Semaglutide
Identification
- Summary
Semaglutide is a glucagon-like peptide 1 receptor agonist used to improve glycemic control in type 2 diabetes mellitus.
- Brand Names
- Ozempic, Rybelsus, Wegovy
- Generic Name
- Semaglutide
- DrugBank Accession Number
- DB13928
- Background
Semaglutide is a glucagon-like peptide 1 (GLP-1) analog used to manage type 2 diabetes along with lifestyle changes, such as dietary restrictions and increased physical activity.1,17 Other members of this drug class include Exenatide and Liraglutide. Semaglutide was developed by Novo Nordisk and approved by the FDA for subcutaneous injection in December 2017.17 The tablet formulation was approved for oral administration in September 2019. Semaglutide works by binding to and activating the GLP-1 receptor, thereby stimulating insulin secretion and reducing blood glucose.16
The subcutaneous injection is administered once weekly and the tablet is administered once a day. Semaglutide offers a competitive advantage over other drugs used to manage diabetes, which may require several daily doses. Clinical trials have determined that this drug reduces glycosylated hemoglobin (HbA1c) levels and reduces body weight, proving to be effective for patients with type 2 diabetes.5 In June 2021, semaglutide was approved by the FDA for chronic weight management in adults with general obesity or overweight who have at least one weight-related condition: this marks semaglutide as the first approved drug for such use since 2014.21
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Semaglutide (DB13928)
- Weight
- Average: 4113.641
Monoisotopic: 4111.11537713 - Chemical Formula
- C187H291N45O59
- Synonyms
- Semaglutide
- Sémaglutide
- External IDs
- NN-9535
- NN9535
- NNC 0113-0217
- NNC-0113-0217
Pharmacology
- Indication
Semaglutide is indicated to improve glycemic control in adults diagnosed with type 2 diabetes mellitus, and is used as an adjunct to diet and exercise.16,17 However, semaglutide is not a suitable first-line drug for diabetes that has not been controlled by diet and exercise. In addition, it has not been studied in patients with pancreatitis. Semaglutide is not intended for use in patients with type 1 diabetes or to treat diabetic ketoacidosis.16
Semaglutide is indicated for chronic weight management in adults with obesity or overweight with at least one weight-related condition (such as high blood pressure, type 2 diabetes, or high cholesterol), for use in addition to a reduced-calorie diet and increased physical activity.20
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- Associated Therapies
- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Semaglutide reduces HbA1c, systolic blood pressure, and body weight.6 After 12 weeks of treatment, semaglutide decreased fasting and postprandial glucose by increasing insulin production and decreasing glucagon secretion (which is normally associated with increases in blood sugar). Semaglutide also lowers fasting triglycerides and VLDL cholesterol, exerting beneficial effects on cardiovascular health.5,13
Special precautions
Semaglutide has been shown to cause medullary thyroid cell carcinoma in rodents. The relevance to humans is unknown, but its advisable not to administer this drug in those with a personal or family history of medullary thyroid carcinoma. Semaglutide also poses a risk of pancreatitis and dehydration. Patients must be adequately hydrated while on semaglutide and are advised to seek medical attention immediately in cases of abdominal pain radiating to the back. Because this drug delays gastric emptying, it is important to monitor for the efficacy or adverse effects of others drugs that are administered orally.17
- Mechanism of action
Mechanism of glycemic control
GLP-1 is a physiological hormone that promotes glycemic control via several different mechanisms, including insulin secretion, slowing gastric emptying, and reducing postprandial glucagon secretion. The homeostasis of glucose is dependent on hormones such as insulin and amylin, which are secreted by the beta cells of the pancreas. Semaglutide is 94% similar to human GLP-1. Analogs of this hormone such as semaglutide stimulate the synthesis of insulin3 by stimulating pancreatic islet cells and reducing glucagon secretion.3 They directly bind with selectivity to the GLP-1 receptor, causing various beneficial downstream effects that reduce blood glucose in a glucose-dependent fashion.17
Mechanism of cardiovascular benefit and weight loss
