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tolterodine (Detrol LA / Detrusitol Neo / Detrusitol Retard)

✓ Approved

Pfizer, Inc. · CHRM1 · 小分子

什么是 tolterodine？

tolterodine 是一种小分子，由Pfizer, 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Detrol LA, Detrusitol Neo, Detrusitol Retard
公司Pfizer, Inc.
药物类别小分子
分子靶点CHRM1, CHRM2, CHRM3, CHRM4
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Pfizer, Inc.

作用机制

分子靶点

tolterodine 作用于 4 个分子靶点：

CHRM1cholinergic receptor muscarinic 1 (M1, HM1)
CHRM2cholinergic receptor muscarinic 2 (HM2)
CHRM3cholinergic receptor muscarinic 3 (HM3, PBS)
CHRM4cholinergic receptor muscarinic 4 (HM4, M4R)
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

tolterodine 针对 2 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Renal and urinary disordersHypertonic bladder✓ Approved
Renal and urinary disordersUrinary incontinence✓ Approved

相关研究文献

PubMedSeminars in thrombosis and hemostasis2026-08-08

Interim Efficacy Analysis of Different Anticoagulation Regimens in Patients with Long-term Implantation of Inferior Vena Cava Filter.

Qi Lei L, Sun Hongzhi H, Wang Yihao Y, Li Huagang H et al.

To analyze the interim efficacy of different anticoagulation regimens for patients with long-term inferior vena cava filter (IVCF) implantation. From August 2021 to August 2024, a retrospective analysis of patients who underwent long-term IVCF implantation in multiple centers was performed. Group A (46 cases) did not receive anticoagulation, Group B (66 cases) received extended secondary prophylaxis dose anticoagulation, and Group C (63 cases) received extended therapeutic dose anticoagulation, with 12 months follow-up. The primary endpoint was lower extremity deep vein thrombosis (LEDVT) recurrence rate. The secondary endpoints were IVCF thrombosis (IVCFT) incidence, bleeding-related adverse events incidence, all-cause mortality, and venous clinical severity score (VCSS). LEDVT recurrence rate and IVCFT incidence in Group A (37.0%, 19.6%) were higher than that in Group B (13.6%, 6.1%) and Group C (15.9%, 4.8%). Bleeding-related adverse events incidence in Group C (17.5%) was higher than that in Group B (4.5%) and Group A (2.2%). There was no significant difference in all-cause mortality among three groups. VCSS at 12 months in Group A was higher than that in Group B and Group C. In the interim follow-up of the extended treatment phase in patients with long-term IVCF implantation, rivaroxaban anticoagulation may reduce LEDVT recurrence and IVCFT occurrence compared to non-anticoagulation, and alleviate patients' clinical symptoms. The extended secondary prophylaxis dose may exhibit comparable efficacy to the extended therapeutic dose, while potentially reducing the bleeding risk.

PMID 42567525
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PubMedPharmaceutical research2026-08-08

Stimulus-Responsive Polymeric Carriers for Gene Delivery: Balancing Endosomal Escape with Nucleic Acid Release.

Hulugalla Kenneth K, Fortenberry Alexander W AW, de Silva Dilusha J DJ, Werfel Thomas T

