Drug Database
FL

fluorouracil (Carac, microsponge)

✓ Approved

Heron Therapeutics, Inc. · TYMS · Small Molecule

What is fluorouracil?

fluorouracil is a small molecule developed by Heron Therapeutics, Inc.. It is approved for therapeutic indications via transdermal.

Drug Profile

Brand NamesCarac, microsponge
CompanyHeron Therapeutics, Inc.
Drug ClassSmall Molecule
Molecular TargetTYMS
RouteTransdermal
StatusApproved
Sources: ClinicalTrials.gov, Heron Therapeutics, Inc.

Mechanism of Action

Molecular Targets

fluorouracil acts on 1 molecular target:

TYMSthymidylate synthetase (DKCD, TMS)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

fluorouracil is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Skin and subcutaneous tissue disordersActinic keratosis✓ Approved

Related Research Articles

PubMedThe Journal of biological chemistry2026-07-25

Human length telomeres restrict the regenerative potential of hematopoietic stem cells in mice.

Rowe Melissa M MM, Tober Joanna J, Ortiz Vivian V, Smoom Riham R et al.

Telomere biology disorders (TBDs), including dyskeratosis congenita (DC) and Hoyeraal-Hreidarsson syndrome (HHS), demonstrate that critically short telomeres cause bone marrow failure. Mutations in RTEL1, encoding a telomere-associated helicase, are among the genetic causes of DC and HHS. However, whether telomere length variation within the physiological human range affects hematopoietic function remains poorly understood. We investigated this question using the "Telomouse" model, which harbors a single amino acid substitution in Rtel1 (Rtel1M492K/M492K) that results in human-length telomeres rather than the considerably longer telomeres characteristic of wild-type Mus musculus. Although Telomice maintain normal steady-state hematopoiesis, proliferative stress induced by serial 5-fluorouracil treatment or bone marrow transplantation into lethally irradiated recipients revealed significant depletion of bone marrow progenitor cells compared to wild-type controls. Nanopore sequencing and fluorescence in situ hybridization demonstrated an elevated frequency of critically short telomeres in stressed Telomouse hematopoietic cells, accompanied by increased DNA damage (γH2AX foci) and apoptotic signaling (cleaved caspase-3). These findings establish that telomere length within the normal human range represents a critical determinant of hematopoietic reserve capacity under proliferative stress, with implications for understanding individual variation in bone marrow resilience and TBD pathophysiology.

PMID 42497987
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PubMedFood and chemical toxicology : an international journal published for the British Industrial Biological Research Association2026-07-25

Luteolin reverses chemoresistance in colorectal cancer cells via TET1/TDG-dependent epigenetic repression of β-catenin.

Kang Kyoung Ah KA, Piao Mei Jing MJ, Senavirathna Herath Mudiyanselage Maheshika Madhuwanthi HMMM, Madhuwantha Mahadurage Pasindu Laksara MPL et al.

Resistance to 5-fluorouracil (5-FU) and oxaliplatin (OXT) remains a major cause of treatment failure in colorectal cancer (CRC). Luteolin, a dietary flavonoid with anticancer properties, has shown therapeutic potential in various malignancies, but its effects on chemotherapy-resistant CRC remain poorly understood. In this study, we investigated whether luteolin restores chemosensitivity in 5-FU-resistant (SNUC5/5-FUR) and OXT-resistant (SNUC5/OXTR) CRC cells and explored the underlying molecular mechanisms. Luteolin reduced cell viability and induced apoptosis in both resistant cell lines. Mechanistically, luteolin suppressed β-catenin expression by downregulating ten-eleven translocation (TET) proteins, increasing DNA methyltransferase (DNMT) expression, enhancing CpG methylation, and reducing TET1 occupancy at the β-catenin promoter. Luteolin also decreased thymine DNA glycosylase (TDG) expression, disrupted the TET1/TDG interaction, and reduced TDG recruitment to the β-catenin promoter. Consistently, knockdown of either TET1 or TDG decreased β-catenin expression, while luteolin further enhanced apoptosis in siTET1- or siTDG-transfected resistant cells. Additionally, luteolin attenuated intracellular reactive oxygen species accumulation and potentiated the cytotoxic effects of 5-FU and OXT in resistant CRC cells. These findings demonstrate that luteolin reverses chemoresistance by suppressing the TET1/TDG-β-catenin axis through epigenetic regulation and modulation of intracellular redox homeostasis, supporting its potential as an adjuvant for CRC chemotherapy.

