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tafluprost + timolol maleate (Tapucom / STN 10111 / STN 1011101)

✓ Approved

Santen Pharmaceutical Co., Ltd. · ADRB1 · Small Molecule

What is tafluprost + timolol maleate?

tafluprost + timolol maleate is a small molecule developed by Santen Pharmaceutical Co., Ltd.. It is approved for therapeutic indications via others or topical.

Drug Profile

Brand NamesTapucom, STN 10111, STN 1011101
CompanySanten Pharmaceutical Co., Ltd.
Drug ClassSmall Molecule
Molecular TargetADRB1, ADRB2, PTGFR
RouteOthers, Topical
StatusApproved
Sources: ClinicalTrials.gov, Santen Pharmaceutical Co., Ltd.

Mechanism of Action

Molecular Targets

tafluprost + timolol maleate acts on 3 molecular targets:

ADRB1adrenoceptor beta 1 (B1AR, RHR)
ADRB2adrenoceptor beta 2 (ADRBR, B2AR)
PTGFRprostaglandin F receptor (FP)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

tafluprost + timolol maleate is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Eye disordersGlaucoma✓ Approved

Related Research Articles

PubMedTherapeutic delivery2026-05-23

Preparation and evaluation of Prochlorperazine Maleate loaded nanostructured lipid carrier for the treatment of schizophrenia.

Maniar Karan K, Yadav Bindu Kumari Nagendra BKN, Shah Shreeraj S

Schizophrenia management using conventional oral antipsychotic formulations is constrained by poor bioavailability, extensive first-pass metabolism, and dose-related systemic adverse effects. Intranasal drug delivery using nanocarrier systems has emerged as a promising strategy for direct brain targeting by bypassing the blood-brain barrier (BBB) via olfactory and trigeminal pathways, thereby enhancing therapeutic efficacy while minimizing peripheral exposure. This study aimed to develop and evaluate Prochlorperazine Maleate-loaded Nanostructured Lipid Carriers (NLCs) for intranasal administration to enhance brain delivery. Prochlorperazine Maleate, a dopamine D2 receptor antagonist used in schizophrenia management, was selected due to its poor oral bioavailability and significant hepatic metabolism. NLCs were prepared using a lipid-based approach and optimized by varying lipid composition and surfactant concentration. The optimized formulation consisted of a solid lipid to liquid lipid ratio of 77.51:22.49 with 1.5% Tween 80. Evaluation parameters included particle size, zeta potential, entrapment efficiency, in vitro drug release, release kinetics, ex vivo permeation, and stability studies. The optimized NLCs exhibited a particle size of 213.40 ± 46.53 nm, zeta potential of -32.7 mV, and entrapment efficiency of approximately 72%. This approach has strong potential for enhancing therapeutic outcomes in schizophrenia.

PMID 42173813
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PubMedACS omega2026-05-18

Beyond Treatment: Electrochemical Phenol Oxidation in Methanol under Different Cell Configurations and Its Implications for Valorization.

Santacruz William W, Navas-Higuero Cristina C, Saez Cristina C, Motheo Artur de Jesus AJ et al.

This study explores electrochemical phenol oxidation in methanolic and aqueous media as a strategy to shift adsorption-based treatments from pollutant removal toward chemical valorization. Using 3D-printed single- and divided-cell reactors with alkaline electrolytes to enhance conductivity, methanol clearly outperformed water: phenol conversions exceeded 50% after 3 h (vs <15% in water), with higher Faradaic efficiencies (>21%) and energy efficiencies up to 3-fold greater, especially in anion exchange membrane (AEM) systems. Speciation analysis revealed that methanol favors diverse, industrially relevant intermediates, including carboxylates (oxalate, malonate, succinate, tartrate, maleate) and methoxylated aromatics, whereas aqueous media predominantly formed benzoquinone and tetrahydroxybenzene, consistent with rapid hydroxyl-radical-driven mineralization. The strong influence of membrane type on phenol transport (AEM > PEM) and the distinct degradation pathways observed (hydroxylation/cleavage in water vs methoxylation/fragmentation in methanol) highlight the critical role of solvent-membrane coupling. Overall, the results demonstrate that electrochemical processing in methanol promotes the formation of identifiable value-added products, indicating potential implications for future resource-oriented wastewater treatment strategies.

