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melatonin

✓ Approved

Clinigen Group · MTNR1A · Small Molecule

What is melatonin?

melatonin is a small molecule developed by Clinigen Group. It is approved for therapeutic indications via oral (po).

Drug Profile

CompanyClinigen Group
Drug ClassSmall Molecule
Molecular TargetMTNR1A, MTNR1B
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Clinigen Group

Mechanism of Action

Molecular Targets

melatonin acts on 2 molecular targets:

MTNR1Amelatonin receptor 1A (MEL-1A-R, MT1)
MTNR1Bmelatonin receptor 1B (FGQTL2, MT2)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

melatonin is developed for 2 unique indications across 1 therapeutic area.

Therapeutic AreaConditionPhase
Psychiatric disordersInsomnia✓ Approved
Psychiatric disordersSleep disorder✓ Approved

Related Research Articles

PubMedBiochemistry. Biokhimiia2026-08-30

Neuroprotective Effect of Subconjunctival Melatonin Injections in 6-Hydroxydopamine-Induced Neurotoxic Eye Damage.

Pavlenko Tatyana A TA, Chesnokova Natalya B NB, Lisovskaya Olga A OA, Beznos Olga V OV et al.

The search for new effective methods of neuroprotection is relevant for the treatment of a wide range of common eye diseases such as age-related macular degeneration, glaucoma, and diabetic retinopathy. Using a rabbit model of neurotoxic eye damage induced by intravitreal injection of the dopaminergic neurotoxin 6-hydroxydopamine (6-OHDA), we studied the effect of subconjunctival injections of 0.1% melatonin solution on pathophysiological and biochemical processes in the eye. Administration of 6-OHDA caused destruction of the retinal pigment epithelium, narrowing of retinal vessels, hemorrhages, decrease in ocular blood flow, and intraocular pressure, as well as reduced activity of α2-macroglobulin and concentrations of matrix metalloproteinase-9 and angiotensin-converting enzyme in the aqueous humor, vitreous body, and retina. Subconjunctival melatonin injections over 9 days resulted in the 2-fold on average reduction of the area of retinal damage, and normalization of the minute volume of ocular blood flow and intraocular pressure. On day 14, an increase in the α2-macroglobulin activity in the aqueous humor (0.66 ± 0.19 vs. 0.49 ± 0.13 nmol/min per 1 mg protein) and vitreous body (0.50 ± 0.15 vs. 0.21 ± 0.07 nmol/min per 1 mg protein, p < 0.05) was observed, along with a decrease in the matrix metalloproteinase-9 concentration (118.4 ± 34.6 vs. 524.3 ± 163.2 ng/mg, p < 0.05) and angiotensin-converting enzyme concentration (371.0 ± 52.1 vs. 596.1 ± 171.5 ng/mg, p < 0.05) in the retina. This indicates reduction in the intensity of inflammation and vascular wall permeability. Melatonin could be considered a promising neuroprotective component in the complex therapy of retinal diseases.

PMID 42669558
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PubMedPain research & management2026-08-29

Association of Baseline Systemic Immune-Inflammation Index With Severe Sleep Disturbance in Patients With Neuropathic Pain: A Prospective Longitudinal Observational Cohort Study.

Zhang Jialei J, Zhang Xiaoling X, Li Jing J, Cao Kai K et al.

Patients with neuropathic pain frequently experience impaired sleep quality. The systemic immune-inflammation index (SII) is a readily available blood-based inflammatory marker, but its association with sleep disturbance in neuropathic pain patients remains insufficiently defined. This single-center prospective longitudinal observational cohort study enrolled 135 patients aged 40-65 years with neuropathic pain confirmed by the DN4 questionnaire, disease duration of 6-12 months, and pain inadequately controlled by conventional medication. Baseline severe sleep disturbance was defined using a prespecified severity-based threshold of PSQI > 10. Fasting blood and first-morning spot urine samples were collected at baseline and at the 1-month follow-up after PRF. SII was calculated as platelet count x neutrophil count/lymphocyte count. Native urinary melatonin concentration was measured by ELISA and reported as an unadjusted spot urine concentration. The primary analysis evaluated the association between baseline SII and severe sleep-disturbance status; post-PRF changes were interpreted as within-subject temporal changes because no control group was included. At baseline, 73 of 135 patients met the prespecified criterion for severe sleep disturbance. Compared to the nonsevere group, the severe group had higher baseline SII (803.03 ± 111.45 vs. 604.21 ± 164.29, p < 0.001) and lower urinary melatonin concentration (8.32 ± 2.17 vs. 9.61 ± 2.72, p = 0.006). At the 1-month follow-up, severe sleep-disturbance status was present in 9 patients (McNemar test, p < 0.001). SII decreased, and urinary melatonin concentration increased in both baseline severity groups (all within-group p < 0.001). In a limited multivariable logistic regression model adjusted for available baseline covariates, baseline SII was associated with severe sleep-disturbance status (adjusted OR per 1-unit increase: 1.011; 95% CI: 1.007-1.014; p < 0.001). Exploratory ROC analysis yielded an apparent in-sample AUC of 0.833. Higher baseline SII was associated with severe sleep-disturbance status in this mixed neuropathic pain cohort. The observed longitudinal changes after PRF should be interpreted cautiously as within-subject temporal changes rather than PRF-specific effects. The findings are exploratory and do not establish causality, a direct inflammatory mechanism, or validated predictive performance. Chinese Registry of Clinical Trials: ChiCTR2500103587.

