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loratadine (Clarityn RediTabs / Claritin Reditabs / loratadine, Zydis)

✓ Approved

Merck & Co. · HRH1 · 小分子

什么是 loratadine？

loratadine 是一种小分子，由Merck & Co.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Clarityn RediTabs, Claritin Reditabs, loratadine, Zydis
公司Merck & Co.
药物类别小分子
分子靶点HRH1
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Merck & Co.

作用机制

分子靶点

loratadine 作用于 1 个分子靶点：

HRH1histamine receptor H1 (HH1R, H1R)
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

loratadine 针对 2 个适应症，涉及 2 个治疗领域。

治疗领域疾病/病症分期
Respiratory, thoracic and mediastinal disordersRhinitis allergic✓ Approved
Skin and subcutaneous tissue disordersUrticaria✓ Approved

相关研究文献

PubMedACS omega2026-10-25

Loratadine Decreases Methicillin-Resistant Staphylococcus aureus Virulence through Global Hemolysin Regulators vraSR and agr.

Dillon Chase C, Marshall Isabel I, Henkel Maggy M, Balogh Halie H et al.

Methicillin-resistantStaphylococcus aureus-(MRSA) is a bacterial pathogen that relies on expression of a wide range of virulence factors. Hemolysins are a diverse collection of cytolytic toxins that promote virulence by being excreted and lysing host blood cells. We previously reported on novel antivirulence compounds that modulate hemolysis in vitro, including a brominated carbazole (compound 8) and the active ingredient in Claritin (loratadine). We analyzed expression and activity of MRSA hemolysins in two hospital-acquired strains. Even with the same staphylococcal cassette chromosome mec (SCCmec) type, the strains displayed unique responses to loratadine where both repression and elevation of hemolysis occurred. These compounds are potentially binding and regulating the master regulatory protein, Stk1, which has known ties to hemolysis inS. aureus. We hypothesized that the modulation of hemolysis by these putative Stk1 inhibitors would extend to community-acquired strains of MRSA. Furthermore, we wanted to determine if Stk1 was the only hemolysis regulatory protein being engaged by these compounds. To test this, we examined compound 8 and loratadine effects on two different USA300 strains, in addition to transposon mutants for a range of hemolysis regulatory genes. We observed strain-specific regulation of hemolysis by Stk1. Loratadine continued to downregulate both alpha and beta hemolytic activity in USA300 JE2 in both Stk1-dependent and independent pathways. Additionally, we report that this antivirulence compound effectively disrupts hemolysis by modulating both agr and vraSR global regulators, contributing to widespread cytotoxin repression. Both alpha hemolysin (hla) and RNAIII/delta hemolysin (hld) mRNA reductions occurred in vitro and in a human cell line model of MRSA infection. Together, these results expand our knowledge of loratadine's mode of action as a virulence modulator.

PMID 42923371
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PubMedChemSusChem2026-10-23

Direct α-C(sp3)─H Alkylation and Arylation of Ethers Enabled by Carbon Nitride/Nickel Metallaphotoredox Catalysis.

de Vries Ibáñez Miguel M MM, Husy Nathan G G NGG, Inico Elisabetta E, Karaca Kaan K et al.

The direct functionalization of α-C(sp3)─H bonds offers a powerful strategy for converting abundant feedstocks and complex molecules into value-added products, yet sustainable catalytic platforms that avoid precious-metal photocatalysts remain underdeveloped. Here, we report a metallaphotoredox system that combines recyclable carbon nitride nanosheets with nickel catalysis for the direct α-C(sp3)─H cross-coupling of ethers, amides, and benzylic substrates under visible light. The method operates at mild temperature in air and enables both α-C(sp3)─C(sp2) and α-C(sp3)─C(sp3) bond formation using aryl and alkyl halides, including challenging ether donors such as THF, 2-MeTHF, 1,4-dioxane, and DME. Broad functional group tolerance is demonstrated across electronically diverse aryl halides, while late-stage alkylation of pharmaceutically relevant molecules including loratadine, caffeine, and fenofibrate highlights the utility of the platform for molecular diversification. The carbon nitride photocatalyst is readily recovered and reused over five cycles without loss of activity, and the process is further translated to continuous flow, providing accelerated reaction kinetics and reduced photocatalyst loading. Mechanistic studies combining Stern-Volmer analysis, radical trapping, cyclic voltammetry, NMR spectroscopy, and DFT calculations support a dual catalytic cycle in which photoexcited carbon nitride promotes oxidative generation of α-heteroatom-stabilized radicals, while nickel mediates radical capture, cross-coupling, and product-forming reductive elimination. This work establishes carbon nitride as an earth-abundant, recyclable alternative to noble-metal photocatalysts for metallaphotoredox C─H functionalization and expands the scope of heterogeneous photocatalysis to direct α-C(sp3)─H cross-coupling.

