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.1,15 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 2017.15 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.14

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, marking semaglutide as the first approved drug for such use since 2014.19 The use of semaglutide in weight management is also approved by Health Canada 20 and the EMA.21

On May 31, 2023, the FDA issued a warning regarding the use of compounded semaglutide after receiving adverse event reports. The use of salt forms of semaglutide, including semaglutide sodium and semaglutide acetate, has not been proven to be safe or effective.23

Type
Small Molecule
Groups
Approved, Investigational
Structure
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.14,15 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.14

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.18,21. Semaglutide it is also indicated for chronic weight management in pediatric patients aged 12 years and older with an initial BMI at the 95th percentile or greater for age and sex.22

Reduce drug development failure rates
Build, train, & validate machine-learning models
with evidence-based and structured datasets.
See how
Build, train, & validate predictive machine-learning models with structured datasets.
See how
Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Adjunct for therapyBmi >27 kg/m2••••••••••••••••••• ••••• ••• •••••••••••••• •••••••• ••••••••••••••••••
Adjunct for therapyBmi >30 kg/m2••••••••••••••••••••••••••
Prevention ofCardiovascular events••••••••••••••••••••• • •••••••• ••••••••• ••••••••••• •••••••••••••• ••••••••••••••••
Adjunct therapy in management ofType ii diabetes mellitus••••••••••••••••••••••••••• ••••••
Associated Therapies
Contraindications & Blackbox Warnings
Prevent Adverse Drug Events Today
Tap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.
Learn more
Avoid life-threatening adverse drug events with our Clinical API
Learn more
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.5,12

Semaglutide has been shown to cause medullary thyroid cell carcinoma in rodents. While its clinical relevance to humans is unknown, the FDA advises 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 other drugs that are administered orally.15

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.15

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

TargetActionsOrganism
AGlucagon-like peptide 1 receptor
agonist
Humans
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.4,15 The absolute bioavailability is 89%.15 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.16

Volume of distribution

The volume of distribution of semaglutide is 8L to 9.4L. It crosses the placenta in rats.4,15

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.11,13,15

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

Hover over products below to view reaction partners

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.14,15

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.15

Adverse Effects
Improve decision support & research outcomes
With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!
See the data
Improve decision support & research outcomes with our structured adverse effects data.
See a data sample
Toxicity

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.16 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.15 There is no antidote to an overdose with semaglutide.16

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.
DrugInteraction
AcarboseThe risk or severity of hypoglycemia can be increased when Acarbose is combined with Semaglutide.
AcebutololThe therapeutic efficacy of Semaglutide can be increased when used in combination with Acebutolol.
AcetazolamideThe therapeutic efficacy of Semaglutide can be increased when used in combination with Acetazolamide.
AcetohexamideSemaglutide may increase the hypoglycemic activities of Acetohexamide.
Acetyl sulfisoxazoleThe therapeutic efficacy of Semaglutide can be increased when used in combination with Acetyl sulfisoxazole.
Food Interactions
  • 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 regions
Our datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.
Access now
Access drug product information from over 10 global regions.
Access now
International/Other Brands
Wegovy (Novo Nordisk)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
OzempicInjection, solution1.34 mg/1mLSubcutaneousA-S Medication Solutions2017-12-06Not applicableUS flag
OzempicSolution2.68 mg / mLSubcutaneousNovo NordiskNot applicableNot applicableCanada flag
OzempicInjection, solution1.34 mg/1mLSubcutaneousNovo Nordisk2017-12-062025-09-30US flag
OzempicInjection, solution2 mg/0.74mlSubcutaneousNovo Nordisk2022-06-08Not applicableEU flag
OzempicInjection, solution1 mg/0.74mlSubcutaneousNovo Nordisk2021-01-22Not applicableEU flag