Polymeric carriers for nucleic acid delivery must overcome two sequential intracellular barriers: escape from the endosome and release of the cargo into the cytosol. These steps are typically treated as independent design problems and optimized separately. This review argues that escape and release are coupled through the same electrostatic and pH-dependent interactions, creating a fundamental tradeoff . The cationic charge that enables a polymer to destabilize endosomal membranes also tightens its grip on the nucleic acid payload, so conditions favoring escape simultaneously inhibit release. We trace this tradeoff across the major strategy classes in the polymeric delivery literature, evaluating each by where and when its trigger acts relative to the escape event. We further assess the assay toolkit for measuring escape and release, and the translational variables that shift the balance in vivo. pH-responsive polymers tune the activation zone for membrane destabilization but cannot decouple escape from binding, since both depend on the same protonation events. Charge-shifting polymers address release more directly by programming a loss of cationic character after endosomal entry. Non-pH triggers, including disulfide, thioketal, diselenide, and esterase-responsive chemistries, off er orthogonal release mechanisms but face spatial and temporal alignment constraints. Characteristic failure modes recur: premature release, redundant triggering, and kinetic misalignment. No existing assay measures endosomal disruption and cargo release state simultaneously, and translational variables including protein corona formation, cell-type-dependent endosomal acidifi cation, and PEG shielding shift the balance in ways in vitro screening does not capture. The tradeoff cannot be resolved by chemistry alone, meaning the responsive trigger considered in isolation. Its resolution requires coordination across spatial (architectural domain segregation), temporal (kinetic alignment of escape and release), and formulation-level (N/P ratio, PEG density, formation pH) design axes.

PMID 42568022
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PubMedAdvanced healthcare materials2026-08-08

An Intelligent Spatially Selective Modified Starch Hydrogel Dressing Breaks the Stability-Efficiency Trade-Off in Bioactive Delivery.

Liu Xiaolu X, Hu Zhenyu Z, Fei Xu X, Li Yao Y et al.

Intelligent controllable-release hydrogel systems hold significant promise for wound management, owing to their capacity for on-demand and precise drug delivery. Nevertheless, existing delivery systems encounter substantial challenges in encapsulation stability and release efficiency, especially for lipophilic active substances. These limitations considerably impair their therapeutic efficacy and, consequently, their ability to promote wound healing. In this study, we designed a novel delivery system by integrating spatially selective catalytically modified starch molecules with a smart stimuli-responsive polymeric hydrogel. The spatial confinement effect of lipase nanoflowers enabled regulated hydrophobic modification of starch. This modified starch-stabilized curcumin Pickering emulsion effectively prolonged curcumin stability, retaining 65% antioxidant activity over 90 days. Furthermore, the Pickering emulsion was incorporated into a thermosensitive hydrogel to construct a drug-controlled release system (C-PNMs). The system exhibited rapid and efficient drug release in response to wound temperature, achieving a release rate of 93.4%, which represented an approximately 50% improvement over other reported systems. The superior bioactivity preservation and intelligent on-demand drug release performance of this system offer a promising strategy for the management of compromised skin.

PMID 42568128
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PubMedEuropean journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V2026-08-08

Electrospun PLA: Gelatin core-shell nanofibers for dual delivery of docetaxel and heparin with enhanced in vitro antiproliferative activity.

Suner Salih Can SC, Oral Ayhan A, Al Ayça Mehmetoğlu AM, Kahraman Erkan E et al.

Despite advances in chemotherapy, the clinical efficacy of docetaxel (Doc) in breast cancer treatment is limited by systemic toxicity and poor delivery efficiency. In this study, electrospun poly(lactic acid) (PLA):gelatin (Gel) core-shell nanofibers were developed as a dual drug delivery system for the co-delivery of Doc and heparin (HP). The core-shell architecture enabled the spatial compartmentalization of hydrophobic Doc within the PLA core and hydrophilic HP within the gelatin shell, allowing independent and controlled release profiles. Nanofibers containing 2, 3, and 5 wt% Doc in the core and corresponding amounts of HP in the shell were successfully fabricated. In vitro release studies performed at pH 3.0, 5.5, and 7.4 (37 °C) demonstrated a compartment-dependent release behavior, where HP exhibited rapid release (̴ 10 h), while Doc showed sustained release (̴ 80 h). These results indicate that the core-shell structure effectively regulates drug diffusion and enables distinct release kinetics for each therapeutic agent. Increased drug loading resulted in higher cumulative release for both agents. Cytotoxicity studies on MCF-7 breast cancer cells revealed that dual drug-loaded nanofibers (5 wt%, 2 mg) significantly reduced cell viability after 72 h, indicating enhanced in vitro antiproliferative activity. While Doc alone exhibited limited cytotoxic effect and HP showed negligible direct cytotoxicity, their combined delivery within the core-shell nanofiber system resulted in a markedly enhanced antiproliferative response. This enhanced effect indicates improved antiproliferative activity associated with dual-drug delivery through the core-shell nanofiber system. Overall, the developed PLA:Gel core-shell nanofibers represent a promising biomaterial-based platform for dual drug delivery of hydrophobic and hydrophilic agents, offering controlled release and promising in vitro antiproliferative activity.

