الفرق بين المراجعتين لصفحة: «ساكساغلبتين»

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| StdInChIKey = QGJUIPDUBHWZPV-SGTAVMJGSA-N
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الساكساغلبتين {{إنج|Saxagliptin}} ([[International Nonproprietary Name|rINN]]) سمي سابقاً  '''BMS-477118''' وهو دواء فموي لمرض السكري من مثبطات DPP-4
الساكساغلبتين {{إنج|Saxagliptin}} ([[International Nonproprietary Name|rINN]]) سمي سابقاً  '''BMS-477118''' وهو دواء فموي لمرض السكري من مثبطات DPP-4  
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'''Saxagliptin''' ([[International Nonproprietary Name|rINN]]), previously identified as '''BMS-477118''', is a new oral hypoglycemic ([[anti-diabetic drug]]) of the new [[DPP-4 inhibitors|dipeptidyl peptidase-4 (DPP-4) inhibitor]] class of drugs.<ref name="ahren">{{cite journal | author = Augeri D ''et al.''
<ref name="ahren">{{cite journal | author = Augeri D ''et al.''
  | title = 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
  | title = 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 = [[Journal of Medicinal Chemistry]] | volume = 48 | issue = 15 | pages = 5025&ndash;5037 | year = 2005
  | journal = [[Journal of Medicinal Chemistry]] | volume = 48 | issue = 15 | pages = 5025&ndash;5037 | year = 2005
  | pmid = 16033281| doi = 10.1021/jm050261p}}</ref> Early development was solely by [[Bristol-Myers Squibb]]; in 2007 [[AstraZeneca]] joined with Bristol-Myers Squibb to co-develop the final compound and collaborate on the marketing of the drug. A New Drug Application for saxagliptin in the treatment of type 2 diabetes was submitted to the FDA in June 2008. It was based on a drug development program with 8 randomized trials: 1 phase 2 dose-ranging (2.5–100&nbsp;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.<ref name="Postgraduate Medicine 2010">{{cite journal | author=Robert Frederich, MD, PhD et al. | title=A Systematic Assessment of Cardiovascular Outcomes in the Saxagliptin Drug Development Program for Type 2 Diabetes | journal=Postgraduate Medicine. | month=May | year=2010 | pages=16–27 | volume=122 | issue=3 | url=http://www.postgradmed.com/index.php?article=2138#none | doi=10.3810/pgm.2010.05.2138 | pmid=20463410}}</ref> In June 2008, it was announced that '''Onglyza''' would be the trade name under which saxagliptin will be marketed.<ref name="Bloomberg">{{cite news| url=http://www.bloomberg.com/apps/news?pid=20601103&sid=amRAcE.Jql6g&refer=news | work=Bloomberg | title=Bristol, Takeda Drugs Offer Alternatives to Januvia (Update2) | date=2008-06-07}}</ref>
  | pmid = 16033281| doi = 10.1021/jm050261p}}</ref>
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:  


The FDA approved Saxagliptin with brand name Onglyza on July 31, 2009.<ref>{{cite news  
* : 1 phase 2 dose-ranging (2.5–100&nbsp;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
.<ref name="Postgraduate Medicine 2010">{{cite journal | author=Robert Frederich, MD, PhD et al. | title=A Systematic Assessment of Cardiovascular Outcomes in the Saxagliptin Drug Development Program for Type 2 Diabetes | journal=Postgraduate Medicine. | month=May | year=2010 | pages=16–27 | volume=122 | issue=3 | url=http://www.postgradmed.com/index.php?article=2138#none | doi=10.3810/pgm.2010.05.2138 | pmid=20463410}}</ref>
في 6-2008 تم الإعلان عن اسم تجاري للدواء '''Onglyza''' .<ref name="Bloomberg">{{cite news| url=http://www.bloomberg.com/apps/news?pid=20601103&sid=amRAcE.Jql6g&refer=news | work=Bloomberg | title=Bristol, Takeda Drugs Offer Alternatives to Januvia (Update2) | date=2008-06-07}}</ref> وافقت إدارة الغذاء والدواء الأمكريكية في 31-7-2009 .<ref>{{cite news  
  | author = Telegram | title = FDA approves diabetes drug from two area manufacturers
  | author = Telegram | title = FDA approves diabetes drug from two area manufacturers
  | url = http://www.telegram.com/article/20090802/NEWS/908020328/1002
  | url = http://www.telegram.com/article/20090802/NEWS/908020328/1002
  | publisher = Worcester Telegram & Gazette Corp. | date = 2 August 2009 | accessdate = 2009-08-02
  | publisher = Worcester Telegram & Gazette Corp. | date = 2 August 2009 | accessdate = 2009-08-02
}}</ref>
}}</ref> ويعتقد أن دور أنزيم Dipeptidyl peptidase-4 في تنظيم سكر الدم هو عبر تدرك glucose-dependent insulinotropic peptide GIP<ref name="mentlein">{{cite journal
 
