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Saxagliptin

MedGen UID:
295028
Concept ID:
C1611934
Organic Chemical; Pharmacologic Substance
Synonyms: (1S,3S,5S)-2-((2S)-2-Amino-2-(3-hydroxyadamantan-1-yl) acetyl)-2-azabicyclo(3.1.0)hexane-3-carbonitrile hydrate; 3-hydroxyadamantylglycine-4,5-methanoprolinenitrile hydrate; saxagliptin
SNOMED CT: Saxagliptin (443087004); Saxagliptin (443066009)
 

Definition

A potent, selective and competitive, cyanopyrrolidine-based, orally bioavailable inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Saxagliptin is metabolized into an, although less potent, active mono-hydroxy metabolite. [from NCI]

Term Hierarchy

CClinical test,  RResearch test,  OOMIM,  GGeneReviews,  VClinVar  
  • CROGVSaxagliptin

Recent clinical studies

Etiology

Koyani CN, Kolesnik E, Wölkart G, Shrestha N, Scheruebel S, Trummer C, Zorn-Pauly K, Hammer A, Lang P, Reicher H, Maechler H, Groschner K, Mayer B, Rainer PP, Sourij H, Sattler W, Malle E, Pelzmann B, von Lewinski D
Biochem Pharmacol 2017 Dec 1;145:64-80. Epub 2017 Aug 30 doi: 10.1016/j.bcp.2017.08.021. PMID: 28859968
Garnock-Jones KP
Drugs 2017 Mar;77(3):319-330. doi: 10.1007/s40265-017-0697-1. PMID: 28176222
Mosenzon O, Leibowitz G, Bhatt DL, Cahn A, Hirshberg B, Wei C, Im K, Rozenberg A, Yanuv I, Stahre C, Ray KK, Iqbal N, Braunwald E, Scirica BM, Raz I
Diabetes Care 2017 Jan;40(1):69-76. Epub 2016 Oct 17 doi: 10.2337/dc16-0621. PMID: 27797925
Abe M, Higuchi T, Moriuchi M, Okamura M, Tei R, Nagura C, Takashima H, Kikuchi F, Tomita H, Okada K
Diabetes Res Clin Pract 2016 Jun;116:244-52. Epub 2016 Apr 26 doi: 10.1016/j.diabres.2016.04.034. PMID: 27321342
Buzzetti R, Pozzilli P, Frederich R, Iqbal N, Hirshberg B
Diabetes Metab Res Rev 2016 Mar;32(3):289-96. Epub 2015 Oct 28 doi: 10.1002/dmrr.2717. PMID: 26385269

Diagnosis

Li FF, Jiang LL, Yan RN, Zhu HH, Zhou PH, Zhang DF, Su XF, Wu JD, Ye L, Ma JH
Medicine (Baltimore) 2016 Oct;95(43):e5229. doi: 10.1097/MD.0000000000005229. PMID: 27787387Free PMC Article
Toh S, Hampp C, Reichman ME, Graham DJ, Balakrishnan S, Pucino F, Hamilton J, Lendle S, Iyer A, Rucker M, Pimentel M, Nathwani N, Griffin MR, Brown NJ, Fireman BH
Ann Intern Med 2016 Jun 7;164(11):705-14. Epub 2016 Apr 26 doi: 10.7326/M15-2568. PMID: 27110660Free PMC Article
Buzzetti R, Pozzilli P, Frederich R, Iqbal N, Hirshberg B
Diabetes Metab Res Rev 2016 Mar;32(3):289-96. Epub 2015 Oct 28 doi: 10.1002/dmrr.2717. PMID: 26385269
Saine ME, Carbonari DM, Newcomb CW, Nezamzadeh MS, Haynes K, Roy JA, Cardillo S, Hennessy S, Holick CN, Esposito DB, Gallagher AM, Bhullar H, Strom BL, Lo Re V 3rd
BMC Pharmacol Toxicol 2015 Apr 2;16:8. doi: 10.1186/s40360-015-0007-z. PMID: 25889498Free PMC Article
Udell JA, Bhatt DL, Braunwald E, Cavender MA, Mosenzon O, Steg PG, Davidson JA, Nicolau JC, Corbalan R, Hirshberg B, Frederich R, Im K, Umez-Eronini AA, He P, McGuire DK, Leiter LA, Raz I, Scirica BM; SAVOR-TIMI 53 Steering Committee and Investigators.
Diabetes Care 2015 Apr;38(4):696-705. Epub 2014 Dec 31 doi: 10.2337/dc14-1850. PMID: 25552421