PMID 42146171
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PubMedNeuroscience research2026-05-15

Direct binding of the neurorehabilitation drug edonerpic maleate to CRMP2 demonstrated by NMR spectroscopy.

Tanaka Meiro M, Ota Wataru W, Arisawa Tetsu T, Takeuchi Koh K et al.

Functional recovery after brain damage, such as stroke, depends on neuronal plasticity that reorganizes synaptic connections in intact brain regions. Edonerpic maleate, a small compound that accelerates rehabilitation-dependent motor recovery, is proposed to produce its effects through direct binding to collapsin response mediator protein 2 (CRMP2) and the resulting enhancement of synaptic AMPA (α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic-acid) receptor trafficking. To confirm this interaction, we employed nuclear magnetic resonance (NMR) spectroscopy using purified CRMP2. ¹H NMR revealed clear attenuation of edonerpic maleate signals in the presence of CRMP2, consistent with formation of a ligand-protein complex. The direct interaction was further confirmed by saturation transfer difference [STD]-NMR, demonstrating the contact-dependent reduction of edonerpic maleate signals upon the saturation of CRMP2. Together, these data provide definitive evidence that edonerpic maleate directly binds to CRMP2 to physically form a stable complex. These findings provide the structural foundation for understanding the pharmacological mechanism of edonerpic maleate and support the development of CRMP2-targeted therapeutics to enhance neurorehabilitation efficacy.

PMID 42134551
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PubMedInternational ophthalmology2026-05-14

Efficacy and safety of netarsudil compared with prostaglandin-based therapies: a Bayesian network meta-analysis.

Liu Jun J, Zuo Meiling M, Liu Xiaodan X

The study aimed to compare the efficacy and safety of netarsudil (NET), alone or in fixed-dose combinations (FDC), in comparison with prostaglandin analogues (PGAs: bimatoprost [BIM], latanoprost [LAT], travoprost [TRA], and tafluprost [TAF]) for the treatment of primary open-angle glaucoma (POAG) or ocular hypertension. Literature search in PubMed, Embase, Cochrane Library, Web of Science (inception to July 2025). Identified 26 randomized controlled trials (RCTs) (5,390 patients). The primary outcome was the mean difference in intraocular pressure (IOP) reduction at 3 months; the secondary outcome was the incidence of conjunctival hyperemia. Pair-wise meta-analysis used Cochrane Review Manager 5.4, Bayesian network meta-analysis via Aggregate Data Drug Information System (ADDIS) with Markov Chain Monte Carlo (MCMC) simulations. Inconsistency assessed via node-splitting, convergence evaluated via Brooks-Gelman-Rubin method. Network meta-analysis showed 3-month IOP -lowering hierarchy: FDC > BIM > TRA > LAT > TAF > NET. Conjunctival hyperemia incidence (highest to lowest): TAF > FDC > NET > BIM > TRA > LAT. Node-splitting confirmed consistency (P ≥ 0.05), convergence was satisfactory. Funnel plots indicated no publication bias for IOP outcomes but potential bias for conjunctival hyperemia. Although NET ranked lower in IOP-lowering efficacy compared to most PGAs and FDC, it demonstrated a favorable safety profile, particularly with a relatively lower incidence of conjunctival hyperemia than TAF and FDC. These findings suggest that NET may serve as a valuable alternative in patients who are intolerant to PGAs or require adjunctive therapy, warranting further investigation in targeted populations.

