Lixisenatide
Identification
- Summary
Lixisenatide is a GLP-1 receptor agonist used for the management of type 2 diabetes mellitus.
- Brand Names
- Adlyxin Starter Kit, Lyxumia, Soliqua
- Generic Name
- Lixisenatide
- DrugBank Accession Number
- DB09265
- Background
Lixisenatide is a glucagon-like peptide-1 (GLP-1) receptor agonist used in the treatment of type II diabetes mellitus (T2DM). It is sold by Sanofi-Aventis under the brand name Adlyxin in the US3 and Lyxumia in the EU.4 Adlyxin recieved FDA approval July 28, 2016.3
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Hormones - Protein Chemical Formula
- Not Available
- Protein Average Weight
- 4858.0 Da
- Sequences
> Lixisenatide Sequence HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK
Download FASTA FormatReferences:
- NIH Inxight Drugs: Lixisenatide [Link]
- Synonyms
- des-38-proline-exendine-4 (Heloderma suspectum)-(1-39)-peptidylpenta-L-lysyl-L-lysinamide
- DesPro38Exendin-4(1-39)-Lys6-NH2
- Lixisenatida
- Lixisénatide
- Lixisenatide
- External IDs
- AQVE-10010
- AVE 0010
- AVE0010
- ZP 10
- ZP10A peptide
Pharmacology
- Indication
Lixisenatide is indicated as an adjunct to diet and exercise to improve glycemic control in adult patients with type II diabetes mellitus.5 It is also available in combination with insulin glargine for the same indication.6
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
- Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Lixisenatide acts as an agonist at the GLP-1 receptor. In the pancreas, this agonism results in increased glucose-stimulated insulin exocytosis by beta islet cells. This produces a reduction in blood glucose due to increased glucose uptake by tissues.1 GLP-1 receptor activation in the GI tract results in delayed gastric emptying which is thought to mediate the effects of lixisenatide on postprandial blood glucose.
- Mechanism of action
The activation of the GLP-1 receptor by lixisenatide results in the activation of adenylyl cyclase.2 This increases the concentration of cyclic adenosine monophosphate in the cell leading to the activation of protein kinase A (PKA) as well as Epac1 and Epac2. PKA, Epac1, and Epac2 are involved the in release of Ca2+ from the endoplasmic reticulum which is known as the "amplification" pathway which increases insulin release when the triggering pathway is activated. By activating this amplification pathway lixisenatide increases glucose stimulated insulin secretion.
Target Actions Organism AGlucagon-like peptide 1 receptor agonistHumans - Absorption
Following subcutaneous administration, the median Tmax of lixisenatide ranged from 1-3.5 hours, with no clinically relevant differences in the rate of absorption noted between possible injection sites (i.e. thigh, abdomen, or arm).5
- Volume of distribution
The apparent volume of distribution following subcutaneous administration is approximately 100 L.5
- Protein binding
Lixisenatide is approximately 55% bound to human plasma proteins.4
- Metabolism
Lixisenatide is likely catabolized via non-specific proteolytic degradation.5
- Route of elimination
Lixisenatide is presumably eliminated via glomerular filtration and proteolytic degradation.5
- Half-life
Following the administration of multiple doses in patients with type II diabetes mellitus, the mean terminal half-life of lixisenatide was approximately 3 hours.5
- Clearance
The mean apparent clearance of lixisenatide is approximately 35 L/h.5
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Thyroid C-cell adenomas occurred in rats when exposed to >15 times human exposure of 20mcg/day.5 Overdose is associated with GI side effects typical of GLP-1 receptor agonists.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Lixisenatide which could result in a higher serum level. Acarbose The risk or severity of hypoglycemia can be increased when Acarbose is combined with Lixisenatide. Acebutolol The therapeutic efficacy of Lixisenatide can be increased when used in combination with Acebutolol. Aceclofenac Aceclofenac may decrease the excretion rate of Lixisenatide which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Lixisenatide which could result in a higher serum level. Acenocoumarol Lixisenatide can cause a decrease in the absorption of Acenocoumarol resulting in a reduced serum concentration and potentially a decrease in efficacy. Acetaminophen Acetaminophen may decrease the excretion rate of Lixisenatide which could result in a higher serum level. Acetazolamide The therapeutic efficacy of Lixisenatide can be increased when used in combination with Acetazolamide. Acetohexamide The risk or severity of hypoglycemia can be increased when Lixisenatide is combined with Acetohexamide. Acetyl sulfisoxazole The therapeutic efficacy of Lixisenatide can be increased when used in combination with Acetyl sulfisoxazole. Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- Take at the same time every day.
