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fluorouracil + salicylic acid (Actikerall / LAS41005 / ADP18998)

✓ Approved

Cipher Pharmaceuticals, Inc. · 小分子 · 小分子

什么是 fluorouracil + salicylic acid?

fluorouracil + salicylic acid 是一种小分子,由Cipher Pharmaceuticals, Inc.研发。该药已获批,用于治疗相关适应症,给药途径:Topical。

药物档案

商品名Actikerall, LAS41005, ADP18998
公司Cipher Pharmaceuticals, Inc.
药物类别小分子
给药途径Topical
状态Approved

治疗适应症

fluorouracil + salicylic acid 针对 2 个适应症,涉及 2 个治疗领域。

治疗领域疾病/病症分期
Skin and subcutaneous tissue disordersActinic keratosis✓ Approved
Surgical and medical proceduresSkin neoplasm excisionPreclinical

相关研究文献

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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PubMedThe New phytologist2026-09-10

A C-repeat binding factor-salicylic acid (CBF-SA) module links wound-induced evaporative cooling to tissue repair in plants.

Balem Joseph Michael JM, Tan Chenjiao C, Dias Nathália Cássia Ferreira NCF, Arnold Mariah M et al.

Repairing damaged tissues is essential for the survival of all organisms. In plants, tissue injury rapidly triggers defense and repair programs. However, the molecular mechanisms linking early injury cues to the later stage of wound repair remain unclear. Here, we show that wounding of Arabidopsis leaves induces localized low temperature at the injury site, likely caused by evaporative cooling, which is accompanied by an activation of cold-responsive genes. Using thermal imaging combined with computer vision and deep learning, we developed a workflow to monitor the dynamics of wound healing in a quantitative, non-invasive, and real-time manner. Mechanistically, we show that C-repeat Binding Factor (CBF) transcription factors are required for the activation of the injury-associated cold response and downstream salicylic acid (SA) signaling. Our findings suggest that the CBF-SA pathway acts coordinately to promote lignin and callose deposition, thereby facilitating wound repair. Together, these findings reveal a link between a wound-induced biophysical cue and the tissue repair program.

PMID 42717275
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PubMedThe Plant cell2026-09-10

Correction to: More than a defense: salicylic acid's secret role in fruit color.

PMID 42720107
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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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PubMedGeobiology2026-09-10

Origins of Improved Hardness in Bioinspired Aragonite Precipitated Under Simulated Biologic Conditions.

Chomhom Boontharee B, Farfan Gabriela A GA, Greeves Samantha S, Penkman Kirsty K et al.

Biogenic aragonite is a composite of mineral and biomolecules that exhibits superior material properties compared to its inorganic analog. This superiority underpins the success of the bioaragonite structures which support coral reefs and shell fisheries, yet the mechanisms improving the physical resilience of bioaragonite are not well understood. In this study, aragonite is synthesised under chemical conditions which simulate those of calcification sites in marine organisms. Aspartic acid, glutamic acid, and glycine in solution are incorporated into the aragonite at concentrations typically observed in marine biominerals and are observed to significantly improve aragonite Vickers hardness. Aspartic acid is incorporated more efficiently than glutamic acid or glycine, but for comparable amounts of amino acid incorporation, glycine improves aragonite hardness significantly more than either aspartic or glutamic acid. Glycine and glutamic acid incorporation reduce the aragonite grain size, thereby improving resilience to indentation via energy dissipation along grain boundaries. In contrast, aspartic acid also improves hardness on a smaller scale, possibly due to crystal structure distortions. These results suggest that amino acid incorporation influences biogenic aragonite hardness via multiple mechanisms and provide a prototype for exploring the influence of more complicated biomineral proteins.

PMID 42720183
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PubMedThe AAPS journal2026-09-10

Verification of a Physiologically-based Pharmacokinetic Model for Predicting CYP3A4-mediated Simvastatin and Simvastatin Acid Drug-drug Interactions.

Morse Bridget L BL, Han Bing B, Alberts Jeffrey J JJ, Posada Maria M MM et al.

Simvastatin is a commonly prescribed medication and a sensitive CYP3A4 substrate requiring dosage modification with CYP3A4 precipitants. Unlike other CYP3A4 substrates, grapefruit juice (GFJ) causes the largest increase in simvastatin exposure of any CYP3A4 inhibitor, leading to misunderstanding of simvastatin fraction escaping CYP3A4 metabolism in the gut (Fg, CYP3A4) and fraction metabolized by CYP3A4 in the liver (fm,CYP3A4). Simvastatin is a prodrug that is converted to the active simvastatin acid, though the mechanisms responsible for in vivo simvastatin acid formation are not well-understood. GFJ also decreases the simvastatin acid:simvastatin exposure ratio, suggesting inhibition of simvastatin acid formation. In the current work, we used a static approach to define simvastatin CYP3A4 parameters, using clinical data with index substrate midazolam; estimated simvastatin Fg,CYP3A4 and fm,CYP3A4 were ~ 0.4 and ~ 0.9, respectively. In vitro data assessing the stability of simvastatin and simvastatin acid demonstrated rapid conversion in gastric fluid that was highly pH-dependent. A simvastatin PBPK model was constructed incorporating these CYP3A4 parameters and simvastatin acid formation in stomach, intestine and plasma. The model reproduced the nonlinear pharmacokinetics of simvastatin and CYP3A4 precipitant effects, thus qualifying the model for prediction of CYP3A4-mediated interactions on both simvastatin and simvastatin acid. Simvastatin overall Fg was estimated as ~ 0.2, lower than the Fg,CYP3A4 due to additional intestinal esterase-mediated formation of simvastatin acid. The simvastatin-GFJ effect was explained by inhibition of this intestinal simvastatin acid formation, along with CYP3A4 inhibition. The unique effect of food on the simvastatin acid:simvastatin exposure ratio could also be replicated using this PBPK model.

PMID 42717157
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