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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

PubMedElectromagnetic biology and medicine2026-11-11

Effects of 900 MHz electromagnetic field exposure on the optic nerve of pregnant rats: Evaluation of melatonin and omega-3.

Kaplan Arife Ahsen AA, Uzun Kübra Nur KN, Altun Gamze G, Aktaş Abit A et al.

This study investigated the effects of 900 MHz electromagnetic field (EMF) exposure on the maternal optic nerve and evaluated the potential modulatory effects of melatonin and omega-3. Pregnant Wistar albino rats were divided into Control, Sham, EMF, EMF+melatonin (EMF+Mel), and EMF+omega-3 (EMF+ω3) groups. The EMF, EMF+Mel, and EMF+ω3 groups were exposed to 900 MHz EMF for 2 h/day throughout the 21-day gestational period. Optic nerves were examined using stereological and transmission electron microscopic methods. The number of myelinated nerve fibers was significantly higher in the EMF group compared to the Sham group, whereas axon diameter, myelin sheath thickness, and g-ratio did not differ significantly among groups. Ultrastructural examination of the EMF group revealed a common axoplasmic vacuolization, separation of myelin lamellae, and degeneration of axons and nerve fiber bundles. Most myelinated fibers in the EMF+Mel group exhibited relatively preserved ultrastructure, although some alterations remained. In contrast, balloon-like vacuolization of the myelin sheath and axoplasm persisted in the EMF+ω3 group. These findings indicate that gestational 900 MHz EMF exposure induces measurable quantitative and ultrastructural alterations in the maternal optic nerve, while melatonin, but not omega-3, appears to provide partial preservation of nerve fiber ultrastructure.

PMID 43012736
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PubMedFood chemistry2026-11-10

Phytomelatonin enrichment through stress-modulated germination: effects of salinity and melatonin priming in edible seeds and its application to soymilk.

Utaida Treechada T, Loypimai Patiwit P, Moongngarm Anuchita A

This study investigated stress-modulated germination combined with melatonin priming for phytomelatonin enrichment in edible seeds, using soybean as a model and extending the approach to 12 edible seed species. Soybean seeds were germinated under control, salinity (0.5% NaCl), melatonin priming (50 μM), and combined salinity-melatonin treatments. Germination performance, ASMT activity, total melatonin content, tryptophan, and serotonin were evaluated. Salinity suppressed germination, whereas melatonin priming restored germination to approximately 80-82% at 72-96 h. Combined treatment markedly increased ASMT activity and total melatonin, reaching 7023.98 ng/g DW at 72 h, compared with 271.52 and 28.39 ng/g DW under control and salinity treatments, respectively. Across 12 species, total melatonin reached 1824-7244 ng/g DW following combined treatment. Germinated soybean was subsequently applied to soymilk production, increasing total melatonin content. This approach provides a food-compatible strategy for phytomelatonin enrichment, although further studies are required to clarify underlying mechanisms and functional relevance.

PMID 43008628
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PubMedAdvanced pharmaceutical bulletin2026-11-10

Design, Characterization, and In-Vitro Targeted Delivery of Melatonin via pH-Responsive Niosome Nanoparticles Decorated with Folate Against Colon Cancer Cells.

Jafari-Gharabaghlou Davoud D, Alali Urjwan U, Al-Tu'ma Fadhil Jawad FJ, Babavalian Hamid H et al.

Utilizing targeted drug delivery in oncology represents a valuable strategy to enhance the therapeutic efficacy of chemotherapy and simultaneously mitigate its adverse effects. Our present investigation focused on harnessing the therapeutic properties of melatonin as an anti-cancer agent and improving its bioavailability by employing a drug delivery system based on folic acid-decorated niosomal nanoparticles. To deliver melatonin, a niosomal and a folic acid decorated niosomal system was used. Nanoparticles were synthesized with the thin film hydration method and characterized by AFM, SEM, DLS, and FT-IR techniques. The cytotoxic effects and changes in gene expression were assessed using MTT and real-time PCR techniques, respectively. Additionally, flow cytometry experiments were conducted to investigate their impact on cell cycle arrest and apoptosis induction. Nanoparticle analysis revealed that the size distribution of blank niosomes, melatonin-loaded niosomal nanoparticles, and melatonin-loaded folic acid-decorated niosomal nanoparticles were 157±8.96 nm, 198±12.34 nm, and 239.9±39.64 nm, respectively. Controlled release studies indicated that over 96 hours, the maximum amount of melatonin released was approximately 60% at pH 7.4 and 73% at pH 5. The results demonstrated enhanced cell cytotoxicity of melatonin when encapsulated in melatonin-loaded folic acid-decorated niosomal compared to pure melatonin and niosomal nanoparticles. Furthermore, melatonin-loaded folic acid-decorated niosomal nanoparticles exhibited superior outcomes in terms of promoting apoptosis and cell cycle arrest compared to other tested substances. Overall, melatonin-loaded folic acid-decorated niosomal nanoparticles demonstrate a significant capability as an effective therapeutic strategy for targeting colorectal cancer cells.

PMID 43005126
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PubMedFood chemistry2026-11-10

Impacts of preharvest melatonin and salicylic acid treatments on storage quality and antioxidant components of seedless 'BRS Vitória' table grapes.

Brito Sinara de Nazaré Santana SNS, Nunes Aline A, Garcia Vitor Augusto Dos Santos VADS, Tecchio Marco Antonio MA et al.

