AbbVie, Inc. · AGTR1 · Small Molecule
eprosartan mesylate + HCTZ is a small molecule developed by AbbVie, Inc.. It is approved for therapeutic indications via oral (po).
| Brand Names | Teveten Combi, Teveten HCT, Teveten Plus |
| Company | AbbVie, Inc. |
| Drug Class | Small Molecule |
| Molecular Target | AGTR1, SLC12A3 |
| Route | Oral (PO) |
| Status | Approved |
eprosartan mesylate + HCTZ acts on 2 molecular targets:
| AGTR1 | angiotensin II receptor type 1 (HAT1R, AT1) |
| SLC12A3 | solute carrier family 12 member 3 (NCCT, NCC) |
eprosartan mesylate + HCTZ is developed for 1 unique indication across 1 therapeutic area.
| Therapeutic Area | Condition | Phase |
|---|---|---|
| Vascular disorders | Hypertension | ✓ Approved |
Anwar Imran I, Zafar Nadiah N, Mahmood Asif A, Zulcaif
[This corrects the article DOI: 10.15171/bi.30257.].
Surendra Shreya S, Sahu Shalini S, Raj Santhosh S, Daniel Nirmal N et al.
Dermatofibrosarcoma protuberans (DFSP) is a rare, slow-growing soft tissue sarcoma arising from dermal fibroblasts. Breast involvement is extremely rare, posing diagnostic and therapeutic challenges. We retrospectively reviewed eight cases of breast DFSP managed at our center over a 10-year period. The cohort included seven females and one male with a median age of 39.1 years. Clinical presentations were diverse: one patient had multiple areolar nodules, five presented with breast lumps including three with recurrent lumps, which is an uncommon presentation for DFSP, one had an ulceroproliferative growth with bleeding, and one presented following excision of a recurrent lump elsewhere with histopathology showing positive margins. Histological diagnosis was confirmed via core biopsy or block review. Four patients had classic DFSP, while three had fibrosarcomatous transformation. All cases of DFSP showed CD34 positivity. Wide local excision was performed in seven patients, and one underwent mastectomy. Two patients received adjuvant radiotherapy. No recurrence was observed within six months. Breast DFSP is rare and requires histopathological confirmation. Core biopsy with appropriate histologic features and CD34 immunostaining aids in diagnosis. Wide local excision remains the primary treatment approach. Radiotherapy is recommended in cases with close or positive margins, recurrence, metastatic disease, or when surgery is not feasible. Targeted therapy with Imatinib Mesylate, a tyrosine kinase inhibitor, is reserved for unresectable or metastatic lesions, provided the COL1A1::PDGFB translocation involving chromosomes 17 and 22 [t (17; 22)] is confirmed. Long term stringent follow up is required as recurrence in breast has been noted 26 years following primary treatment in literature.
Haas Simon Cornelius SC, Hou Bingchen B, Peters Andreas Sebastian AS, Hatzl Johannes J et al.
Oxidative stress plays a central role in the development and progression of abdominal aortic aneurysms (AAA), as it severely impairs the function and survival of vascular smooth muscle cells (VSMCs). MitoQ (mitoquinone mesylate), a mitochondria-specific antioxidant, was shown to reverse age-related arterial stiffening and improve vascular endothelial function, among other things, by interacting with the NRF2 signalling pathway. The aim of this study was to compare how long-term treatment with low doses of MitoQ affects the NRF2 stress response in VSMCs, derived from different origins (AAA-SMC, healthy aortic SMC, and immortalized VSMC (iHAoSMC)). We found a significant reduction in NRF2 and KEAP1 levels in the aortic wall of patients with AAA, accompanied by increased 8-OHdG levels, indicating defects in the response to oxidative stress. In contrast, relative NRF2 expression in tissue extracts and VSMC-enriched areas was higher in patients with AAA than in healthy aortic tissue. In vitro, baseline NRF2 protein levels were significantly higher in AAA-SMC and in iHAoSMC than in VSMC from healthy aorta, whereas NRF2 activity did not differ between AAA-derived and healthy VSMC. AAA-derived SMC were found to be less vulnerable against toxic concentrations of MitoQ than healthy VSMC, and the cell viability was differentially affected by H2O2. Acute oxidative stress by H2O2 increased NRF2 activity in AAA-SMC and iHAoSMC, but not in healthy VSMC. Pre-treatment of the cells for 7 days with low-dose (10 nM) MitoQ resulted in significantly increased NRF2 activity in AAA-SMC and iHAoSMC, but not in healthy VSMC, which was accompanied by a significant reduction of ROS production, particularly in AAA-derived SMC. Our data demonstrate that prolonged treatment with low doses of MitoQ has a protective effect, particularly on VSMCs from AAA, without affecting healthy aortic VSMCs. Moreover, immortalized cells can be used as a model for investigating oxidative stress responses in AAA-SMC, even though they do not react in exactly the same way. Overall, our findings confirm the cytoprotective potential of MitoQ to limit oxidative stress, particularly in AAA-SMC that is clinically observed in the abdominal aneurysm wall.