Dipeptidyl peptidase-4's role in [[blood glucose]] regulation is thought to be through degradation of [[glucose-dependent insulinotropic peptide|GIP]]<ref name="mentlein">{{cite journal
  | last = Mentlein | first = R | authorlink =  | coauthors = Gallwitz, B; Schmidt, WE
  | last = Mentlein | first = R | authorlink =  | coauthors = Gallwitz, B; Schmidt, WE
  | date = 15 June 1993 | accessdate = 2007-01-11
  | date = 15 June 1993 | accessdate = 2007-01-11
سطر 69: سطر 72:
  | journal = [[European Journal of Biochemistry]] | volume = 214 | issue = 3 | pages = 829&ndash;835
  | journal = [[European Journal of Biochemistry]] | volume = 214 | issue = 3 | pages = 829&ndash;835
  | doi =  10.1111/j.1432-1033.1993.tb17986.x| pmid = 8100523 | url =  
  | doi =  10.1111/j.1432-1033.1993.tb17986.x| pmid = 8100523 | url =  
}}</ref> and the degradation of [[Glucagon-like peptide-1|GLP-1]].<ref name=mentlein/><ref name="ahren2">{{cite journal
}}</ref> وتدرك Glucagon-like peptide-1 GLP-1 .<ref name=mentlein/><ref name="ahren2">{{cite journal
  | last = Ahrén | first = Bo | coauthors = Landin-Olsson, Mona; Jansson, Per-Anders; Svensson, Maria; Holmes, David; Schweizer, Anja
  | last = Ahrén | first = Bo | coauthors = Landin-Olsson, Mona; Jansson, Per-Anders; Svensson, Maria; Holmes, David; Schweizer, Anja
  | year = 2004 | month = May | accessdate = 2007-01-11
  | year = 2004 | month = May | accessdate = 2007-01-11
سطر 76: سطر 79:
  | doi =  10.1210/jc.2003-031907| pmid = 15126524 | url = http://jcem.endojournals.org/cgi/content/full/89/5/2078
  | doi =  10.1210/jc.2003-031907| pmid = 15126524 | url = http://jcem.endojournals.org/cgi/content/full/89/5/2078
  }}</ref>
  }}</ref>
 
<!--
Bristol-Myers Squibb announced on 27 December 2006 that [[Otsuka Pharmaceutical Co.]] has been granted exclusive rights to develop and commercialize the compound in Japan.  Under the licensing agreement, Otsuka will be responsible for all development costs, but Bristol-Myers Squibb retains rights to co-promote saxagliptin with Otsuka in Japan.<ref>{{cite press release
Bristol-Myers Squibb announced on 27 December 2006 that [[Otsuka Pharmaceutical Co.]] has been granted exclusive rights to develop and commercialize the compound in Japan.  Under the licensing agreement, Otsuka will be responsible for all development costs, but Bristol-Myers Squibb retains rights to co-promote saxagliptin with Otsuka in Japan.<ref>{{cite press release
  | title = Bristol-Myers Squibb and Otsuka Pharmaceutical Co., Ltd. Announce Exclusive Licensing Agreement for Diabetes Compound Saxagliptin in Japan
  | title = Bristol-Myers Squibb and Otsuka Pharmaceutical Co., Ltd. Announce Exclusive Licensing Agreement for Diabetes Compound Saxagliptin in Japan
سطر 134: سطر 137:
*[[Development of dipeptidyl peptidase-4 inhibitors]]
*[[Development of dipeptidyl peptidase-4 inhibitors]]


-->
==المصادر==
==المصادر==
{{reflist}}
{{reflist}}
سطر 142: سطر 147:
*[http://www.forbes.com/2004/01/26/cx_mh_rl_diabetestearsheet_5.html The race to get DPP-4 inhibitors to market] - Forbes.com
*[http://www.forbes.com/2004/01/26/cx_mh_rl_diabetestearsheet_5.html The race to get DPP-4 inhibitors to market] - Forbes.com
*{{cite web|url=http://www.medpagetoday.com/Washington-Watch/Washington-Watch/13555|title=Saxagliptin First Diabetes Drug to Pass FDA Cardiovascular Safety Review|last=Walker|first=Emily P.|work=}}
*{{cite web|url=http://www.medpagetoday.com/Washington-Watch/Washington-Watch/13555|title=Saxagliptin First Diabetes Drug to Pass FDA Cardiovascular Safety Review|last=Walker|first=Emily P.|work=}}
-->
{{بذرة}}
{{بذرة}}
{{Oral hypoglycemics}}
{{Oral hypoglycemics}}

مراجعة 09:28، 28 مارس 2013

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 N
ATC code A10BH03
PubChem CID 11243969
DrugBank DB06335
ChemSpider 9419005 YesY
UNII 8I7IO46IVQ N
ChEMBL CHEMBL385517 YesY
Chemical data
Formula C18H25N3O2 
Mol. mass 315.41 g/mol
 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

  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. 
  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)
  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. 
  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);
  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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