Categories

ATC Codes
A10BJ06 — Semaglutide
Drug Categories
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
  1. 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]
  2. 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]
  3. 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]
  4. 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]
  5. 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]
  6. 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]
  7. 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]
  8. 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]
  9. 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]
  10. 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]
  11. 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]
  12. FDA Briefing Document: Semaglutide subcutaneous once-weekly [Link]
  13. FDA Briefing Document: Endocrinologic and Metabolic Drugs Advisory Committee Meeting [Link]
  14. FDA Approved Drug Products: RYBELSUS (semaglutide) tablets, for oral use [Link]
  15. FDA Approved Drug Products: OZEMPIC (semaglutide) injection, for subcutaneous use [Link]
  16. EMA Approved Drug Products: Ozempic (semaglutide) subcutaneous injection [Link]
  17. DailyMed: Rybelsus (semaglutide) oral tablet [Link]
  18. FDA Approved Drug Products: WEGOVY (semaglutide) injection, for subcutaneous use [Link]
  19. FDA Press Announcements: FDA Approves New Drug Treatment for Chronic Weight Management, First Since 2014 [Link]
  20. Novo Nordisk New Release: Health Canada approves Wegovy™ for the treatment of adults with obesity [Link]
  21. EMA Approved Drug Products: Wegovy (semaglutide) Subcutaneous Injection [Link]
  22. FDA Approved Drug Products: WEGOVY (semaglutide) injection, for subcutaneous use (December 2022) [Link]
  23. US Food & Drug Administration: Medications Containing Semaglutide Marketed for Type 2 Diabetes or Weight Loss [Link]
  24. FDA Approved Drug Proucts: WEGOVY (semaglutide) injection, for subcutaneous use (July 2023) [Link]
ChemSpider
34985066
BindingDB
50121400
RxNav
1991302
ChEBI
167574
ChEMBL
CHEMBL3616752
PharmGKB
PA166305021
Wikipedia
Semaglutide

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingOtherAging / Impaired Glucose Tolerance / Overweight and Obesity / Type 2 Diabetes Mellitus1
4Active Not RecruitingTreatmentAging / Obesity1
4Active Not RecruitingTreatmentObesity2
4CompletedDiagnosticHealthy Volunteers (HV)1
4CompletedOtherType 2 Diabetes Mellitus1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, solutionParenteral; Subcutaneous0.25 MG
Injection, solutionParenteral; Subcutaneous0.5 MG
Injection, solutionParenteral; Subcutaneous1 MG
Injection, solutionParenteral; Subcutaneous1.34 MG/ML
Injection, solutionParenteral; Subcutaneous2 mg
Injection, solutionSubcutaneous0.25 mg/0.19ml
Injection, solutionSubcutaneous0.5 mg/0.37ml
Injection, solutionSubcutaneous0.68 mg/1mL
Injection, solutionSubcutaneous1 mg/0.74ml
Injection, solutionSubcutaneous1.34 mg/1mL
Injection, solutionSubcutaneous2 mg/0.74ml
Injection, solutionSubcutaneous2.68 mg/1mL
SolutionSubcutaneous0.68 mg / mL
SolutionSubcutaneous1 mg / act
SolutionSubcutaneous1.34 mg / mL
SolutionSubcutaneous1.340 mg
SolutionSubcutaneous2.68 mg / mL
Injection, solution0.25 mg
Injection, solution0.5 mg
Injection, solutionSubcutaneous1.34 mg/ml
Injection, solution1 mg
SolutionSubcutaneous1.34 mg
TabletOral14 mg/1
TabletOral14 mg
TabletOral3 mg
TabletOral3 mg/1
TabletOral3.0 mg
TabletOral7 mg
TabletOral7 mg/1
Injection, solutionSubcutaneous0.25 mg
Injection, solutionSubcutaneous0.25 mg/0.5mL
Injection, solutionSubcutaneous0.5 mg
Injection, solutionSubcutaneous0.5 mg/0.5mL
Injection, solutionSubcutaneous1 mg
Injection, solutionSubcutaneous1.0 mg/0.5mL
Injection, solutionSubcutaneous1.7 mg/0.75mL
Injection, solutionSubcutaneous1.7 mg
Injection, solutionSubcutaneous2.4 mg/0.75mL
Injection, solutionSubcutaneous2.4 mg
SolutionSubcutaneous0.25 mg / 0.5 mL
SolutionSubcutaneous0.5 mg / 0.5 mL
SolutionSubcutaneous0.68 mg
SolutionSubcutaneous1 mg / 1.5 mL
SolutionSubcutaneous1 mg / 0.5 mL
SolutionSubcutaneous1.7 mg / 0.75 mL
SolutionSubcutaneous2 mg / 1.5 mL
SolutionSubcutaneous2.4 mg / 0.75 mL
SolutionSubcutaneous4 mg / 3 mL
SolutionSubcutaneous6.8 mg / 3 mL
SolutionSubcutaneous9.6 mg / 3 mL
Injection, solution1.7 mg
Injection, solution2.4 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8672898Yes2014-03-182022-07-02US flag
US8684969Yes2014-04-012026-04-20US flag
US9132239Yes2015-09-152032-08-01US flag
US8920383Yes2014-12-302027-01-17US flag
US6899699Yes2005-05-312022-07-01US flag
US9108002Yes2015-08-182026-07-26US flag
US8114833Yes2012-02-142026-02-13US flag
US9486588Yes2016-11-082022-07-02US flag
US9457154Yes2016-10-042028-03-27US flag
USRE46363Yes2017-04-112027-02-03US flag
US9687611Yes2017-06-272027-08-27US flag
US9775953Yes2017-10-032027-01-17US flag
US8129343No2012-03-062029-01-29US flag
US8536122No2013-09-172026-03-20US flag
US8579869Yes2013-11-122023-12-30US flag
US7762994Yes2010-07-272024-11-23US flag
US9861757Yes2018-01-092026-07-20US flag
US9616180Yes2017-04-112026-07-20US flag
US10220155Yes2019-03-052027-01-17US flag
US10335462No2019-07-022033-06-21US flag
US10357616No2019-07-232026-01-20US flag
US9278123No2016-03-082031-12-16US flag
US10278923No2019-05-072034-05-02US flag
US10376652No2019-08-132026-01-20US flag
US10086047No2018-10-022031-12-16US flag
US10933120No2021-03-022033-03-15US flag
US10960052No2021-03-302031-12-16US flag
US10888605No2021-01-122038-08-24US flag
US9764003No2017-09-192033-06-21US flag
US11097063No2021-08-242026-07-17US flag
US11311679No2006-01-202026-01-20US flag
US11318191No2021-02-172041-02-17US flag
US11382957No2011-12-162031-12-16US flag
US11446443No2005-10-202025-10-20US flag
US11752198No2018-08-242038-08-24US flag
US11759501No2013-03-152033-03-15US flag
US11759502No2013-03-152033-03-15US flag
US11759503No2013-03-152033-03-15US flag

