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desloratadine + pseudoephedrine (Clarinex D / Aerinaze)

✓ Approved

Merck & Co. · HRH1 · Small Molecule

What is desloratadine + pseudoephedrine?

desloratadine + pseudoephedrine is a small molecule developed by Merck & Co.. It is approved for therapeutic indications via oral (po).

Drug Profile

Brand NamesClarinex D, Aerinaze
CompanyMerck & Co.
Drug ClassSmall Molecule
Molecular TargetHRH1
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Merck & Co.

Mechanism of Action

Molecular Targets

desloratadine + pseudoephedrine acts on 1 molecular target:

HRH1histamine receptor H1 (HH1R, H1R)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

desloratadine + pseudoephedrine is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Immune system disordersSeasonal allergy✓ Approved

Related Research Articles

PubMedJournal of chemical information and modeling2026-07-14

Discovery and Mechanism of Action of a Novel Desloratadine Derivative Inhibiting Mycobacterium tuberculosis 3-Dehydroquinate Synthase.

Belachew Aweke Mulu AM, Li Haizhou H, Tian Xirong X, Liu Zhiyong Z et al.

Mycobacterium tuberculosis, the etiological agent of tuberculosis (TB), remains a leading cause of mortality from infectious disease worldwide. The continued emergence of multidrug-resistant strains highlights the urgent need for new therapeutic agents with novel mechanisms of action. Here, we report the discovery and comprehensive characterization of DL25, a synthetic desloratadine-derived small molecule exhibiting potent antimycobacterial activity (minimum inhibitory concentration (MIC) 2-4 μg/mL against multiple mycobacterial species). Using a supra-inhibitory DL25 selection strategy, we isolated and characterized spontaneous resistant mutants. Whole-genome sequencing identified recurrent mutations in aroB, which encodes 3-dehydroquinate synthase (DHQS), an essential enzyme of the shikimate pathway. Consistent with target involvement, aroB overexpression reduced susceptibility to DL25, while DL25 decreased DHQS-associated biochemical activity in vitro with an apparent IC50 of approximately 5.0 μg/mL. In addition, DL25 exhibited concentration- and time-dependent bactericidal activity and showed partial synergy with several established antitubercular agents. Structural modeling, molecular docking, and 100 ns molecular dynamics simulations supported stable binding of DL25 within the DHQS active site and identified interactions with residues implicated in substrate recognition and catalysis. Collectively, the genetic, biochemical, and computational findings support DHQS as a biologically relevant target associated with DL25 activity and establish DL25 as a promising lead-like scaffold for the development of future shikimate pathway-directed antimycobacterial agents. More broadly, this study demonstrates the value of integrating genetic, biochemical, and computational approaches for mechanism-guided antituberculosis drug discovery.

PMID 42447414
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PubMedCells2026-07-13

Plant-Derived Diamine Oxidase Modulation of Histamine-Induced Ca2+ Release in Intestinal Caco-2 Cells: A Cellular System to Evaluate Its Histaminase Efficacy.

Neree Armelle Tchoumi AT, Jumarie Catherine C, Marcocci Lucia L, Pietrangeli Paola P et al.

Histamine accumulation is associated with allergic reactions and intestinal dysfunction through activation of H1R Receptors (H1Rs) and subsequent intracellular Ca2+ mobilization. Although antihistamines such as desloratadine block H1Rs to alleviate symptoms, they may induce adverse effects (dizziness, nausea, neurological disorders). Diamine oxidases (DAOs) catalyze the oxidative deamination of histamine to imidazole acetaldehyde with consumption of oxygen and concomitant production of hydrogen peroxide and ammonia. Instead of blocking H1R, we have proposed vegetal diamine oxidase (vDAO) as an enzymatic approach to decompose histamine. This study investigated whether vDAO, by degrading histamine, could modulate histamine-induced Ca2+ mobilization compared with desloratadine. Using intestinal Caco-2 cultured cells loaded with the fluorescent Ca2+ indicator Fluo-4 AM, intracellular calcium (Ca2+) dynamics were analyzed by confocal microscopy following histamine stimulation. vDAO significantly downregulated histamine-induced Ca2+ mobilization. Notably, at a fixed histamine concentration sufficient to trigger Ca2+ release, vDAO achieved the same level of calcium mobility inhibition at a concentration three-fold lower than that of desloratadine, suggesting a high efficiency of DAO. These findings indicate that histamine degradation with orally administrable DAO may reduce Ca2+ signaling in intestinal epithelial cells, providing a promising approach to reduce histamine-related damage or a reinforcement of current antihistamine anti-inflammatory medication based on histamine receptor blockade.

