Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials
ABSTRACT Background: Dipeptidyl peptidase-4 (DPP-4) inhibitors are a new class of oral antihyperglycemic agents that enhance the body's ability to regulate blood glucose by increasing the active levels of incretins, glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic peptide (G...
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| Veröffentlicht in: | Current medical research and opinion 2008-02, Vol.24 (2), p.489-496 |
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| container_title | Current medical research and opinion |
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| creator | Karasik, Avraham Aschner, Pablo Katzeff, Harvey Davies, Michael J. Stein, Peter P. |
| description | ABSTRACT
Background: Dipeptidyl peptidase-4 (DPP-4) inhibitors are a new class of oral antihyperglycemic agents that enhance the body's ability to regulate blood glucose by increasing the active levels of incretins, glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). There are numerous DPP-4 inhibitors in development with sitagliptin as the first approved agent for the treatment of patients with type 2 diabetes.
Objective: The purpose of this review is to provide an overview of the clinical trial results with sitagliptin.
Methods: Clinical trials published between January 2005 (first sitagliptin publication) and November 2007 were included in this review. Medline was searched using the search terms: MK-0431 or sitagliptin.
Findings: Sitagliptin, an oral, once-daily, and highly selective DPP-4 inhibitor, has been evaluated in clinical trials as monotherapy, as add-on therapy, or as initial combination therapy with metformin. Sitagliptin provided effective fasting and postprandial glycemic control in a wide range of patients with type 2 diabetes. Markers of β-cell function (HOMA-β and proinsulin/insulin ratio) were improved with sitagliptin treatment. In these clinical trials, sitagliptin was generally well tolerated with an overall incidence of adverse experiences comparable to placebo, a low risk of hypoglycemia or gastrointestinal adverse experiences, and a neutral effect on body weight. The findings presented in this review are limited to the specific patient population enrolled in each clinical trial and for durations for up to 1 year. Future clinical studies should evaluate whether this class of agents has the potential to delay progression and/or prevent type 2 diabetes.
Conclusions: Sitagliptin has been shown to be effective and well-tolerated in various treatment regimens and may be considered for both initial therapy and as add-on therapy for patients with type 2 diabetes. |
| doi_str_mv | 10.1185/030079908X261069 |
| format | Article |
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Background: Dipeptidyl peptidase-4 (DPP-4) inhibitors are a new class of oral antihyperglycemic agents that enhance the body's ability to regulate blood glucose by increasing the active levels of incretins, glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). There are numerous DPP-4 inhibitors in development with sitagliptin as the first approved agent for the treatment of patients with type 2 diabetes.
Objective: The purpose of this review is to provide an overview of the clinical trial results with sitagliptin.
Methods: Clinical trials published between January 2005 (first sitagliptin publication) and November 2007 were included in this review. Medline was searched using the search terms: MK-0431 or sitagliptin.
Findings: Sitagliptin, an oral, once-daily, and highly selective DPP-4 inhibitor, has been evaluated in clinical trials as monotherapy, as add-on therapy, or as initial combination therapy with metformin. Sitagliptin provided effective fasting and postprandial glycemic control in a wide range of patients with type 2 diabetes. Markers of β-cell function (HOMA-β and proinsulin/insulin ratio) were improved with sitagliptin treatment. In these clinical trials, sitagliptin was generally well tolerated with an overall incidence of adverse experiences comparable to placebo, a low risk of hypoglycemia or gastrointestinal adverse experiences, and a neutral effect on body weight. The findings presented in this review are limited to the specific patient population enrolled in each clinical trial and for durations for up to 1 year. Future clinical studies should evaluate whether this class of agents has the potential to delay progression and/or prevent type 2 diabetes.
