Astellas Pharma · ADRA1A · Small Molecule
tamsulosin is a small molecule developed by Astellas Pharma. It is approved for therapeutic indications via oral (po).
| Brand Names | tamsulosin WOWTAB, Harnal D |
| Company | Astellas Pharma |
| Drug Class | Small Molecule |
| Molecular Target | ADRA1A |
| Route | Oral (PO) |
| Status | Approved |
tamsulosin acts on 1 molecular target:
| ADRA1A | adrenoceptor alpha 1A (ALPHA1AAR, ADRA1C) |
tamsulosin is developed for 1 unique indication across 1 therapeutic area.
| Therapeutic Area | Condition | Phase |
|---|---|---|
| Reproductive system and breast disorders | Benign prostatic hyperplasia | ✓ Approved |
Buranakarn Thanyaporn T, Tantilertanant Yanee Y, Tagami Junji J, Pimkhaokham Somsinee S
[This corrects the article DOI: 10.7759/cureus.115871.].
López Ferrándiz Lucia L, Pardo Rios Manuel M, Lopez Lopez Carmen Amalia CA, Tortosa Alcázar José J et al.
Mass-casualty incident (MCI) triage is difficult to teach and assess under realistic operational conditions. Immersive virtual reality (VR) may provide a standardized and operationally relevant platform for evaluating triage decision-making and prioritization of immediate life-saving interventions during disaster preparedness exercises. To evaluate performance in MCI triage and prioritization of immediate life-saving interventions using an immersive VR scenario embedded in a NATO civil-military emergency management exercise, while also describing participants' perceptions of usefulness, ease of use, immersion, and physical comfort. This cross-sectional observational study was conducted during the NATO Emergency Management Exercise "Bulgaria 2025" in Montana, Bulgaria. Civilian and military first responders who completed the immersive scenario and post-experience questionnaire were included. The VR assessment, delivered through Meta Quest 3 headsets and haptic vests, comprised 14 triage items and 2 immediate life-saving intervention items. The reference standard for triage categorization was based on the Simple Triage and Rapid Treatment (START) algorithm. The primary outcome was item-level accuracy. Secondary outcomes included perceived usefulness, ease of use, immersion, physical comfort, and perceived contribution of haptic feedback. A total of 102 valid post-simulation questionnaires were analyzed. Participants had a mean age of 34.3 years (SD 8.8), were predominantly male (98.0%), mainly military-affiliated (86.3%), and had a median of 10 years of professional experience. Triage performance was heterogeneous: accuracy exceeded 75% in several core items. Perceived usefulness and ease of use were high, with composite medians of 7.0 (IQR 6.0-7.0) and 7.0 (IQR 6.5-7.0), respectively. Presence/immersion was also high (median 6.25, IQR 5.5-7.0), and discomfort was low (median 1.0, IQR 1.0-2.0). In a NATO civil-military emergency management exercise, immersive VR was highly acceptable, usable, and well tolerated, while revealing substantial item-level variability in MCI triage decisions and immediate life-saving intervention choices. These findings suggest that immersive VR may offer a feasible and operationally relevant platform for standardized assessment of disaster triage performance and for identifying specific decision bottlenecks relevant to preparedness and interoperability.
Panaei Mohadese M, Mahani Mohamad M, Divsar Faten F, Khakbaz Faeze F
To develop and evaluate a glutathione (GSH)-responsive "Off-On" drug delivery system based on thiol-functionalized N-doped carbon dots (SNCDs) for controlled intracellular release of disulfiram (DSF). SNCDs were synthesized using a solvothermal technique and subsequently characterized using dynamic laser scattering, high-resolution electron imaging, UV-Vis spectrophotometry, and Fourier-transform infrared spectroscopy (FTIR). DSF was immobilized onto SNCDs through redox-cleavable disulfide linkages, and loading efficiency was determined by UV-Vis analysis. The in vitro drug release kinetics were examined under simulated physiological (pH 7.4) and tumor-relevant acidic (pH 5.4) conditions, evaluating the impact of glutathione (GSH) by performing experiments with and without its inclusion. Cytotoxicity and compatibility studies in MCF-7 breast tumor cells, evaluated via MTT test, were used to investigate SNCD biocompatibility and the anticancer performance of DSF-SNCDs. The FTIR spectra confirmed effective thiol functionalization and revealed oxygenated and nitrogenous groups on the particle surface suitable for disulfide linkage formation. DSF loading efficiency reached approximately 75%. Under non-reducing conditions, DSF-SNCDs exhibited minimal premature release (≤30% over 24 h at pH 7.4 and 5.4), demonstrating an "Off" state. In contrast, the presence of 5% (w/v) GSH at pH 5.4 triggered rapid DSF release, achieving approximately 80% cumulative release within 24 h, corresponding to the "On" state through reductive disulfide bond cleavage. Bare SNCDs showed high biocompatibility (>85% cell viability at 50 µg/mL), whereas DSF-SNCDs produced significantly enhanced cytotoxicity under GSH conditions, confirming redox-activated drug release. SNCDs provide an effective GSH-responsive nanoplatform for DSF delivery, combining high drug loading, excellent stability under non-reducing conditions, and efficient intracellular drug release under reductive environments. This strategy minimizes premature drug leakage while enhancing anticancer activity, demonstrating strong potential for cancer therapy.