PMID 42439652
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PubMedThe World Allergy Organization journal2026-07-12

Forecasting seasonal allergic rhinitis through integrated analysis of social media and online drug sales data.

Tong Xunliang X, Fang Chuangsen C, Jiang Xiaowei X, Liu Lan L et al.

Allergic rhinitis (AR) is a highly prevalent, seasonally variable disease that poses a growing public health challenge. Conventional surveillance based on clinic visits and surveys is slow and may miss self-medicating patients. Integrating environmental monitoring with digital traces such as search queries and online drug purchases may provide more timely insight into allergen exposure, symptom awareness, and medication demand. We analyzed daily data for urban Beijing from March 1, 2022 to October 15, 2024, including pollen concentration (grains per 1000 mm3), the Baidu search index for "allergic rhinitis," and online purchase rates of 4 oral second-generation H1-antihistamines (loratadine, desloratadine, cetirizine, levocetirizine) from the Meituan platform, standardized per 100,000 population. Cross-correlation functions were computed on pre-whitened series to assess lead-lag relationships. A single-mediator regression framework applied to pre-whitened data and estimated with Newey-West heteroskedasticity- and autocorrelation-consistent standard errors quantified the mediating role of the Baidu Index between pollen and antihistamine purchases. ARIMAX (1,1,1) models with different exogenous inputs (pollen only, Baidu Index only, both combined) and a naïve random-walk benchmark were used to forecast 1-, 2-, 3-, and 7-day demand; performance was evaluated using RMSE, MAPE, and Pearson correlation (PCC). All 3 series exhibited pronounced and recurrent seasonal patterns, with Baidu search activity rising in close temporal alignment with pollen peaks and antihistamine purchases typically lagging by 1-2 days. Pre-whitened cross-correlations remained moderate and statistically significant around lag 0, indicating genuine contemporaneous associations after removing the shared seasonal component. Mediation analysis showed that pollen concentration had a significant total effect on antihistamine purchase rates (β = 0.34, 95% CI [0.13, 0.54]), of which approximately 47% was transmitted indirectly via the Baidu Index (indirect β = 0.16, 95% CI [0.08, 0.25]). The ARIMAX (1,1,1) model integrating both pollen and Baidu Index achieved the best forecasting performance (1-day RMSE = 3.80, MAPE = 7.68%, PCC = 0.89) and consistently outperformed single-predictor models and the random-walk benchmark across all horizons. Pollen exposure influences antihistamine demand both directly and indirectly through public information-seeking behavior captured by the Baidu Index, and integrating environmental and digital data enables timely surveillance of seasonal allergic-rhinitis-related medication use.

PMID 42436900
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PubMedPharmacological reports : PR2026-07-11

The onset of posterior reversible encephalopathy syndrome (PRES) and reversible cerebral vasoconstriction syndrome (RCVS) with the use of decongestant agents: a European pharmacovigilance analysis.

Anatriello Antonietta A, Cantone Andrea A, Pentella Ciro C, Vastarella Maria Giovanna MG et al.

On December 1st, 2023, the Pharmacovigilance Risk Assessment Committee (PRAC) published a safety warning against using pseudoephedrine in patients with severe or uncontrolled hypertension and severe acute or chronic kidney disease for the risk of developing posterior reversible encephalopathy syndrome (PRES) or reversible cerebral vasoconstriction syndrome (RCVS). Based on this consideration and the availability of other decongestants with the same mechanism of action as pseudoephedrine in the European market, we decided to conduct a safety study to evaluate cases of RCVS or PRES reported with other decongestants. A European, retrospective, post-marketing surveillance study was conducted to describe individual case safety reports (ICSRs) of RCVS and PRES reported with decongestants and to compare the likelihood of reporting these events among decongestants. Data were retrieved from the EudraVigilance database from January 1st, 2001, to December 31st, 2025. A total of 65 ICSRs reported PRES or RCVS with decongestants, most of which referred to female patients aged 18-64 years. A disproportionate reporting of RCVS was found for xylometazoline (reporting odds ratio, ROR: 3.39; 95% confidence interval, CI: 1.94-5.93) and phenylephrine (ROR: 2.00; 95% CI: 1.11-3.61), and a disproportionate reporting of PRES for ephedrine (ROR: 6.44; 95% CI: 1.80-23.10) and phenylephrine (ROR: 3.47; 95% CI: 1.22-9.88) compared to all other decongestants. Our results suggest that all decongestants should be used with caution, and attention should be paid to signs and symptoms of PRES and RCVS when taking these medicines.