Conclusions: Sitagliptin has been shown to be effective and well-tolerated in various treatment regimens and may be considered for both initial therapy and as add-on therapy for patients with type 2 diabetes.</description><identifier>ISSN: 0300-7995</identifier><identifier>EISSN: 1473-4877</identifier><identifier>DOI: 10.1185/030079908X261069</identifier><identifier>PMID: 18182122</identifier><identifier>CODEN: CMROCX</identifier><language>eng</language><publisher>England: Informa UK Ltd</publisher><subject>Blood Glucose ; Diabetes Mellitus, Type 2 - drug therapy ; DPP-IV ; Gastric Inhibitory Polypeptide ; Glucagon-Like Peptide 1 ; Glycemic control ; Humans ; Hypoglycemic Agents - administration & dosage ; Hypoglycemic Agents - pharmacokinetics ; Hypoglycemic Agents - therapeutic use ; Incretins ; Incretins - therapeutic use ; Insulin-Secreting Cells - drug effects ; Metformin - therapeutic use ; MK-0431 ; Pyrazines - administration & dosage ; Pyrazines - pharmacokinetics ; Pyrazines - therapeutic use ; Sitagliptin Phosphate ; Triazoles - administration & dosage ; Triazoles - pharmacokinetics ; Triazoles - therapeutic use ; Type 2 diabetes</subject><ispartof>Current medical research and opinion, 2008-02, Vol.24 (2), p.489-496</ispartof><rights>2008 Informa UK Ltd. All rights reserved: reproduction in whole or part not permitted 2008</rights><rights>Copyright Librapharm Feb 2008</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c474t-797cb14501fe2d05033abda3b31499e99656b2bcfcf67d5ba662964f60d386833</citedby><cites>FETCH-LOGICAL-c474t-797cb14501fe2d05033abda3b31499e99656b2bcfcf67d5ba662964f60d386833</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.tandfonline.com/doi/pdf/10.1185/030079908X261069$$EPDF$$P50$$Ginformaworld$$H</linktopdf><linktohtml>$$Uhttps://www.tandfonline.com/doi/full/10.1185/030079908X261069$$EHTML$$P50$$Ginformaworld$$H</linktohtml><link.rule.ids>314,780,784,27922,27923,59645,59751,60434,60540,61219,61254,61400,61435</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/18182122$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Karasik, Avraham</creatorcontrib><creatorcontrib>Aschner, Pablo</creatorcontrib><creatorcontrib>Katzeff, Harvey</creatorcontrib><creatorcontrib>Davies, Michael J.</creatorcontrib><creatorcontrib>Stein, Peter P.</creatorcontrib><title>Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials</title><title>Current medical research and opinion</title><addtitle>Curr Med Res Opin</addtitle><description>ABSTRACT
Background: Dipeptidyl peptidase-4 (DPP-4) inhibitors are a new class of oral antihyperglycemic agents that enhance the body's ability to regulate blood glucose by increasing the active levels of incretins, glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). There are numerous DPP-4 inhibitors in development with sitagliptin as the first approved agent for the treatment of patients with type 2 diabetes.
Objective: The purpose of this review is to provide an overview of the clinical trial results with sitagliptin.
Methods: Clinical trials published between January 2005 (first sitagliptin publication) and November 2007 were included in this review. Medline was searched using the search terms: MK-0431 or sitagliptin.
Findings: Sitagliptin, an oral, once-daily, and highly selective DPP-4 inhibitor, has been evaluated in clinical trials as monotherapy, as add-on therapy, or as initial combination therapy with metformin. Sitagliptin provided effective fasting and postprandial glycemic control in a wide range of patients with type 2 diabetes. Markers of β-cell function (HOMA-β and proinsulin/insulin ratio) were improved with sitagliptin treatment. In these clinical trials, sitagliptin was generally well tolerated with an overall incidence of adverse experiences comparable to placebo, a low risk of hypoglycemia or gastrointestinal adverse experiences, and a neutral effect on body weight. The findings presented in this review are limited to the specific patient population enrolled in each clinical trial and for durations for up to 1 year. Future clinical studies should evaluate whether this class of agents has the potential to delay progression and/or prevent type 2 diabetes.
Conclusions: Sitagliptin has been shown to be effective and well-tolerated in various treatment regimens and may be considered for both initial therapy and as add-on therapy for patients with type 2 diabetes.