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eprosartan mesylate + HCTZ (Teveten Combi / Teveten HCT / Teveten Plus)

✓ Approved

AbbVie, Inc. · AGTR1 · 小分子

什么是 eprosartan mesylate + HCTZ？

eprosartan mesylate + HCTZ 是一种小分子，由AbbVie, Inc.研发。该药已获批，用于治疗相关适应症，给药途径：Oral (PO)。

药物档案

商品名Teveten Combi, Teveten HCT, Teveten Plus
公司AbbVie, Inc.
药物类别小分子
分子靶点AGTR1, SLC12A3
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, AbbVie, Inc.

作用机制

分子靶点

eprosartan mesylate + HCTZ 作用于 2 个分子靶点：

AGTR1angiotensin II receptor type 1 (HAT1R, AT1)
SLC12A3solute carrier family 12 member 3 (NCCT, NCC)
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

eprosartan mesylate + HCTZ 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
Vascular disordersHypertension✓ Approved

相关研究文献

PubMedThe protein journal2026-10-25

Interactions of Veterinary Antibiotics with Purified Bovine Milk Alkaline Phosphatase: A Combined In Vitro Kinetic and Theoretical DFT/HF/M06-2X Study.

Bilen Çiğdem Ç, Tüzün Burak B, Gencer Nahit N

Alkaline phosphatase (AP, EC 3.1.3.1) is a key metalloenzyme and has been widely used as a reliable marker for milk pasteurization. Milk containing antibiotic residues tends to inhibit AP function, which can result in faulty pasteurization determination. AP from bovine milk was purified by a purification strategy involving butanol homogenization, rennet precipitation, and Sephadex G-100 gel filtration chromatography. The enzyme was purified 53.43-fold with a specific activity of 7516.40 EU/mg. Kinetic characterization showed a KM value of 2.27 mM (Vmax value: 555.56 EU/min); substrate was p-nitrophenyl phosphate. Electrophoretic studies verified the purity and molecular nature of the product enzyme. To functionally validate the identity of the purified enzyme, tetramisole hydrochloride was evaluated as a standard reference inhibitor, yielding a potent IC₅₀ value of 0.045 mM. Fifteen veterinary drugs and antibiotics were used to test the inhibitory effects of purified milk AP in vitro. Among the antibiotic compounds tested, Danofloxacin Mesylate induced the strongest antibiotic inhibition (IC50: 3.36 mM). Gentamycin Sulfate, Metamizole Sodium, Enrofloxacin, Kanamycin Sulfate, Sulfadimidine Sodium, and Neomycin Sulfate had IC50 values ranging between 22.89 and 312.13 mM of inhibition in AP, while Dexamethasone, Oxytetracycline Hydrochloride, Marbofloxacin, Tilmicosin, Doxycycline Monohydrate, Tylosin, Florfenicol and Flunixin Meglumine made no detected inhibition in the presence of 0.5 mM p-nitrophenyl phosphate. The molecular docking studies were additionally performed that the density functional theory (DFT), Hartree-Fock (HF), and M06-2X calculations were used to validate the experimental results with the 6-31++G(d,p) basis set. The theoretical results also reported that Oxytetracycline Hydrochloride, Tilmicosin, and Doxycycline Monohydrate displayed superior electronic reactivity, lower energy gaps between HOMO-LUMO, and more electrophilic character compared with the other compounds. These results are the first complete assessment of the impact of veterinary antibiotics in milk AP and underscore the possible role of antibiotic residues in establishing the reliability of pasteurization control measures.

PMID 42927595
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PubMedMacromolecular rapid communications2026-10-22

Protic Poly(Diallylammonium Sulfonate)s: Toward Water-Processable Fluorine-Free Ionic Materials.

Pairetti Yuliana Y, Rolandi Ana Clara AC, Casado Nerea N, Forsyth Maria M et al.