PMID 42497930
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PubMedOncology research2026-07-25

Stable Disease Achieved with Sequential Immunochemotherapy and Anti-Angiogenic TKI in Recurrent Metastatic Hidradenocarcinoma: A Case Report and Literature Review.

Wen Shidi S, Wang Lu L, Jiang Ying Y, Zhang Zhiyang Z et al.

Background: Hidradenocarcinoma is a rare and highly aggressive malignancy with limited therapeutic options. This report describes the clinical course and treatment response of a patient with recurrent metastatic hidradenocarcinoma treated with sequential immunochemotherapy combined with anti-angiogenic therapy, with the aim of providing further insight into potential treatment strategies for this rare malignancy. Case Description: A 60-year-old male initially presented in 2020 with scrotal erythema and was diagnosed with hidradenocarcinoma after surgery. Despite surgical treatment, he developed recurrent disease with diffuse metastases. First-line chemoimmunotherapy (sintilimab, cisplatin, 5-fluorouracil; six cycles) achieved a progression-free survival (PFS) of 6 months. Following disease progression, second-line therapy (toripalimab, nab-paclitaxel, anlotinib; eight cycles) was administered, resulting in sustained stable disease with a subsequent PFS of 8 months. Radiotherapy was used for brain metastases. The total follow-up duration exceeded 4 years until the patient was lost to follow-up in December 2024. Conclusions: This case suggests that sequential programmed death-1 (PD-1) blockade-based immunochemotherapy combined with anti-angiogenic therapy may provide clinically meaningful disease control in metastatic hidradenocarcinoma, even in the setting of low programmed death-ligand 1 (PD-L1) expression and microsatellite stability. Our findings support a potential role for immunotherapy in sweat gland carcinomas and highlight the importance of individualized multimodal treatment strategies for this rare malignancy. Further studies are needed to identify predictive biomarkers and establish optimal therapeutic approaches.

PMID 42500584
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PubMedBioorganic chemistry2026-07-25

Investigation of novel 4-substituted piperazine-pyrrolo[2,3-d]pyrimidine N-phenylacetamides as MELK-targeted anticancer agents for breast cancer therapy.

Makwana Shivangi S, Pandey Vivek V, Shah Umang U, Imran Mohd M et al.

The study reports design and synthesis of two series of pyrrolo[2,3-d]pyrimidine-N-phenylacetamide derivatives based on 1-(2,3-dichlorophenyl) piperazine (9a-f) and 1-((4-chlorophenyl) (phenyl)methyl) piperazine (10a-f). Compounds were characterized using 1H NMR, 19F NMR, 13C NMR, and HRMS spectral analyses. Post-chemical characterization, UALCAN analysis revealed elevated expression of MELK at both RNA and protein level in breast cancer, hence studies were conducted in MCF-7 cells. Of the two derivatives, piperazine-substituted compounds 9a-f (dichlorophenyl) showed better activity than 10a-f (chlorobenzhydryl) in the MTT assay. 9b and 9d exhibited modest IC50 of 13.84 ± 1.02 μM and 13.5 ± 1.29 μM, respectively, compared to routine drug 5-fluorouracil, which showed an IC50 of 17.77 ± 1.59 μM. However, a series 10a-f exhibited good to moderate to average cytotoxicity. Further analysis revealed both 9b and 9d exert an inhibitory effect by causing cell death, S-phase cell cycle arrest, and inhibiting migratory potential by upregulating E-Cadherin and downregulating the MMP-9. Molecular docking with the MELK protein revealed favorable binding to key active-site residues. Additionally, 100 ns molecular dynamics simulations confirmed conformational stability and dynamic behavior stable ligand-protein complex throughout the simulation, further western blotting analysis showed direct action of 9b and 9d on MELK expression with later being more prominent. In silico ADME study predicts that compound 9b demonstrates more favorable pharmacokinetic properties than 9d, including adherence to Lipinski's rule, improved oral absorption, enhanced Caco-2/MDCK permeability, and favorable BBB, skin permeability, and plasma protein binding, suggesting their potential as MELK- targeted leads for anticancer candidates.

