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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/07/19 19:00:46」(JST)

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Alogliptin (trade name Nesina in the US^[1] and Vipidia in Europe^[2]) is an orally administered anti-diabetic drug in the DPP-4 inhibitor class,^[3] developed by Syrrx, a company which was acquired by Takeda Pharmaceutical Company in 2005.^[4] Like other medications for the treatment of Type 2 diabetes, alogliptin does not decrease the risk of heart attack and stroke. Like other members of the gliptin class, it causes little or no weight gain, exhibits relatively little risk of causing hypoglycemia, and exhibits relatively modest glucose-lowering activity. Alogliptin and other gliptins are commonly used in combination with metformin in patients whose diabetes cannot adequately be controlled with metformin alone.^[5] In April 2016, the U.S. FDA added a warning about increased risk of heart failure.^[6]

Medical uses

Alogliptin is a dipeptidyl peptidase-4 inhibitor that decreases blood sugar similar to the other.^[7]

Side effects

Adverse events include mild hypoglycemia based on clinical studies.^[8]^[9]^[10] It may cause severe joint pain.^[11]

Alogliptin is not associated with increased weight, increased risk of cardiovasular events.^[12]^[13] In April 2016, the U.S. FDA added a warning about increased risk of heart failure.^[6]

Market access

Alogliptin tablets sales in Mainland China. Specification is 25mg * 10 tablets.

In December 2007, Takeda submitted a New Drug Application (NDA) for alogliptin to the United States Food and Drug Adminiistration (USFDA),^[14] after positive results from Phase III clinical trials.^[1] In September 2008, the company also filed for approval in Japan,^[15] winning approval in April 2010.^[14] The company also filed a Marketing Authorization Application (MAA) elsewhere outside the United States, which was withdrawn in June 2009 needing more data.^[15] The first USFDA NDA failed to gain approval and was followed by a pair of NDAs (one for alogliptin and a second for a combination of alogliptin and pioglitazone) in July 2011.^[14] In 2012, Takeda received a negative response from the USFDA on both of these NDAs, citing a need for additional data.^[14]

In 2013 the FDA approved the drug in three formulations: As a stand-alone with the brand-name Nesina. Combined with metformin using the name Kazano, and when combined with pioglitazone as Oseni.