This study evaluated preharvest melatonin (M) and salicylic acid (SA) effects on 'BRS Vitória' grapes stored at 5 °C for 15 days. Treatments included M (0.02, 0.05, 0.1 mmol L-1), SA (1.0 mmol L-1), and their combinations. 0.1 mmol L-1 M and 1.0 mmol L-1 SA + 0.02 mmol L-1 M (SAM 0.02) significantly reduced mass loss and berry drop, with SAM 0.02 preventing decay throughout storage. These treatments enhanced total phenolics (from 59.71 to 359.35 mg 100 g-1), flavonoids, and antioxidant activity (>70% by DPPH). HPLC revealed increased gallic acid, resveratrol, and malvidin-3,5-diglucoside. Furthermore, elicitation triggered metabolic shifts, raising endogenous melatonin and polyamines (spermidine, spermine), which improved membrane stability and stress tolerance. Toxic biogenic amines remained well below safety thresholds, validating the protocol for commercial use. Preharvest M and SA are effective, sustainable strategies to enhance the bioactive profile and shelf life of hybrid grapes.

PMID 43008625
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PubMedVeterinary research forum : an international quarterly journal2026-11-10

A combination of melatonin and nicotinamide mononucleotide alleviates inflammation and enhances isolated heart function in aged rats following ischemia-reperfusion injury.

Amanzadeh Paria P, Pourheydar Bagher B, Akbari-Gharalari Naeimeh N, Chodari Leila L et al.

Aging markedly increases vulnerability to cardiovascular disorders, including acute coronary syndrome and coronary artery disease. Although melatonin (M) and nicotinamide mono-nucleotide (N) have each shown cardioprotective properties, their combined effects on ischemia-reperfusion (IR) injury in the aged heart remain unclear. This study investigated co-administration of M and N enhances cardiac functional recovery and reduces inflammatory responses following myocardial IR injury in aged rats. Forty adult male Wistar rats (n = 8/group) were randomly assigned to five groups: Sham, IR, M (IR + M), N (IR + N), and N + M (IR + N + M). Cardiac function was evaluated after IR by measuring coronary flow, heart rate, left ventricular end-diastolic pressure, and left ventricular developed pressure. Melatonin was administered at 50.00 µM in the reperfusion solution for 15 min after 30 min of ischemia, N was administered intraperitoneally at 100 mg kg-1 every other day for 28 days. Creatine kinase and inflammatory markers, including interleukin IL-1β, IL-6, tumor necrosis factor-alpha, and nuclear factor kappa B, were also assessed. IR significantly impaired coronary flow and heart rate, both of which were improved by M and N treatment. These agents also reduced left ventricular end-diastolic pressure and improved left ventricular developed pressure recovery, with the combined therapy producing the greatest effect. Likewise, creatine kinase and inflammatory marker levels were significantly elevated in the IR group but markedly reduced by treatment, especially by combined administration. These findings suggest that M and N exert additive cardioprotective effects against IR injury in aged rats.

PMID 43005678
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PubMedFrontiers in aging neuroscience2026-11-10

Ramelteon suppresses astrocytic senescence via MT1-cAMP axis to protect dopaminergic neurons.

Gu Chao C, Chen Yajing Y, Du Xiaohuan X, Li Fang F et al.

Astrocytic senescence is increasingly recognized as a critical contributor to the pathogenesis of Parkinson's disease (PD). Ramelteon, a clinically approved MT1/MT2 melatonin receptor agonist, has demonstrated neuroprotective effects in various neurological disorders. However, whether Ramelteon can inhibit astrocytic senescence and the underlying mechanisms remain unknown. An in vivo MPTP-induced mouse model of PD was used to evaluate the therapeutic potential of Ramelteon. An in vitro long-term culture-induced replicative senescence model (40 days in vitro, DIV) and MPP+-induced premature senescence model in primary astrocytes were employed. Immunoblotting, real-time quantitative PCR, immunofluorescence, SA-β-gal staining, and immunohistochemistry were performed to assess astrocytic senescence, dopaminergic neuronal survival, and motor function. Ramelteon treatment significantly attenuated MPTP-induced dopaminergic neuronal loss in the substantia nigra compacta (SNc) and improved motor deficits in mice. In vitro, Ramelteon markedly suppressed both replicative and MPP+-induced astrocytic senescence, as evidenced by decreased p16Ink4a and SA-β-gal activity, restored LaminB1 expression, and reduced senescence-associated secretory phenotype (SASP) factors (IL-6, IL-1β, CXCL10, and MMP9). Mechanistically, knockdown of Mtnr1a (encoding MT1), but not Mtnr1b (encoding MT2), largely abolished the anti-senescence effects of Ramelteon. MT1 activation inhibited adenylate cyclase (AC) activity and reduced intracellular cyclic adenosine monophosphate (cAMP) levels. Notably, senescent astrocytes exhibited elevated cAMP levels, and the cAMP inhibitor SQ22536 mimicked while the cAMP analog dbcAMP reversed the anti-senescence effects of Ramelteon. Furthermore, Ramelteon reduced mitochondrial ROS (mitoROS) production in senescent astrocytes through MT1-cAMP signaling. Our findings demonstrate that Ramelteon inhibits astrocytic senescence through MT1 receptor-mediated cAMP suppression and mitochondrial ROS reduction, thereby protecting DA neurons in a PD mouse model. This study identifies Ramelteon as a potential therapeutic agent for PD by suppressing astrocytic senescence through MT1 activation.

PMID 43005157
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