- Take before a meal. Take lixisenatide within one hour before the first meal of the day.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Adlyxin Injection, solution 100 ug/1mL Subcutaneous sanofi-aventis U.S. LLC 2016-07-27 Not applicable US Adlyxine Solution 20 mcg / act Subcutaneous Sanofi Aventis 2017-09-12 2023-09-15 Canada Adlyxine Solution 10 mcg / act Subcutaneous Sanofi Aventis 2017-09-12 2023-05-04 Canada Lyxumia Injection, solution 20 μg Subcutaneous SANOFI WINTHROP INDUSTRIE 2016-09-08 Not applicable EU Lyxumia Injection, solution 20 μg Subcutaneous SANOFI WINTHROP INDUSTRIE 2016-09-08 Not applicable EU Lyxumia Injection, solution 20 μg Subcutaneous SANOFI WINTHROP INDUSTRIE 2016-09-08 Not applicable EU Lyxumia Injection, solution 10 μg Subcutaneous SANOFI WINTHROP INDUSTRIE 2016-09-08 Not applicable EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Adlyxin Lixisenatide (50 ug/1mL) + Lixisenatide (100 ug/1mL) Injection, solution; Kit Subcutaneous sanofi-aventis U.S. LLC 2016-07-27 Not applicable US Adlyxin Lixisenatide (50 ug/1mL) + Lixisenatide (100 ug/1mL) Injection, solution; Kit Subcutaneous sanofi-aventis U.S. LLC 2016-07-27 Not applicable US Adlyxine Lixisenatide (0.05 mg / mL) + Lixisenatide (0.1 mg / mL) Kit; Solution Subcutaneous Sanofi Aventis 2017-09-12 2018-10-08 Canada Adlyxine Lixisenatide (0.05 mg / mL) + Lixisenatide (0.1 mg / mL) Kit; Solution Subcutaneous Sanofi Aventis 2017-09-12 2018-10-08 Canada LYXUMIA SOLUTION FOR INJECTION IN PRE-FILLED PEN 10MCG AND 20MCG (50mcg/mL and 100mcg/mL) Lixisenatide (0.05 mg/mL) + Lixisenatide (0.1 mg/mL) Injection, solution Subcutaneous SANOFI-AVENTIS SINGAPORE PTE. LTD. 2014-10-30 Not applicable Singapore LYXUMIA SOLUTION FOR INJECTION IN PRE-FILLED PEN 10MCG AND 20MCG (50mcg/mL and 100mcg/mL) Lixisenatide (0.05 mg/mL) + Lixisenatide (0.1 mg/mL) Injection, solution Subcutaneous SANOFI-AVENTIS SINGAPORE PTE. LTD. 2014-10-30 Not applicable Singapore Soliqua Lixisenatide (33 mcg / mL) + Insulin glargine (100 unit / mL) Solution Subcutaneous Sanofi Aventis 2018-09-12 Not applicable Canada Soliqua 100/33 Lixisenatide (33 ug/1mL) + Insulin glargine (100 U/1mL) Injection, solution Subcutaneous sanofi-aventis U.S. LLC 2016-11-21 Not applicable US SOLİQUA SOLOSTAR 100 U/ML + 33 MCG/ML SC ENJEKSİYONLUK ÇÖZELTİ İÇEREN KULLANIMA HAZIR KALEM, 3 KALEM Lixisenatide (33 mcg/mL) + Insulin glargine (100 U/mL) Injection, solution Subcutaneous SANOFİ SAĞLIK ÜRÜNLERİ LTD. ŞTİ. 2020-08-14 Not applicable Turkey SOLİQUA SOLOSTAR 100 U/ML + 33 MCG/ML SC ENJEKSİYONLUK ÇÖZELTİ İÇEREN KULLANIMA HAZIR KALEM, 5 KALEM Lixisenatide (33 mcg/mL) + Insulin glargine (100 U/mL) Injection, solution Subcutaneous SANOFİ SAĞLIK ÜRÜNLERİ LTD. ŞTİ. 2020-08-14 Not applicable Turkey
Categories
- ATC Codes
