melatonin
Melatonin (5-methoxy N-acetyltryptamine) is a hormone synthesized and released from the pineal gland at night, which acts on specific high affinity G-protein coupled receptors to regulate various aspects of physiology and behaviour, including circadian and seasonal responses, and some retinal, cardiovascular and immunological functions. Melatonin is also made synthetically and available without a prescription as an over-the-counter (OTC) dietary supplement in the U.S. Melatonin supplementation has many uses, however, it has been widely studied for treatment of jet lag and sleep disorders. Parents may consider using melatonin to help their child who has a trouble falling asleep. A medical professional should always evaluate insomnia or other sleeping disorders in children. Additionally, melatonin has been shown to protect against oxidative stress in various, highly divergent experimental systems. There are many reasons for its remarkable protective potential. In mammals, melatonin binds to a number of receptor subtypes including high-affinity (MT1 and MT2) and low-affinity (MT3, nuclear orphan receptors) binding sites, which are distributed throughout the central nervous system and periphery. — NCATS
Clinical trial activity
433 trials · 372 clinical orgs · 0 marketing orgs
Earliest trial started Nov 1, 1995 (NCT00869128)
Timeline
Indications
Approved for
Studied for
- Abdominal Pain · Phase 1
- Acute Coronary Syndrome · Phase 2/Phase 3
- Acute Febrile Encephalopathy · Phase 1
- Acute Kidney Injury · Phase 3
- Air Travel · Phase 2/Phase 3
- Alcohol-Related Disorders · Phase 2
- Altitude Sickness · Early Phase 1
- Alveolar Bone Loss · Phase 3
- Alzheimer Disease · Phase 3
- Amyotrophic Lateral Sclerosis · Phase 2
- Analgesia · Phase 2/Phase 3
- Anesthesia · Phase 4
- Anxiety · Phase 4
- Anxiety Disorders · Phase 3
- Aortic Aneurysm · Phase 2/Phase 3
- Arthritis, Rheumatoid · Phase 1
- Arthroplasty · Phase 4
- Asphyxia · Phase 1/Phase 2
- Atrial Fibrillation · Phase 2
- Attention Deficit Disorder with Hyperactivity · Phase 4
- Autism Spectrum Disorder · Phase 3
- Autistic Disorder · Phase 1
- Autoimmune Diseases · Phase 1/Phase 2
- Autoimmune Diseases of the Nervous System · Phase 1/Phase 2
- Autonomic Nervous System Diseases · Early Phase 1
- Back Pain · Phase 3
- Bariatric Surgery · Phase 4
- Barrett Esophagus · Phase 3
- Benzodiazepines · Phase 3
- Binge-Eating Disorder · Phase 1/Phase 2
- Biological Availability · Phase 2
- Bipolar Disorder · Phase 4
- Blindness · Phase 2
- Blood Glucose · Phase 3
- Blood Pressure · Phase 3
- Bone Diseases, Metabolic · Phase 1
- Brain Concussion · Phase 2/Phase 3
- Brain Injuries · Phase 2
- Brain Injuries, Traumatic · Phase 4
- Breast Neoplasms · Phase 3
- Burns · Phase 2
- Carcinoma, Non-Small-Cell Lung · Phase 3
- Cardiomyopathies · Phase 1
- Carotid Stenosis · Phase 4
- Central Serous Chorioretinopathy · Phase 2/Phase 3
- Cesarean Section · Phase 1/Phase 2
- Child · Phase 4
- Chromosome Deletion · Phase 1
- Chronic Periodontitis · Phase 2
- Chronobiology Disorders · Phase 1/Phase 2
- Cognition Disorders · Phase 2
- Cognitive Aging · Phase 2
