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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/07/31 11:40:07」(JST)

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Lixisenatide (trade name Lyxumia and Adlyxin) is a once-daily injectable GLP-1 receptor agonist for the treatment of diabetes, discovered by Zealand Pharma A/S of Denmark and licensed and developed by Sanofi.^[1] Lixisenatide was accepted for review by the US FDA on February 19, 2013, and approved by the European Commission on February 1, 2013.^[2] On September 12, 2013, Sanofi delayed the approval process in the US, citing internal data from a cardiovascular risk study. Lixisenatide received FDA approval on July 28, 2016.^[3]

Mechanism of action

GLP-1 is a naturally-occurring peptide that is released within minutes of eating a meal. It is known to suppress glucagon secretion from pancreatic alpha cells and stimulate insulin secretion by pancreatic beta cells. GLP-1 receptor agonists are used as an add-on treatment for type 2 diabetes and their use is endorsed by the European Association for the Study of Diabetes, the American Diabetes Association, the American Association of Clinical Endocrinologists and the American College of Endocrinology.

Physical and chemical properties

Lixisenatixe has been described as "des-38-proline-exendin-4 (Heloderma suspectum)-(1–39)-peptidylpenta-L-lysyl-L-lysinamide", meaning it is derived from the first 39 amino acids in the sequence of the peptide exendin-4, found in the Gila monster (Heloderma suspectum), omitting proline at position 38 and adding six lysine residues. Its complete sequence is:^[4]

H–His–Gly–Glu–Gly–Thr–Phe–Thr–Ser–Asp–Leu–Ser–Lys–Gln–Met–Glu–Glu–Glu–Ala–Val–Arg–Leu–Phe–Ile–Glu–Trp–Leu–Lys–Asn–Gly–Gly–Pro–Ser–Ser–Gly–Ala–Pro–Pro–Ser–Lys–Lys–Lys–Lys–Lys–Lys–NH₂

References

^ Christensen, M; Knop, FK; Holst, JJ; Vilsboll, T (2009). "Lixisenatide, a novel GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus". IDrugs : the investigational drugs journal. 12 (8): 503–13. PMID 19629885.
^ "Sanofi New Drug Application for Lixisenatide Accepted for Review by FDA". Drugs.com/PR Newsire. 19 February 2013.
^ "FDA approves Adlyxin to treat type 2 diabetes". FDA. 28 July 2016. Retrieved 28 July 2016.
^ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended INN: List 61" (PDF). WHO Drug Information. 23 (1): 66f. 2009.

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UpToDate Contents

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1. 2型糖尿病治療のためのGlucagon-like peptide-1受容体拮抗剤 glucagon like peptide 1 receptor agonists for the treatment of type 2 diabetes mellitus

English Journal

Lixisenatide reduces postprandial hyperglycaemia via gastrostatic and insulinotropic effects.

Becker R1, Stechl J, Steinstraesser A, Golor G, Pellissier F.
Diabetes/metabolism research and reviews.Diabetes Metab Res Rev.2015 Mar 14. doi: 10.1002/dmrr.2647. [Epub ahead of print]
BACKGROUND: Lixisenatide is a once-daily, prandial, short-acting glucagon-like peptide-1 receptor agonist. Its main antidiabetic effect is to delay gastric emptying to control postprandial plasma glucose (PPG) excursions. The dose-response relationship of the integrated insulinotropic and gastrostat
PMID 25773712

Glucagon-like peptide-1 receptor agonists as insulin add-on therapy in patients with inadequate glycemic control in type 2 diabetes mellitus: lixisenatide as a new therapeutic option.

