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dihydroergotamine mesylate (INP104 / I104 / Trudhesa)

✓ Approved

Impel Pharmaceuticals Inc · HTR1D · 小分子

什么是 dihydroergotamine mesylate?

dihydroergotamine mesylate 是一种小分子,由Impel Pharmaceuticals Inc研发。该药已获批,用于治疗相关适应症,给药途径:Inhaled、Intranasal。

药物档案

商品名INP104, I104, Trudhesa
公司Impel Pharmaceuticals Inc
药物类别小分子
分子靶点HTR1D
给药途径Inhaled, Intranasal
状态Approved

作用机制

分子靶点

dihydroergotamine mesylate 作用于 1 个分子靶点:

HTR1D5-hydroxytryptamine receptor 1D (HTR1DA, HT1DA)
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

dihydroergotamine mesylate 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
Nervous system disordersMigraine✓ Approved

相关研究文献

PubMedFrontiers in pharmacology2026-06-05

Original research a real-world study of adverse events of nafamostat mesylate and sodium citrate based on the world health organization-VigiAccess database.

Xu Mengting M, Wang Ziyi Z, Yu Binbin B

While nafamostat mesylate (NM) and sodium citrate serve as commonly used extracorporeal anticoagulants in clinical practice, the characteristics and potential risks of their adverse events (AEs) need to be systematically evaluated. This study comparatively analyzed the reporting characteristics of the AEs of the above-mentioned two drugs based on the World Health Organization Adverse Drug Reaction Reporting Database (WHO-VigiAccess), to identify their safety signals and provide evidence-based guidance for optimizing their clinical uses. Mining of the global AE reporting data of NM and sodium citrate was conducted using the WHO-VigiAccess database, with the data collected until 29 December 2024. Statistical analysis was performed using the Reporting Odds Ratio (ROR), the Proportional Reporting Ratio (PRR), the Bayesian Confidence Propagation Neural Network (BCPNN), and the Empirical Bayes Geometric Mean (EBGM). The signal strengths of the AEs of the two drugs at the system organ class and preferred term levels were systematically evaluated in combination with the standardized coding MedDRA. This study included 1,572 NM-related reports (59 AEs) and 485 sodium citrate-related reports (102 AEs). NM AEs were mainly concentrated in immune system diseases (23.80%), skin and subcutaneous tissue diseases (16.25%), and gastrointestinal diseases (10.10%), with strong disproportionality signals observed for thrombosis in devices (n = 18, ROR = 264.71), shock (n = 119, ROR = 186.27) and anaphylactoid shock (n = 4, ROR = 143.45). In contrast, sodium citrate-related AEs primarily included systemic diseases with various reactions at the administration site (15.75%) and gastrointestinal disorders (11.63%). The reporting proportion of mortality for sodium citrate (2.83%) was higher than that for NM, although this finding may be influenced by reporting bias and confounding by indication. In addition, this study detected signals not described in the instructions, such as citrate toxicity (ROR = 6,740.61) and spinal muscular atrophy (ROR = 665.94). Both drugs shared several high-incidence AEs, including pruritus, vomiting and dyspnea, but there are significant differences in gender, age and geographical distribution. The use of NM was associated with a strong disproportionality signal for severe immune-related AEs, such as anaphylactic shock, and requires strengthened monitoring. The metabolic complications of sodium citrate and its exposure risks during pregnancy require targeted optimization of medication strategies. Real-world data suggested that both drugs may cause AEs that were not mentioned in the instructions, so risk management needs to be improved through dynamic pharmacological vigilance. This study provided important references for individualized selection and safety management of anticoagulation regimens for patients requiring hemodialysis.

PMID 42244882
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PubMedThe International journal of artificial organs2026-06-04

Clinical efficacy of anticoagulants in patients with uremic cerebral hemorrhage receiving continuous renal replacement therapy.