- Colitis, Ulcerative · Phase 2
- Colostomy · Phase 2
- Congenital, Hereditary, and Neonatal Diseases and Abnormalities · Phase 3
- Coronavirus Infections · Phase 2/Phase 3
- COVID-19 · Phase 2/Phase 3
- Critical Illness · Phase 4
- Deep Sedation · Phase 4
- Delirium · Phase 4
- Dementia · Phase 4
- Dengue Virus · Phase 2
- Dental Anxiety · Phase 4
- Dental Implantation · Phase 4
- Dentofacial Deformities · Phase 2
- Depression · Phase 4
- Dermatitis, Atopic · Phase 2/Phase 3
- Dermatology · Phase 1
- Developmental Disabilities · Phase 3
- Diabetes Mellitus · Phase 4
- Diabetes Mellitus, Type 1 · Early Phase 1
- Diabetes Mellitus, Type 2 · Phase 2
- Diabetic Neuropathies · Phase 2
- Diabetic Retinopathy · Phase 3
- Dialysis · Phase 3
- Disorders of Excessive Somnolence · Phase 2
- DNA Repair-Deficiency Disorders · Phase 4
- Drug-Related Side Effects and Adverse Reactions · Phase 4
- Dysmenorrhea · Phase 2
- Dyspepsia · Phase 1
- Dyssomnias · Phase 3
- Electroencephalography · Phase 3
- Emergence Delirium · Phase 4
- Endometriosis · Phase 2
- Endotoxemia · Phase 4
- Enterocolitis, Necrotizing · Phase 4
- Epilepsy · Phase 3
- Epilepsy, Generalized · Phase 4
- Essential Hypertension · Phase 2
- Eye Diseases · Phase 2/Phase 3
- Fatigue · Phase 2/Phase 3
- Fatigue Syndrome, Chronic · Phase 4
- Feeding and Eating Disorders · Phase 4
- Fertilization in Vitro · Phase 3
- Fetal Growth Retardation · Phase 4
- Fibromyalgia · Phase 2/Phase 3
- Gastroesophageal Reflux · Phase 3
- Gastrointestinal Neoplasms · Phase 3
- General Surgery · Early Phase 1
- Glucose Metabolism Disorders · Phase 1/Phase 2
- Growth and Development · Phase 2
- Head and Neck Neoplasms · Phase 2
- Healthy Volunteers · Phase 4
- Heart · Phase 1
- Heart Arrest · Phase 4
- Heart Failure · Phase 2
- Heart Failure, Systolic · Phase 2
- Hematoma · Phase 1
- Hemodialysis, Home · Phase 3
- Hemodynamics · Phase 2/Phase 3
- Herpes Genitalis · Phase 4
- Hot Flashes · Phase 1/Phase 2
- Hypertension · Phase 2
- Hypertension, Pulmonary · Phase 3
- Hypotension, Orthostatic · Early Phase 1
- Hypoxia-Ischemia, Brain · Early Phase 1
- Infant Mortality · Phase 3
- Infant, Premature · Phase 4
- Infant, Premature, Diseases · Phase 1
- Infertility · Phase 4
- Inflammation · Phase 3
- Insulin Resistance · Phase 1
- Intellectual Disability · Phase 1
- Intubation · Phase 2/Phase 3
- Irritable Bowel Syndrome · Phase 3
- Ischemia · Early Phase 1
- Ischemic Stroke · Phase 4
- Jet Lag Syndrome · Phase 2
- Keratosis, Actinic · Phase 2
- Kidney Failure, Chronic · Phase 2/Phase 3
- Laryngoscopy · Phase 2/Phase 3
- Lennox Gastaut Syndrome · Phase 4
- Leukemia, Lymphoid · Phase 1
- Liver Diseases · Phase 4
- Liver Transplantation · Phase 3
- Low Back Pain · Phase 3
- Lung Neoplasms · Phase 3
- Lymphoma · Phase 2
- Macula Lutea · Phase 2/Phase 3
- Major Depressive Disorder · Phase 2
- Matrix Metalloproteinases · Phase 4
- Melanoma · Phase 3
- Melanosis · Phase 4
- Melatonin · Phase 4
- Menopause · Phase 2/Phase 3
- Mental Disorders · Phase 2/Phase 3
- Mental Health · Phase 3
- Metabolic Diseases · Phase 1
- Metabolic Syndrome · Phase 2