Gómez-Huelgas R, Azriel S, Puig-Domingo M, Vidal J, Pablos-Velasco Pd.
International journal of clinical pharmacology and therapeutics.Int J Clin Pharmacol Ther.2015 Mar;53(3):230-40. doi: 10.5414/CP202052.
Despite the variety of therapeutic options for the management of type 2 diabetes mellitus, many patients fail to meet glycated hemoglobin (HbA1c) targets. The relative contribution of postprandial plasma glucose (PPG) to overall HbA1c is estimated at 40 - 60%, with the effect of PPG on HbA1c being p
PMID 25066229

Efficacy and safety of lixisenatide in Japanese patients with type 2 diabetes mellitus inadequately controlled by sulfonylurea with or without metformin: Subanalysis of GetGoal-S.

Onishi Y1, Niemoeller E2, Ikeda Y3, Takagi H3, Yabe D4, Seino Y4.
Journal of diabetes investigation.J Diabetes Investig.2015 Mar;6(2):201-9. doi: 10.1111/jdi.12275. Epub 2014 Sep 24.
AIMS/INTRODUCTION: This was a subanalysis of Japanese patients included in the glucagon-like peptide-1 receptor agonist AVE0010 in patients with type 2 diabetes mellitus for glycemic control and safety evaluation (GetGoal-S) study - a 24-week, randomized, placebo-controlled study of lixisenatide in
PMID 25802728

Japanese Journal

GLP-1受容体作動薬 (特集糖尿病治療薬update : 適正な血糖管理を目指して) -- (糖尿病治療薬の薬効と適応基準)

真下大和,江藤一弘
日本臨床 73(3), 433-437, 2015-03
NAID 40020367139

症例報告リキシセナチド・インスリングラルギンの併用療法により肥満・血糖コントロールの改善を認めた糖尿病性腎症合併2型糖尿病の1例

大城陽代,川崎啓正,小松工芽
肥満研究 = Journal of Japan Society for the Study of Obesity : 日本肥満学会誌 20(3), 180-184, 2014
NAID 40020321278

Related Pictures

Lyxumia (lixisenatide) should be injected Lixisenatide que ayuda a tratar la Lixisenatide works by controlling blood Sanofi to withdraw the lixisenatide New top-line results for study of lixisenatide Efficacy and Safety of Lixisenatide Versus Agonist Lyxumia (lixisenatide) | diaTribe Lixisenatide para a venda – Peptides do