In hypercholesterolemia, semaglutide is believed to reduce the progression of atherosclerosis via decreased gut permeability and decreased inflammation.7 Weight loss is believed to occur via the reduction of appetite and food cravings after semaglutide administration. 2,8
Target Actions Organism AGlucagon-like peptide 1 receptor agonistHumans - Absorption
The Cmax of semaglutide was 10.9 nmol/L, with AUC of 3123.4 nmol h/L and a Tmax of 56 h in one clinical trial, achieved within 1-3 days.4,17 The absolute bioavailability is 89%.17 Steady-state concentration of the oral tablet is achieved in 4-5 weeks.10 Average steady state concentrations of semaglutide are the mean steady state concentrations after dosing at 0.5mg to 1mg range from 16 nmol/L to 30 nmol/L.18
- Volume of distribution
The volume of distribution of semaglutide is 8L to 9.4L. It crosses the placenta in rats.4,17
- Protein binding
Semaglutide binds with high affinity to plasma albumin, promoting high levels of drug stability.2 It is more than 99% bound to albumin.11,15,17
- Metabolism
Semaglutide is cleaved at the peptide backbone, followed by β‐oxidation of the fatty acid chain.11 Naturally occurring GLP‐1 is quickly metabolized by dipeptidyl peptidase‐4 (DPP‐4) and other enzymes, which is ubiquitous in human tissues. Chemical structure modifications render semaglutide less susceptible to enzymatic degradation by gastrointestinal DPP‐4 enzymes.11 It is slowly and extensively metabolized, with about 83% of the administered dose measured in the plasma as unchanged drug. Neural endopeptidase (NEP) is another enzyme that metabolizes this drug. DPP-4 inactivates semaglutide, truncating the N-terminal segment while NEP hydrolyzes peptide bondsSix different metabolites of semaglutide have been identified in human plasma. The major metabolite, named P3, accounts for about 7.7% of an ingested dose.4
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- Route of elimination
This drug is mainly cleared by the kidneys, and is found excreted in both the urine and feces.11 The main elimination route is the urine by corresponding to 53% of an ingested radiolabeled dose, with 18.6% found in the feces. A smaller amount of 3.2% was found to be exhaled.4 Hepatic impairment does not appear to affect the clearance of this drug and dose adjustments are not required in patients with decreased liver function.11
- Half-life
One of the major properties of semaglutide is its long half-life of 168 h.4 The long half-life is attributed to its albumin binding. This lowers the renal clearance and protects semaglutide from metabolic breakdown.16,17
- Clearance
The clearance rate of semaglutide is 0.039 L/h according to one clinical study.4 On the FDA label, semaglutide clearance is reported to be about 0.05 L/h in patients with type 2 diabetes mellitus.17
- Adverse Effects
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Overdoses of up to 4 mg in one ingestion have been reported, with nausea being the most commonly reported symptom. All patients in clinical trials who experienced an overdose recovered fully.18 Appropriate supportive care should be given according and dictated by the patient's condition. Prolonged observation and treatment may be required, as the half-life of this drug is about one week.17 There is no antidote to an overdose with semaglutide.18
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAcarbose The risk or severity of hypoglycemia can be increased when Acarbose is combined with Semaglutide. Acebutolol The therapeutic efficacy of Semaglutide can be increased when used in combination with Acebutolol. Acetazolamide The therapeutic efficacy of Semaglutide can be increased when used in combination with Acetazolamide. Acetohexamide Semaglutide may increase the hypoglycemic activities of Acetohexamide. Acetyl sulfisoxazole The therapeutic efficacy of Semaglutide can be increased when used in combination with Acetyl sulfisoxazole. Acetylsalicylic acid The risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Semaglutide. Albiglutide The risk or severity of hypoglycemia can be increased when Albiglutide is combined with Semaglutide. Alclometasone The risk or severity of hyperglycemia can be increased when Alclometasone is combined with Semaglutide. Alogliptin The risk or severity of hypoglycemia can be increased when Alogliptin is combined with Semaglutide. Amcinonide The risk or severity of hyperglycemia can be increased when Amcinonide is combined with Semaglutide. 
