Semaglutide

Identification

Name

Semaglutide

Accession Number

DB13928

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

Type

Small Molecule

Groups

Approved, Investigational

Structure

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MOLSDFPDBSMILESInChI

Similar Structures

Structure for Semaglutide (DB13928)

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Weight

Average: 4113.641
Monoisotopic: 4111.11537713

Chemical Formula

C₁₈₇H₂₉₁N₄₅O₅₉

Synonyms

• Semaglutide

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

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

• Type 2 Diabetes Mellitus

Contraindications & Blackbox Warnings

Learn about our commercial Contraindications & Blackbox Warnings data.

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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	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.^4,17 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

Hover over products below to view reaction partners

• Semaglutide
  • P3 semaglutide
  • U7 semaglutide
    • U6 semaglutide

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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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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
Unlock Additional Data
Acarbose	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.

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
A severity rating for each drug interaction, from minor to major.
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Evidence Level
Evidence Level
A rating for the strength of the evidence supporting each drug interaction.
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Action
Action
An effect category for each drug interaction. Know how this interaction affects the subject drug.
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Food Interactions

• Take on an empty stomach. Take 30 minutes before the first meal of the day.
• Take with plain water. Do not exceed 4 ounces of water (1/2 cup).

Products

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Unlock Additional Data
Ozempic	Injection, solution	1.34 mg/1mL	Subcutaneous	Novo Nordisk	2017-12-06	Not applicable
Ozempic	Injection, solution	1.34 mg/1mL	Subcutaneous	Novo Nordisk	2020-09-30	Not applicable
Ozempic	Injection, solution	1.34 mg/1mL	Subcutaneous	REMEDYREPACK INC.	2019-06-11	Not applicable
Ozempic	Solution	1 mg	Subcutaneous	Novo Nordisk	2018-02-22	Not applicable
Ozempic	Injection, solution	1.34 mg/1mL	Subcutaneous	Novo Nordisk	2017-12-06	Not applicable
Ozempic	Injection, solution	1.34 mg/1mL	Subcutaneous	A-S Medication Solutions	2017-12-06	Not applicable
Ozempic	Solution	1.34 mg	Subcutaneous	Novo Nordisk	2018-02-22	Not applicable
Rybelsus	Tablet	14 mg/1	Oral	Novo Nordisk	2019-09-20	Not applicable
Rybelsus	Tablet	3 mg	Oral	Novo Nordisk	2020-04-19	Not applicable
Rybelsus	Tablet	3 mg/1	Oral	Novo Nordisk	2019-09-20	Not applicable

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

ATC Codes

A10BJ06 — Semaglutide

• A10BJ — Glucagon-like peptide-1 (GLP-1) analogues
• A10B — BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
• A10 — DRUGS USED IN DIABETES
• A — ALIMENTARY TRACT AND METABOLISM

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) 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 / Valine and derivatives / N-acyl-alpha amino acids / Tryptamines and derivatives / Serine and derivatives / Alpha amino acid amides / Alanine and derivatives / Amphetamines and derivatives / 3-alkylindoles / Imidazolyl carboxylic acids and derivatives / 1-hydroxy-2-unsubstituted benzenoids / Aralkylamines / Substituted pyrroles / N-acyl amines / Heteroaromatic compounds / Secondary carboxylic acid amides / Amino acids / Primary carboxylic acid amides / Secondary alcohols / Guanidines / Dialkyl ethers / Carboxylic acids / Carboximidamides / Azacyclic compounds / Primary alcohols / Hydrocarbon derivatives / Organic oxides / Monoalkylamines / Carbonyl compounds / Imines

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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 / Amphetamine or derivatives / Aralkylamine / Arginine or derivatives / Aromatic heteropolycyclic compound / Aspartic acid or derivatives / Azacycle / Azole / Benzenoid / Carbonyl group / Carboxamide group / Carboximidamide / Carboxylic acid / Carboxylic acid derivative / Dialkyl ether / Ether / Fatty acyl / Fatty amide / Glutamic acid or derivatives / Glutamine or derivatives / Guanidine / Heteroaromatic compound / Histidine or derivatives / Hydrocarbon derivative / Imidazole / Imidazolyl carboxylic acid derivative / Imine / Indole / Indole or derivatives / Isoleucine or derivatives / Leucine or derivatives / Monocyclic benzene moiety / N-acyl-alpha amino acid or derivatives / N-acyl-alpha-amino acid / N-acyl-amine / N-substituted-alpha-amino acid / Organic nitrogen compound / Organic oxide / Organic oxygen compound / Organoheterocyclic compound / Organonitrogen compound / Organooxygen compound / Phenol / Phenylalanine or derivatives / Polypeptide / Primary alcohol / Primary aliphatic amine / Primary amine / Primary carboxylic acid amide / Pyrrole / Secondary alcohol / Secondary carboxylic acid amide / Serine or derivatives / Substituted pyrrole / Triptan / Tyrosine or derivatives / Valine or derivatives