PMID 42912554
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PubMedRSC advances2026-10-17

Functional evaluation of loratadine-cyclodextrin complexes: comprehensive solid-state characterisation, biopharmaceutical assessment and stability profiling.

Pocrnić Marijana M, Potrzebowski Marek J MJ, Jug Mario M, Galić Nives N

Loratadine (LOR) is a poorly water-soluble antihistaminic drug whose solubility can be significantly enhanced in water and biorelevant media through inclusion complexation with β-cyclodextrins (β-CDs), as we have shown previously. In this work, we investigated the biopharmaceutical properties and chemical stability of LOR : β-CDs 1 : 1 and 1 : 2 complexes in the solid state, prepared by two different methods: (i) solvent-free mechanochemical grinding in a high-energy vibrational mill, and (ii) spray-drying, as a traditional solvent-based technique. Altogether, 16 different systems were prepared using LOR, β-CD and its derivatives, namely hydroxypropyl-β-cyclodextrin (HP-β-CD), randomly methylated-β-cyclodextrin (RM-β-CD), and sulfobutylether-β-cyclodextrin (SBE-β-CD). Detailed solid-state characterization by differential scanning calorimetry (DSC), X-ray powder diffraction, ATR-FTIR and solid-state NMR was performed, indicating different levels of drug amorphization. Biopharmaceutical evaluation via in vitro dissolution testing and in vitro permeability assay across biomimetic membranes revealed that LOR dissolution and permeability depend on CD's type, LOR-to-CD molar ratio, and the method used for complex preparation. The influence of β-CDs on LOR stability under stress conditions, including photostability and accelerated stability studies, was determined using UHPLC-HR MS/MS. The structures of degradation products, including five previously unknown, were proposed. Obtained complexes, especially those prepared by grinding, demonstrated great potential for further formulation development.

PMID 42889714
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PubMedInternational journal of molecular sciences2026-10-16

Unveiling Novel Molecular Candidate Targets of Loratadine, Raloxifene, and Sorafenib in Hepatocellular Carcinoma.

Villarruel-Melquiades Fernanda F, Noyola-Díaz Martha M, Martínez-Gudiño Gelacio G, Mendoza-Garrido María Eugenia ME et al.

Hepatocellular carcinoma (HCC) remains a major global health burden. We have recently demonstrated the synergistic cytotoxicity elicited by the combination of loratadine, raloxifene, and sorafenib in liver cancer cells. In this study, we investigated the potential mechanistic basis of this novel multi-drug regimen by identifying candidate protein targets of the three drugs. Potential protein targets of each drug were identified using the Drug Affinity Responsive Target Stability (DARTS) assay in protein extracts from the HCC cell line HuH7, and molecular docking was performed to predict binding modes and explore the structural feasibility of these drug-target interactions. Bioinformatics analyses were conducted to predict biological functions, molecular interactions, and clinical relevance. We identified 147 potential candidate DARTS-stabilized proteins for loratadine, 191 for sorafenib, and 157 for raloxifene; a proportion of these candidate proteins maintained a statistically significant association with overall survival in HCC patients: 20.14% for loratadine, 22.93% for raloxifene, and 24.47% for sorafenib. Cross-referencing with public databases confirmed several previously documented targets-complementing our experimental approach-while revealing numerous previously unreported target candidates. Docking analyses predicted favorable binding interactions between the drugs and several proteins, such as the putative complex between loratadine and N-glycanase 1 (NGLY1), whose expression correlates with reduced overall survival in HCC patients. Functional enrichment analysis showed that several targets are involved in hallmarks of cancer. Clinically relevant candidate targets of loratadine, raloxifene, and sorafenib were identified. However, as these candidate protein targets were identified exclusively in HuH7 cells, they may not fully generalize across all HCC models without further validation. Nevertheless, our results suggest that loratadine, raloxifene and sorafenib modulate key pathways involved in tumorigenesis. These findings strengthen the use of this combination as a promising therapeutic strategy for HCC and provide new opportunities for the identification of novel targets, prognostic markers, and molecular vulnerabilities suitable for pharmacological intervention in HCC and other malignancies and diseases.