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- Take on an empty stomach. For oral use of semaglutide, take 30 minutes before the first meal of the day.
- Take with plain water. For oral use of semaglutide, do not exceed 4 ounces of water (1/2 cup).
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- International/Other Brands
- Wegovy (Novo Nordisk)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ozempic Solution 1.34 mg / mL Subcutaneous Novo Nordisk 2018-02-22 Not applicable Canada 
Ozempic Injection, solution 1.34 mg/1mL Subcutaneous A-S Medication Solutions 2017-12-06 Not applicable US 
Ozempic Injection, solution 1.34 mg/1mL Subcutaneous Novo Nordisk 2017-12-06 Not applicable US Ozempic Injection, solution 0.5 mg Subcutaneous Novo Nordisk 2021-01-22 Not applicable EU 
Ozempic Injection, solution 1.34 mg/1mL Subcutaneous Novo Nordisk 2020-09-30 Not applicable US Ozempic Injection, solution 0.5 mg Subcutaneous Novo Nordisk 2021-01-22 Not applicable EU Ozempic Injection, solution 1 mg Subcutaneous Novo Nordisk 2021-01-22 Not applicable EU Ozempic Solution 1 mg / act Subcutaneous Novo Nordisk 2018-02-22 Not applicable Canada Ozempic Injection, solution 1.34 mg/1mL Subcutaneous REMEDYREPACK INC. 2019-06-11 Not applicable US Ozempic Injection, solution 0.25 mg Subcutaneous Novo Nordisk 2021-01-22 Not applicable EU
Categories
- ATC Codes
- A10BJ06 — Semaglutide
- Drug Categories
- Alimentary Tract and Metabolism
- Amino Acids, Peptides, and Proteins
- Blood Glucose Lowering Agents
- Drugs Used in Diabetes
- Gastrointestinal Hormones
- GLP-1 Agonists
- Glucagon-like peptide-1 (GLP-1) analogues
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Incretin Mimetics
- Pancreatic Hormones
- Peptide Hormones
- Peptides
- Proteins
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as polypeptides. These are peptides containing ten or more amino acid residues.
- Kingdom
- Organic compounds
- Super Class
- Organic Polymers
- Class
- Polypeptides
- Sub Class
- Not Available
- Direct Parent
- Polypeptides
- Alternative Parents
- Peptides / Tyrosine and derivatives / Arginine and derivatives / Phenylalanine and derivatives / Histidine and derivatives / Glutamine and derivatives / Glutamic acid and derivatives / Aspartic acid and derivatives / Isoleucine and derivatives / Leucine and derivatives show 29 more
- Substituents
- 1-hydroxy-2-unsubstituted benzenoid / 3-alkylindole / Alanine or derivatives / Alcohol / Alpha peptide / Alpha-amino acid amide / Alpha-amino acid or derivatives / Amine / Amino acid / Amino acid or derivatives show 56 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 53AXN4NNHX
- CAS number
- 910463-68-2
- InChI Key
- DLSWIYLPEUIQAV-CCUURXOWSA-N
- InChI