In this work, we report the synthesis of a new family of fluorine-free protic poly(ionic liquid)s via free-radical cyclopolymerization of protic diallylammonium monomers. Protic ionic liquid monomers based on diallylmethylammonium (DAMAH+) and diallylammonium (DAAH2 +), combined with different alkyl sulfonate counter-anions, were first prepared. Cyclopolymerization yielded a systematic series of six poly(diallylammonium) cations, five of which are newly reported here, combining two polymer backbones-poly(DAMAH+) and the newly incorporated poly(DAAH2 +)-with three fluorine-free sulfonate anions, namely mesylate (MsO-), ethylsulfonate (EsO-), and dodecylbenzenesulfonate (DBsO-); the previously reported poly(DAMAH+MsO-) analogue was included for direct comparison within the same series. Systematic characterization reveals how the interplay between polymer backbone and counter-anion governs solubility in water and organic solvents, glass transition temperatures (20-55°C), thermal stability (up to 300°C), and ionic conductivity (up to 10-3 S cm-1 at 100°C). The combination of their physicochemical properties, electrochemical stability, and water processability highlights these polymers as a versatile fluorine-free platform for electrochemical technologies. To demonstrate this potential, selected polymers were evaluated as water-processable binders for LiFePO4 cathodes, where they delivered competitive rate capability and stable electrode performance compared to PVDF. Their protic ionic character further suggests opportunities for future applications toward proton-conducting materials. Overall, this work introduces a sustainable platform for the development of fluorine-free ionic polymers with broad potential for electrochemical technologies.

PMID 42904760
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PubMedAnti-cancer agents in medicinal chemistry2026-10-19

Imatinib-Based Derivative: Synthesis, Computational Modeling, and Experimental Anticancer Activity.

Saidov Ravshan R, Gulyamov Shokhid S, Elmurodov Laziz L, Makhkamov Mukhriddin M et al.

Cancer remains one of the major causes of death worldwide. Tyrosine kinase inhibitors (TKIs) represent an important class of targeted anticancer agents because they block key oncogenic signaling pathways. Imatinib mesylate was among the first TKIs introduced in clinical oncology and has significantly improved the treatment of several malignancies. Nevertheless, its clinical use is associated with adverse effects, which highlights the need to develop modified derivatives with improved efficacy and reduced toxicity. In the present work, a new compound, imatinib aescinate, was prepared by dissolving imatinib and aescin separately in ethyl alcohol and combining the solutions under continuous stirring, followed by filtration and acetone-induced precipitation. For identification and structural characterization, the compound was analyzed using UV and FTIR spectroscopy, scanning electron microscopy with energy-dispersive spectroscopy (SEM-EDS), X-ray diffraction (XRD), thermogravimetric-differential thermal analysis (TGA/DTA), and HPLC. Antiproliferative activity was assessed in MCF-7 breast cancer cells using a CCK-8 cell viability assay (24 h), and wound closure was evaluated using a scratch assay. To understand potential molecular interactions, molecular dynamics simulations together with MM-PBSA binding energy calculations were also performed. The synthesized compound exhibited greater antiproliferative activity against MCF-7 cells than either imatinib mesylate or aescin alone. The IC50 values determined from a 24 h CCK-8 assay were: imatinib aescinate 15.16 μM, aescin alone 23.55 μM, and imatinib mesylate 76.66 μM. Imatinib aescinate also inhibited MCF-7 wound closure in a concentration-dependent manner in the scratch assay. Computational analysis indicated stable binding of imatinib aescinate to the BCR-ABL tyrosine kinase (PDB ID: 2HYY). Molecular dynamics simulations suggested reduced conformational flexibility of the protein-ligand complex, and MM-PBSA calculations supported favorable binding energy. Imatinib aescinate was approximately fivefold more potent than imatinib mesylate and 1.6-fold more potent than aescin, indicating enhanced antiproliferative activity. Its concentration-dependent inhibition of wound closure also suggests potential antimigratory effects, although reduced cell proliferation may contribute to this result. Computational findings supported stable and favorable binding to BCR-ABL; however, the underlying mechanism requires experimental confirmation. Further studies should evaluate kinase inhibition, toxicity, and in vivo efficacy. Overall, the results indicate that imatinib aescinate shows enhanced antiproliferative activity against MCF-7 cells compared with its individual components. Computational predictions suggest that the compound may interact with kinase targets; however, direct biochemical validation is required before definitive mechanistic conclusions can be drawn. These findings identify imatinib aescinate as a promising candidate for further preclinical investigation as a potential anticancer agent.

PMID 42895164
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PubMedArchives of toxicology2026-10-16

N-nitroso-hydrochlorothiazide: in vivo mutagenicity evaluation in a transgenic rodent model.

Ott Gregory R GR, Griffin Troy T, Bebb Kate K, Marinkovic Marina M et al.