PMID 42497764
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PubMedJGH open : an open access journal of gastroenterology and hepatology2026-07-25

Pediatric Colorectal Cancer in Africa: A Multicenter Study on Epidemiology, Management, and Outcomes Between 2000 and 2023.

van Heerden Jaques J, Balagadde-Kambugu Joyce J, Nyakato Veronica V, Mwa Pamela P et al.

Colorectal cancer (CRC) is increasing in Africa, yet reports in children and adolescents are limited. We describe the epidemiology, management, and survival outcomes of CRC in African children. Retrospective data of children under 19 years diagnosed with CRC between 2000 and 2023 were collected from 14 African countries. Patient and tumor characteristics and treatment data were described and survival outcomes analyzed. GLOBOCAN data were used to evaluate age-related geographical distribution of CRC. Hundred-and-eight patients, 57.4% males, were diagnosed with a mean age of 14.9 (range 5-18) years. The mean symptom-onset-to-diagnosis duration was 90 days (range 2-1200). Most common symptoms were abdominal discomfort (70.6%) and change in bowel habits (57.8%). The commonest primary site was the ascending colon (30.6%) with a mean tumor size of 64.3 mm (range 30-150 mm) and 37% presenting in stage III and 36.1% in stage IV. Most (83.3%) tumors were confirmed on histology, of which 78.7% were adenocarcinoma. Carcinoembryonic antigen was performed in 38.9% of patients. Complete resection was achieved in 55.6% of cases, while 18.5% received radiotherapy. Folinic acid, Fluorouracil, Oxaliplatin (FOLFOX) was the first line chemotherapy in 48.1% of patients. A third of patients were lost to follow-up while 25.6% experienced disease progression. The 2-year and 5-year overall survival rates were 40.0% and 16.9%, respectively. Disease stage (p = 0.07) and degree of resection (p = 0.02) predicted outcomes. Pediatric CRC is characterized by delayed diagnosis and advanced stage presentation, contributing to a significantly lower overall survival compared to adults. Focused research and multidisciplinary management are needed to understand pediatric CRC and improve outcomes.

PMID 42499621
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PubMedCureus2026-07-25

Synchronous HER2-Positive Breast and Gastric Cancers: A Dual Diagnostic Challenge With a Single Treatment Possibility.

Morka Jeremi J, Biernat Paula P, Czerwinska Anna A, Cybulska Klaudia K et al.

Synchronous primary malignancies are rare and represent a significant diagnostic and therapeutic challenge, particularly when both tumors share a targetable molecular alteration. We present a case of synchronous human epidermal growth factor receptor 2 (HER2)-positive breast and gastric cancers treated using a common HER2-directed strategy. A 77-year-old female was admitted with a right breast lesion classified as Breast Imaging Reporting and Data System (BI-RADS) 5. A core needle biopsy was performed, which confirmed a grade 2 invasive ductal carcinoma. The results showed positivity for estrogen receptor and progesterone receptor, a HER2 immunohistochemical score of 2+, and a Ki-67 index of 15%. Chromogenic in situ hybridization (CISH) confirmed HER2 amplification, establishing a luminal B/HER2-positive subtype (cT4b cN0 cM0). The patient was started on a course of tamoxifen treatment. During the course of treatment, there was a progression of dysphagia and rapid weight loss, which prompted further investigation. A CT scan revealed thickening of the gastric cardia. Following the failure of gastroscopies due to esophageal stenosis, exploratory laparoscopy was performed. The histopathological examination revealed that the gastric cardia tumor was grade 1 tubular adenocarcinoma, with HER2 overexpression (immunohistochemistry (IHC) 3+), proficient mismatch repair (pMMR)/microsatellite stability (MSS) status, and no hormone receptor expression. Due to the unresectable nature of the disease, the patient received a combination of palliative mFOLFOX6 (leucovorin calcium (folinic acid), fluorouracil, and oxaliplatin) and trastuzumab, in addition to ongoing endocrine therapy. Following four cycles, imaging showed disease stabilization, with decreased cancer antigen 19-9 (CA 19-9) and carcinoembryonic antigen (CEA) levels, and evidence of local tumor regression. Despite an initial positive response, the patient subsequently experienced disease progression and clinical deterioration after three months. The overall survival rate was 11.25 months. This case demonstrates the importance of comprehensive molecular diagnostics and the potential of HER2-targeted therapy as a unified treatment approach for synchronous HER2-positive malignancies.

PMID 42500763
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