- InChI=1S/C187H291N45O59/c1-18-105(10)154(180(282)208-108(13)159(261)216-133(86-114-89-200-119-50-40-39-49-117(114)119)170(272)218-129(82-102(4)5)171(273)228-152(103(6)7)178(280)215-121(53-44-72-199-186(192)193)162(264)201-91-141(242)209-120(52-43-71-198-185(190)191)161(263)204-94-151(257)258)230-172(274)131(83-111-45-33-31-34-46-111)219-167(269)126(64-69-149(253)254)214-166(268)122(51-41-42-70-195-144(245)98-290-79-78-289-76-74-197-145(246)99-291-80-77-288-75-73-196-139(240)66-61-127(183(285)286)211-140(241)54-37-29-27-25-23-21-19-20-22-24-26-28-30-38-55-146(247)248)212-158(260)107(12)206-157(259)106(11)207-165(267)125(60-65-138(189)239)210-142(243)92-202-163(265)123(62-67-147(249)250)213-168(270)128(81-101(2)3)217-169(271)130(85-113-56-58-116(238)59-57-113)220-175(277)135(95-233)223-177(279)137(97-235)224-179(281)153(104(8)9)229-174(276)134(88-150(255)256)221-176(278)136(96-234)225-182(284)156(110(15)237)231-173(275)132(84-112-47-35-32-36-48-112)222-181(283)155(109(14)236)227-143(244)93-203-164(266)124(63-68-148(251)252)226-184(287)187(16,17)232-160(262)118(188)87-115-90-194-100-205-115/h31-36,39-40,45-50,56-59,89-90,100-110,118,120-137,152-156,200,233-238H,18-30,37-38,41-44,51-55,60-88,91-99,188H2,1-17H3,(H2,189,239)(H,194,205)(H,195,245)(H,196,240)(H,197,246)(H,201,264)(H,202,265)(H,203,266)(H,204,263)(H,206,259)(H,207,267)(H,208,282)(H,209,242)(H,210,243)(H,211,241)(H,212,260)(H,213,270)(H,214,268)(H,215,280)(H,216,261)(H,217,271)(H,218,272)(H,219,269)(H,220,277)(H,221,278)(H,222,283)(H,223,279)(H,224,281)(H,225,284)(H,226,287)(H,227,244)(H,228,273)(H,229,276)(H,230,274)(H,231,275)(H,232,262)(H,247,248)(H,249,250)(H,251,252)(H,253,254)(H,255,256)(H,257,258)(H,285,286)(H4,190,191,198)(H4,192,193,199)/t105-,106-,107-,108-,109+,110+,118-,120-,121-,122-,123-,124-,125-,126-,127+,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,152-,153-,154-,155-,156-/m0/s1
- IUPAC Name
- 17-{[(1R)-3-[(2-{2-[({2-[2-({[(5S)-5-[(2S)-2-[(2S)-2-[(2S)-2-{2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S)-2-[(2S,3R)-2-[(2S)-2-[(2S,3R)-2-{2-[(2S)-2-{2-[(2S)-2-amino-3-(1H-imidazol-5-yl)propanamido]-2-methylpropanamido}-4-carboxybutanamido]acetamido}-3-hydroxybutanamido]-3-phenylpropanamido]-3-hydroxybutanamido]-3-hydroxypropanamido]-3-carboxypropanamido]-3-methylbutanamido]-3-hydroxypropanamido]-3-hydroxypropanamido]-3-(4-hydroxyphenyl)propanamido]-4-methylpentanamido]-4-carboxybutanamido]acetamido}-4-carbamoylbutanamido]propanamido]propanamido]-5-{[(1S)-1-{[(1S)-1-{[(1S,2S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-1-{[(1S)-4-carbamimidamido-1-[({[(1S)-4-carbamimidamido-1-[(carboxymethyl)carbamoyl]butyl]carbamoyl}methyl)carbamoyl]butyl]carbamoyl}-2-methylpropyl]carbamoyl}-3-methylbutyl]carbamoyl}-2-(1H-indol-3-yl)ethyl]carbamoyl}ethyl]carbamoyl}-2-methylbutyl]carbamoyl}-2-phenylethyl]carbamoyl}-3-carboxypropyl]carbamoyl}pentyl]carbamoyl}methoxy)ethoxy]ethyl}carbamoyl)methoxy]ethoxy}ethyl)carbamoyl]-1-carboxypropyl]carbamoyl}heptadecanoic acid
- SMILES
- CC[C@H](C)[C@H](NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[C@@H](NC(=O)CCCCCCCCCCCCCCCCC(O)=O)C(O)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)C(C)(C)NC(=O)[C@@H](N)CC1=CN=CN1)[C@@H](C)O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(O)=O
References
- Synthesis Reference
Synthesis of Semaglutide[J]. CJPH, 2018, 49(06): 742-.
