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melatonin

✓ Approved

Clinigen Group · MTNR1A · 小分子

什么是 melatonin？

melatonin 是一种小分子，由Clinigen Group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

公司Clinigen Group
药物类别小分子
分子靶点MTNR1A, MTNR1B
给药途径Oral (PO)
状态Approved
来源： ClinicalTrials.gov, Clinigen Group

作用机制

分子靶点

melatonin 作用于 2 个分子靶点：

MTNR1Amelatonin receptor 1A (MEL-1A-R, MT1)
MTNR1Bmelatonin receptor 1B (FGQTL2, MT2)
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

melatonin 针对 2 个适应症，涉及 1 个治疗领域。

治疗领域疾病/病症分期
Psychiatric disordersInsomnia✓ Approved
Psychiatric disordersSleep disorder✓ Approved

相关研究文献

PubMedDoklady biological sciences : proceedings of the Academy of Sciences of the USSR, Biological sciences sections2026-08-04

Continuous Light Exposure as Factor in Pro-Senescent Liver Remodeling: Key Role of Melatonin Deficiency.

Areshidze D A DA, Kozlova M A MA, Anurkina A I AI, Moskalev A A AA

Circadian rhythm disruption is a risk factor for metabolic and age-associated diseases. The liver is a key target of such desynchronosis. The effect of chronic continuous light exposure and the corrective effect of melatonin on the liver status were investigated in rats. Desynchronosis mediated by melatonin deficiency was shown to induce the formation of a pro-senescent and metabolically dysfunctional liver phenotype. Melatonin administration significantly reduced the severity of the identified disorders and prevented statistically significant deviations in most of the parameters under study. The results, together with previous data on ultrastructural damage to hepatocytes and a negative impact of desynchronosis on lifespan, indicate that chronic continuous light exposure is a significant pro-gerontological factor and that melatonin is an effective agent for correcting the associated disturbances of liver homeostasis.

PMID 42550425
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PubMedAdvanced healthcare materials2026-08-04

Stability of Medicinal Nanoemulsions to Spaceflight: Insights From the StarMed Experiment.

Adebowale Modupe M, Long Nguyen Van Duc NVD, Williams Philip M PM, Hauslage Jens J et al.

Space missions require liquid drug formulations that remain physically stable and exhibit predictable release under launch, microgravity, and handling stresses. This study examined melatonin‑loaded nanoemulsions flown on the MAPHEUS‑15 sounding rocket, comparing an uncoated nanoemulsion (MN) with a chitosan‑coated nanoemulsion (CCN). Droplet size, polydispersity index (PDI), and zeta potential were measured at Day 0 and after spaceflight, ground vibration testing, matched ground controls, and laboratory storage. Melatonin release was quantified by dynamic dialysis and interpreted using a compartmental mass-transfer model. Melatonin‑loaded nanoemulsion (MN) showed a modest, systematic increase in droplet size under all post‑experiment conditions, with unchanged PDI and zeta potential, consistent with time‑dependent coalescence and Ostwald ripening rather than a specific microgravity effect. CCN maintained essentially unchanged droplet size, PDI, and zeta potential, indicating interfacial steric stabilization by chitosan. For MN, ageing and sounding‑rocket exposure increased the apparent fraction of melatonin available to the aqueous phase, but normalized release profiles overlapped when scaled to the fitted maximum releasable fraction, suggesting unchanged intrinsic release kinetics. In CCN, both the accessible fraction and the release profile were preserved. Overall, chitosan coating enhanced dimensional and release stability, supporting interfacial polymer coatings as a strategy for robust liquid pharmaceutical formulations for future space medicine.

PMID 42549747
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PubMedNeoplasma2026-08-04

Neuroimmune treatment of advanced solid tumors: 3-year survival after angiotensin 1-7, pineal indoles, and cannabinoids.

Lissoni Paolo P, Monzon Alejandra A, Marroccoli Savino S, Di Fede Giuseppe G et al.

In a recent study, the exogenous administration of angiotensin 1-7 (Ang 1,7) together with melatonin, 5-methoxytryptamine, and cannabidiol increased 1-year survival in advanced cancer patients, underlining the utility of neuromodulation in oncology. We now report a single-arm interventional study to evaluate the effectiveness of introducing Ang 1-7 in the neuroimmune regime, including pineal indoles and cannabinoids. Two cohorts of patients with advanced solid tumors refractory to standard oncologic treatments and with an estimated life expectancy of less than six months were studied. The full neuroimmune regimen cohort consisted of 100 consecutive patients treated over the last three years with Ang 1-7, pineal indoles, and cannabinoids, while the comparator cohort included 212 consecutive patients treated between 2015 and 2019 with pineal indoles and cannabinoids alone. Gastroprotected capsules of Ang 1-7 coupled with cyclodextrin were administered at 0.5 mg p.o. twice/day. Melatonin (100 mg) and 5-methoxytryptamine (20 mg) were given p.o. at bedtime and in the early afternoon, respectively. Cannabidiol or cannabigerol (in the case of glioblastoma) was given at 20 mg p.o. twice/day. Clinical response, disease control, and overall survival, along with the lymphocyte-to-monocyte ratio, were evaluated. In the full regimen cohort, disease control was achieved in 67 of 100 patients, with objective tumor regression observed in 23%. In the comparator cohort, disease control was obtained in 111 of 212 patients, with objective regression in 8%. Three-year overall survival was significantly higher in the full regimen cohort (37%) compared with the comparator cohort (19%). Both treatments were associated with a significant increase in the lymphocyte-to-monocyte ratio, suggesting an improvement in systemic immune status. The addition of Ang 1-7 to a neuroimmune regimen combining pineal indoles and cannabinoids was associated with improved disease control and long-term survival in patients with end-stage solid tumors lacking effective therapeutic options.

