Active Ingredient History
Sitagliptin (MK-0431), chemically (2R)-4-Oxo-4-[3- (trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl]-1-(2,4,5-trifl uorophenyl)butan-2-amine has a very high selectivity towards DPP-4, with an IC(50) of 18 nM. There is no affinity towards other DDP enzymes (DPP- 8 and DPP-9). It has been approved for the treatment of type 2 diabetes in the USA and Europe and is registered by the name Januvia (Merck Pharmaceuticals, Whitehouse Station, NJ, USA). In healthy volunteers and in patients with type 2 diabetes of different ethnic background, the tolerability of different doses given once or twice daily is good. The drug works to competitively inhibit a protein/enzyme, dipeptidyl peptidase 4 (DPP-4), that results in an increased amount of active incretins (GLP-1 and GIP), reduced amount of release of glucagon (diminishes its release) and increased release of insulin. Sitagliptin is an incretin enhancer and the first marketed medication belonging to the gliptin class. In fact, no published literature exists regarding incidence or severity of hypoglycemia when sitagliptin is used off-label in combined with insulin therapy. However, is recommended to use methods to avoid hypoglycemia when using this off-label combination. Approximately 79% of sitagliptin is excreted unchanged in the urine with metabolism being a minor pathway of elimination. Elimination of sitagliptin occurs primarily via renal excretion and involves active tubular secretion. Sitagliptin is a substrate for human organic anion transporter-3 (hOAT-3), which may be involved in the renal elimination of sitagliptin NCATS
Drug Pricing (per unit)
Note: This drug pricing data is preliminary, incomplete, and may contain errors.
Combination drugs
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
| Organization | Org Type | FDA approvals | Clinical Trials involvement | Org ID | Force Sort |
|---|
Abortion, Habitual (Phase 4)
Abortion, Spontaneous (Phase 3)
Acanthosis Nigricans (Phase 4)
Acromegaly (Phase 4)
Acute Coronary Syndrome (Phase 4)
Acute-On-Chronic Liver Failure (Phase 4)
Adenocarcinoma (Phase 2)
Adenocarcinoma, Bronchiolo-Alveolar (Phase 2)
Adenocarcinoma of Lung (Phase 2)
Adenomatous Polyposis Coli (Phase 2)
Adenomatous Polyps (Phase 2)
Aging (Phase 4)
Albuminuria (Phase 4)
Altitude Sickness (Phase 4)
Alzheimer Disease (Phase 3)
Amenorrhea (Phase 4)
Anemia (Phase 1)
Anemia, Sickle Cell (Early Phase 1)
Angina Pectoris (Phase 4)
Angina, Unstable (Phase 4)
Anovulation (Phase 4)
Anxiety Disorders (Phase 1)
Art (Phase 1/Phase 2)
Arteriosclerosis (Phase 4)
Arthritis, Rheumatoid (Phase 2)
Ascites (Phase 2)
Asthma (Phase 2/Phase 3)
Ataxia Telangiectasia (Phase 4)
Atherosclerosis (Phase 4)
Atrial Fibrillation (Phase 4)
Auditory Diseases, Central (Phase 4)
Autism Spectrum Disorder (Phase 4)
Autoimmune Diseases (Phase 1)
Barrett Esophagus (Phase 2)
beta-Thalassemia (Phase 4)
Bipolar Disorder (Phase 4)
Blood Glucose (Phase 4)
Blood Platelet Disorders (Phase 2/Phase 3)
Body Weight (Phase 4)
Body Weight Changes (Phase 1/Phase 2)
Bone Diseases (Phase 2)
Bone Marrow Cells (Phase 2)
Brain Neoplasms (Phase 3)
BRCA1 Protein (Phase 3)
Breast Diseases (Phase 4)
Breast Neoplasms (Phase 3)
Brenner Tumor (Phase 2)
Burns (Phase 2/Phase 3)
Carcinoma (Phase 2)
Carcinoma, Adenosquamous (Phase 2)
Carcinoma, Hepatocellular (Phase 3)
Carcinoma, Mucoepidermoid (Phase 2)
Carcinoma, Non-Small-Cell Lung (Phase 2)
Carcinoma, Ovarian Epithelial (Phase 2)