Li Zhenhua Z, Liu Kun K

Hemodialysis can significantly prolong the survival of uremia patients, but uremia and long-term hemodialysis can also cause complications. This study aimed to compare the clinical efficacy between the menostat mesylate and sodium citrate as anticoagulants in patients receiving CRRT. The clinical data of 80 patients with uremic cerebral hemorrhage in our hospital from January 2020 to October 2022 were collected and randomly divided into observation (nelostat anticoagulation, n = 40) and control (citrate and sodium anticoagulation, n = 40) groups. Physiological parameters, CRRT filter life, coagulation function index, activated whole blood coagulation time (ACT), anticoagulation efficiency rate, and incidence of adverse reactions were compared between the two groups. The physiological index, coagulation function index, ACT value, and anticoagulation efficiency were higher in the observation group than in the control group (p < 0.05). The observation group also demonstrated a longer CRRT filter life and lower incidence of adverse reactions than those in the control group (both p < 0.5). Naphlimostat mesylate demonstrated a good anticoagulant effect and was safe for use in CRRT.

PMID 42237693
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PubMedCellular signalling2026-06-04

Drug repurposing for pancreatic cancer: Lomitapide Mesylate as a potent HK2 inhibitor discovered via virtual screening.

Tan Xin X, Zhang Ying Y, Liu Miao M, Wang Fan F et al.

Pancreatic cancer has an early diagnosis rate below 5% and is largely resistant to conventional chemotherapy. Aerobic glycolysis, a metabolic hallmark, drives Epithelial-Mesenchymal Transition (EMT) to promote tumor progression and drug resistance. Hexokinase 2 (HK2) is the rate-limiting enzyme that initiates glycolysis. It is specifically overexpressed in pancreatic cancer cells and is a potential therapeutic target. To identify HK2 inhibitors, we performed structure-based virtual screening of over 70,000 compounds. The top candidate, Lomitapide Mesylate (LM), was validated through molecular docking, molecular dynamics simulations, Drug Affinity Responsive Target Stability (DARTS), and Cellular Thermal Shift Assay (CETSA), confirming direct HK2 binding. In vitro, LM inhibited HK2 activity, exerting anti-proliferative and pro-apoptotic effects. In a mouse organoid-derived xenograft model, LM monotherapy suppressed tumor growth. Importantly, LM combined with gemcitabine significantly enhanced anti-tumor efficacy, indicating potential to reverse gemcitabine resistance. Mechanistically, this synergy was linked to LM-mediated reversal of HK2-driven EMT. Thus, LM inhibits HK2 to block EMT and synergize with gemcitabine, offering a novel therapeutic strategy.

PMID 42235623
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PubMedBMC nephrology2026-06-04

Hemodialysis-related allergic reactions: a retrospective cohort study of clinical presentations, etiologies, and management.

Lu Jing-Yao JY, Ke Qi Q, Li Jun J, Lv Wen-Qing WQ et al.

This study aimed to investigate the etiology, clinical manifestations, management strategies, and clinical outcome of hemodialysis-related allergic reactions. A retrospective cohort study was conducted to analyze clinical data from patients who experienced hemodialysis-related allergic reactions at the Affiliated Hospital of Jiangnan University between January 2020 and December 2025. Patients undergoing maintenance hemodialysis-with no prior history of these allergic reactions-served as the control group. Their clinical characteristics and reaction profiles were systematically analyzed. A total of 40 cases of hemodialysis-related allergic reactions were identified as the study group. Isolated pruritus and skin rash were observed in 25 patients (62.5%); hemodialysis-related leukopenia and thrombocytopenia, in 4 cases (10.0%); and severe anaphylactic reactions, in five cases (12.5%); Five cases exhibited atypical hemodialysis-related allergic reactions (12.5%), including hypotension within 10 min of hemodialysis initiation, malaise, nausea, and vomiting. The predominant etiological factors identified were hypersensitivity to the hemodialyzer membrane (n = 11, 27.5%), AVF needles kits and hemodialysis extracorporeal circuit tubing (Ethylene Oxide Residue) (n = 27, 67.5%), and Nafamostat Mesylate (n = 2, 5%). Thorough saline pre-rinsing of the extracorporeal circuit remained the primary preventive strategy against EO-induced hypersensitivity. Switching to irradiated-sterilized acetate-membrane or wet-membrane dialyzers effectively prevented dialyzer hypersensitivity reaction. Glucocorticoid administration was effective in mitigating severe anaphylactic reactions. Patients in the study group exhibited significantly higher plasma eosinophil counts and C-reactive protein concentrations, and significantly lower hemoglobin levels, and serum albumin concentrations compared with the control group. Hemodialysis-related allergic reactions are primarily attributable to hypersensitivity responses to dialyzer membranes, residual ethylene oxide in extracorporeal circuit components, and occasionally Nafamostat Mesylate administered during the procedure. Glucocorticoid administration was effective in attenuating severe anaphylactic reactions. Allergic reactions that repeatedly occur during hemodialysis may be associated with an underlying chronic micro-inflammatory state.

