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

Type

Small Molecule

Groups

Approved, Investigational

Structure

Similar Structures

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

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Associated Conditions

Associated Therapies

Chronic Weight Management therapy

Contraindications & Blackbox Warnings

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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.^5,12

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

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.^4,15 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

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.^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

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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.

Drug	Interaction
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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.

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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).

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International/Other Brands

Wegovy (Novo Nordisk)

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
Ozempic	Injection, solution	1 mg/0.74ml	Subcutaneous	Novo Nordisk	2021-01-22	Not applicable
Ozempic	Solution	1.34 mg / mL	Subcutaneous	Novo Nordisk	2018-02-22	Not applicable
Ozempic	Injection, solution	0.5 mg/0.37ml	Subcutaneous	Novo Nordisk	2021-01-22	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	2020-09-30	Not applicable
Ozempic	Injection, solution	1.34 mg/1mL	Subcutaneous	A-S Medication Solutions	2017-12-06	Not applicable
Ozempic	Injection, solution	2 mg/0.74ml	Subcutaneous	Novo Nordisk	2022-06-08	Not applicable
Ozempic	Injection, solution	1 mg/0.74ml	Subcutaneous	Novo Nordisk	2021-01-22	Not applicable
Ozempic	Injection, solution	0.25 mg/0.19ml	Subcutaneous	Novo Nordisk	2021-01-22	Not applicable
Ozempic	Injection, solution	1.34 mg/1mL	Subcutaneous	Novo Nordisk	2017-12-06	Not applicable

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]
FDA Briefing Document: Semaglutide subcutaneous once-weekly [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]
EMA Approved Drug Products: 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]
Novo Nordisk New Release: Health Canada approves Wegovy™ for the treatment of adults with obesity [Link]
EMA Approved Drug Products: Wegovy (semaglutide) Subcutaneous Injection [Link]

External Links

ChemSpider: 34985066
BindingDB: 50121400
RxNav: 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 / Type 2 Diabetes Mellitus	1
4	Not Yet Recruiting	Diagnostic	Healthy Subjects (HS)	1
4	Not Yet Recruiting	Treatment	(NAFLD) / Diabetes Mellitus / Liver Transplant; Complications / Non Alcoholic Steatohepatitis (NASH)	1
4	Not Yet Recruiting	Treatment	Aging / Obesity	1
4	Not Yet Recruiting	Treatment	Atrial Fibrillation / BMI >27 kg/m2 / Obesity	1
4	Not Yet Recruiting	Treatment	Clozapine / GLP - 1 / Metabolic Disturbances / Olanzapine / Schizophrenia / Type 2 Diabetes Mellitus	1
4	Not Yet Recruiting	Treatment	Type 2 Diabetes With Renal Manifestations	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/0.19ml
Injection, solution	Subcutaneous	0.5 mg/0.37ml
Injection, solution	Subcutaneous	1 mg/0.74ml
Injection, solution	Subcutaneous	1.34 mg/1mL
Injection, solution	Subcutaneous	2 mg/0.74ml
Injection, solution	Subcutaneous	2.68 mg/1mL
Solution	Subcutaneous	1 mg / act
Solution	Subcutaneous	1.34 mg / mL
Solution	Subcutaneous	2.68 mg / mL
Injection, solution	Subcutaneous	1.34 mg/ml
Solution	Subcutaneous	1.34 mg
Tablet	Oral	14 mg/1
Tablet	Oral	3 mg/1
Tablet	Oral	7 mg/1
Tablet	Oral	14 mg
Tablet	Oral	3 mg
Tablet	Oral	7 mg
Injection, solution	Subcutaneous	0.25 mg
Injection, solution	Subcutaneous	0.25 mg/0.5mL
Injection, solution	Subcutaneous	0.5 mg/0.5mL
Injection, solution	Subcutaneous	0.5 mg
Injection, solution	Subcutaneous	1 mg
Injection, solution	Subcutaneous	1.0 mg/0.5mL
Injection, solution	Subcutaneous	1.7 mg/0.75mL
Injection, solution	Subcutaneous	1.7 mg
Injection, solution	Subcutaneous	2.4 mg/0.75mL
Injection, solution	Subcutaneous	2.4 mg
Solution	Subcutaneous	0.25 mg / 0.5 mL
Solution	Subcutaneous	0.5 mg / 0.5 mL
Solution	Subcutaneous	1 mg / 0.5 mL
Solution	Subcutaneous	1.7 mg / 0.75 mL
Solution	Subcutaneous	2.4 mg / 0.75 mL

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
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
US10933120	No	2021-03-02	2033-03-15
US10960052	No	2021-03-30	2031-12-16
US10888605	No	2021-01-12	2038-08-24
US9764003	No	2017-09-19	2033-06-21
US11097063	No	2021-08-24	2026-07-17

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

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Details1. Glucagon-like peptide 1 receptor

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]
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]
Barnett A. (2012). Type 2 diabetes (2nd ed.). Oxford.
FDA Approved Drug Products: OZEMPIC (semaglutide) injection, for subcutaneous use [Link]

Enzymes

Details1. Dipeptidyl peptidase 4

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]

Details2. Neprilysin

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]

Details3. Lipoprotein lipase

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]

Details4. Alpha-amylase 1

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

Details1. Serum albumin

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 at December 06, 2017 17:44 / Updated at June 03, 2022 07:24

Semaglutide

Identification

Structure for Semaglutide (DB13928)

Pharmacology

Interactions

Products

Categories

Chemical Identifiers

References

Clinical Trials

Pharmacoeconomics

Properties

Spectra

Targets

References

Enzymes

References

References

References

References

Carriers

References