N-nitrosamine drug substance related impurities (NDSRIs) are considered to be within the "cohort of concern" (CoC) due to their potential mutagenic carcinogenicity. However, increasing evidence indicates variability in mutagenic potency across this class. N-nitroso-hydrochlorothiazide (N-nitroso-HCTZ), an impurity associated with hydrochlorothiazide, has shown positive results in bacterial mutagenicity (Ames) assays, although mechanistic studies suggest these findings are likely driven by reactive degradation products rather than the parent compound. To further characterize mutagenic potential in vivo, a transgenic rodent (TGR) gene mutation assay was conducted in the Muta™Mouse test system. Male mice were administered N-nitroso-HCTZ by oral gavage at 0, 18.5, 55.7, 167, 500, or 750 mg/kg/day for 28 consecutive days. Mutant frequency (lacZ) was evaluated in liver and glandular stomach at 167, 500, and 750 mg/kg/day. Systemic exposure was confirmed in a toxicokinetic study following a single 750 mg/kg dose. N-nitroso-HCTZ was well tolerated, and no statistically significant increases in mutant frequency were observed in either tissue at any evaluated dose. All values were within historical control ranges, while the positive control demonstrated the anticipated response. Under the conditions of this study, N-nitroso-HCTZ did not induce gene mutations in vivo.

PMID 42881286
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PubMedMolecules (Basel, Switzerland)2026-10-16

Coffee Husk-Derived Activated Carbon for the Adsorptive Removal of Imatinib Mesylate from Water: Kinetic, Isotherm, Thermodynamic, and DFT Studies.

Párraga-García Vivian V, Chiquito Jeniffer J, Montero-Calderón Carolina C, Manangon-Perugachi Lucia E LE et al.

Coffee husk-derived activated carbon prepared by H3PO4 chemical activation was investigated for the removal of imatinib mesylate from aqueous solutions. Structural and chemical characterization using N2 physisorption, SEM, FTIR, Raman spectroscopy, and thermogravimetric analysis revealed a porous carbon matrix containing oxygenated functional groups and a defective turbostratic structure. The adsorption behavior was evaluated through batch experiments by examining the effects of pH, adsorbent dosage, particle size, contact time, and initial drug concentration. Under optimized conditions (300 µm particle size, 0.6 g adsorbent dosage, and pH 6), imatinib mesylate removal reached 97.9%, with equilibrium achieved within 60 min. The adsorption kinetics followed the pseudo-second-order model (R2 = 0.946-0.984), while equilibrium data were best described by the Sips isotherm model (R2 > 0.99), indicating adsorption on a heterogeneous surface. Density functional theory calculations confirmed the contribution of oxygen-containing groups, with carboxyl-functionalized carbon exhibiting the strongest interaction with imatinib mesylate (-105.3 kJ mol-1). These findings highlight the potential of coffee husk-derived activated carbon as a sustainable adsorbent for pharmaceutical contaminant removal.

PMID 42883159
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PubMedOpen medicine (Warsaw, Poland)2026-10-13

Developing and evaluating per-protocol adherence definitions in a large pragmatic clinical trial: insights from the Diuretic Comparison Project.

Anand Sonia T ST, Hau Cynthia C, Davenport Michael J MJ, Ishani Areef A et al.

Pragmatic clinical trials leveraging real-world data, such as the Diuretic Comparison Project (DCP), present unique challenges in measuring treatment adherence compared to traditional randomized controlled trials. In DCP, medications were managed through routine VA care and monitored via pharmacy claims, requiring tailored methods to assess adherence beyond standard measures like medication possession ratio (MPR). To develop a data-driven approach to define protocol treatment adherence for pragmatic comparative effectiveness trials. Structured EHR pharmacy dispense records guided categorization of treatment changes for two diuretics - chlorthalidone (CTD) and hydrochlorothiazide (HCTZ). We examined fill intervals, total drug supply, filling patterns among others to identify prescribing characteristics informing medication adherence definitions and time censoring for per-protocol analysis. Nonadherence was defined as having a gap (>90-days pause in assigned treatment), switch (receiving the other study medication), or discontinuation (without CTD/HCTZ for >90-days). 5,476 patients met nonadherence criteria - 2,851 (52 %) in CTD and 2,625 (48 %) in HCTZ. Switching occurred earlier in CTD patients, gaps were more common in HCTZ, but discontinuation was similar between groups. Defining adherence requires complex decision-making hybrid framework entailing both clinical and statistical expertise. Pragmatic studies should allow flexibility to generate data-driven, clinically-sensitive measures that appropriately describe trial compliance.

PMID 42866310
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