Properties

State
Liquid
Experimental Properties
PropertyValueSource
water solubility<1 mg/mLhttps://www.selleck.cn/msds/MSDS_S9697.pdf
Predicted Properties
PropertyValueSource
logP-18Chemaxon
pKa (Strongest Acidic)2.74Chemaxon
pKa (Strongest Basic)12.26Chemaxon
Physiological Charge-4Chemaxon
Hydrogen Acceptor Count67Chemaxon
Hydrogen Donor Count57Chemaxon
Polar Surface Area1646.18 Å2Chemaxon
Rotatable Bond Count149Chemaxon
Refractivity1048.56 m3·mol-1Chemaxon
Polarizability427.61 Å3Chemaxon
Number of Rings6Chemaxon
Bioavailability0Chemaxon
Rule of FiveNoChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available
Chromatographic Properties
Collision Cross Sections (CCS)
Not Available

Targets

Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
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
  1. 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]
  2. 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]
  3. Htike ZZ, Zaccardi F, Papamargaritis D, Webb DR, Khunti K, Davies MJ: Efficacy and safety of glucagon-like peptide-1 receptor agonists in type 2 diabetes: A systematic review and mixed-treatment comparison analysis. Diabetes Obes Metab. 2017 Apr;19(4):524-536. doi: 10.1111/dom.12849. Epub 2017 Feb 17. [Article]
  4. Barnett A. (2012). Type 2 diabetes (2nd ed.). Oxford.
  5. 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
  1. 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]
  2. 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
  1. 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
  1. 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
  1. 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
  1. 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]
  2. FDA Approved Drug Products: OZEMPIC (semaglutide) injection, for subcutaneous use [Link]

Drug created at December 06, 2017 17:44 / Updated at November 03, 2023 23:34