- General References
- Gotfredsen CF, Molck AM, Thorup I, Nyborg NC, Salanti Z, Knudsen LB, Larsen MO: The human GLP-1 analogs liraglutide and semaglutide: absence of histopathological effects on the pancreas in nonhuman primates. Diabetes. 2014 Jul;63(7):2486-97. doi: 10.2337/db13-1087. Epub 2014 Mar 7. [Article]
- Blundell J, Finlayson G, Axelsen M, Flint A, Gibbons C, Kvist T, Hjerpsted JB: Effects of once-weekly semaglutide on appetite, energy intake, control of eating, food preference and body weight in subjects with obesity. Diabetes Obes Metab. 2017 Sep;19(9):1242-1251. doi: 10.1111/dom.12932. Epub 2017 May 5. [Article]
- Lee YS, Jun HS: Anti-diabetic actions of glucagon-like peptide-1 on pancreatic beta-cells. Metabolism. 2014 Jan;63(1):9-19. doi: 10.1016/j.metabol.2013.09.010. Epub 2013 Oct 17. [Article]
- Jensen L, Helleberg H, Roffel A, van Lier JJ, Bjornsdottir I, Pedersen PJ, Rowe E, Derving Karsbol J, Pedersen ML: Absorption, metabolism and excretion of the GLP-1 analogue semaglutide in humans and nonclinical species. Eur J Pharm Sci. 2017 Jun 15;104:31-41. doi: 10.1016/j.ejps.2017.03.020. Epub 2017 Mar 16. [Article]
- Ahren B, Atkin SL, Charpentier G, Warren ML, Wilding JPH, Birch S, Holst AG, Leiter LA: Semaglutide induces weight loss in subjects with type 2 diabetes regardless of baseline BMI or gastrointestinal adverse events in the SUSTAIN 1 to 5 trials. Diabetes Obes Metab. 2018 Sep;20(9):2210-2219. doi: 10.1111/dom.13353. Epub 2018 Jun 12. [Article]
- Andreadis P, Karagiannis T, Malandris K, Avgerinos I, Liakos A, Manolopoulos A, Bekiari E, Matthews DR, Tsapas A: Semaglutide for type 2 diabetes mellitus: A systematic review and meta-analysis. Diabetes Obes Metab. 2018 Sep;20(9):2255-2263. doi: 10.1111/dom.13361. Epub 2018 Jun 10. [Article]
- Rakipovski G, Rolin B, Nohr J, Klewe I, Frederiksen KS, Augustin R, Hecksher-Sorensen J, Ingvorsen C, Polex-Wolf J, Knudsen LB: The GLP-1 Analogs Liraglutide and Semaglutide Reduce Atherosclerosis in ApoE(-/-) and LDLr(-/-) Mice by a Mechanism That Includes Inflammatory Pathways. JACC Basic Transl Sci. 2018 Nov 21;3(6):844-857. doi: 10.1016/j.jacbts.2018.09.004. eCollection 2018 Dec. [Article]
- Kim KK: Understanding the Mechanism of Action and Clinical Implications of Anti-Obesity Drugs Recently Approved in Korea. Korean J Fam Med. 2019 Mar;40(2):63-71. doi: 10.4082/kjfm.19.0013. Epub 2019 Mar 20. [Article]
- Bucheit J, Pamulapati LG, Carter NM, Malloy K, Dixon D, Sisson E: Oral Semaglutide: A Review of the First Oral Glucagon-Like Peptide-1 Receptor Agonist. Diabetes Technol Ther. 2019 Aug 22. doi: 10.1089/dia.2019.0185. [Article]
- Hall S, Isaacs D, Clements JN: Pharmacokinetics and Clinical Implications of Semaglutide: A New Glucagon-Like Peptide (GLP)-1 Receptor Agonist. Clin Pharmacokinet. 2018 Dec;57(12):1529-1538. doi: 10.1007/s40262-018-0668-z. [Article]
- Jensen L, Kupcova V, Arold G, Pettersson J, Hjerpsted JB: Pharmacokinetics and tolerability of semaglutide in people with hepatic impairment. Diabetes Obes Metab. 2018 Apr;20(4):998-1005. doi: 10.1111/dom.13186. Epub 2018 Jan 17. [Article]
- Barnett A. (2012). Type 2 diabetes (2nd ed.). Oxford.