</description><subject>Blood Glucose</subject><subject>Diabetes Mellitus, Type 2 - drug therapy</subject><subject>DPP-IV</subject><subject>Gastric Inhibitory Polypeptide</subject><subject>Glucagon-Like Peptide 1</subject><subject>Glycemic control</subject><subject>Humans</subject><subject>Hypoglycemic Agents - administration & dosage</subject><subject>Hypoglycemic Agents - pharmacokinetics</subject><subject>Hypoglycemic Agents - therapeutic use</subject><subject>Incretins</subject><subject>Incretins - therapeutic use</subject><subject>Insulin-Secreting Cells - drug effects</subject><subject>Metformin - therapeutic use</subject><subject>MK-0431</subject><subject>Pyrazines - administration & dosage</subject><subject>Pyrazines - pharmacokinetics</subject><subject>Pyrazines - therapeutic use</subject><subject>Sitagliptin Phosphate</subject><subject>Triazoles - administration & dosage</subject><subject>Triazoles - pharmacokinetics</subject><subject>Triazoles - therapeutic use</subject><subject>Type 2 diabetes</subject><issn>0300-7995</issn><issn>1473-4877</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2008</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><recordid>eNp9kc1rFTEUxYMo9lndu5Lgoiun5mMmk9RVqR8VChZUcBeSzI2TMl8mGR_vvzeP96BY0EW4gfs7h8M9CL2k5JxS2bwlnJBWKSJ_MEGJUI_QhtYtr2rZto_RZr-uyr45Qc9SuiOEMqnUU3RCJZWMMrZB69eQzc8hLDlMb7DB729vqxqHqQ825DliX17uAecIJo8wZTx7vJgcyjfhbcg9zrsFMMNdMBYypIviEuF3gO0ejeD2IjeEKTgzFJ9ghvQcPfFlwIvjPEXfP374dnVd3Xz59Pnq8qZydVvnEr11ltYNoR5YRxrCubGd4ZbTWilQSjTCMuu886LtGmuEYErUXpCOSyE5P0VnB98lzr9WSFmPITkYBjPBvCbdEiYJI6SArx-Ad_Map5JNs3JhWexogcgBcnFOKYLXSwyjiTtNid73oR_2USSvjr6rHaG7FxwLKMC7AxCmcurRbOc4dDqb3TBHH83kQtL8P_YXf6l7MEPunYlwn_-f4j8ZianY</recordid><startdate>200802</startdate><enddate>200802</enddate><creator>Karasik, Avraham</creator><creator>Aschner, Pablo</creator><creator>Katzeff, Harvey</creator><creator>Davies, Michael J.</creator><creator>Stein, Peter P.</creator><general>Informa UK Ltd</general><general>Taylor & Francis</general><general>Informa Healthcare</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>3V.</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>88I</scope><scope>8AF</scope><scope>8AO</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>M0S</scope><scope>M1P</scope><scope>M2P</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>Q9U</scope><scope>S0X</scope><scope>7X8</scope></search><sort><creationdate>200802</creationdate><title>Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials</title><author>Karasik, Avraham ; 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Background: Dipeptidyl peptidase-4 (DPP-4) inhibitors are a new class of oral antihyperglycemic agents that enhance the body's ability to regulate blood glucose by increasing the active levels of incretins, glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). There are numerous DPP-4 inhibitors in development with sitagliptin as the first approved agent for the treatment of patients with type 2 diabetes.
Objective: The purpose of this review is to provide an overview of the clinical trial results with sitagliptin.
Methods: Clinical trials published between January 2005 (first sitagliptin publication) and November 2007 were included in this review. Medline was searched using the search terms: MK-0431 or sitagliptin.
Findings: Sitagliptin, an oral, once-daily, and highly selective DPP-4 inhibitor, has been evaluated in clinical trials as monotherapy, as add-on therapy, or as initial combination therapy with metformin. Sitagliptin provided effective fasting and postprandial glycemic control in a wide range of patients with type 2 diabetes. Markers of β-cell function (HOMA-β and proinsulin/insulin ratio) were improved with sitagliptin treatment. In these clinical trials, sitagliptin was generally well tolerated with an overall incidence of adverse experiences comparable to placebo, a low risk of hypoglycemia or gastrointestinal adverse experiences, and a neutral effect on body weight. The findings presented in this review are limited to the specific patient population enrolled in each clinical trial and for durations for up to 1 year. Future clinical studies should evaluate whether this class of agents has the potential to delay progression and/or prevent type 2 diabetes.
Conclusions: Sitagliptin has been shown to be effective and well-tolerated in various treatment regimens and may be considered for both initial therapy and as add-on therapy for patients with type 2 diabetes.</abstract><cop>England</cop><pub>Informa UK Ltd</pub><pmid>18182122</pmid><doi>10.1185/030079908X261069</doi><tpages>8</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0300-7995 |
| ispartof | Current medical research and opinion, 2008-02, Vol.24 (2), p.489-496 |
| issn | 0300-7995 1473-4877 |
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| source | MEDLINE; Taylor & Francis Medical Library - CRKN; Taylor & Francis Journals Complete |
| subjects | Blood Glucose Diabetes Mellitus, Type 2 - drug therapy DPP-IV Gastric Inhibitory Polypeptide Glucagon-Like Peptide 1 Glycemic control Humans Hypoglycemic Agents - administration & dosage Hypoglycemic Agents - pharmacokinetics Hypoglycemic Agents - therapeutic use Incretins Incretins - therapeutic use Insulin-Secreting Cells - drug effects Metformin - therapeutic use MK-0431 Pyrazines - administration & dosage Pyrazines - pharmacokinetics Pyrazines - therapeutic use Sitagliptin Phosphate Triazoles - administration & dosage Triazoles - pharmacokinetics Triazoles - therapeutic use Type 2 diabetes |
| title | Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials |
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