PMID 42237261
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PubMedSaudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society2026-06-03

Design, optimization and characterization of mucoadhesive buccal film as a novel delivery system for doxazosin mesylate.

Maraie Nidhal Khazaal NK, Wannas Ali N AN

Doxazosin mesylate is a selective α1-adrenergic receptor antagonist with low oral bioavailability due to poor aqueous solubility and extensive first-pass hepatic metabolism. This study aimed to design and optimize a doxazosin mucoadhesive buccal film to overcome hepatic metabolism and enable rapid drug onset. The buccal films were prepared by solvent casting, using a Plackett-Burman design to screen formulation variables affecting ex vivo mucoadhesive force, followed by a 22 full factorial design to optimize in vitro drug release by varying the concentrations of HPMC, the main film-forming polymer, and glycerin, a plasticizer. The prepared films were characterized for physico-mechanical properties, surface pH, mucoadhesive force, swelling properties, and drug release. In addition, the optimized formula was further characterized by scanning electron microscopy and ex vivo permeation study. The screening study showed that mucoadhesive strength ranged from 28 to 41 g, with the polymer type, polymer concentration, plasticizer type, and plasticizer concentration identified as the most influential variables. The optimized formula (FF3), containing 66 w/w% HPMC K15M and 21 w/w% glycerin, achieved 100% drug release within 15 min with acceptable film properties, in addition, SEM analysis showed a relatively uniform and compact surface with slight undulations, furthermore the ex vivo permeation reached 91% within 15 min, corresponding to a cumulative permeated amount of 1820 µg, a cumulative amount per unit area of 2275 µg/cm2, and an estimated steady-state flux of 12750 µg/cm2/h. It was concluded that the developed buccal film is a promising system for improving doxazosin bioavailability and providing rapid therapeutic onset.

PMID 42234364
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PubMedExpert review of neurotherapeutics2026-05-31

STS101 nasal powder as a new treatment option for acute migraine with or without aura in adults.

Ong Bradley B, Monteith Teshamae S TS

Although effective acute migraine therapies are available, unmet treatment needs such as nausea, vomiting, or delayed gastric emptying remain. STS101 is a novel dihydroergotamine (DHE) nasal powder designed to treat acute migraine with a simple single. A targeted PubMed and ClinicalTrials.gov search was performed from database inception through October 2025 using the keywords "STS101," "dihydroergotamine," "migraine," and "intranasal powder." Eligible sources included English-language clinical studies, trial registry records, regulatory documents, and relevant conference abstracts addressing STS101 formulation, pharmacokinetics, efficacy, safety, and/or regulatory development. Data from Phase 1 pharmacokinetic trials, the Phase 3 EMERGE and SUMMIT randomized controlled trials, and the ASCEND long-term safety study are discussed. The pivotal efficacy trials did not meet their 2-hour co-primary endpoints. Later time-point analyses suggested possible clinical benefit, including higher rates of pain freedom and most bothersome symptom freedom from 3 to 48 hours. STS101 may be useful for some patients who prefer a non-oral intranasal rescue option or have had inadequate responses to triptans, gepants or other DHE forms of administration. Its clinical role will likely depend on how clinicians weigh its delivery platform, DHE pharmacology, tolerability, and place relative to other available intranasal options.

PMID 42217235
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