- FDA Briefing Document: Semaglutide subcutaneous once-weekly [Link]
- Novo Nordisk News [Link]
- FDA Briefing Document: Endocrinologic and Metabolic Drugs Advisory Committee Meeting [Link]
- FDA Approved Drug Products: RYBELSUS (semaglutide) tablets, for oral use [Link]
- FDA Approved Drug Products: OZEMPIC (semaglutide) injection, for subcutaneous use [Link]
- Summary of Product Characteristics: Ozempic (semaglutide) subcutaneous injection [Link]
- DailyMed: Rybelsus (semaglutide) oral tablet [Link]
- FDA Approved Drug Products: WEGOVY (semaglutide) injection, for subcutaneous use [Link]
- FDA Press Announcements: FDA Approves New Drug Treatment for Chronic Weight Management, First Since 2014 [Link]
- External Links
- ChemSpider
- 34985066
- BindingDB
- 50121400
- 1991302
- ChEBI
- 167574
- ChEMBL
- CHEMBL3616752
- Wikipedia
- Semaglutide
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Type 2 Diabetes Mellitus 1 4 Completed Other Type 2 Diabetes Mellitus 1 4 Completed Treatment Altered taste / Central Neural Response / Gastric Emptying / Polycystic Ovarian Syndrome (PCOS) / Semaglutide / Tongue Tissue Transcriptome 1 4 Completed Treatment BMI >27 kg/m2 / Healthy Subjects (HS) / Obesity (Disorder) / Type 2 Diabetes Mellitus 1 4 Not Yet Recruiting Basic Science Chronic Inflammation / Intestinal Permeability / Type 2 Diabetes Mellitus 1 4 Not Yet Recruiting Basic Science Glucose Metabolism Disorders (Including Diabetes Mellitus) / Type 2 Diabetes Mellitus 1 4 Not Yet Recruiting Diagnostic Healthy Subjects (HS) 1 4 Not Yet Recruiting Treatment Clozapine / GLP - 1 / Metabolic Disturbances / Olanzapine / Schizophrenia / Type 2 Diabetes Mellitus 1 4 Not Yet Recruiting Treatment Impaired Glucose Tolerance / Postpartum disorder 1 4 Not Yet Recruiting Treatment Type 2 Diabetes Mellitus 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Parenteral; Subcutaneous 0.25 MG Injection, solution Parenteral; Subcutaneous 0.5 MG Injection, solution Parenteral; Subcutaneous 1 MG Injection, solution Parenteral; Subcutaneous 1.34 MG/ML Injection, solution Subcutaneous 0.25 mg Injection, solution Subcutaneous 0.5 mg Injection, solution Subcutaneous 1 mg Injection, solution Subcutaneous 1.34 mg/1mL Solution Subcutaneous 1 mg / act Solution Subcutaneous 1.34 mg / mL Injection, solution Subcutaneous 1.34 mg/ml Solution Subcutaneous 1.34 mg Injection, solution Subcutaneous Tablet Oral 14 mg/1 Tablet Oral 14 MG Tablet Oral 3 MG Tablet Oral 3 mg/1 Tablet Oral 7 MG Tablet Oral 7 mg/1 Injection, solution Subcutaneous 0.25 mg/0.5mL Injection, solution Subcutaneous 0.5 mg/0.5mL Injection, solution Subcutaneous 1.0 mg/0.5mL Injection, solution Subcutaneous 1.7 