Identification

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Name
Semaglutide
Accession Number
DB13928
Type
Small Molecule
Groups
Approved, Investigational
Description

Semaglutide is a glucagon-like peptide 1 (GLP-1) analog used to manage type 2 diabetes along with lifestyle changes 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 2019.16

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

Structure
Thumb
Synonyms
  • Semaglutide
External IDs
NN-9535 / NN9535 / NNC 0113-0217 / NNC-0113-0217
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
OzempicInjection, solution1.34 mg/1mLSubcutaneousNovo Nordisk2017-12-06Not applicableUs
OzempicSolution1 mgSubcutaneousNovo Nordisk2018-02-22Not applicableCanada
OzempicInjection, solution1.34 mg/1mLSubcutaneousREMEDYREPACK INC.2019-06-11Not applicableUs
OzempicSolution1.34 mgSubcutaneousNovo Nordisk2018-02-22Not applicableCanada
OzempicInjection, solution1.34 mg/1mLSubcutaneousNovo Nordisk2017-12-06Not applicableUs
RybelsusTablet14 mg/1OralNovo Nordisk2019-09-20Not applicableUs
RybelsusTablet7 mg/1OralNovo Nordisk2019-09-20Not applicableUs
RybelsusTablet3 mg/1OralNovo Nordisk2019-09-20Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories
UNII
53AXN4NNHX
CAS number
910463-68-2
Weight
Average: 4113.641
Monoisotopic: 4111.11537713
Chemical Formula
C187H291N45O59
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-4-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=CNC=N1)[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

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

It is important to note that 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

Associated Conditions
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% homologous 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

TargetActionsOrganism
AGlucagon-like peptide 1 receptor
agonist
Humans
Additional Data Available
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Contraindications

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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.19

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

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

Toxicity

The oral LD50 of semaglutide is 270 mg/kg in the rat.18

Overdose Overdoses of up to 4mg in one ingestion have been reported. Nausea was the most commonly reported symptom. All patients in clinical trials that reported an overdose recovered fully.19 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 1 week.17 There is no antidote to an overdose with semaglutide.19

Affected organisms
  • Humans and other mammals
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
2,4-thiazolidinedioneThe risk or severity of hypoglycemia can be increased when 2,4-thiazolidinedione is combined with Semaglutide.
5-(2-methylpiperazine-1-sulfonyl)isoquinolineThe therapeutic efficacy of Semaglutide can be increased when used in combination with 5-(2-methylpiperazine-1-sulfonyl)isoquinoline.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the hypoglycemic activities of Semaglutide.
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.
Acetylsalicylic acidThe risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with Semaglutide.
AgmatineThe risk or severity of hypoglycemia can be increased when Agmatine is combined with Semaglutide.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

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Food Interactions
Not Available

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. [PubMed:24608440]
  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. [PubMed:28266779]
  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. [PubMed:24140094]
  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. [PubMed:28323117]
  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. [PubMed:29766634]
  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. [PubMed:29756388]
  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. [PubMed:30623143]
  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. [PubMed:30929417]
  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. [PubMed:31436480]
  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. [PubMed:29915923]
  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. [PubMed:29205786]
  12. Barnett A. (2012). Type 2 diabetes (2nd ed.). Oxford.
  13. FDA Reports [Link]
  14. Novo Nordisk News [Link]
  15. FDA Reports [Link]
  16. Rybelsus tablets [Link]
  17. Ozempic injection FDA label [Link]
  18. Semaglutide MSDS [Link]
  19. Ozempic, Medicines UK document [Link]
External Links
ChemSpider
34985066
BindingDB
50121400
ChEMBL
CHEMBL3616752
Wikipedia
Semaglutide
ATC Codes
A10BJ06 — Semaglutide
AHFS Codes
  • 68:20.06 — Incretin Mimetics

