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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

PubMedFrontiers in oncology2026-08-06

A single-arm phase II trial of UGT1A1 genotype-guided high-dose irinotecan rechallenge in refractory metastatic colorectal cancer.

Kim Hana H, Hong Joohyun J, Kong Sun-Young SY, Choi Moon Ki MK

There is an unmet need for optimal third- or later-line treatment options for refractory or metastatic colorectal cancer (mCRC) patients. This phase II study investigated whether high-dose irinotecan rechallenge based on UGT1A1 genotype improves the 12-week disease control rate (12w DCR), objective response rate (ORR), progression-free survival (PFS), overall survival (OS), and safety in refractory mCRC patients. Patients who had previously received more than two lines of chemotherapy, including 5-fluorouracil, oxaliplatin, irinotecan and had shown either a partial response or durable response for more than 24 weeks to irinotecan were included. Patients without the defective allele of UGT1A1 (UGT1A1 *1/*1) and one defective allele (UGT1A1 *1/*6, *1/*28) were treated with intravenous irinotecan at doses of 300 mg/m2 and 250 mg/m2, respectively, every 2 weeks until disease progression or unacceptable toxicity. A total of 32 patients was enrolled between October 2020 and March 2023. The primary endpoint, 12w DCR was 40.6% (13 of 32 patients). The ORR was 15.6% (5 of 32). The median OS was 9.3 months (95% CI, 5.3 to 13.3) and the median PFS was 2.9 months (95% CI, 2.5 to 3.3). Grade 3 or higher adverse events were observed in 19 patients (59.4%). Dose reduction due to adverse events occurred in 9 patients (50.0%) in UGT1A1 wild-type group and 4 patients (28.6%) in the heterozygous group. High-dose irinotecan rechallenge guided by UGT1A1 genotype was feasible and showed meaningful disease control in third-line or later settings for mCRC patients previously responsive to irinotecan.

PMID 42558275
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PubMedJournal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners2026-08-05

Preparation efficiency and operational risk of two dosage forms of fluorouracil in PIVAS workflow: A retrospective comparative study.

Chen Huo-Shu HS, Su Ling L, Liu Feng-Ting FT, Xu Xiao-Li XL et al.

ObjectiveTo compare the efficiency and operational risks of preparing two forms of fluorouracil (solution and powder) for injection in the Pharmacy Intravenous Admixture Service (PIVAS).MethodsA retrospective analysis was conducted to assess a total of 100 preparation records of two forms (solution and powder; 50 records each) of fluorouracil at a tertiary hospital from May 2024 to December 2025. The configuration efficiency was assessed by the time spent and the number of configuration steps; the operational risks were evaluated by operational abnormalities and adverse events recorded in the PIVAS management system.ResultsThe average preparation time for solution-form fluorouracil was significantly shorter than that of the powder-form counterpart [(673.58 ± 279.74) seconds vs. (1049.34 ± 540.48) seconds, P < 0.05], with a reduction of over 42.86% in preparation steps (≤4 steps vs. ≥ 7 steps). Two adverse events occurred with powder-form fluorouracil during the analysis period: one involved the formation of insoluble particles after drug reconstitution, and the other was due to operational error leading to liquid leakage. No adverse events were reported in relation to solution-form fluorouracil.ConclusionIn scenarios of limited resources or high workloads in the PIVAS, it is advisable to prioritize the use of solution-form fluorouracil under certain conditions to enhance efficiency and reduce operational risks. The findings may provide some clinical evidence for optimizing clinical dosage form and risk management.

PMID 42555094
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PubMedCancer management and research2026-08-05

Astragalin Suppresses Colorectal Carcinogenesis by Targeting Proliferation, Oxidative Stress, and Inflammation.

Shareef Suhayla Hamad SH, Nanakaly Haween Toufiq HT, Ahmed Salam Adil SA, Gheni Noor Ali NA et al.