mg/0.75mL Injection, solution Subcutaneous 2.4 mg/0.75mL - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US8672898 Yes 2014-03-18 2022-07-02 US US8684969 Yes 2014-04-01 2026-04-20 US US9132239 Yes 2015-09-15 2032-08-01 US US8920383 Yes 2014-12-30 2027-01-17 US US6899699 Yes 2005-05-31 2022-07-01 US US9108002 Yes 2015-08-18 2026-07-26 US US8114833 Yes 2012-02-14 2026-02-13 US US9486588 Yes 2016-11-08 2022-07-02 US US9457154 Yes 2016-10-04 2028-03-27 US USRE46363 Yes 2017-04-11 2027-02-03 US US9687611 Yes 2017-06-27 2027-08-27 US US9775953 Yes 2017-10-03 2027-01-17 US US8129343 No 2012-03-06 2029-01-29 US US8536122 No 2013-09-17 2026-03-20 US US8579869 Yes 2013-11-12 2023-12-30 US US7762994 Yes 2010-07-27 2024-11-23 US US9861757 Yes 2018-01-09 2026-07-20 US US9616180 Yes 2017-04-11 2026-07-20 US US10220155 Yes 2019-03-05 2027-01-17 US US10335462 No 2019-07-02 2033-06-21 US US10357616 No 2019-07-23 2026-01-20 US US9278123 No 2016-03-08 2031-12-16 US US10278923 No 2019-05-07 2034-05-02 US US10376652 No 2019-08-13 2026-01-20 US US10086047 No 2018-10-02 2031-12-16 US US10933120 No 2021-03-02 2033-03-15 US US10960052 No 2021-03-30 2031-12-16 US US10888605 No 2021-01-12 2038-08-24 US US9764003 No 2017-09-19 2033-06-21 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility <1 mg/mL https://www.selleck.cn/msds/MSDS_S9697.pdf - Predicted Properties
Property Value Source logP -18 ChemAxon pKa (Strongest Acidic) 2.74 ChemAxon pKa (Strongest Basic) 12.26 ChemAxon Physiological Charge -4 ChemAxon Hydrogen Acceptor Count 67 ChemAxon Hydrogen Donor Count 57 ChemAxon Polar Surface Area 1646.18 Å2 ChemAxon Rotatable Bond Count 149 ChemAxon Refractivity 1048.56 m3·mol-1 ChemAxon Polarizability 427.61 Å3 ChemAxon Number of Rings 6 ChemAxon Bioavailability 0 ChemAxon Rule of Five No ChemAxon Ghose Filter No ChemAxon Veber's Rule No ChemAxon MDDR-like Rule Yes ChemAxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Transmembrane signaling receptor activity
- Specific Function
- This is a receptor for glucagon-like peptide 1. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
- Gene Name
- GLP1R
- Uniprot ID
- P43220
- Uniprot Name
- Glucagon-like peptide 1 receptor
- Molecular Weight
- 53025.22 Da
References
- Lee YS, Jun HS: Anti-diabetic actions of glucagon-like peptide-1 on pancreatic beta-cells. Metabolism. 2014 Jan;63(1):9-19. doi: 10.1016/j.metabol.2013.09.010. Epub 2013 Oct 17. [Article]
- Durante C, Russo D, Verrienti A, Filetti S: XL184 (cabozantinib) for medullary thyroid carcinoma. Expert Opin Investig Drugs. 2011 Mar;20(3):407-413. doi: 10.1517/13543784.2011.559163. [Article]
- Barnett A. (2012). Type 2 diabetes (2nd ed.). Oxford.