PMID 42567422
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PubMedACS omega2026-08-08

Research on the Prevention and Control of Blast Impact Pressure in Deep Holes and the Mechanism of Coordinated Extraction of Harmful Gases.

Men Jinlong J, Xiong Bibo B, Wang Zehua Z, Ye Zhenpeng Z et al.

Uncontrolled carbon monoxide (CO) release after deep-hole roof pressure-relief blasting remains a safety problem because conventional shallow drainage often fails to match the strata where blast gases are generated and retained. Here, we clarify the permeability-contrast-controlled retention mechanism and propose an integrated blasting-sealing-extraction framework that couples field diagnosis at the A503 working face, dynamic fracture modeling, confined explosion tests, adsorption-diffusion analysis, and industrial validation. The method uses the critical distance between the fracture front and the coal seam to constrain charge length and places extraction boreholes in the roof gas-enrichment zone rather than only in the coal seam. The A503 measurements showed that the sandstone roof permeability (2.1 × 10-13 m2) was about 41 times lower than that of the coal seam (8.7 × 10-12 m2), creating a low-permeability CO retention zone. Numerical simulations gave an effective blasting influence radius of approximately 6.5 m and showed that the control hole extended the connected plastic zone to about 10 m. Field mass-balance data showed that the optimized scheme increased the CO extraction rate from 4.43% to 82.21%, reduced ventilation discharge from 11.96% to 3.91%, and lowered the residual CO fraction from 83.61% to approximately 13.9%. These results show that the mechanism-guided matching of fracture control, sealing, and targeted roof-strata extraction converts postblasting CO control from delayed ventilation dilution to active capture at the enrichment zone.

PMID 42569146
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PubMedSubstance use & addiction journal2026-08-08

Correlates of Post-Release Overdose Among Women With Opioid Use Disorder Returning to the Community Following Jail Incarceration.

Dickson Megan F MF, Monticello Krystina K, Pike Erika E, Webster J Matthew JM et al.

Previous research indicates that opioid overdose risk is significantly higher during community reentry following incarceration, particularly for women. However, there is a limited understanding of factors specifically associated with women's overdose risk post-jail release. This study examines the relationship between individual risk factors, structural vulnerabilities, and nonfatal overdose during the 3 months following jail release among a sample of women with opioid use disorder (OUD). Women (N = 900) in this study were randomly selected from 9 Kentucky jails, screened for OUD, and interviewed as part of the Justice Community Opioid Innovation Network trial (NCT04069624) funded by the National Institute on Drug Abuse. The sample consisted of women who completed the 3-month follow-up interview post-release and had complete data on all variables of interest (n = 754). Bivariate analyses assessed relationships between post-release nonfatal overdose and individual-level factors (eg, demographic characteristics) and structural vulnerabilities (eg, unstable housing and food insecurity). Firth logistic regression was then used to further examine independent correlates of nonfatal overdose during community reentry. According to analyses, 31 women (4.1%) reported a nonfatal overdose during the 3 months post-jail release. Regression results indicated that odds of overdosing post-release were higher for women who had overdosed previously in their lifetime (P = .004). Injection drug use (P < .001) and unstable housing (P = .048) during the follow-up period also increased the odds of overdose. These results suggest that both individual risk factors and structural vulnerabilities may contribute to increased overdose risk for women with OUD returning to the community post-incarceration. Overdose prevention interventions should include strategies for mitigating these reentry challenges. ClinicalTrials.gov ID NCT04069624; https://clinicaltrials.gov/study/NCT04069624.

PMID 42568290
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