Colorectal cancer (CRC) is a leading cause of cancer-related death worldwide. This study evaluated astragalin's (AST) anti-proliferative and chemopreventive effects on CRC. AST's effects were assessed in vitro on Caco-2 and HT-29 cells and in vivo on azoxymethane (AOM)-induced aberrant crypt foci (ACF) in rats. Rats received AST (50 or 100 mg/kg, 60 days) or 5-fluorouracil (5-FU) (35 mg/kg, 5 days). AST inhibited Caco-2 and HT-29 cell growth (IC50: 20.15-34.50 µg/mL). In AOM-induced rats, AST reduced ACF formation, improved colon histology, downregulated β-catenin, and upregulated Bax. AST also enhanced superoxide dismutase (SOD) and catalase (CAT) activities, reduced malondialdehyde (MDA) levels, and modulated tumor necrosis factor alpha (TNF-α), interlukin-6 (IL-6), and IL-10 levels. AST demonstrated chemopreventive activity against CRC by exerting antiproliferative, antioxidant, and anti-inflammatory effects, supporting its potential as a therapeutic agent.

PMID 42553650
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PubMedMolecular and biochemical parasitology2026-08-04

Modulatory Role of Blastocystis-Derived Solubilized Antigens in Colorectal Carcinogenesis: A Systematic Review.

Noor Razali Nur Amani Syakirin NAS, Mohd Akmal Nur Anurah Hani NAH, Wardina Mohd Khir Nur Eisya NE, Kean Aaron Khoo Hooi AKH et al.

Colorectal cancer develops through complex interactions between genetic alterations, immune responses, and the intestinal microenvironment. Increasing evidence suggests that intestinal parasites may also contribute to colorectal carcinogenesis (CRC). Blastocystis sp. (Blastocystis) is one of the most common intestinal protozoans worldwide. Although its role in disease remains controversial, it has been associated with chronic inflammation and disruption of normal gut homeostasis. Therefore, this systematic review aimed to summarize the current experimental evidence on the immunomodulatory effects and potential role of Blastocystis solubilized antigens (BSA) in CRC. A systematic literature search was conducted following PRISMA guidelines in PubMed, Scopus, Web of Science, and CINAHL. Six eligible experimental studies investigating the effects of BSA on colorectal cancer cell lines (HCT116 and HT-29) and peripheral blood mononuclear cells (PBMCs) were included. The included studies demonstrated that BSA influences several biological processes associated with CRC. Symptomatic isolates, particularly Subtype 3 (ST3), showed the strongest biological effects by promoting colorectal cancer cell proliferation, increasing the expression of pro-inflammatory and tumour-associated mediators, and reducing p53-mediated apoptosis. BSA also increased the gene expression of NF-κB and Nrf2 and reduced the effectiveness of the chemotherapeutic agent 5-fluorouracil (5-FU). In addition, BSA altered cytokine production in PBMCs, with chemotherapy-treated colorectal cancer patients exhibiting reduced immune responsiveness compared to healthy individuals. Overall, the available evidence suggests that Blastocystis, particularly ST3, may contribute to CRC through immune modulation, promotion of tumour-related cellular pathways, and reduced chemotherapy sensitivity. However, the limited number of available studies highlights the need for further experimental and clinical investigations to clarify the role of Blastocystis in CRC and treatment outcomes.

PMID 42546905
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PubMedFrontiers in oncology2026-08-04

Treatment patterns and outcomes of patients with a diagnosis of metastatic pancreatic adenocarcinoma in the United States, 2019-2024.

Fuldeore Rupali R, Tan Chia Jie CJ, Kimura Tomomi T, Farrokhi Pegah P et al.