PMID 42883895
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PubMedThe Journal of allergy and clinical immunology2026-10-16

Comparative efficacy and safety of antihistamines, increased antihistamine dosing, and antihistamine adjuncts for chronic urticaria: a systematic review, dose-response, and network meta-analysis of randomized trials.

Chu Alexandro W L AWL, Zhao Irene X IX, Rayner Daniel G DG, Guyatt Gordon H GH et al.

Chronic urticaria is a common immune-mediated condition characterized by wheals (itch and hives), angioedema, or both, lasting for greater than six weeks. It is managed with H1 antihistamines as the first-line therapy. Fundamental unresolved questions remain regarding the comparative benefits and harms of antihistamines and their adjuncts, and of H1 antihistamine dose-escalation. To analyze the comparative benefits and harms of antihistamines and their adjuncts (H2 blockers or montelukast), and of H1 antihistamine dose-escalation. As part of updating the American Academy of Allergy, Asthma & Immunology and American College of Allergy, Asthma and Immunology Joint Task Force on Practice Parameters Chronic Urticaria guidelines, we searched MEDLINE, EMBASE, CENTRAL, and regulatory databases from inception to March 17, 2025, for randomized trials addressing antihistamines or their adjuncts for chronic urticaria. Paired reviewers independently screened records, extracted data, and assessed risk of bias. Random effects network and dose-response meta-analyses addressed urticaria activity (composed of itch and wheal scores), angioedema activity, urticaria-related quality of life, and harms including sedation. The GRADE approach informed certainty of evidence ratings. CRD42022367280. 211 trials (22,187 participants) evaluated 55 unique treatments. Bilastine, desloratadine, fexofenadine, and levocetirizine are among the most effective in improving overall urticaria activity, urticaria-related quality of life, and sleep disturbance. Cetirizine and loratadine are among the most effective in reducing overall urticaria activity and its subcomponents, with cetirizine also among the most effective in improving urticaria-related quality of life. Escalating from a single to quadruple daily dose may yield diminishing additional benefit. Second-generation agents as a class may be more effective than first-generation agents in improving urticaria activity and sleep disturbance. Sedation risk likely increases with higher doses, with first-generation agents (e.g., diphenhydramine, hydroxyzine) and doxepin among the most sedating; cetirizine, ketotifen, levocetirizine, and rupatadine among the intermediate sedating; and bepotastine, bilastine, desloratadine, ebastine, fexofenadine, and loratadine among the least sedating. Adding montelukast (moderate certainty) or an H2 blocker (very low certainty) to a second-generation agent may further reduce urticaria activity. For chronic urticaria, second-generation agents differ in their efficacy and safety. First-generation agents are less beneficial and more harmful. Escalating to higher daily doses may provide additional benefits but likely increases sedation.

PMID 42887704
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PubMedFrontiers in medicine2026-10-13

Vitiligo developing during dupilumab treatment in a child with atopic dermatitis: a case report and literature review.

Yu Peng P, Wei Fenglei F

An 8-year-11-month-old girl with severe atopic dermatitis had previously received treatments including topical hydrocortisone butyrate, pimecrolimus, tacrolimus, hormone ointment encapsulation, and narrowband ultraviolet B (NB-UVB) phototherapy. She also took oral antihistamines such as cetirizine and loratadine, but these interventions provided limited relief, and her pruritus persisted. In August 2023, she began dupilumab therapy with a 400 mg subcutaneous loading dose, followed by 200 mg subcutaneous injections every two weeks. Vitiligo developed three months after dupilumab initiation in this child with severe atopic dermatitis and improved with combination therapy while dupilumab was continued. Together with previously published reports, this observation supports a possible temporal association between dupilumab exposure and vitiligo development; however, causality cannot be established from the currently available evidence.

PMID 42865691
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