PMID 42667120
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PubMedACS omega2026-08-28

μPADs for a Safer Night's Sleep: An Alternative for Quality Control of Melatonin Pharmaceutical Formulations.

Ramos Ana Julia Aparecida AJA, Brazaca Laís Canniatti LC, Rossini Eduardo Luiz EL, Lima Manoel de Jesus de Aquino MJA et al.

Melatonin, known as the "sleep hormone," has its primary function in regulating the circadian cycle, a 24 h sleep-wake pattern that leads to significant physical, mental, and behavioral changes. The use of melatonin in pharmaceutical formulations gained popularity as a tool to combat sleep disorders such as insomnia and has been increasing in the last few decades. Melatonin-based pharmaceutical formulations are classified as dietary supplements, which leads to a different perspective on the necessity of strict quality control for these products. There are already extensive descriptions in the literature of the serious side effects associated with the administration of those formulations, including, for example, higher dosages than indicated on the label or contamination by other hormones. Still, there is a gap in devices that could make an easy and low-cost determination of melatonin. This work presents a paper-based sensor for the quality control of melatonin in pharmaceutical formulations, utilizing the modified Van Urk reaction. This reaction causes a color change from white to blue on the paper surface, correlating with the melatonin concentration. The constructed sensor performed well in quantifying melatonin in solid (0.22 mg/tablet) and liquid (0.20 mg/drop) pharmaceutical formulations, considering the maximum standard deviation when compared with results obtained by a gold-standard technique (liquid chromatography). The developed method demonstrated good linearity (R2 = 0.9915) over a melatonin concentration range of 40-300 mg L-1 and exhibited a specific response to the hormone when tested against the vehicles and excipients of the pharmaceutical formulations. Therefore, the proposed sensor demonstrates excellent potential as an inexpensive tool for quality control, introducing an innovative approach to the use of paper-based microfluidic devices in this field.

PMID 42662326
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PubMedFrontiers in nutrition2026-08-28

Dietary melatonin, chronotype, and night eating syndrome in relation to sleep quality among adults.

Geylani Selda S, Demirel Ozbek Yagmur Y, Arslan Nurgul N

Dietary melatonin has attracted increasing interest because of its potential relevance to circadian regulation and sleep health. However, evidence regarding its relationship with chronotype, night eating behaviors, and sleep quality remains limited. This study aimed to examine the associations among estimated dietary melatonin intake, chronotype, night eating behaviors, and sleep quality in adults and to explore the cross-sectional indirect association among chronotype, night eating behaviors, and sleep quality. This cross-sectional study was conducted in Istanbul, Türkiye, between November 2024 and June 2025 and included 325 adults aged 18-65 years. Sleep quality was assessed using the Pittsburgh Sleep Quality Index (PSQI), chronotype using the Morningness-Eveningness Questionnaire (MEQ), and night eating behaviors using the Night Eating Questionnaire (NEQ). Dietary melatonin intake was estimated using a modified food frequency questionnaire based on melatonin-containing foods. Pearson correlation analysis, multiple linear regression, binary logistic regression, and an exploratory cross-sectional indirect-association analysis using PROCESS Model 4 were performed. Mean total dietary melatonin intake was 10.485 ± 13.306 μg/day. PSQI scores were positively correlated with NEQ scores (r = 0.537, p < 0.001) and negatively correlated with MEQ scores (r = -0.159, p = 0.004). In the multiple linear regression model, NEQ score was positively associated with PSQI score (B = 0.198, standardized β = 0.491, 95% CI: 0.156-0.239, p < 0.001), whereas MEQ score was negatively associated with PSQI score (B = -0.067, standardized β = -0.189, 95% CI: -0.102 to -0.032, p < 0.001). Female sex and chronic disease presence were also statistically significant, whereas total and evening dietary melatonin intake were not associated with PSQI score after adjustment for the measured covariates. In the logistic regression model for night eating syndrome risk, PSQI score (OR = 1.328, 95% CI: 1.185-1.488, p < 0.001) and MEQ score (OR = 0.941, 95% CI: 0.897-0.988, p < 0.001) were statistically significant. The exploratory indirect-association analysis identified a statistically significant indirect association among chronotype, night eating behaviors, and sleep quality. Eveningness tendency and higher night eating scores were associated with poorer sleep quality, whereas estimated dietary melatonin intake was not associated with sleep quality after adjustment for the measured covariates. These findings should be interpreted as cross-sectional and hypothesis-generating. Longitudinal and intervention studies are needed to clarify temporal relationships and to determine whether chronotype-informed or chrononutrition-based approaches influence sleep-related outcomes.

