, TMS)
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

fluorouracil 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
Skin and subcutaneous tissue disordersActinic keratosis✓ Approved

相关研究文献

PubMedInternational journal of cancer2026-09-10

Comparative Effectiveness of Induction Chemotherapy Regimens in Pediatric and Adolescent Locally Advanced Nasopharyngeal Carcinoma: A Retrospective IPTW Analysis.

Xie Rui-Ling RL, Zou Ye-Hao YH, Chen Zi-Xuan ZX, Zhang Ling-Ling LL et al.

Induction chemotherapy (IC) is a first-line treatment for locally advanced nasopharyngeal carcinoma (LA-NPC). However, data on the efficacy and safety of different IC regimens in pediatric patients remain scarce, as this group is often excluded from clinical trials. This retrospective study analyzed pediatric NPC patients (age ≤ 21 years) who received IC between 2006 and 2022. To balance confounding factors, inverse probability of treatment weighting (IPTW) was applied. Among 493 included patients, the median follow-up was 69 months. Before adjustment, the taxane-plus-platinum (TP) group showed significantly shorter distant metastasis-free survival (DMFS) than the non-TP group, who received TP plus 5-fluorouracil or capecitabine (TPF/C), platium plus 5-fluorouracil (PF) or gemcitabine plus platium (GP), (p = 0.032). Similar results were observed after IPTW adjustment. And overall survival and progression-free survival did not differ significantly between TP group and non-TP group. Conversely, the non-TP regimen was associated with a higher incidence of any grade toxicities (92.0% vs. 98.4%; p = 0.002). Subgroup analysis revealed that TP-based IC was associated with worse DMFS in patients aged ≤ 14 years, those with EBV-DNA ≤ 4000 copies/mL, and those with N3 stage disease. For pediatric LA-NPC, a non-TP IC regimen was associated with superior DMFS compared to a TP regimen, despite a higher rate of toxicities. The potential disadvantage of TP in younger/high-risk patients is hypothesis-generating and requires validation.

PMID 42720413
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PubMedFrontiers in medicine2026-09-10

Real-time LC-OCT monitoring of scalp hypertrophic actinic keratosis clearance following cryotherapy, laser, and 5-fluorouracil therapy.

Bortone Giulio G, Coppolelli Vincenzo V, Gargano Luca L, Svara Francesca F et al.

Assessment of treatment response in hypertrophic actinic keratoses (hAKs) remains largely dependent on clinical examination and dermoscopy, although apparent clearance may not reflect complete resolution of imaging features associated with residual disease. Line-field confocal optical coherence tomography (LC-OCT) enables non-invasive, longitudinal visualization of epidermal, dermal-epidermal junction, and superficial dermal changes at near-cellular resolution. To characterize LC-OCT response patterns in scalp hAKs treated with ablative CO2 laser, cryotherapy, or topical 0.5% 5-fluorouracil/10% salicylic acid, and to evaluate the potential role of LC-OCT in identifying persistent imaging features suggestive of incomplete treatment response requiring retreatment or treatment escalation. This retrospective study included 150 scalp hAKs classified at baseline as KIN 2-3 and PRO II-III, allocated to CO2 laser, cryotherapy, or topical 5-FU/SA groups. LC-OCT images acquired during routine follow-up were evaluated at baseline and post-treatment time points for stratum corneum thickness, epidermal thickness, keratinocyte atypia, PRO score, dermal-epidermal junction undulation index, intercellular edema, vascular pattern, and modality-specific structural changes. Treatment response was assessed according to LC-OCT-defined imaging criteria rather than histopathological confirmation. Cryotherapy produced early sub-epidermal blistering, followed by partial imaging response requiring repeated sessions in 40% of lesions. CO2 laser induced immediate epidermal ablation, rapid re-epithelialization, and complete response after retreatment in residual cases, with long-term LC-OCT evidence of dermal collagen remodeling. Topical 5-FU/SA showed heterogeneous responses; 65% of lesions, mainly KIN 3/PRO III, required escalation to a physical modality. LC-OCT enables non-invasive monitoring of treatment-related hAKs modifications and may identify persistent imaging abnormalities despite apparent clinical resolution, supporting individualized sequential treatment strategies.