PMID 42549589
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PubMedOral diseases2026-08-04

Mapping the Bioenergetic Landscape of Oral Cancer Stem Cells: A Systematic Review.

de Sá Rodrigo Elísio RE, da Rocha Rebeca Barbosa RB, Alves Benedito Dos Santos BDS, de Carvalho Maria Eduarda de Araujo MEA et al.

Oral squamous cell carcinoma (OSSC) remains highly lethal, with resistance largely driven by cancer stem cells (CSCs). Mitochondrial reprogramming supports CSC redox control, self-renewal, and survival. This systematic review aimed to synthesize mitochondrial mechanisms sustaining CSCs in OSCC and evaluate their therapeutic relevance. Following PRISMA guidelines and a PROSPERO protocol (CRD420251088208), we searched major databases for studies investigating mitochondrial biogenesis, dynamics, mitophagy, or redox regulation in oral CSCs. Extracted data included molecular pathways, functional roles, and pharmacological targeting. Ten studies were eligible. Evidence shows that mitochondrial remodeling, through PGC-1α/ERRα-mediated biogenesis, DRP1-dependent fission, BNIP3/PINK1-regulated mitophagy, and NRF2-driven antioxidant signaling, supports metabolic flexibility and drug tolerance. These pathways activate stemness regulators, including EGFR/JNK/SOX2, YAP/CCN1, and SIRT1/PGC-1α, promoting adaptation and recurrence. Pharmacological interventions targeting these nodes, such as DRP1 inhibitors, SIRT1 or ERRα antagonists, and mitophagy-modulating agents (melatonin, verteporfin), showed potential to sensitize CSCs to conventional therapies. Mitochondria act as central regulators of CSC biology in OSCC and represent actionable therapeutic targets. Integrating mitochondrial dynamics, metabolism, and redox control provides a framework for overcoming resistance. Further preclinical and clinical studies are needed to translate these vulnerabilities into effective OSCC therapies. PROSPERO, CRD420251088208.

PMID 42547908
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PubMedAnimal genetics2026-08-03

A Functional SNP in the Promoter Region of Ovine IDO2 Associated With Melatonin Levels via Affecting Transcription Activity by CLOCK.

Jiang Xunping X, Chi Shaxuan S, Wang Xiaodong X, Chen Mengya M et al.

Sheep seasonal reproduction is regulated by photoperiod via melatonin. Indoleamine 2,3-dioxygenase 2 (IDO2), an enzyme involved in tryptophan metabolism through the kynurenine pathway and belonging to the IDO family, may contribute to melatonin homeostasis, but its role in reproductive seasonality remains unclear. In this study, genome-wide selection analyses combining Z(FST) and XP-EHH between seasonal and non-seasonal sheep identified a selection signature encompassing the IDO2 region and revealed g.-809T>C as a functional candidate variant within this region. Experiments employing electrophoretic mobility shift assay (EMSA) and luciferase assays revealed that this site lies within the CLOCK transcription factor binding domain. The -809C variant reduced promoter activity compared to -809T (p < 0.05). Sheep with the CC genotype had higher plasma melatonin levels than TC/TT counterparts (p < 0.05). These findings suggest that the g.-809C allele decreases IDO2 transcription by reducing CLOCK binding affinity, thereby potentially affecting IDO2-associated tryptophan/melatonin metabolism and increasing melatonin levels, which may contribute to photoperiodic responses in sheep. This IDO2 variation provides new insights into the genetic regulation of melatonin-mediated reproductive seasonality and represents a potential marker for genetic improvement of reproductive seasonal traits in sheep.

PMID 42543215
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PubMedBiosensors & bioelectronics2026-08-03

Au nanocoral-gated needle-type organic electrochemical transistor for ultrasensitive in vivo melatonin detection.

Zhong Junchi J, Zhao Qiang Q, Yang Biru B, Tang Lina L et al.

Melatonin is a key endocrine output of the circadian system, but its low endogenous abundance and dynamic fluctuation make accurate detection in biological samples challenging. Here, we report a highly sensitive needle-type organic electrochemical transistor (OECT) biosensor for melatonin detection based on an Au nanocoral-gated acupuncture needle. A hierarchically nanoporous coral-like Au structure was fabricated on the needle surface via a dynamic hydrogen bubble templating strategy, generating a high-surface-area and highly electroactive gate for immobilization of a thiolated melatonin aptamer. By integrating this recognition-enhancing nanostructured gate with the intrinsic signal amplification capability of the OECT, the platform efficiently converts interfacial molecular recognition into amplified electrical outputs. The optimized biosensor achieved a detection limit of 160 fM, showed good selectivity against structurally related interferents, and maintained reliable performance in serum-containing media. In rat plasma, the biosensor showed satisfactory agreement with ELISA and accurately tracked the circadian secretion profile of melatonin. Moreover, the needle-type configuration enabled skin-interfaced measurements and interstitial-fluid detection without causing obvious extensive tissue damage under short-term insertion conditions. The platform further resolved circadian phase shifts induced by light-dark reversal, demonstrating its ability to study physiologically meaningful endocrine dynamics. These results highlight this OECT platform as a promising strategy for low-abundance melatonin analysis, minimally invasive biosensing, and circadian rhythm analysis.

PMID 42546381
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