- Migraine Disorders · Phase 3
- Motor Activity · Early Phase 1
- Mucositis · Phase 2
- Multiple Sclerosis · Phase 1/Phase 2
- Multiple Sclerosis, Relapsing-Remitting · Phase 2
- Myocardial Infarction · Phase 2
- Myocardial Ischemia · Phase 2
- Narcotics · Phase 2
- Neoadjuvant Therapy · Phase 3
- Neonatal Sepsis · Phase 1/Phase 2
- Neoplasms · Phase 3
- Nervous System Diseases · Phase 1/Phase 2
- Neurodevelopmental Disorders · Phase 3
- Nocturia · Phase 2
- Nocturnal Enuresis · Phase 2
- Obesity · Phase 3
- Optic Nerve Hypoplasia · Early Phase 1
- Orthognathic Surgery · Phase 2/Phase 3
- Orthopedic Procedures · Phase 3
- Orthostatic Intolerance · Phase 1/Phase 2
- Osteoporosis · Phase 1
- Osteoporosis, Postmenopausal · Phase 4
- Ovarian Diseases · Phase 2/Phase 3
- Oxidative Stress · Phase 4
- Pain · Phase 4
- Parkinson Disease · Phase 4
- Periodontal Diseases · Phase 4
- Periodontitis · Phase 4
- Peritoneal Dialysis · Phase 3
- Pharmacokinetics · Phase 1/Phase 2
- Pinealoma · Early Phase 1
- Pneumonia · Phase 1/Phase 2
- Polycystic Ovary Syndrome · Phase 4
- Post-Concussion Syndrome · Phase 2/Phase 3
- Postoperative Complications · Phase 4
- Postoperative Pain · Phase 4
- Posture · Phase 4
- Prediabetic State · Phase 3
- Pregnancy Complications · Phase 3
- Premature Birth · Phase 2/Phase 3
- Premedication · Phase 4
- Procedural Sedation · Phase 3
- Prognathism · Phase 2/Phase 3
- Prostheses and Implants · Phase 1
- Psychophysiologic Disorders · Phase 3
- Psychotic Disorders · Phase 4
- Pulmonary Arterial Hypertension · Phase 3
- Quality of Life · Phase 1/Phase 2
- Radiodermatitis · Phase 2
- Recurrence · Phase 4
- REM Sleep Behavior Disorder · Phase 4
- Renal Dialysis · Phase 3
- Renal Insufficiency, Chronic · Phase 2/Phase 3
- Reperfusion Injury · Phase 2
- Retrognathia · Phase 2/Phase 3
- Safety · Phase 1
- Schizophrenia · Phase 4
- Seizures, Febrile · Phase 4
- Self-Injurious Behavior · Phase 1
- Sepsis · Phase 3
- Shock, Septic · Phase 4
- Sleep · Phase 2/Phase 3
- Sleep Apnea, Obstructive · Phase 4
- Sleep Deprivation · Phase 3
- Sleep Disorders, Circadian Rhythm · Phase 4
- Sleep Disorders, Intrinsic · Phase 4
- Sleep Initiation and Maintenance Disorders · Phase 3
- Sleep Quality · Phase 4
- Sleep Wake Disorders · Phase 4
- Smoking · Phase 4
- Somatosensory Disorders · Phase 2/Phase 3
- Spinal Cord Injuries · Phase 1
- Squamous Cell Carcinoma of Head and Neck · Phase 3
- Stillbirth · Phase 3
- Stomatitis · Phase 1/Phase 2
- Stroke · Phase 4
- Substance Withdrawal Syndrome · Phase 1/Phase 2
- Sunburn · Phase 1
- Tachycardia · Phase 1/Phase 2
- Thrombotic Stroke · Phase 4
- Tooth Abnormalities · Phase 3
- Treatment Outcome · Phase 4
- Vascular Calcification · Phase 4
- Vascular System Injuries · Phase 4
- Ventilation · Phase 4
- Visual Acuity · Phase 2/Phase 3
- Wasting Syndrome · Phase 2
- Wound Healing · Phase 2
Mechanism of action
- Melatonin receptorAGONIST
Melatonin receptor agonist
- Melatonin receptorAGONIST
Melatonin receptor agonist
Sleep promoting activity.
Active at the MT1, MT2 and MT3 receptors but the MT1 and MT2 are thought to be most relevant to the mechanism of action.
