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

References:

1. NIH Inxight Drugs: Lixisenatide [Link]

Download FASTA Format

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

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Associated Conditions

• Type 2 Diabetes Mellitus

Contraindications & Blackbox Warnings

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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	agonist	Humans

Absorption

Following subcutaneous administration, the median T_max 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

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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.

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• Withdrawn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

Drug	Interaction
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Abacavir	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.

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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

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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
Adlyxine	Solution	20 mcg / act	Subcutaneous	Sanofi Aventis	2017-09-12	2023-09-15
Adlyxine	Solution	10 mcg / act	Subcutaneous	Sanofi Aventis	2017-09-12	2023-05-04
Lyxumia	Injection, solution	20 μg	Subcutaneous	SANOFI WINTHROP INDUSTRIE	2016-09-08	Not applicable
Lyxumia	Injection, solution	20 μg	Subcutaneous	SANOFI WINTHROP INDUSTRIE	2016-09-08	Not applicable
Lyxumia	Injection, solution	20 μg	Subcutaneous	SANOFI WINTHROP INDUSTRIE	2016-09-08	Not applicable
Lyxumia	Injection, solution	10 μg	Subcutaneous	SANOFI WINTHROP INDUSTRIE	2016-09-08	Not applicable

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
Adlyxin	Lixisenatide (50 ug/1mL) + Lixisenatide (100 ug/1mL)	Injection, solution; Kit	Subcutaneous	sanofi-aventis U.S. LLC	2016-07-27	Not applicable
Adlyxine	Lixisenatide (0.05 mg / mL) + Lixisenatide (0.1 mg / mL)	Kit; Solution	Subcutaneous	Sanofi Aventis	2017-09-12	2018-10-08
Adlyxine	Lixisenatide (0.05 mg / mL) + Lixisenatide (0.1 mg / mL)	Kit; Solution	Subcutaneous	Sanofi Aventis	2017-09-12	2018-10-08
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
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
Soliqua	Lixisenatide (33 mcg / mL) + Insulin glargine (100 unit / mL)	Solution	Subcutaneous	Sanofi Aventis	2018-09-12	Not applicable
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
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
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

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

A10BJ03 — Lixisenatide

• 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 that are Mainly Renally Excreted
• Drugs Used in Diabetes
• GLP-1 Agonists
• Glucagon-like peptide-1 (GLP-1) analogues
• Incretin Mimetics

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

1. 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]
2. 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]
3. Adlyxin FDA Approval Announcement [Link]
4. EMA CHMP Assessment Report: Lyxumia (lixisenatide) [Link]
5. FDA Approved Drug Products: Adlyxin (lixisenatide) injection for subcutaneous use (Sept 2023) [Link]
6. 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

RxNav

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
US9233211	No	2016-01-12	2024-03-02
US8603044	No	2013-12-10	2024-03-02
US8512297	No	2013-08-20	2024-09-15
US8679069	No	2014-03-25	2025-04-12
US8992486	No	2015-03-31	2024-06-05
US8556864	No	2013-10-15	2024-03-03
US7918833	Yes	2011-04-05	2028-03-23
US9561331	No	2017-02-07	2024-08-28
US9623189	No	2017-04-18	2024-08-19
US9610409	No	2017-04-04	2024-03-02
US9526844	No	2016-12-27	2024-03-02
US9604008	No	2017-03-28	2024-03-02
US9533105	No	2017-01-03	2024-08-17
US9408979	No	2016-08-09	2024-03-02
US9604009	No	2017-03-28	2024-08-16
US9072836	No	2015-07-07	2032-03-15
US9084853	No	2015-07-21	2031-10-05
US8882721	No	2014-11-11	2031-06-28
US9511193	No	2016-12-06	2032-01-19
USRE45313	No	2014-12-30	2020-07-12
US8475414	No	2013-07-02	2030-12-28
US9308329	No	2016-04-12	2030-12-28
US8915888	No	2014-12-23	2030-06-08
US9408893	No	2016-08-09	2032-08-27
US9526764	No	2016-12-27	2029-10-09
US9707176	No	2017-07-18	2030-11-11
US9775954	No	2017-10-03	2024-03-02
US9827379	No	2017-11-28	2024-03-02
US9821032	No	2017-11-21	2032-05-09
US9855388	No	2018-01-02	2029-04-24
US9440029	No	2016-09-13	2032-01-30
US9950039	No	2018-04-24	2035-12-10
US9981013	No	2018-05-29	2030-08-30
US9717852	No	2017-08-01	2033-04-08
US10028910	No	2018-07-24	2030-11-11
US10029011	No	2018-07-24	2032-08-02
US10117909	No	2018-11-06	2029-10-09
US10201663	No	2019-02-12	2034-03-10

Properties

State

Liquid

Experimental Properties

Not Available

Targets

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insights and accelerate drug research.

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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

1. 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]
2. 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]
3. Gallwitz B: Novel Therapeutic Approaches in Diabetes. Endocr Dev. 2016;31:43-56. doi: 10.1159/000439372. Epub 2016 Jan 19. [Article]
4. 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]

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Drug created at October 27, 2015 21:41 / Updated at October 06, 2023 23:49