References

^ ^a ^b "Takeda Submits New Drug Application for Alogliptin (SYR-322) in the U.S." (Press release). Takeda Pharmaceutical Company. January 4, 2008. Retrieved January 9, 2008.
^ Vipidia: EPAR summary for the public (European Medicines Agency)
^ Feng, Jun; Zhang, Zhiyuan; Wallace, Michael B.; Stafford, Jeffrey A.; Kaldor, Stephen W.; Kassell, Daniel B.; Navre, Marc; Shi, Lihong; Skene, Robert J.; Asakawa, Tomoko; Takeuchi, Koji; Xu, Rongda; Webb, David R.; Gwaltney II, Stephen L. (2007). "Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV". J. Med. Chem. 50 (10): 2297–2300. doi:10.1021/jm070104l. PMID 17441705.
^ [1]
^ "www.aace.com" (PDF).
^ ^a ^b "Safety Alerts for Human Medical Products - Diabetes Medications Containing Saxagliptin and Alogliptin: Drug Safety Communication - Risk of Heart Failure". www.fda.gov. Retrieved 7 April 2016.
^ Saisho, Y (2015). "Alogliptin benzoate for management of type 2 diabetes.". Vascular health and risk management 11: 229–43. doi:10.2147/VHRM.S68564. PMID 25914541.
^ Seino, Yutaka; Fujita, Tetsuya; Hiroi, Shinzo; Hirayama, Masashi; Kaku, Kohei (September 2011), "Efficacy and safety of alogliptin in Japanese patients with type 2 diabetes mellitus: a randomized, double-blind, dose-ranging comparison with placebo, followed by a long-term extension study (abstract only)", Current Medical Research and Opinion 27 (9): 1781–1792, doi:10.1185/03007995.2011.599371, PMID 21806314, retrieved April 26, 2012
^ Kutoh, Eiji; Ukai, Yasuhiro (2012), "Alogliptin as an initial therapy in patients with newly diagnosed, drug naïve type 2 diabetes: a randomized, control trial (abstract only)", Endocrine (January 17, 2012) 41: 435–41, doi:10.1007/s12020-012-9596-0, PMID 22249941, retrieved April 26, 2012
^ Bosi, Emanuele; Ellis, G.C.; Wilson, C.A.; Fleck, P.R. (October 2011), "Alogliptin as a third oral antidiabetic drug in patients with type 2 diabetes and inadequate glycaemic control on metformin and pioglitazone: a 52-week, randomized, double-blind, active-controlled, parallel-group study", Diabetes, Obesity and Metabolism (October 27, 2011) 13 (12): 1088–1096, doi:10.1111/j.1463-1326.2011.01463.x, retrieved April 26, 2012
^ "DPP-4 Inhibitors for Type 2 Diabetes: Drug Safety Communication - May Cause Severe Joint Pain". FDA. 2015-08-28. Retrieved 1 September 2015.
^ White WB, Cannon CP, Heller SR, et al. (October 2013). "Alogliptin after acute coronary syndrome in patients with type 2 diabetes". N. Engl. J. Med. 369 (14): 1327–35. doi:10.1056/NEJMoa1305889. PMID 23992602.
^ White WB, Zannad F (January 2014). "Saxagliptin, alogliptin, and cardiovascular outcomes". N. Engl. J. Med. 370 (5): 484. doi:10.1056/NEJMc1313880. PMID 24482824.
^ ^a ^b ^c ^d Grogan, Kevin (April 26, 2012), "FDA wants yet more data on Takeda diabetes drug alogliptin", PharmaTimes (PharmaTimes), PharmaTimes online, retrieved April 26, 2012
^ ^a ^b "GEN News Highlights: Takeda Pulls MAA for Type 2 Diabetes Therapy". Genetic Engineering & Biotechnology News. June 4, 2009.

UpToDate Contents

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1. 2型糖尿病の治療のためのジペプチジルペプチダーゼ4（DPP-4）阻害剤 dipeptidyl peptidase 4 dpp 4 inhibitors for the treatment of type 2 diabetes mellitus
2. 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
3. 高齢患者における2型糖尿病の治療 treatment of type 2 diabetes mellitus in the older patient
4. 2型糖尿病における持続性高血糖のマネージメント management of persistent hyperglycemia in type 2 diabetes mellitus

English Journal

Alogliptin as a third oral antidiabetic drug in patients with type 2 diabetes and inadequate glycaemic control on metformin and pioglitazone: a 52-week, randomized, double-blind, active-controlled, parallel-group study.

Bosi E, Ellis GC, Wilson CA, Fleck PR.SourceDepartment of Internal Medicine, Diabetes & Endocrinology Unit, San Raffaele Scientific Institute and Vita-Salute San Raffaele University, Milan, Italy. bosi.emanuele@hsr.it
Diabetes, obesity & metabolism.Diabetes Obes Metab.2011 Dec;13(12):1088-96. doi: 10.1111/j.1463-1326.2011.01463.x.
AIM: To assess the efficacy and safety of adding alogliptin versus uptitrating pioglitazone in patients with type 2 diabetes and inadequate glycaemic control on metformin and pioglitazone.METHODS: In this randomized, double-blind, active-controlled, parallel-group study, patients with type 2 diabete
PMID 21733058

Long-Term Dipeptidyl-Peptidase 4 Inhibition Reduces Atherosclerosis and Inflammation via Effects on Monocyte Recruitment and Chemotaxis.

