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外観
白色～わずかにうすい黄色、結晶性粉末～粉末
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溶解性
メタノールに可溶
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用途
速効型インスリン分泌促進化 合物です。フェニルアラニン誘導体で、膵β 細胞膜の SU受容体に結合しカリウムチャン ネルを閉じることによりインスリン分泌促進 作用を示します。
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用途
速効型インスリン分泌促進化
合物です。フェニルアラニン誘導体で、膵β
細胞膜のSU 受容体に結合しカリウムチャネ
ルを閉じることによりインスリン分泌促進作
用を示します。
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効能
糖尿病治療薬, 血糖降下薬, スルホニル尿素受容体作動薬
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商品名
スターシス (アステラス製薬); ファスティック (EAファーマ)
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説明
Nateglinide is a N-acylated D-phenylalanine marketed in
Japan as novel orally active insulinotropic agent for the treatment of type-2
diabetes mellitus. It belongs to the class of nonsulfonylureas and shows some
structural similarity to repaglinide, the only other representative in this family. In
single pancreatic beta-cells isolated from rats, Nateglinide was found to
specifically block the ATP-sensitive K+ channel resulting in an increase in
intracellular calcium concentration. This primary action would underlie the
mechanism by which Nateglinide markedly stimulates or potentiates, depending
on glucose concentrations, insulin secretion from pancreatic beta-cells. Clinical
studies demonstrated a good safety profile with a low potential for
hypoglycemia. The pharmacokinetic profile was consistent with the changes of
the blood glucose and plasma insulin level. Interestingly, Nateglinide exerts a
rapid onset and short duration of action due to a rapid absorption and clearance.
Unlike other similar agents, Nateglinide suppresses postprandial glucose
elevations.
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化学的特性
Cyrstalline Solid
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定義
ChEBI: An N-acyl-D-phenylalanine resulting from the formal condensation of the amino group of D-phenylalanine with the carboxy group of trans-4-isopropylcyclohexanecarboxylic acid. An orally-ad
inistered, rapidly-absorbed, short-acting insulinotropic agent, it is used for the treatment of type 2 diabetes mellitus.
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一般的な説明
Although nateglinide, N-(4-isopropylcyclohexanecarbonyl)-D-phenylalanine (Starlix), belongs tothe metaglinides, it is a phenylalanine derivative and representsa novel drug in the management of type 2 diabetes.
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作用機序
Approved in the United States in late 2000, nateglinide is a rapidly absorbed insulin secretagogue that has a mechanism of
action similar to that of repaglinide, with effects appearing within 20 minutes following oral dosing.
Bioavailability is 73%,
and it is 98% protein bound, primarily to albumin. Nateglinide is tissue selective, with low affinity for cardiac and skeletal
muscle.
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代謝
It is metabolized in the liver, with 16% excreted in the urine unchanged. The major metabolites are hydroxyl
derivatives (CYP2C9, 70%; CYP3A4, 30%) that are further conjugated to the glucuronide derivatives.