Approval history
- approved—
Chemistry & pharmacology
SMILES
COC1=CC2=C(NC=C2CCNC(C)=O)C=C1- Mol. weight
- 232.2783 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaMelatonin ↗
- NCATSJL5DK93RCL ↗
- ChEMBLCHEMBL45 ↗
Also known as
- 5-methoxy-n-acetyltryptamine
- 5-methoxy-n-acetyltryptamine
- bci-049
- circadin
- circadin
- circadin
- circadin
- general nutrit
- health aid
- heidadouppi
- icenia
- life ext
- melapure
- melapure
- melatol
- melatonin
- melatonin
- melatonin
- melatonin
- melatonin
- melatonin
- melatonin
- melatonin
- melatonin
- melatonine
- melatonine
- melatonine
- n-(2-(5-methoxy-1h-indol-3-yl)ethyl)acetamide
- n-(2-(5-methoxy-1h-indol-3-yl)ethyl)acetamide
- n-[2-(5-methoxyindol-3-yl)ethyl]acetamide
- n-[2-(5-methoxyindol-3-yl)ethyl]acetamide
- n-acetyl-5-methoxytryptamine
- n-acetyl-5-methoxytryptamine
- n-acetyl-5-methoxytryptamine
- n-acetyl-5-methoxytryptamine
- natrol
- natrol
- nature's blend
- natures bounty
- quality health
- s.gard
- travelag
- vespro
- vytalonin
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07221968 | Phase 2 | Jul 1, 2026 | Hugo W. Moser Research Institute at Kennedy Krieger, Inc., Johns Hopkins University |
| NCT07305350 | Phase 2 | Dec 10, 2025 | University of Child Health Sciences and Children's Hospital, Lahore |
| NCT07096635 | N/A | Oct 1, 2025 | Assiut University |
| NCT07138443 | N/A | Aug 31, 2025 | Baylor University |
| NCT07046429 | N/A | Aug 5, 2025 | American Association for the Study of Liver Diseases, Cornell University |
| NCT07067307 | Phase 1/Phase 2 (Phase 2) | Jul 31, 2025 | Mansoura University |
| NCT07036796 | Phase 2 | Jul 4, 2025 | Ain Shams University |
| NCT07036367 | Phase 4 | Jul 1, 2025 | Al Azhar University |
| NCT07169383 | Phase 2 | Jun 28, 2025 | PAEC General Hospital, Islamabad |
| NCT07162272 | Phase 4 | Jun 25, 2025 | Ain Shams University |
| NCT06949904 | Phase 1/Phase 2 (Phase 2) | May 31, 2025 | College of Physicians and Surgeons Pakistan |
| NCT07003243 | Phase 1 | May 26, 2025 | University of Baghdad |
| NCT06996171 | N/A | May 5, 2025 | CMH Kharian Medical College |
| NCT06935292 | Phase 2/Phase 3 (Phase 3) | Apr 30, 2025 | Tanta University |
| NCT07062757 | N/A | Mar 30, 2025 | Bezmialem University |
| NCT06872944 | Early Phase 1 (Phase 1) | Mar 21, 2025 | Cairo University |
| NCT06859957 | Phase 3 | Mar 19, 2025 | Erasmus University Rotterdam |
| NCT07307677 | N/A | Mar 11, 2025 | Bangladesh Medical University |
| NCT06802913 | Early Phase 1 (Phase 1) | Feb 28, 2025 | Woolcock Institute of Medical Research |
| NCT06846086 | Phase 1 | Feb 20, 2025 | Tanta University |
Organizations
Research & Development (372)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| University of Copenhagen | Academic/Hospital | 20 | 16 | 4 | 2005 |
| Ain Shams University | Academic/Hospital | 19 | 18 | 4 | 2013 |
| Harvard University | Academic/Hospital | 16 | 13 | 5 | 2005 |
| Neurim Pharmaceuticals Ltd. | For profit | 12 | 9 | 4 | 1995 |
| Oregon Health and Science University | Academic/Hospital | 9 | 7 | 3 | 1997 |
| Tel Aviv University | Academic/Hospital | 9 | 9 | 4 | 2004 |
| Cairo University | Academic/Hospital | 8 | 8 | 4 | 2018 |
| Aarhus University | Academic/Hospital | 7 | 5 | 5 | 2012 |
| National Institutes of Health (NIH) | Government | 7 | 1 | 3 | 1997 |
| Tanta University | Academic/Hospital | 7 | 7 | 5 | 2012 |
| University of Texas at Houston | Academic/Hospital | 6 | 6 | 4 | 2004 |
| Emory University | Academic/Hospital | 5 | 4 | 2 | 2009 |
| Isfahan University | Academic/Hospital | 5 | 5 | 3 | 2010 |
| Kuhnil Pharmaceutical Co., Ltd. | For profit | 5 | 3 | 3 | 2011 |
| University of California, San Diego | Academic/Hospital | 5 | 4 | 3 | 2004 |
| University of Sao Paulo | Academic/Hospital | 5 | 4 | 4 | 2015 |
| University of Toronto | Academic/Hospital | 5 | 5 | 3 | 2010 |
| Al Azhar University | Academic/Hospital | 4 | 3 | 3 | 2023 |
| Alexandria University | Academic/Hospital | 4 | 4 | 2 | 2018 |
| Duquesne University | Academic/Hospital | 4 | 4 | 2 | 2008 |