ساكساغلبتين

ساكساغلبتين
Systematic (IUPAC) name
	(1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxy-1-adamantyl); acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile
Clinical data
AHFS/Drugs.com	Consumer Drug Information
MedlinePlus	a610003
Licence data	EMA:Link, US FDA:link
Pregnancy cat.	?
Legal status	POM (UK) ℞-only (US)
Routes	Oral
Identifiers
CAS number	361442-04-8
ATC code	A10BH03
PubChem	CID 11243969
DrugBank	DB06335
ChemSpider	9419005
UNII	8I7IO46IVQ
ChEMBL	CHEMBL385517
Chemical data
Formula	C18H25N3O2
Mol. mass	315.41 g/mol
	SMILES O=C(N1[C@H](C#N)C[C@@H]2C[C@H]12)[C@@H](N)C35CC4CC(C3)CC(O)(C4)C5;
	InChI InChI=1S/C18H25N3O2/c19-8-13-2-12-3-14(12)21(13)16(22)15(20)17-4-10-1-11(5-17)7-18(23,6-10)9-17/h10-15,23H,1-7,9,20H2/t10?,11?,12-,13+,14+,15-,17?,18?/m1/s1 ; Key:QGJUIPDUBHWZPV-SGTAVMJGSA-N ;
(what is this?) (verify);

الساكساغلبتين (بالإنجليزية: Saxagliptin) (rINN) سمي سابقاً BMS-477118 وهو دواء فموي لمرض السكري من مثبطات DPP-4

^[1] تم تطويره بداية من شكرة بريستول مايرز سكويب ثم في 2007 اشتركت أسترازنيكا في التططوير إلى المنتج النهائي وشاركت في تسويق الدواء، وتم طرح ترخيص تسويق تطبيق دواء جديد NDA لإدارة الغذاء والدواء الأمريكية FDA كدواء لعلاج السكري من النمط الثاني في 6-2008 بناء على ثمانية تجارب بنمط العشوائية:

: 1 phase 2 dose-ranging (2.5–100 mg/d) study;
6 phase 3, 24-week controlled trials with additional controlled follow-up from 12 to 42 months, double-blinded throughout;
and one 12-week mechanism-of-action trial with a 2-year follow-up period

.^[2] في 6-2008 تم الإعلان عن اسم تجاري للدواء Onglyza .^[3] وافقت إدارة الغذاء والدواء الأمكريكية في 31-7-2009 .^[4] ويعتقد أن دور أنزيم Dipeptidyl peptidase-4 في تنظيم سكر الدم هو عبر تدرك glucose-dependent insulinotropic peptide GIP^[5] وتدرك Glucagon-like peptide-1 GLP-1 .^[5]^[6]

المصادر

↑ Augeri D; et al. (2005). "Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes". Journal of Medicinal Chemistry. 48 (15): 5025–5037. PMID 16033281. doi:10.1021/jm050261p.
↑ Robert Frederich, MD, PhD; et al. (2010). "A Systematic Assessment of Cardiovascular Outcomes in the Saxagliptin Drug Development Program for Type 2 Diabetes". Postgraduate Medicine. 122 (3): 16–27. PMID 20463410. doi:10.3810/pgm.2010.05.2138. Unknown parameter |month= ignored (|date= suggested) (help)
↑ "Bristol, Takeda Drugs Offer Alternatives to Januvia (Update2)". Bloomberg. 2008-06-07.
↑ Telegram (2 August 2009). "FDA approves diabetes drug from two area manufacturers". Worcester Telegram & Gazette Corp. Retrieved 2009-08-02.
↑ ^5٫0 ^5٫1 Mentlein, R; Gallwitz, B; Schmidt, WE (15 June 1993). "Dipeptidyl-peptidase IV hydrolyses gastric inhibitory polypeptide, glucagon-like peptide-1(7-36)amide, peptide histidine methionine and is responsible for their degradation in human serum". European Journal of Biochemistry. 214 (3): 829–835. PMID 8100523. doi:10.1111/j.1432-1033.1993.tb17986.x. Cite uses deprecated parameter |coauthors= (help); |access-date= requires |url= (help)
↑ Ahrén, Bo; Landin-Olsson, Mona; Jansson, Per-Anders; Svensson, Maria; Holmes, David; Schweizer, Anja (2004). "Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in type 2 diabetes". Journal of Clinical Endocrinology & Metabolism. 89 (5): 2078–2084. PMID 15126524. doi:10.1210/jc.2003-031907. Retrieved 2007-01-11. Unknown parameter |month= ignored (|date= suggested) (help); Cite uses deprecated parameter |coauthors= (help)

روابط خارجية

Official site
قالب:UTGlucagon
The race to get DPP-4 inhibitors to market - Forbes.com
Walker, Emily P. "Saxagliptin First Diabetes Drug to Pass FDA Cardiovascular Safety Review".

هذه بذرة تحتاج للنمو والتحسين، فساهم في إثرائها بالمشاركة في تحريرها.

[ahren-1] Augeri D; et al. (2005). "Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes". Journal of Medicinal Chemistry. 48 (15): 5025–5037. PMID 16033281. doi:10.1021/jm050261p.

[Postgraduate_Medicine_2010-2] Robert Frederich, MD, PhD; et al. (2010). "A Systematic Assessment of Cardiovascular Outcomes in the Saxagliptin Drug Development Program for Type 2 Diabetes". Postgraduate Medicine. 122 (3): 16–27. PMID 20463410. doi:10.3810/pgm.2010.05.2138. Unknown parameter |month= ignored (|date= suggested) (help)

[Bloomberg-3] "Bristol, Takeda Drugs Offer Alternatives to Januvia (Update2)". Bloomberg. 2008-06-07.

[4] Telegram (2 August 2009). "FDA approves diabetes drug from two area manufacturers". Worcester Telegram & Gazette Corp. Retrieved 2009-08-02.

[mentlein-5] 5٫0 ^5٫1 Mentlein, R; Gallwitz, B; Schmidt, WE (15 June 1993). "Dipeptidyl-peptidase IV hydrolyses gastric inhibitory polypeptide, glucagon-like peptide-1(7-36)amide, peptide histidine methionine and is responsible for their degradation in human serum". European Journal of Biochemistry. 214 (3): 829–835. PMID 8100523. doi:10.1111/j.1432-1033.1993.tb17986.x. Cite uses deprecated parameter |coauthors= (help); |access-date= requires |url= (help)

[ahren2-6] Ahrén, Bo; Landin-Olsson, Mona; Jansson, Per-Anders; Svensson, Maria; Holmes, David; Schweizer, Anja (2004). "Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in type 2 diabetes". Journal of Clinical Endocrinology & Metabolism. 89 (5): 2078–2084. PMID 15126524. doi:10.1210/jc.2003-031907. Retrieved 2007-01-11. Unknown parameter |month= ignored (|date= suggested) (help); Cite uses deprecated parameter |coauthors= (help)

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ساكساغلبتين

المصادر

روابط خارجية

قائمة التصفح

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