Liao Rongqiang R, Ruan Yi Y, Zhang Ke K, Liu Maoxia M
Baicalin (BAI) is a natural flavonoid with antitumor potential, but its poor water solubility and low bioavailability limit clinical use. Mesoporous silica nanoparticles are promising drug carriers due to their large surface area and tunable pore structure, yet premature drug leakage remains a key challenge. A multifunctional nanoplatform, designated as BPCD@BAI@BMSN, was constructed to enable efficient baicalin loading, pH-responsive gated release, and biotin-mediated active tumor targeting. A novel biotin-ε-polylysine-cyclodextrin (BPCD) conjugate was synthesized via EDCI/NHS coupling and characterized by NMR and GPC. Hollow mesoporous silica nanoparticles (BMSN) were prepared by the Stöber method, surface-modified with benzothiazole. The BPCD conjugate was coated onto the nanoparticle surface via cyclodextrin-benzothiazole host-guest self-assembly. The resulting nanoparticles were characterized by TEM, DLS, zeta potential, FTIR, and TGA. Drug loading, pH-responsive release, cytotoxicity against SMMC-7721 cells, cellular uptake evaluated by confocal microscopy and flow cytometry, and in vivo antitumor efficacy in nude mice were systematically evaluated. BPCD@BAI@BMSN exhibited near-spherical morphology with a particle size of approximately 200 nm, a positive zeta potential of +10 mV, a drug loading of 19.85%, and an encapsulation efficiency of 89.6%. Cumulative baicalin release reached approximately 62% at pH 5.5, whereas only about 6% was released at pH 7.4, confirming acid-triggered gated release. The blank carrier showed no significant cytotoxicity with cell viability above 95%, while drug-loaded nanoparticles exhibited enhanced cytotoxicity at pH 6.8. Biotin-functionalized nanoparticles demonstrated significantly higher cellular uptake and tumor accumulation compared to non-targeted controls. In vivo, BPCD@BAI@BMSN achieved a tumor growth inhibition rate of 72.5% compared to the control group, with no obvious toxicity to major organs observed during the 21-day treatment period. BPCD@BAI@BMSN integrates high drug loading, pH-responsive supramolecular gating, and active tumor targeting into a single nanoplatform, offering a promising strategy for baicalin delivery with enhanced antitumor efficacy and favorable short-term biosafety.
Buranakarn Thanyaporn T, Tantilertanant Yanee Y, Tagami Junji J, Pimkhaokham Somsinee S
Coronal leakage and restoration failure remain significant contributors to the failure of endodontic treatments. This study aimed to evaluate the influence of different adhesive systems and treatment protocols, specifically immediate endodontic sealing (IES) and delayed endodontic sealing (DES), on bond strength. Sixty extracted human mandibular third molars were prepared to expose the pulp chamber dentin and randomly assigned to six groups according to the adhesive systems (OptiBond™ FL (Kerr Dental, California, United States) or Single Bond Universal adhesive (Solventum Corporation, Eagan, Minnesota, United States)) and the treatment protocols (control, IES, and DES). Sodium hypochlorite irrigation was performed based on experimental protocols. Following composite restoration, specimens were thermocycled for artificial aging and subsequently sectioned into beams for microtensile bond strength (µTBS) testing (10 teeth per group). Data were analyzed using two-way ANOVA and Kruskal-Wallis with Dunn's post hoc test (α = 0.05). A significant interaction between adhesive system and treatment protocol was identified (p < 0.05). With OptiBond FL, IES produced significantly higher µTBS values than DES (52.85 ± 7.22 MPa vs 40.98 ± 5.76 MPa; p < 0.05) and was comparable to the control group (57.59 ± 7.18 MPa; p > 0.05). The OptiBond FL group demonstrated significantly higher bond strength than the Single Bond Universal group under all conditions (p < 0.05), whereas the IES-Single Bond Universal adhesive (34.43 ± 5.97 MPa) and DES-Single Bond Universal adhesive (30.27 ± 5.49 MPa) groups showed significantly lower µTBS values than the control-Single Bond Universal adhesive (41.12 ± 4.85 MPa; p < 0.05). Failure mode analysis revealed predominantly adhesive failures in all groups. Within the limitations of the in vitro study, IES with OptiBond FL resulted in higher µTBS than DES.
Xiong Xiaoran X, Liu Yi Y, Zhu Yaohong Y, Wang Jiufeng J et al.
Bovine viral diarrhea virus (BVDV), one of the most important viral pathogens in cattle, causes serious economic losses due to immunosuppression and persistent infections. Previous studies have shown a tight connection between virus infection and lipid metabolism, particularly in the formation and degradation of lipid droplets (LDs). However, the pathogenic mechanism of BVDV infection and the molecular mechanisms by which viral proteins reprogram lipid metabolism remain unclear. We found that BVDV increased cellular LD accumulation by enhancing the production of new lipids, accelerating exogenous fatty acid uptake, and elevating diacylglycerol acyltransferase (DGAT)-dependent esterification of fatty acids (FAs). The generated LDs subsequently release free fatty acids (FFAs) via adipose triglyceride lipase/hormone-sensitive lipase (ATGL/HSL)-dependent lipolysis. This lipolysis-dependent release of FFAs is accelerated and transferred to mitochondria for oxidation by increasing contact between LDs and mitochondria, thereby promoting viral replication. Furthermore, BVDV core protein targets the surface of LDs, increasing and recruiting fatty acid synthase (FASN) and ATGL to promote LD mobilization. Meanwhile, the core protein interacts with mitochondria, linking mitochondria to LDs and facilitating the release of FAs for efficient fatty acid oxidation. Collectively, this study demonstrates that the BVDV core protein regulates cellular lipid metabolism to support BVDV replication, contributing to understanding the pathogenetic mechanisms by which BVDV interacts with host cells.
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