- A10AE54 — Insulin glargine and lixisenatide
- A10AE — Insulins and analogues for injection, long-acting
- A10A — INSULINS AND ANALOGUES
- A10 — DRUGS USED IN DIABETES
- A — ALIMENTARY TRACT AND METABOLISM
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 74O62BB01U
- CAS number
- 320367-13-3
References
- General References
- Lorenz M, Pfeiffer C, Steinstrasser A, Becker RH, Rutten H, Ruus P, Horowitz M: Effects of lixisenatide once daily on gastric emptying in type 2 diabetes--relationship to postprandial glycemia. Regul Pept. 2013 Aug 10;185:1-8. doi: 10.1016/j.regpep.2013.04.001. Epub 2013 May 9. [Article]
- Doyle ME, Egan JM: Mechanisms of action of glucagon-like peptide 1 in the pancreas. Pharmacol Ther. 2007 Mar;113(3):546-93. Epub 2006 Dec 28. [Article]
- Adlyxin FDA Approval Announcement [Link]
- EMA CHMP Assessment Report: Lyxumia (lixisenatide) [Link]
- FDA Approved Drug Products: Adlyxin (lixisenatide) injection for subcutaneous use (Sept 2023) [Link]
- FDA Approved Drug Products: Soliqua (insulin glargine and lixisenatide) injection for subcutaneous use (Sept 2023) [Link]
- External Links
- KEGG Drug
- D09729
- PubChem Compound
- 131704317
- PubChem Substance
- 310265161
- ChemSpider
- 17295846
- 1440051
- ChEBI
- 85662
- ChEMBL
- CHEMBL2108336
- Wikipedia
- Lixisenatide
- MSDS
- Download (80 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Basic Science Type 2 Diabetes Mellitus 1 4 Completed Treatment Diabetes Mellitus / Diabetic Kidney Disease (DKD) / Diabetic Nephropathy / Glucagon-Like Peptide 1 1 4 Completed Treatment Diabetes / Type 2 Diabetes Mellitus 1 4 Completed Treatment Type 2 Diabetes Mellitus 4 4 Recruiting Diagnostic Healthy Subjects (HS) / Type 1 Diabetes Mellitus 1 4 Terminated Treatment Type 2 Diabetes Mellitus 1 4 Unknown Status Treatment Type 2 Diabetes Mellitus 1 3 Completed Treatment Acute Coronary Syndrome (ACS) 1 3 Completed Treatment Type 2 Diabetes Mellitus 31 3 Terminated Treatment Type 2 Diabetes Mellitus 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Subcutaneous 100 ug/1mL Injection, solution; kit Subcutaneous Kit; solution Subcutaneous Solution Subcutaneous 10 mcg / act Solution Subcutaneous 20 mcg / act Injection Injection, solution Parenteral; Subcutaneous 10 MICROGRAMMI Injection, solution Parenteral; Subcutaneous 20 MICROGRAMMI Injection, solution Subcutaneous 10 μg Injection, solution Subcutaneous 20 μg Solution Subcutaneous 0.15 mg/3ml Solution Subcutaneous 0.3 mg/3ml Injection, solution 10 mcg Injection, solution Subcutaneous 10 mcg/0.2ml Injection, solution 20 mcg Injection, solution Subcutaneous 20 mcg/0.2ml Injection, solution Subcutaneous 50 mcg/mL Injection, solution Subcutaneous 0.05 mg/mL Injection, solution Subcutaneous 100 mcg/mL Solution Subcutaneous 0.05 mg Solution Subcutaneous 0.1 mg