Shah Z, Kampfrath T, Deiuliis JA, Zhong J, Pineda C, Ying Z, Xu X, Lu B, Moffatt-Bruce S, Durairaj R, Sun Q, Mihai G, Maiseyeu A, Rajagopalan S.SourceDavis Heart & Lung Research Institute, 473 W 12th Ave, Room 110, Columbus, OH 43210. sanjay.rajagopalan@osumc.edu.
Circulation.Circulation.2011 Nov 22;124(21):2338-49. Epub 2011 Oct 17.
Background- Dipeptidyl-peptidase 4 (DPP-4) inhibitors are increasingly used to accomplish glycemic targets in patients with type II diabetes mellitus. Because DPP-4 is expressed in inflammatory cells, we hypothesized that its inhibition will exert favorable effects in atherosclerosis. Methods and R
PMID 22007077

Japanese Journal

高選択的DPP-4阻害薬アログリプチン安息香酸塩(ネシーナ^【○!R】錠)の薬理作用および臨床効果

武内浩二,藤田哲也,廣居伸蔵
日本薬理学雑誌 137(1), 43-50, 2011-01-01
高選択的DPP-4阻害薬アログリプチン安息香酸塩（ネシーナ®錠）は2型糖尿病に対する治療薬である．アログリプチンは医薬分子構造設計（SBDD）技術を駆使して創製され，DPP-4の活性部位と共有結合は形成せず，静電相互作用，水素結合，π-πスタッキングなどの種々の相互作用をバランス良く，かつ効率的に利用することにより，DPP-4選択的に強力に結合する．2型糖尿病モデル動物において，アログリ …
NAID 10027747338

症例報告アログリプチンとボグリボースの併用効果を持続血糖モニターで確認できた1例

森博子,岡田洋右,黒住旭 [他]
糖尿病 54(6), 425-429, 2011-06
NAID 40018920118

Related Pictures

Generic Name and Formulations: Nesina (alogliptin) for type 2 diabetes The image above shows a crystal structure File:Alogliptin.svg получить увеличенное alogliptin benzoate m wt 461 51 alogliptin

★リンクテーブル★

リンク元

「アログリプチン」

Alogliptin
Systematic (IUPAC) name
	2-({6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl}methyl)benzonitrile
Clinical data
Trade names	Nesina, Vipidia; Kazano, Vipidomet (with metformin); Oseni, Incresync (with pioglitazone)
Pregnancy; category	US: B (No risk in non-human studies); ;
Routes of; administration	Oral
Legal status
Legal status	℞ (Prescription only);
Pharmacokinetic data
Bioavailability	100%
Protein binding	20%
Metabolism	Limited, hepatic (CYP2D6- and 3A4-mediated)
Biological half-life	12–21 hours
Excretion	Renal (major) and fecal (minor)
Identifiers
CAS Number	850649-62-6
ATC code	A10BH04 (WHO)
PubChem	CID 11450633
IUPHAR/BPS	6319
ChemSpider	9625485
UNII	JHC049LO86
KEGG	D06553
ChEBI	CHEBI:72323
ChEMBL	CHEMBL376359
Synonyms	SYR-322
Chemical data
Formula	C18H21N5O2
Molar mass	339.39 g/mol
	SMILES N#Cc3ccccc3CN\1C(=O)N(C)C(=O)/C=C/1N2CCC[C@@H](N)C2 ;
	InChI InChI=1S/C18H21N5O2/c1-21-17(24)9-16(22-8-4-7-15(20)12-22)23(18(21)25)11-14-6-3-2-5-13(14)10-19/h2-3,5-6,9,15H,4,7-8,11-12,20H2,1H3/t15-/m1/s1 ; Key:ZSBOMTDTBDDKMP-OAHLLOKOSA-N ;
(what is this?) (verify)

　　[★]

英: alogliptin
商: ネシーナ
関: ジペプチジルペプチダーゼ4阻害薬

用量

1日1回25mgを投与する。

中等度以上の腎機能障害患者における投与量

	血清クレアチニン（mg/dL）※	クレアチニンクリアランス（Ccr，mL/min）	投与量
中等度腎機能障害患者	男性：1.4＜～≦2.4 女性：1.2＜～≦2.0	30≦～＜50	12.5mg、1日1回
高度腎機能障害患者／末期腎不全患者	男性：＞2.4 女性：＞2.0	＜30	6.25mg、1日1回
末期腎不全患者については、血液透析との時間関係は問わない。※：Ccrに相当する換算値（年齢60歳、体重65kg）

[takedapr28864-1] "Takeda Submits New Drug Application for Alogliptin (SYR-322) in the U.S." (Press release). Takeda Pharmaceutical Company. January 4, 2008. Retrieved January 9, 2008.