PMID 42718796
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PubMedCureus2026-09-09

Beware the Ides of Chemotherapy: A Report on Hyperammonemic Encephalopathy Induced by FOLFOX-6 (5-Fluorouracil, Leucovorin, and Oxaliplatin).

Ts Sudarsh S, Balaji Sriram S, K Dharani D, S Krithika K et al.

Hyperammonemic encephalopathy is an uncommon but potentially life-threatening and reversible cause of acute altered sensorium, most often associated with hepatic dysfunction but increasingly recognized in patients receiving chemotherapy. We report the case of a 50-year-old woman who developed progressive disorientation and reduced responsiveness one hour after completing her first cycle of FOLFOX-6 (5-fluorouracil, leucovorin, and oxaliplatin) following hemicolectomy for splenic flexure carcinoma. Initial neuroimaging and infectious workup were unremarkable. Despite correction of transient renal dysfunction, neurological status did not improve. Serum ammonia was markedly elevated, and a diagnosis of non-hepatic hyperammonemic encephalopathy secondary to chemotherapy was made. Prompt discontinuation of FOLFOX and initiation of lactulose resulted in rapid and complete clinical recovery. This case highlights the importance of early recognition of chemotherapy-induced metabolic encephalopathy, particularly fluoropyrimidine-associated toxicity, and emphasizes serum ammonia estimation in unexplained post-chemotherapy neurological deterioration to ensure timely management and favorable outcomes.

PMID 42713158
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PubMedContemporary oncology (Poznan, Poland)2026-09-09

Omitting the 5-fluorouracil bolus in metastatic colorectal cancer: impact on survival and toxicity in a retrospective multicentre cohort.

Sohaib Ahmed A, Hebesh Eman H EH, Elabd Naglaa Said NS, Korani Omnia O et al.

The clinical value of the 5-fluorouracil (5-FU) bolus in modern multidrug regimens for metastatic colorectal cancer (mCRC) is uncertain, with concerns about added haematologic toxicity. This study assessed the impact of omitting the 5-FU bolus on survival and toxicity in patients receiving mFOLFOX6-based chemotherapy. In this retrospective multicentre cohort, 267 mCRC patients treated between June 2020 and June 2024 at Menoufia University Hospitals and the National Cancer Institute, Cairo University, received either bolus-free nbFOLFOX (n = 141) or standard mFOLFOX6 (n = 126), with or without bevacizumab or anti-epidermal growth factor receptor therapy. Progression-free survival (PFS) and overall survival were analysed using Kaplan-Meier and Cox models. Bolus omission produced a statistically significant but clinically small PFS improvement (mean 10.029 vs. 9.319 months; hazard ratio [HR] 1.532, 95% CI: 1.194-1.967; p = 0.001). Overall survival was similar between groups (mean 21.7 vs. 20.7 months; median 20.667 vs. 20.633 months; HR 1.242, 95% CI: 0.966-1.597; p = 0.089). Multivariate analysis identified bolus inclusion as an independent predictor of inferior PFS (HR 1.433, p = 0.006). High-grade neutropenia was significantly reduced with nbFOLFOX (14.9% vs. 25.4%, p = 0.019). Omitting the 5-FU bolus does not compromise survival and reduces haematologic toxicity, supporting individualised treatment decisions, particularly in settings of drug shortages or high toxicity risk.

PMID 42712824
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PubMedDrug and chemical toxicology2026-09-09

Insights into the protective role of trigonelline in 5-fluorouracil-induced lung injury: targeting oxidative stress, inflammation, and apoptosis.

Uslu Hamit H, Atila Uslu Gözde G, Çoban Taha Abdulkadir TA, Şahin Mahmut M et al.