- FDA Approved Drug Products: OZEMPIC (semaglutide) injection, for subcutaneous use [Link]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Virus receptor activity
- Specific Function
- Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation. Acts as a positive regulator of T-cell coactivation, by bindi...
- Gene Name
- DPP4
- Uniprot ID
- P27487
- Uniprot Name
- Dipeptidyl peptidase 4
- Molecular Weight
- 88277.935 Da
References
- Blundell J, Finlayson G, Axelsen M, Flint A, Gibbons C, Kvist T, Hjerpsted JB: Effects of once-weekly semaglutide on appetite, energy intake, control of eating, food preference and body weight in subjects with obesity. Diabetes Obes Metab. 2017 Sep;19(9):1242-1251. doi: 10.1111/dom.12932. Epub 2017 May 5. [Article]
- Jensen L, Helleberg H, Roffel A, van Lier JJ, Bjornsdottir I, Pedersen PJ, Rowe E, Derving Karsbol J, Pedersen ML: Absorption, metabolism and excretion of the GLP-1 analogue semaglutide in humans and nonclinical species. Eur J Pharm Sci. 2017 Jun 15;104:31-41. doi: 10.1016/j.ejps.2017.03.020. Epub 2017 Mar 16. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Zinc ion binding
- Specific Function
- Thermolysin-like specificity, but is almost confined on acting on polypeptides of up to 30 amino acids (PubMed:15283675, PubMed:8168535). Biologically important in the destruction of opioid peptide...
- Gene Name
- MME
- Uniprot ID
- P08473
- Uniprot Name
- Neprilysin
- Molecular Weight
- 85513.225 Da
References
- Jensen L, Helleberg H, Roffel A, van Lier JJ, Bjornsdottir I, Pedersen PJ, Rowe E, Derving Karsbol J, Pedersen ML: Absorption, metabolism and excretion of the GLP-1 analogue semaglutide in humans and nonclinical species. Eur J Pharm Sci. 2017 Jun 15;104:31-41. doi: 10.1016/j.ejps.2017.03.020. Epub 2017 Mar 16. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Triglyceride lipase activity
- Specific Function
- The primary function of this lipase is the hydrolysis of triglycerides of circulating chylomicrons and very low density lipoproteins (VLDL). Binding to heparin sulfate proteogylcans at the cell sur...
- Gene Name
- LPL
- Uniprot ID
- P06858
- Uniprot Name
- Lipoprotein lipase
- Molecular Weight
- 53162.07 Da
References
- FDA Briefing Document: Endocrinologic and Metabolic Drugs Advisory Committee Meeting [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Metal ion binding
- Specific Function
- Not Available
- Gene Name
- AMY1A
- Uniprot ID
- P04745
- Uniprot Name
- Alpha-amylase 1
- Molecular Weight
- 57767.49 Da
References
- FDA Briefing Document: Endocrinologic and Metabolic Drugs Advisory Committee Meeting [Link]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Toxic substance binding
- Specific Function
- Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Serum albumin
- Molecular Weight
- 69365.94 Da
References
- Blundell J, Finlayson G, Axelsen M, Flint A, Gibbons C, Kvist T, Hjerpsted JB: Effects of once-weekly semaglutide on appetite, energy intake, control of eating, food preference and body weight in subjects with obesity. Diabetes Obes Metab. 2017 Sep;19(9):1242-1251. doi: 10.1111/dom.12932. Epub 2017 May 5. [Article]
- FDA Approved Drug Products: OZEMPIC (semaglutide) injection, for subcutaneous use [Link]
Drug created on December 06, 2017 17:44 / Updated on October 24, 2021 16:00