Carcinoma, Renal Cell (Phase 1/Phase 2)
Carcinoma, Squamous Cell (Phase 2)
Cardiovascular Diseases (Phase 4)
Cholangiocarcinoma (Phase 1/Phase 2)
Cholestasis, Intrahepatic (Phase 2/Phase 3)
Cholesterol, LDL (Phase 4)
Chondrosarcoma (Phase 1/Phase 2)
Chronic Periodontitis (Phase 2/Phase 3)
Cognitive Dysfunction (Phase 4)
Colitis, Ulcerative (Phase 2)
Colonic Neoplasms (Phase 2)
Colorectal Neoplasms (Phase 3)
Coronary Artery Bypass (Phase 3)
Coronary Artery Disease (Phase 4)
Coronary Disease (Phase 4)
Coronary Restenosis (Phase 4)
COVID-19 (Phase 3)
Critical Illness (Phase 3)
Cushing Syndrome (Phase 2/Phase 3)
Cystic Fibrosis (Phase 3)
Dementia (Phase 2)
Dementia, Vascular (Phase 2)
Depression (Phase 4)
Diabetes, Gestational (Phase 4)
Diabetes Insipidus (Phase 1)
Diabetes Mellitus, Type 1 (Phase 4)
Diabetic Foot (Phase 3)
Diabetic Neuropathies (Phase 3)
Diabetic Retinopathy (Early Phase 1)
Diet (Early Phase 1)
Dipeptidyl-Peptidase IV Inhibitors (Phase 4)
Drug Interactions (Phase 1)
Drugs, Generic (Phase 1)
Drugs, Investigational (Phase 3)
Dyslipidemias (Phase 4)
Endocrine System Diseases (Phase 2)
Endometrial Hyperplasia (Phase 2)
Endometrial Neoplasms (Phase 4)
Endometriosis (Phase 2/Phase 3)
Endothelial Cells (Phase 4)
Endothelium (Phase 4)
Epidermal Growth Factor (Phase 2)
Erectile Dysfunction (Phase 1)
Erythrocytes, Abnormal (Phase 2)
Esophageal Neoplasms (Phase 2)
Exercise (Phase 4)
Fallopian Tube Neoplasms (Phase 2)
Fasting (Phase 1)
Fatty Liver (Phase 4)
Fibromyalgia (Phase 2)
Fibrosis (Phase 3)
Frail Elderly (Phase 3)
Frailty (Phase 2)
Gastroparesis (Phase 2)
General Surgery (Phase 4)
Genetic Diseases, Inborn (Phase 4)
Geographic Atrophy (Phase 2)
Glioblastoma (Phase 2)
Glioma (Phase 1/Phase 2)
Gliosarcoma (Phase 1)
Glomerulosclerosis, Focal Segmental (Phase 1)
Glucocorticoids (Phase 4)
Glucose Intolerance (Phase 4)
Glucose Metabolism Disorders (Phase 4)
Glycated Hemoglobin A (Phase 4)
Glycemic Control (Phase 3)
Gonadal Disorders (Phase 4)
Graft vs Host Disease (Phase 3)
Gynecology (Phase 3)
Hamartoma (Phase 2)
Head and Neck Neoplasms (Phase 2)
Healthy Volunteers (Phase 4)
Hearing Loss, Sensorineural (Phase 2/Phase 3)
Heart Diseases (Phase 3)
Heart Failure (Phase 4)
Heart Failure, Diastolic (Phase 2)
Heart Failure, Systolic (Phase 4)
Heart Ventricles (Phase 4)
Hemangiosarcoma (Phase 2)
Hematopoietic Stem Cell Transplantation (Phase 3)
Hemoglobins (Early Phase 1)
Hepatic Encephalopathy (Phase 4)
Hepatic Insufficiency (Phase 1)
Hepatitis (Phase 2)
Hepatitis C (Phase 4)
Hepatitis C, Chronic (Phase 4)
HIV (Phase 2)
HIV-Associated Lipodystrophy Syndrome (Phase 2)
HIV Infections (Phase 4)
Hospitalization (Phase 4)
Hyperandrogenism (Phase 3)
Hypercholesterolemia (Phase 3)
Hyperglycemia (Phase 4)
Hyperinsulinism (Phase 4)
Hyperlactatemia (Phase 1/Phase 2)
Hyperlipidemias (Phase 3)
Hyperplasia (Phase 3)
Hypertension (Phase 4)
Hypertriglyceridemia (Phase 4)
Hypertrophy, Left Ventricular (Phase 4)
Hypoglycemia (Phase 4)
Hypoglycemic Agents (Phase 4)
Hypogonadism (Phase 3)
Infertility (Phase 4)
Infertility, Female (Phase 3)
Inflammation (Phase 4)
Inflammatory Bowel Diseases (Phase 4)
Insulin Resistance (Phase 4)
Insulin Secretion (Phase 4)
Intermittent Claudication (Phase 4)
Iron Metabolism Disorders (Phase 2/Phase 3)
Islets of Langerhans Transplantation (Phase 3)
Ketosis (Phase 4)
Kidney Failure, Chronic (Phase 4)
Kidney Neoplasms (Phase 2)
Kidney Transplantation (Phase 2)
Lactation Disorders (Phase 1/Phase 2)