Yenduri Suvarna S, H Shashank S, K Naga Prashant NP
A very sensitive and eco-friendly second-derivative spectrofluorimetric method was developed for simultaneous analysis of hydrochlorothiazide (HCTZ), amlodipine besylate (AML), and telmisartan (TEL) in pharmaceutical products and human plasma. Native fluorescence of HCTZ (λex267/λem295 nm), AML (λex362/λem415 nm), and TEL (λex292/λem369 nm) was used together with fluorescence enhancement achieved through sodium lauryl sulfate micelles at optimum excitation/emission wavelengths for all other analytes being analyzed. Overlap of spectroscopic data was able to be resolved through second-derivative spectrofluorimetry without prior separation. Method validation was performed according to ICH Q2(R1) guidelines; results showed excellent linearity (R2 > 0.999) across a concentration range of 3-18, 2-10, and 10-50 ng/mL for HCTZ, AML, and TEL, respectively. Accuracy, precision and robustness were demonstrated with %RSD values below two. Application of the method to pharmaceutical product and spiked plasma samples gave satisfactory recoveries with minimal matrix interference. Assessment of method greenness was conducted using AGREE Prep, MoGAPI, AGSA, SAMI, Ma Tool, CACI, and WECA metrics, all of which indicate superior environmental sustainability. The proposed method is simple, fast, low-cost, ultra-sensitive, and suitable for routine quality control and/or bioanalytical analysis.
Susmitha Aggarapu A, Rajitha Galla G, Eri Gireesh Kumar GK, Orupalli Kavya K et al.
Impurity profiling is a critical quality and safety requirement for structurally complex anticancer agents. This review critically analyses impurity-profiling literature (1997-2025) for three tinibs, imatinib mesylate (IMM), dasatinib (DST), and nilotinib, and three taxanes, paclitaxel (PTX), docetaxel (DTX), and cabazitaxel (CTX), encompassing 54 analytical studies. Across the compiled dataset, reversed-phase HPLC accounted for 63.6% of methods, UPLC/ ultra-high-performance LC (UHPLC) for 16.4%, LC-MS/High-Resolution Mass Spectrometry (HRMS) for 9.1%, and GC-MS for 5.5%; high-performance thin-layer chromatography (HPTLC)-MS, headspace GC, and SFC appeared in isolated reports. HPLC/UPLC methods demonstrated LODs of 0.005-2 µg mL-1, whereas LC-MS/MS achieved LODs as low as 0.003-0.005 ng mL-1 for genotoxic impurities in tinibs. GC-based methods were especially valuable for volatile impurities and residual sulfonates, with detection in the low-ppb to sub-µg mL-1 range. Tinib impurity profiles are dominated by process-related, oxidative, nitrosamine, and genotoxic species, while taxane profiles are characterized by epimerization products, deacetylated derivatives, side-chain cleavage products, and precursor-related impurities. Regulatory implications under ICH Q3A(R2), Q3B(R2), M7(R2), S9, and Q3C are discussed, including dose-normalised threshold of toxicological concern (TTC) calculations. An impurity-type versus analytical-technique matrix is proposed to guide method selection. Critical analytical gaps are identified, and future directions encompassing green analytical chemistry (GAC), process analytical technology (PAT), and AI-assisted impurity prediction are outlined.
Jijin Robert K RK, Sreelekha Mariswamy K MK, Arsha N N, Babu Beneesh P BP
Herein, we report the azide-alkyne cycloaddition reactions of highly reactive propiolaldehyde without any metal catalyst, base, or any other additives. The propiolaldehyde, generated in situ from propargyl mesylate in DMSO, readily annulated onto organic azides in the absence of metal catalyst, affording 1,2,3-triazole-4-carboxaldehydes with excellent regioselectivity. Furthermore, these triazole aldehydes were engaged in a number of one-pot cascade reactions yielding heterobiaryls and heteroterphenyl hybrids. The synthetic utility of the methodology was demonstrated through the gram-scale synthesis of the antiepileptic drug Rufinamide.
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