PMID 42133103
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PubMedJournal of pharmaceutical and biomedical analysis2026-05-13

Comprehensive impurity profiling and stability assessment of indacaterol maleate integrating LC-MS and in silico genotoxicity.

Aydın Çağla Ç, Yazar Yücel Y, Yılmaz Halil H, Bellur Atici Esen E et al.

This study describes the development and validation of stability-indicating analytical methods for indacaterol maleate, an ultra-long-acting β2-adrenoceptor agonist used in asthma and chronic obstructive pulmonary disease (COPD). RP-HPLC-UV methods were established for quantifying indacaterol and its related substances, while LC-QDa-MS and high-resolution LC-QTOF-MS were employed for impurity identification and structural elucidation. All methods were developed and validated in accordance with ICH guidelines to support comprehensive assessment of process-related impurities and degradation behavior. Eight potential impurities were identified, synthesized, and fully characterized. The validated RP-HPLC-UV assay and related substances methods were applied to forced degradation studies under thermal, photolytic, oxidative, neutral, acidic, and alkaline conditions, as well as to accelerated and long-term stability samples. Trace-level impurities were structurally elucidated using LC-QDa-MS and LC-QTOF-MS. In silico mutagenicity assessment of thirteen impurities using Nexus software classified IND-B ((R)-8-(benzyloxy)-5-(2-bromo-1-hydroxyethyl)-quinolin-2(1H)-one) as a Class 3 potential genotoxic impurity due to its alkyl bromide moiety. Although the TTC-based limit for IND-B (based on the ICH M7 threshold of 1.5 µg/day for a maximum daily dose of 300 µg) corresponds to ≤ 0.5%, all specified impurities were conservatively controlled at ≤ 0.15% and unspecified impurities at ≤ 0.10%, in line with ICH M7 and Q3A guidelines. The RP-HPLC-UV assay and related substances methods demonstrated specificity, precision, accuracy, linearity, and robustness, confirming their suitability as stability-indicating methods. Overall, this integrated approach provides a robust framework for impurity profiling, stability assessment, and genotoxic risk evaluation of indacaterol maleate, ensuring regulatory compliance and product quality throughout shelf life.

PMID 42119498
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PubMedAmerican journal of physiology. Regulatory, integrative and comparative physiology2026-05-11

Intracardiac neuromodulation of pacemaker rate in the adult zebrafish heart in vitro.

O'Shea Keegan P D KPD, Long Zachary D ZD, Smith Frank M FM

Heart rate (HR) in vertebrates is determined by the discharge frequency of cardiac pacemaker cells, which are innervated by the autonomic nervous system. The portion of this system located within the heart, the intracardiac nervous system (ICNS), transmits impulses to cardiac effectors for control of cardiac output. Central autonomic neurons modulate the heart through sympathetic (acceleratory) and parasympathetic (inhibitory) axons in the vagosympathetic trunks. In the classical model of cardiac control, the balance between sympathetic and parasympathetic efferent signals determines HR. Recent evidence of spontaneous neural activity within the ICNS in isolated hearts suggests a local regulatory element incardiac control. We examined the potential for ICNS modulation of HR in the isolated zebrafish heart, using atropine to block parasympathetic drive to the pacemaker, and timolol to block sympathetic drive. Atropine (3, 10, 30 µM) evoked tachycardia of similar magnitude at 22 and 28 ° C. Timolol (3, 10 and 30 µM) caused bradycardia at both temperatures, with greater proportional HR responses to all doses at the higher temperature. Our results suggest that both sympathetic and parasympathetic outputs from the ICNS influence the pacemaker, with the degree of sympathetic drive being temperature-sensitive. Intrinsic HR, obtained after dual antagonist application, was not significantly different from HR before drug application so the effects of sympathetic and parasympathetic drive on pacemaker rate appeared to be evenly balanced. We propose that the ICNS in the isolated zebrafish heart is capable of modulating HR in the absence of extracardiac autonomic inputs.

PMID 42113566
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