[2] Vipidia: EPAR summary for the public (European Medicines Agency)

[pmid17441705-3] Feng, Jun; Zhang, Zhiyuan; Wallace, Michael B.; Stafford, Jeffrey A.; Kaldor, Stephen W.; Kassell, Daniel B.; Navre, Marc; Shi, Lihong; Skene, Robert J.; Asakawa, Tomoko; Takeuchi, Koji; Xu, Rongda; Webb, David R.; Gwaltney II, Stephen L. (2007). "Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV". J. Med. Chem. 50 (10): 2297–2300. doi:10.1021/jm070104l. PMID 17441705.

[4] [1]

[5] "www.aace.com" (PDF).

[FDA2016-6] "Safety Alerts for Human Medical Products - Diabetes Medications Containing Saxagliptin and Alogliptin: Drug Safety Communication - Risk of Heart Failure". www.fda.gov. Retrieved 7 April 2016.

[7] Saisho, Y (2015). "Alogliptin benzoate for management of type 2 diabetes.". Vascular health and risk management 11: 229–43. doi:10.2147/VHRM.S68564. PMID 25914541.

[seino2011-8] Seino, Yutaka; Fujita, Tetsuya; Hiroi, Shinzo; Hirayama, Masashi; Kaku, Kohei (September 2011), "Efficacy and safety of alogliptin in Japanese patients with type 2 diabetes mellitus: a randomized, double-blind, dose-ranging comparison with placebo, followed by a long-term extension study (abstract only)", Current Medical Research and Opinion 27 (9): 1781–1792, doi:10.1185/03007995.2011.599371, PMID 21806314, retrieved April 26, 2012

[kutoh2012-9] Kutoh, Eiji; Ukai, Yasuhiro (2012), "Alogliptin as an initial therapy in patients with newly diagnosed, drug naïve type 2 diabetes: a randomized, control trial (abstract only)", Endocrine (January 17, 2012) 41: 435–41, doi:10.1007/s12020-012-9596-0, PMID 22249941, retrieved April 26, 2012

[bosi2011-10] Bosi, Emanuele; Ellis, G.C.; Wilson, C.A.; Fleck, P.R. (October 2011), "Alogliptin as a third oral antidiabetic drug in patients with type 2 diabetes and inadequate glycaemic control on metformin and pioglitazone: a 52-week, randomized, double-blind, active-controlled, parallel-group study", Diabetes, Obesity and Metabolism (October 27, 2011) 13 (12): 1088–1096, doi:10.1111/j.1463-1326.2011.01463.x, retrieved April 26, 2012

[11] "DPP-4 Inhibitors for Type 2 Diabetes: Drug Safety Communication - May Cause Severe Joint Pain". FDA. 2015-08-28. Retrieved 1 September 2015.

[12] White WB, Cannon CP, Heller SR, et al. (October 2013). "Alogliptin after acute coronary syndrome in patients with type 2 diabetes". N. Engl. J. Med. 369 (14): 1327–35. doi:10.1056/NEJMoa1305889. PMID 23992602.

[13] White WB, Zannad F (January 2014). "Saxagliptin, alogliptin, and cardiovascular outcomes". N. Engl. J. Med. 370 (5): 484. doi:10.1056/NEJMc1313880. PMID 24482824.

[grogan2012-14] Grogan, Kevin (April 26, 2012), "FDA wants yet more data on Takeda diabetes drug alogliptin", PharmaTimes (PharmaTimes), PharmaTimes online, retrieved April 26, 2012

[geneng2009-15] "GEN News Highlights: Takeda Pulls MAA for Type 2 Diabetes Therapy". Genetic Engineering & Biotechnology News. June 4, 2009.

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案内

alogliptin