Injection, solution Solution Subcutaneous Injection, solution Subcutaneous Injection, solution Subcutaneous 100 units/ml Injection, solution Cutaneous; Parenteral - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US9011391 No 2015-04-21 2024-03-26 US US9233211 No 2016-01-12 2024-03-02 US US8603044 No 2013-12-10 2024-03-02 US US8512297 No 2013-08-20 2024-09-15 US US8679069 No 2014-03-25 2025-04-12 US US8992486 No 2015-03-31 2024-06-05 US US8556864 No 2013-10-15 2024-03-03 US US7918833 Yes 2011-04-05 2028-03-23 US US9561331 No 2017-02-07 2024-08-28 US US9623189 No 2017-04-18 2024-08-19 US US9610409 No 2017-04-04 2024-03-02 US US9526844 No 2016-12-27 2024-03-02 US US9604008 No 2017-03-28 2024-03-02 US US9533105 No 2017-01-03 2024-08-17 US US9408979 No 2016-08-09 2024-03-02 US US9604009 No 2017-03-28 2024-08-16 US US9072836 No 2015-07-07 2032-03-15 US US9084853 No 2015-07-21 2031-10-05 US US8882721 No 2014-11-11 2031-06-28 US US9511193 No 2016-12-06 2032-01-19 US USRE45313 No 2014-12-30 2020-07-12 US US8475414 No 2013-07-02 2030-12-28 US US9308329 No 2016-04-12 2030-12-28 US US8915888 No 2014-12-23 2030-06-08 US US9408893 No 2016-08-09 2032-08-27 US US9526764 No 2016-12-27 2029-10-09 US US9707176 No 2017-07-18 2030-11-11 US US9775954 No 2017-10-03 2024-03-02 US US9827379 No 2017-11-28 2024-03-02 US US9821032 No 2017-11-21 2032-05-09 US US9855388 No 2018-01-02 2029-04-24 US US9440029 No 2016-09-13 2032-01-30 US US9950039 No 2018-04-24 2035-12-10 US US9981013 No 2018-05-29 2030-08-30 US US9717852 No 2017-08-01 2033-04-08 US US10028910 No 2018-07-24 2030-11-11 US US10029011 No 2018-07-24 2032-08-02 US US10117909 No 2018-11-06 2029-10-09 US US10201663 No 2019-02-12 2034-03-10 US
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets

- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Transmembrane signaling receptor activity
- Specific Function
- This is a receptor for glucagon-like peptide 1. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
- Gene Name
- GLP1R
- Uniprot ID
- P43220
- Uniprot Name
- Glucagon-like peptide 1 receptor
- Molecular Weight
- 53025.22 Da
References
- Nadkarni P, Chepurny OG, Holz GG: Regulation of glucose homeostasis by GLP-1. Prog Mol Biol Transl Sci. 2014;121:23-65. doi: 10.1016/B978-0-12-800101-1.00002-8. [Article]
- Lorenz M, Lawson F, Owens D, Raccah D, Roy-Duval C, Lehmann A, Perfetti R, Blonde L: Differential effects of glucagon-like peptide-1 receptor agonists on heart rate. Cardiovasc Diabetol. 2017 Jan 13;16(1):6. doi: 10.1186/s12933-016-0490-6. [Article]
- Gallwitz B: Novel Therapeutic Approaches in Diabetes. Endocr Dev. 2016;31:43-56. doi: 10.1159/000439372. Epub 2016 Jan 19. [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]
Drug created at October 27, 2015 21:41 / Updated at October 06, 2023 23:49