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentHepatobiliary disorders / Non-Alcoholic Fatty Liver Disease (NAFLD)1
1CompletedBasic ScienceDiabetes Mellitus (DM) / Healthy Volunteers1
1CompletedTreatmentBMI >27 kg/m2 / BMI >30 kg/m21
1CompletedTreatmentBMI >30 kg/m2 / Diabetes Mellitus (DM) / Healthy Volunteers / Metabolism and Nutrition Disorder1
1CompletedTreatmentDiabetes Mellitus (DM) / Healthy Volunteers13
1CompletedTreatmentDiabetes Mellitus (DM) / Healthy Volunteers / Type 2 Diabetes Mellitus9
1CompletedTreatmentDiabetes Mellitus (DM) / Hepatic Impaired / Type 2 Diabetes Mellitus1
1CompletedTreatmentDiabetes Mellitus (DM) / Impaired Renal Function / Type 2 Diabetes Mellitus1
1CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus9
1CompletedTreatmentMetabolism and Nutrition Disorders / Overweight or Obesity1
1CompletedTreatmentObesity and Overweight1
1CompletedTreatmentType 2 Diabetes Mellitus4
1Not Yet RecruitingTreatmentHealthy Volunteers / Type 2 Diabetes Mellitus1
1RecruitingBasic ScienceType 2 Diabetes Mellitus1
1RecruitingTreatmentBMI >27 kg/m2 / BMI >30 kg/m21
1RecruitingTreatmentHealthy Volunteers / Type 2 Diabetes Mellitus3
1RecruitingTreatmentType 2 Diabetes Mellitus1
1TerminatedTreatmentBMI >27 kg/m2 / BMI >30 kg/m21
2Active Not RecruitingTreatmentHepatobiliary disorders / Non-Alcoholic Steatohepatitis1
2CompletedTreatmentBMI >30 kg/m2 / Metabolism and Nutrition Disorder1
2CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus3
2CompletedTreatmentHealthy Volunteers Diabetes Mellitus, Type 2 / Healthy Volunteers Obesity / Healthy Volunteers Overweight1
2Not Yet RecruitingTreatmentParkinson's Disease (PD)1
2Not Yet RecruitingTreatmentType 2 Diabetes Mellitus1
2RecruitingBasic ScienceNon-Alcoholic Fatty Liver Disease (NAFLD) / Non-Alcoholic Steatohepatitis1
2RecruitingTreatmentBMI >30 kg/m2 / Human Immunodeficiency Virus Infection(HIV)/Acquired Immunodeficiency Syndrome (AIDS) / Lipohypertrophy1
2RecruitingTreatmentHealthy Volunteers Diabetes Mellitus, Type 2 / Healthy Volunteers Obesity / Healthy Volunteers Overweight1
2RecruitingTreatmentNon-Alcoholic Steatohepatitis1
2RecruitingTreatmentNonalcoholic Steatohepatitis1
2, 3RecruitingTreatmentType 1 Insulin-Dependent Diabetes Mellitus1
3Active Not RecruitingTreatmentBMI >27 kg/m2 / BMI >30 kg/m24
3Active Not RecruitingTreatmentBMI >30 kg/m2 / Metabolism and Nutrition Disorder1
3Active Not RecruitingTreatmentMetabolism and Nutrition Disorder / Overweight or Obesity1
3CompletedTreatmentDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus23
3RecruitingTreatmentBMI >27 kg/m2 / BMI >30 kg/m23
3RecruitingTreatmentType 2 Diabetes Mellitus9
4CompletedOtherType 2 Diabetes Mellitus1
4Not Yet RecruitingTreatmentType 2 Diabetes With Renal Manifestations1
4RecruitingTreatmentCoronary Artery Disease / Type 2 Diabetes Mellitus1
4RecruitingTreatmentType 2 Diabetes Mellitus1
Not AvailableActive Not RecruitingNot AvailableDiabetes Mellitus (DM) / Type 2 Diabetes Mellitus1
Not AvailableActive Not RecruitingNot AvailableType 2 Diabetes Mellitus3
Not AvailableEnrolling by InvitationNot AvailableType 2 Diabetes Mellitus3
Not AvailableNot Yet RecruitingNot AvailableType 2 Diabetes Mellitus1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, solutionSubcutaneous1.34 mg/1mL
SolutionSubcutaneous1 mg
SolutionSubcutaneous1.34 mg
TabletOral14 mg/1
TabletOral3 mg/1
TabletOral7 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8672898Yes2014-03-182022-07-02Us
US8684969Yes2014-04-012026-04-20Us
US9132239Yes2015-09-152032-08-01Us
US8920383Yes2014-12-302027-01-17Us
US6899699Yes2005-05-312022-07-01Us
US9108002Yes2015-08-182026-07-26Us
US8114833Yes2012-02-142026-02-13Us
US9486588Yes2016-11-082022-07-02Us
US9457154Yes2016-10-042028-03-27Us
USRE46363Yes2017-04-112027-02-03Us
US9687611Yes2017-06-272027-08-27Us
US9775953Yes2017-10-032027-01-17Us
US8129343No2012-03-062029-01-29Us
US8536122No2013-09-172026-03-20Us
US8579869Yes2013-11-122023-12-30Us
US7762994Yes2010-07-272024-11-23Us
US9861757Yes2018-01-092026-07-20Us
US9616180Yes2017-04-112026-07-20Us
US10220155Yes2019-03-052027-01-17Us
US10335462No2013-06-212033-06-21Us
US10357616No2006-01-202026-01-20Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

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Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
logP-17ChemAxon
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
Refractivity1047.99 m3·mol-1ChemAxon
Polarizability427.73 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

Taxonomy

Classification
Not classified

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
  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. [PubMed:24140094]
  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. [PubMed:21314233]
  3. Barnett A. (2012). Type 2 diabetes (2nd ed.). Oxford.
  4. Ozempic injection FDA label [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. [PubMed:28266779]
  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. [PubMed:28323117]
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. [PubMed:28323117]
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 Reports [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 Reports [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. [PubMed:28266779]
  2. Ozempic injection FDA label [Link]

Drug created on December 06, 2017 10:44 / Updated on November 16, 2019 10:48