★リンクテーブル★

リンク元

「リキシセナチド」

Lixisenatide
Clinical data
Trade names	Lyxumia
License data	EU EMA: Lixisenatide;
Routes of; administration	Subcutaneous injection
Legal status
Legal status	UK: POM (Prescription only);
Identifiers
CAS Number	827033-10-3
ATC code	A10BX10 (WHO)
PubChem	CID 16139342
IUPHAR/BPS	7387
ChemSpider	17295846
ChEBI	CHEBI:85662
Chemical data
Formula	C215H347N61O65S
Molar mass	4858.49 g/mol
	SMILES CCC(C)C(C(=O)NC(CCC(=O)O)C(=O)NC(Cc1c[nH]c2c1cccc2)C(=O)NC(CC(C)C)C(=O)NC(CCCCN)C(=O)NC(CC(=O)N)C(=O)NCC(=O)NCC(=O)N3CCCC3C(=O)NC(CO)C(=O)NC(CO)C(=O)NCC(=O)NC(C)C(=O)N4CCCC4C(=O)N5CCCC5C(=O)NC(CO)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)N)NC(=O)C(Cc6ccccc6)NC(=O)C(CC(C)C)NC(=O)C(CCCNC(=N)N)NC(=O)C(C(C)C)NC(=O)C(C)NC(=O)C(CCC(=O)O)NC(=O)C(CCC(=O)O)NC(=O)C(CCC(=O)O)NC(=O)C(CCSC)NC(=O)C(CCC(=O)N)NC(=O)C(CCCCN)NC(=O)C(CO)NC(=O)C(CC(C)C)NC(=O)C(CC(=O)O)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C(Cc7ccccc7)NC(=O)C(C(C)O)NC(=O)CNC(=O)C(CCC(=O)O)NC(=O)CNC(=O)C(Cc8cnc[nH]8)N ;
	InChI InChI=1S/C215H347N61O65S/c1-16-115(10)173(210(337)256-141(68-74-170(299)300)194(321)261-148(94-122-98-232-126-50-24-23-49-124(122)126)199(326)258-143(89-111(2)3)196(323)247-134(58-32-40-83-223)189(316)262-149(96-160(226)285)180(307)235-100-161(286)233-104-165(290)274-85-42-60-156(274)207(334)267-154(108-280)206(333)265-151(105-277)181(308)237-101-162(287)239-117(12)213(340)276-87-44-62-158(276)214(341)275-86-43-61-157(275)208(335)268-153(107-279)204(331)249-132(56-30-38-81-221)187(314)246-131(55-29-37-80-220)186(313)245-130(54-28-36-79-219)185(312)244-129(53-27-35-78-218)184(311)243-128(52-26-34-77-217)183(310)242-127(176(227)303)51-25-33-76-216)272-201(328)146(92-120-45-19-17-20-46-120)260-197(324)144(90-112(4)5)257-190(317)135(59-41-84-231-215(228)229)255-209(336)172(114(8)9)271-177(304)116(11)240-182(309)138(65-71-167(293)294)251-192(319)139(66-72-168(295)296)252-193(320)140(67-73-169(297)298)253-195(322)142(75-88-342-15)254-191(318)137(63-69-159(225)284)250-188(315)133(57-31-39-82-222)248-203(330)152(106-278)266-198(325)145(91-113(6)7)259-200(327)150(97-171(301)302)263-205(332)155(109-281)269-212(339)175(119(14)283)273-202(329)147(93-121-47-21-18-22-48-121)264-211(338)174(118(13)282)270-164(289)103-236-179(306)136(64-70-166(291)292)241-163(288)102-234-178(305)125(224)95-123-99-230-110-238-123/h17-24,45-50,98-99,110-119,125,127-158,172-175,232,277-283H,16,25-44,51-97,100-109,216-224H2,1-15H3,(H2,225,284)(H2,226,285)(H2,227,303)(H,230,238)(H,233,286)(H,234,305)(H,235,307)(H,236,306)(H,237,308)(H,239,287)(H,240,309)(H,241,288)(H,242,310)(H,243,311)(H,244,312)(H,245,313)(H,246,314)(H,247,323)(H,248,330)(H,249,331)(H,250,315)(H,251,319)(H,252,320)(H,253,322)(H,254,318)(H,255,336)(H,256,337)(H,257,317)(H,258,326)(H,259,327)(H,260,324)(H,261,321)(H,262,316)(H,263,332)(H,264,338)(H,265,333)(H,266,325)(H,267,334)(H,268,335)(H,269,339)(H,270,289)(H,271,304)(H,272,328)(H,273,329)(H,291,292)(H,293,294)(H,295,296)(H,297,298)(H,299,300)(H,301,302)(H4,228,229,231)/t115-,116-,117-,118+,119+,125-,127-,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,138-,139-,140-,141-,142-,143-,144-,145-,146-,147-,148-,149-,150-,151-,152-,153-,154-,155-,156-,157-,158-,172-,173-,174-,175-/m0/s1 ; Key:XVVOERDUTLJJHN-IAEQDCLQSA-N ;

　　[★]

英: lixisenatide
商: リキスミア
関: GLP-1

GLP-1受容体作動薬

[1] Christensen, M; Knop, FK; Holst, JJ; Vilsboll, T (2009). "Lixisenatide, a novel GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus". IDrugs : the investigational drugs journal. 12 (8): 503–13. PMID 19629885.

[2] "Sanofi New Drug Application for Lixisenatide Accepted for Review by FDA". Drugs.com/PR Newsire. 19 February 2013.

[3] "FDA approves Adlyxin to treat type 2 diabetes". FDA. 28 July 2016. Retrieved 28 July 2016.

[4] "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended INN: List 61" (PDF). WHO Drug Information. 23 (1): 66f. 2009.

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案内

lixisenatide