Approximately half of patients with pancreatic cancer present with metastatic disease at diagnosis, for whom 5-year survival remains ~3%. This retrospective study assessed treatment patterns, characteristics associated with first-line (1L) regimen selection, and real-world survival and treatment outcomes in US patients with metastatic pancreatic adenocarcinoma (mPAC). US adults newly diagnosed with mPAC between 1 January 2019 and 1 August 2024 from the electronic health record-derived Flatiron Health Research Database were included. Treatment patterns across the first three lines of therapy were summarized among patients who initiated systemic therapy within 180 days of metastatic diagnosis. Associations between baseline characteristics and 1L regimen selection (across multiple regimen categories) were evaluated using multinomial logistic regression. Overall survival (OS) and time-to-treatment discontinuation (TTD) were assessed using standard survival methods. Among 9,439 patients with mPAC, 6,279 initiated 1L systemic therapy. The most common 1L regimens were gemcitabine plus nab-paclitaxel (Gem-Nab; 41.5%) and folinic acid (leucovorin), fluorouracil (FU), irinotecan, and oxaliplatin (FOLFIRINOX) (36.3%). Mean time to 1L initiation after metastatic diagnosis was 26.9 days. Patients receiving 1L FOLFIRINOX were generally younger, more frequently had baseline Eastern Cooperative Oncology Group performance status 0 or 1, more often presented with de novo metastatic disease, had higher socioeconomic indicators, and were more likely to be treated in academic centers compared with patients receiving Gem-Nab. Overall, 33.5% of patients did not receive systemic therapy within 180 days of metastatic diagnosis. Median OS was longer among patients treated with FOLFIRINOX than among those treated with Gem-Nab [10.7 vs 7.6 months; adjusted hazard ratio (HR), 0.47; 95% confidence interval (CI), 0.43-0.51; P < 0.001]. Median TTD was also longer for FOLFIRINOX compared with Gem-Nab (4.7 vs 3.4 months). Among treated patients, clinical and sociodemographic factors strongly influenced regimen selection, and FOLFIRINOX use was associated with longer survival and treatment persistence than Gem-Nab; although these findings should be interpreted as associative given the substantial differences in patient characteristics between treatment groups. Conversely, one-third of patients did not initiate systemic therapy within 180 days of metastatic diagnosis, which may reflect unmet need or gaps in access to care.

PMID 42548575
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PubMedRadiology2026-08-04

Comparison of Second-line Hepatic Arterial Infusion Chemotherapy and Tyrosine Kinase Inhibitors in Advanced Hepatocellular Carcinoma.

Yoo Jae-Sung JS, Tak Kwon Yong KY, Cho Hee Sun HS, Han Ji Won JW et al.

Background With the advent of immune checkpoint inhibitor-based combination therapy, treatment sequencing for advanced hepatocellular carcinoma (HCC) has become increasingly complex. The Barcelona Clinic Liver Cancer (BCLC) 2026 recommendations emphasize individualized decision-making. Purpose To compare clinical outcomes of hepatic arterial infusion chemotherapy (HAIC) and tyrosine kinase inhibitors (TKIs) in patients with advanced HCC after atezolizumab-bevacizumab (AB) failure, within the BCLC 2026 treatment paradigm. Materials and Methods This multicenter retrospective study included patients who received AB and subsequently received either HAIC or a TKI between March 2022 and August 2025. HAIC used a cisplatin-fluorouracil regimen, and TKIs were given at standard doses. Tumor response and progression-free survival (PFS) were assessed using contrast-enhanced multiphase CT or liver MRI according to routine clinical practice. Imaging was reviewed by radiologists blinded to treatment allocation. Inverse probability of treatment weighting (IPTW) was applied for age, sex, Eastern Cooperative Oncology Group performance status, Child-Pugh class, portal vein tumor thrombosis, and tumor burden based on the up-to-seven criteria. Results This study included 90 patients (mean age, 62 years ± 10.9 [SD]; 73 men; HAIC group, n = 51; TKI group, n = 39). Baseline tumor burden was higher in the HAIC group than in the TKI group (percentage of patients with tumors beyond the up-to-seven criteria: 88% [45 of 51] vs 64% [25 of 39]; P = .01). In unweighted analyses, median overall survival (OS) was similar between the HAIC and TKI groups (10.4 vs 6.4 months; P = .62), whereas PFS favored HAIC over TKIs (median, 5.3 vs 3.6 months; P = .008). Objective response rate and disease control rate were higher with HAIC than with TKIs (objective response rate: 35% [18 of 51] vs 5% [two of 39], P = .002; disease control rate: 67% [34 of 51] vs 26% [10 of 39], P < .001). After IPTW, HAIC remained associated with longer PFS than TKIs (median, 7.1 vs 3.4 months; P < .001), and OS remained similar between groups (median, 10.5 vs 6.3 months; P = .32). Conclusion In patients with advanced HCC, after AB failure, second-line HAIC yielded higher response rates and longer PFS than TKIs. © RSNA, 2026 Supplemental material is available for this article. See also the editorial by Deyirmendjian and Tang in this issue.

PMID 42550027
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