5-Fluorouracil (5-FU) is an effective chemotherapeutic agent; however, its clinical use is frequently limited by toxicity in normal tissues, including the lungs. This study investigated the prophylactic protective effect of trigonelline (TRIG), a naturally occurring alkaloid, against 5-FU-induced pulmonary injury, with particular emphasis on oxidative stress, inflammation, and apoptosis. Twenty-eight male Sprague-Dawley rats were randomly assigned to four groups (n = 7): Control, TRIG, 5-FU, and TRIG + 5-FU. TRIG (50 mg/kg) was administered orally for seven consecutive days before a single intraperitoneal injection of 5-FU (100 mg/kg). Pulmonary injury was evaluated using biochemical, histopathological, and immunohistochemical analyses. Administration of 5-FU reduced body weight gain, increased relative lung weight, disrupted oxidant-antioxidant homeostasis, and induced histopathological alterations in lung tissue. These changes were accompanied by increased TNF-α, NFκB-p65, MAPK, and Bax expression together with decreased Bcl-2 expression, indicating activation of inflammatory and apoptotic pathways. Prophylactic TRIG administration restored oxidant-antioxidant balance, suppressed TNF-α, NFκB-p65, MAPK, and Bax expression, increased Bcl-2 expression, and markedly improved histopathological findings, demonstrating attenuation of oxidative stress, inflammation, and apoptosis. TRIG protects against 5-FU-induced pulmonary injury through coordinated antioxidant, anti-inflammatory, and anti-apoptotic mechanisms. These findings provide experimental evidence supporting the prophylactic use of TRIG as a potential adjunctive strategy for reducing chemotherapy-associated pulmonary toxicity. Further experimental and preclinical studies are warranted to validate its efficacy, elucidate its molecular targets, and evaluate its translational potential.

PMID 42712054
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PubMedLancet (London, England)2026-09-09

Perioperative durvalumab plus fluorouracil, leucovorin, oxaliplatin, and docetaxel for resectable gastric and gastro-oesophageal junction adenocarcinoma (MATTERHORN): final results of overall survival and event-free survival by pathological response in a global, randomised, double-blind, placebo-controlled, multicentre, phase 3 trial.

Janjigian Yelena Y YY, Al-Batran Salah-Eddin SE, Wainberg Zev A ZA, Muro Kei K et al.

Durvalumab plus perioperative fluorouracil, leucovorin, oxaliplatin, and docetaxel (FLOT) previously improved event-free survival and pathological complete response in resectable gastric and gastro-oesophageal junction adenocarcinoma. We aimed to examine its effect on overall survival. MATTERHORN is a global, randomised, double-blind, placebo-controlled, multicentre, phase 3 trial that took place in 147 medical centres in 20 countries (representing Asia, Europe, North America, and South America). Adults with histologically documented resectable gastric or gastro-oesophageal junction adenocarcinoma (eligible for radical surgery; stage II-IVa) not previously treated with anticancer therapy were eligible. Participants were randomly assigned (1:1) to perioperative durvalumab plus FLOT or placebo plus FLOT. Blocked randomisation (unique randomisation number via an interactive response technology system and randomisation and trial supply management system) was stratified by geographical region, clinical lymph node status, and PD-L1 expression. Participants were centrally assigned using the interactive response technology system and randomisation and trial supply management system. Participants received durvalumab 1500 mg or placebo intravenously every 4 weeks on day 1 of each cycle plus FLOT intravenously every 2 weeks on days 1 and 15 of each cycle for four cycles (two neoadjuvant and two adjuvant), followed by durvalumab 1500 mg or placebo intravenously every 4 weeks on day 1 of each cycle for ten additional cycles. Participants, investigators, and those assessing outcomes were masked. The previously reported primary outcome was event-free survival; overall survival in the intention-to-treat population was a key secondary endpoint and is the main endpoint reported here. Safety data were collected throughout treatment and the follow-up period (up to and including 90 days after the last dose of the trial drug) and were analysed in participants who received at least one dose of trial treatment; these data were reported previously and are summarised here. MATTERHORN is closed to recruitment but is ongoing and registered with ClinicalTrials.gov (NCT04592913). From Nov 17, 2020, to Sept 2, 2022, 1258 participants were enrolled and 948 were randomly assigned; 474 were randomly assigned to durvalumab and 474 to placebo. In a total of 948 participants, the median age was 62 years (IQR 54-68), 682 (72%) were male, and 266 (28%) were female. Overall survival significantly improved in the durvalumab versus placebo group (hazard ratio 0·78, 95% CI 0·63-0·96; p=0·021; significance threshold p<0·0499). Adverse events with the outcome of death possibly related to any trial treatment occurred in 6 (1%) of 475 participants in the durvalumab group and 2 (<1%) of 469 participants in the placebo group. Perioperative durvalumab plus FLOT improved overall survival versus placebo plus FLOT and is a new standard treatment option for patients with resectable gastric or gastro-oesophageal junction adenocarcinoma. AstraZeneca.

PMID 42716074
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