PMID 42662821
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PubMedPharmaceutical development and technology2026-08-28

Innovative Hybrid Microneedle Patch for Co-delivery of Varenicline and Melatonin: Development, Characterization, and Potential for Smoking Cessation.

Shahriari Mohammad Hassan MH, Salmani Hossein H, Ghiass Mohammad Adel MA, Kamali Nader N et al.

This study aimed to develop a microneedle patch loaded with varenicline and melatonin to improve patient compliance and enhance transdermal delivery for smoking cessation. Smoking remains a major public health challenge. While varenicline is effective, oral administration can cause adverse effects, and vaccine-like approaches are limited by nicotine's small size. A painless, microneedle patch delivering varenicline together with melatonin could improve patient adherence and provide sustained delivery. Microneedle arrays were fabricated using a blend of polyvinyl alcohol (PVA) and polyvinylpyrrolidone (PVP), with Tween-80 added to enhance varenicline solubility. Comprehensive mechanical characterization, including nanoindentation, scratch testing, and atomic force microscopy, was performed. In vitro drug release and transdermal permeation studies were conducted, complemented by histological evaluation and fluorescence imaging. The microneedles exhibited high hardness, flexibility, and uniform surface topography, enabling effective skin penetration. In vitro studies showed cumulative transdermal permeation of 34.3% for varenicline and 41.6% for melatonin over 48 hours. The dual-drug-loaded microneedles demonstrated a sustained release profile. Histological analysis confirmed the creation of microchannels without damaging surrounding tissues. The combination of varenicline and melatonin in the microneedle shows promise in overcoming the limitations of current smoking cessation therapies, offering a patient-friendly and effective intervention. Future studies should include comparisons with commercial therapies and ex vivo dissolution studies (Q8).

PMID 42663429
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PubMedBiomaterials2026-08-28

Single-cell transcriptomic-driven design of cascade-responsive hydrogel with bioinspired nanocellular pacemaker for aged bone regeneration.

Gu Hui-Yun HY, Bao Peng P, Qu Wen-Qiang WQ, Lv Xiao-Dong XD et al.

Age-related bone defects remain poorly repaired due to a vicious cycle involving senescent bone marrow mesenchymal stem cells (BMSCs) and pro-inflammatory macrophages. We unveil circadian disruption as the underlying driver via single-cell transcriptomics and propose an "internal clock-repairing, external immunity-reprogramming" strategy. Inspired by cardiac pacemakers that sense signals and rectify rhythms, we engineer nanocellular pacemakers (AMC) with a "sense-release-regulate" paradigm for aged bone regeneration. AMC comprises melatonin-loaded, cobalt-based metal-organic frameworks (MOF) coated with membrane vesicles derived from the new generation of probiotic Akkermansia muciniphila. The cobalt-based MOF functions as an artificial sensor that specifically senses senescence-associated signals to release melatonin in the senescent microenvironment. The targeted delivery of melatonin repairs the internal clock and rejuvenates BMSCs by precisely regulating circadian rhythms to inhibit p53 and TNF signaling pathways. While probiotic membrane on AMC actively reprograms macrophages toward a pro-regenerative M2 phenotype in the senescent niche. To enable minimally invasive delivery, a dual-network hydrogel with reactive oxygen species-responsive boronic ester bonds is developed for spatiotemporal release of AMC. In aged mice, this cascade-responsive therapeutic system fully repairs bone defects within 4 weeks by breaking the senescence-inflammation vicious cycle, offering a novel "cellular pacing" paradigm for age-related tissue repair.

PMID 42664713
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