Therapy

Garnock-Jones KP
Drugs 2017 Mar;77(3):319-330. doi: 10.1007/s40265-017-0697-1. PMID: 28176222
Ekholm E, Hansen L, Johnsson E, Iqbal N, Carlsson B, Chen H, Hirshberg B
Endocr Pract 2017 Mar;23(3):258-265. Epub 2016 Nov 16 doi: 10.4158/EP161323.OR. PMID: 27849380
Vakkalagadda B, Lubin S, Reynolds L, Liang D, Marion AS, LaCreta F, Boulton DW
Clin Ther 2016 Aug;38(8):1890-9. Epub 2016 Aug 2 doi: 10.1016/j.clinthera.2016.07.005. PMID: 27491280
Abe M, Higuchi T, Moriuchi M, Okamura M, Tei R, Nagura C, Takashima H, Kikuchi F, Tomita H, Okada K
Diabetes Res Clin Pract 2016 Jun;116:244-52. Epub 2016 Apr 26 doi: 10.1016/j.diabres.2016.04.034. PMID: 27321342
Buzzetti R, Pozzilli P, Frederich R, Iqbal N, Hirshberg B
Diabetes Metab Res Rev 2016 Mar;32(3):289-96. Epub 2015 Oct 28 doi: 10.1002/dmrr.2717. PMID: 26385269

Prognosis

Boulton DW
Clin Pharmacokinet 2017 Jan;56(1):11-24. doi: 10.1007/s40262-016-0421-4. PMID: 27282159
Li FF, Jiang LL, Yan RN, Zhu HH, Zhou PH, Zhang DF, Su XF, Wu JD, Ye L, Ma JH
Medicine (Baltimore) 2016 Oct;95(43):e5229. doi: 10.1097/MD.0000000000005229. PMID: 27787387Free PMC Article
Cahn A, Raz I, Mosenzon O, Leibowitz G, Yanuv I, Rozenberg A, Iqbal N, Hirshberg B, Sjostrand M, Stahre C, Im K, Kanevsky E, Scirica BM, Bhatt DL, Braunwald E
Diabetes Care 2016 Aug;39(8):1329-37. Epub 2016 May 23 doi: 10.2337/dc15-2763. PMID: 27222508
Schernthaner G, Durán-Garcia S, Hanefeld M, Langslet G, Niskanen L, Östgren CJ, Malvolti E, Hardy E
Diabetes Obes Metab 2015 Jul;17(7):630-8. Epub 2015 Apr 7 doi: 10.1111/dom.12461. PMID: 25761977
Leiter LA, Teoh H, Braunwald E, Mosenzon O, Cahn A, Kumar KM, Smahelova A, Hirshberg B, Stahre C, Frederich R, Bonnici F, Scirica BM, Bhatt DL, Raz I; SAVOR-TIMI 53 Steering Committee and Investigators.
Diabetes Care 2015 Jun;38(6):1145-53. Epub 2015 Mar 10 doi: 10.2337/dc14-2868. PMID: 25758769

Clinical prediction guides

Boulton DW
Clin Pharmacokinet 2017 Jan;56(1):11-24. doi: 10.1007/s40262-016-0421-4. PMID: 27282159
Vakkalagadda B, Lubin S, Reynolds L, Liang D, Marion AS, LaCreta F, Boulton DW
Clin Ther 2016 Aug;38(8):1890-9. Epub 2016 Aug 2 doi: 10.1016/j.clinthera.2016.07.005. PMID: 27491280
Cahn A, Raz I, Mosenzon O, Leibowitz G, Yanuv I, Rozenberg A, Iqbal N, Hirshberg B, Sjostrand M, Stahre C, Im K, Kanevsky E, Scirica BM, Bhatt DL, Braunwald E
Diabetes Care 2016 Aug;39(8):1329-37. Epub 2016 May 23 doi: 10.2337/dc15-2763. PMID: 27222508
Toh S, Hampp C, Reichman ME, Graham DJ, Balakrishnan S, Pucino F, Hamilton J, Lendle S, Iyer A, Rucker M, Pimentel M, Nathwani N, Griffin MR, Brown NJ, Fireman BH
Ann Intern Med 2016 Jun 7;164(11):705-14. Epub 2016 Apr 26 doi: 10.7326/M15-2568. PMID: 27110660Free PMC Article
Jain R
Adv Ther 2015 Nov;32(11):1065-84. Epub 2015 Nov 17 doi: 10.1007/s12325-015-0262-9. PMID: 26578430Free PMC Article

Recent systematic reviews

Dhillon S
Drugs 2015 Oct;75(15):1783-96. doi: 10.1007/s40265-015-0473-z. PMID: 26403305
Iqbal N, Parker A, Frederich R, Donovan M, Hirshberg B
Cardiovasc Diabetol 2014 Feb 4;13:33. doi: 10.1186/1475-2840-13-33. PMID: 24490835Free PMC Article
Davidson JA
J Manag Care Pharm 2014 Feb;20(2):120-9. doi: 10.18553/jmcp.2014.20.2.120. PMID: 24456313
Hirshberg B, Parker A, Edelberg H, Donovan M, Iqbal N
Diabetes Metab Res Rev 2014 Oct;30(7):556-69. doi: 10.1002/dmrr.2502. PMID: 24376173
Karyekar CS, Frederich R, Ravichandran S
Int J Clin Pract 2013 Aug;67(8):759-67. Epub 2013 Jun 24 doi: 10.1111/ijcp.12212. PMID: 23795975Free PMC Article

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