show 56 more

Molecular Framework

Aromatic heteropolycyclic compounds

External Descriptors

Not Available

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-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[[email protected]](C)[[email protected]](NC(=O)[[email protected]](CC1=CC=CC=C1)NC(=O)[[email protected]](CCC(O)=O)NC(=O)[[email protected]](CCCCNC(=O)COCCOCCNC(=O)COCCOCCNC(=O)CC[[email protected]@H](NC(=O)CCCCCCCCCCCCCCCCC(O)=O)C(O)=O)NC(=O)[[email protected]](C)NC(=O)[[email protected]](C)NC(=O)[[email protected]](CCC(N)=O)NC(=O)CNC(=O)[[email protected]](CCC(O)=O)NC(=O)[[email protected]](CC(C)C)NC(=O)[[email protected]](CC1=CC=C(O)C=C1)NC(=O)[[email protected]](CO)NC(=O)[[email protected]](CO)NC(=O)[[email protected]@H](NC(=O)[[email protected]](CC(O)=O)NC(=O)[[email protected]](CO)NC(=O)[[email protected]@H](NC(=O)[[email protected]](CC1=CC=CC=C1)NC(=O)[[email protected]@H](NC(=O)CNC(=O)[[email protected]](CCC(O)=O)NC(=O)C(C)(C)NC(=O)[[email protected]@H](N)CC1=CNC=N1)[[email protected]@H](C)O)[[email protected]@H](C)O)C(C)C)C(=O)N[[email protected]@H](C)C(=O)N[[email protected]@H](CC1=CNC2=C1C=CC=C2)C(=O)N[[email protected]@H](CC(C)C)C(=O)N[[email protected]@H](C(C)C)C(=O)N[[email protected]@H](CCCNC(N)=N)C(=O)NCC(=O)N[[email protected]@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. [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]
20. DailyMed: Rybelsus (semaglutide) oral tablet [Link]

External Links

ChemSpider

34985066

BindingDB

50121400

RxNav

1991302

ChEMBL

CHEMBL3616752

Wikipedia

Semaglutide

AHFS Codes

• 68:20.06 — Incretin Mimetics

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Completed	Other	Type 2 Diabetes Mellitus	1
4	Completed	Treatment	BMI >27 kg/m2 / BMI >30 kg/m2 / Healthy Volunteers / Type 2 Diabetes Mellitus	1
4	Not Yet Recruiting	Treatment	Type 2 Diabetes Mellitus	1
4	Not Yet Recruiting	Treatment	Type 2 Diabetes With Renal Manifestations	1
4	Recruiting	Treatment	Central Neural Response / Gastric Emptying / Polycystic Ovarian Syndrome / Semaglutide / Taste altered / Taste, Altered / Tongue Tissue Transcriptome	1
4	Recruiting	Treatment	Coronary Artery Disease (CAD) / Type 2 Diabetes Mellitus	1
4	Recruiting	Treatment	Type 2 Diabetes Mellitus	1
3	Active Not Recruiting	Treatment	BMI >27 kg/m2 / BMI >30 kg/m2	4
3	Active Not Recruiting	Treatment	Metabolism and Nutrition Disorders / Overweight or Obesity	1
3	Active Not Recruiting	Treatment	Type 2 Diabetes Mellitus	3

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection, solution	Cutaneous; Parenteral	0.25 MG
Injection, solution	Cutaneous; Parenteral	0.5 MG
Injection, solution	Cutaneous; Parenteral	1 MG
Injection, solution	Cutaneous; Parenteral	1.34 MG/ML
Injection, solution	Subcutaneous	1.34 mg/1mL
Solution	Subcutaneous	1 mg
Injection, solution		1.34 mg/1mL
Solution	Subcutaneous	1.34 mg
Solution
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

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
Unlock Additional Data
US8672898	Yes	2014-03-18	2022-07-02
US8684969	Yes	2014-04-01	2026-04-20
US9132239	Yes	2015-09-15	2032-08-01
US8920383	Yes	2014-12-30	2027-01-17
US6899699	Yes	2005-05-31	2022-07-01
US9108002	Yes	2015-08-18	2026-07-26
US8114833	Yes	2012-02-14	2026-02-13
US9486588	Yes	2016-11-08	2022-07-02
US9457154	Yes	2016-10-04	2028-03-27
USRE46363	Yes	2017-04-11	2027-02-03
US9687611	Yes	2017-06-27	2027-08-27
US9775953	Yes	2017-10-03	2027-01-17
US8129343	No	2012-03-06	2029-01-29
US8536122	No	2013-09-17	2026-03-20
US8579869	Yes	2013-11-12	2023-12-30
US7762994	Yes	2010-07-27	2024-11-23
US9861757	Yes	2018-01-09	2026-07-20
US9616180	Yes	2017-04-11	2026-07-20
US10220155	Yes	2019-03-05	2027-01-17
US10335462	No	2019-07-02	2033-06-21
US10357616	No	2019-07-23	2026-01-20
US9278123	No	2016-03-08	2031-12-16
US10278923	No	2019-05-07	2034-05-02
US10376652	No	2019-08-13	2026-01-20
US10086047	No	2018-10-02	2031-12-16

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

Property	Value	Source
logP	-17	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	1047.99 m3·mol-1	ChemAxon
Polarizability	427.73 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

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Drug created on December 06, 2017 10:44 / Updated on October 26, 2020 22:41