PMID 42432411
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PubMedScientific reports2026-07-07

AI-assisted versus manual sustainability assessment of a high-throughput LC-MS/MS method for psychotropic and OTC drugs of abuse in human plasma.

Yamani Hend Z HZ, Hesham Khaled K, Tawakkol Shereen M SM, Hussein Lobna A LA et al.

A rapid, sensitive, and selective LC-MSMS method was developed and validated for the quantification of dextromethorphan (DXM), pseudoephedrine (PSE), olanzapine (OLA), and fluoxetine (FLU) in human plasma. Mixture 1 (DXM/PSE) and mixture 2 (OLA/FLU) are fixed-dose combinations commonly misused at high doses for their euphoric effects. The proposed method employed a simple protein precipitation technique for sample preparation, using a cost-effective cross-over internal standard strategy; OLA for mixture 1 and DXM for mixture 2. Chromatographic separation was achieved on a Hypersil GOLD column (100 × 3 mm, 1.9 µm) using an isocratic mobile phase consisting of acetonitrile and 0.1% formic acid (70:30, v/v) at a flow rate of 0.3 mL/min. The short runtime of 2.5 min enables high-throughput analysis. Detection was performed in positive ionization mode using multiple reaction monitoring (MRM). The method exhibited linearity over concentration ranges of 0.05-25.0 ng/mL for DXM, 2.0-1000.0 ng/mL for PSE, 0.2-20.0 ng/mL for OLA, and 0.5-50.0 ng/mL for FLU with lower limits of quantification (LLOQs) of 0.05, 2.0, 0.2, and 0.5 ng/mL, respectively. The method was successfully validated in accordance with FDA and ICH bioanalytical method validation guidelines, demonstrating satisfactory selectivity, accuracy, and precision. The validated method demonstrated high extraction recovery (> 90%), limited, reproducible matrix effects (IS-normalized matrix factor CV ≤ 15%). This study represents a novel application of artificial intelligence (AI)-assisted evaluation, utilizing a universally accessible model to assess the greenness and whiteness of the proposed LC-MS/MS method through the Auto-AGREE and Auto-RGB 12 frameworks. The AI-generated assessments demonstrated high agreement with traditional metrics, highlighting the potential of AI tools to provide rapid and objective holistic sustainability evaluations for the global analytical community.

PMID 42409859
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PubMedCommunications chemistry2026-07-02

Exploring the photodynamical landscape of biomimetic lumichrome-ephedrine-class amine complexes across femtosecond to millisecond regimes.

Jena Subhrakant S, de la Hoz Tomás Mario M, Organero Juan Ángel JÁ, Moreno Ferrer Miquel M et al.

Flavin-amine interactions are central to neurotransmitter metabolism, yet how H-bonding and amine structure govern excited-state pathways remains unclear. Using lumichrome (LC) as a biomimetic model, we examine interactions and photobehaviour with sympathomimetic amines, norephedrine (Neph), ephedrine (Eph), and pseudoephedrine (Peph). In water, LC with amines readily forms anions. In dichloromethane, H-bonding drives ultrafast single-proton transfer (SPT) in the LC-Neph complex (~800 fs), followed by population redistribution (~14 ps) and a long-lived anion (τ ~5.4 ns), while LC-Eph and LC-Peph complexes show shorter lifetimes (~4.3-4.8 ns). Control experiments with phenethylamine confirm that the amine group drives SPT-mediated anion formation. Computational calculations support excitation-induced charge redistribution and SPT-mediated zwitterionic stabilisation. Nanosecond-millisecond transient absorption shows minor triplet quenching by Neph (τ ~0.74 → 0.66 μs), but Eph and Peph enhance quenching (τ ~0.45-0.55 μs) and photoproduct formation. This study unravels LC-sympathomimetic amine interactions, offering an avenue to interrogate excited-state pathways in flavin photochemistry.

PMID 42386889
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