Larynx (Phase 2)
Leukemia, Lymphocytic, Chronic, B-Cell (Phase 2)
Leukemia, Monocytic, Acute (Phase 1)
Leukemia, Myeloid, Acute (Phase 2)
Leukemia, Myeloid, Chronic-Phase (Phase 1)
Leukemia, Myelomonocytic, Acute (Phase 1)
Leukoplakia, Oral (Phase 2)
Li-Fraumeni Syndrome (Phase 1)
Lip (Phase 2)
Lipodystrophy (Phase 4)
Lipoproteins (Phase 3)
Liver Cirrhosis (Phase 4)
Liver Diseases (Phase 4)
Liver Neoplasms (Phase 3)
Lung Neoplasms (Phase 2)
Lupus Erythematosus, Systemic (Phase 4)
Lymphoma (Phase 1)
Lymphoma, Large B-Cell, Diffuse (Phase 2)
Lymphoma, Non-Hodgkin (Phase 2)
Lymphoma, T-Cell, Cutaneous (Phase 2)
Macrophages (Phase 3)
Macular Degeneration (Phase 2)
Malaria (Phase 1)
Malaria, Falciparum (Phase 1/Phase 2)
Masked Hypertension (Phase 4)
Melanoma (Phase 2)
Memory Disorders (Phase 2)
Menopause (Phase 4)
Metabolic Diseases (Phase 4)
Metabolic Syndrome (Phase 4)
Metabolism (Phase 2/Phase 3)
Metformin (Phase 4)
Migraine Disorders (Phase 3)
Mitochondrial Diseases (Phase 2)
Mouth (Phase 2)
Movement Disorders (Phase 2)
Multiple Myeloma (Phase 2)
Multiple Organ Failure (Phase 3)
Muscular Dystrophies (Phase 2)
Muscular Dystrophy, Duchenne (Phase 3)
Mutation (Phase 3)
Mycosis Fungoides (Phase 2)
Myelodysplastic Syndromes (Phase 2)
Myocardial Infarction (Phase 4)
Myocardial Ischemia (Phase 4)
Myoma (Phase 1/Phase 2)
Neoplasms (Phase 4)
Neoplasms, Adipose Tissue (Phase 4)
Neuralgia (Phase 1)
Neuroendocrine Tumors (Phase 2)
Non-alcoholic Fatty Liver Disease (Phase 4)
Nutritional and Metabolic Diseases (Phase 2)
Obesity (Phase 4)
Obesity, Abdominal (Phase 4)
Optic Atrophy (Phase 2/Phase 3)
Organic Cation Transporter 2 (Phase 4)
Oropharyngeal Neoplasms (Phase 2)
Ovarian Neoplasms (Phase 2)
Overweight (Phase 4)
Ovulation (Phase 3)
Oxidative Stress (Phase 2)
Pancreatic Neoplasms (Phase 4)
Pancreatitis (Phase 4)
Patients (Phase 1)
Pediatric Obesity (Phase 4)
Peptic Ulcer (Phase 2/Phase 3)
Percutaneous Coronary Intervention (Phase 4)
Periodontitis (Phase 2/Phase 3)
Peripheral Arterial Disease (Phase 4)
Pharmacokinetics (Phase 1)
Pharmacology (Phase 4)
Pharynx (Phase 2)
Pituitary ACTH Hypersecretion (Phase 4)
Pleural Effusion, Malignant (Phase 2)
Polycystic Kidney, Autosomal Dominant (Phase 2)
Polycystic Ovary Syndrome (Phase 4)
Polymorphism, Genetic (Phase 4)
Postmenopause (Phase 2)
Prediabetic State (Phase 4)
Pregnancy (Phase 4)
Pregnancy Complications (Phase 2/Phase 3)
Pregnancy in Diabetics (Phase 4)
Prognosis (Phase 4)
Prostatic Neoplasms (Phase 4)
Psoriasis (Phase 3)
Psychotic Disorders (Phase 4)
Pulmonary Arterial Hypertension (Phase 2)
Pulmonary Disease, Chronic Obstructive (Phase 4)
Rectal Neoplasms (Phase 2)
Renal Dialysis (Phase 1)
Renal Insufficiency (Phase 3)
Renal Insufficiency, Chronic (Phase 3)
Reperfusion Injury (Phase 4)
Reproductive Health (Phase 2)
Safety (Phase 2)
Sarcoma (Phase 2)
Schizophrenia (Phase 4)
Sezary Syndrome (Phase 2)
Short Bowel Syndrome (Phase 4)
Small Cell Lung Carcinoma (Phase 2)
Squamous Cell Carcinoma of Head and Neck (Phase 1/Phase 2)
Therapeutic Equivalency (Phase 1)
Therapeutics (Phase 2)
Thyroid Cancer, Papillary (Phase 1)
Thyroid Neoplasms (Phase 1)
Toxemia (Phase 3)
Tryptophan (Early Phase 1)
Urinary Bladder Neoplasms (Phase 2)
Uterine Cervical Neoplasms (Phase 2)
Uterine Neoplasms (Phase 2/Phase 3)
Vascular Diseases (Phase 4)
Weight Gain (Phase 4)
| Trial | Phase | Start Date | Organizations | Indications |
|---|
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