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Therapeutic equivalence of vildagliptin 100 mg once daily modified release to 50 mg twice daily immediate release formulation: An open-label, randomized, two-period, single- and multiple-dose, 6-day crossover study
Vildagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor to treat type 2 diabetes mellitus, is available as immediate release (IR) tablets administered at 50 mg twice daily (BID). A 100 mg modified release (MR) formulation was developed for once daily (QD) dosing. This study aimed to compare the the...
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| Published in: | Diabetes & metabolic syndrome clinical research & reviews 2022-03, Vol.16 (3), p.102438-102438, Article 102438 |
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| container_end_page | 102438 |
| container_issue | 3 |
| container_start_page | 102438 |
| container_title | Diabetes & metabolic syndrome clinical research & reviews |
| container_volume | 16 |
| creator | Sangana, Ramachandra Mittal, Hemant Barsainya, Sarita Hoermann, Aldo Borde, Parag Naik, Sachin Thorat, Anup Vilas Zhang, Jie Valentin, Marie-Anne Kalluri, Sampath |
| description | Vildagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor to treat type 2 diabetes mellitus, is available as immediate release (IR) tablets administered at 50 mg twice daily (BID). A 100 mg modified release (MR) formulation was developed for once daily (QD) dosing. This study aimed to compare the therapeutic equivalence of vildagliptin 100 mg MR QD (test) and 50 mg IR BID (reference) formulations at steady state under fasting conditions.
This was an open-label, randomized, two-period, single- and multiple-dose, two-way crossover, steady state study conducted in healthy adult subjects. Both vildagliptin formulations were administered for six days. Endpoints included pharmacodynamic equivalence, pharmacokinetic parameters, and tolerability of both formulations.
Thirty subjects were enrolled and 26 completed both treatments. Maximum plasma concentration and exposure achieved with test was lower than reference formulation on day 1 and 6. The DPP-4 enzyme inhibition over time (DPP-4-AUEC0-24) was comparable between the formulations. Both formulations were well tolerated.
This study confirms the therapeutic equivalence of vildagliptin IR and MR formulations for DPP-4 enzyme inhibition over time. The study supports vildagliptin 100 mg MR QD as a useful therapeutic alternative to 50 mg IR BID formulation to possibly improve treatment adherence and patient compliance. Long-term safety of the vildagliptin 100 mg MR QD formulation is not evaluated in this study.
•To address patients' treatment adherence needs, vildagliptin 100 mg once daily modified release formulation was developed.•Study confirms therapeutic equivalence (DPP4 enzyme inhibition over time) between IR and MR formulations of vildagliptin.•Vildagliptin 100 mg MR once daily formulation can be used as therapeutic alternative to 50 mg IR twice daily tablet in India. |
| doi_str_mv | 10.1016/j.dsx.2022.102438 |
| format | article |
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This was an open-label, randomized, two-period, single- and multiple-dose, two-way crossover, steady state study conducted in healthy adult subjects. Both vildagliptin formulations were administered for six days. Endpoints included pharmacodynamic equivalence, pharmacokinetic parameters, and tolerability of both formulations.
Thirty subjects were enrolled and 26 completed both treatments. Maximum plasma concentration and exposure achieved with test was lower than reference formulation on day 1 and 6. The DPP-4 enzyme inhibition over time (DPP-4-AUEC0-24) was comparable between the formulations. Both formulations were well tolerated.
This study confirms the therapeutic equivalence of vildagliptin IR and MR formulations for DPP-4 enzyme inhibition over time. The study supports vildagliptin 100 mg MR QD as a useful therapeutic alternative to 50 mg IR BID formulation to possibly improve treatment adherence and patient compliance. Long-term safety of the vildagliptin 100 mg MR QD formulation is not evaluated in this study.
•To address patients' treatment adherence needs, vildagliptin 100 mg once daily modified release formulation was developed.•Study confirms therapeutic equivalence (DPP4 enzyme inhibition over time) between IR and MR formulations of vildagliptin.•Vildagliptin 100 mg MR once daily formulation can be used as therapeutic alternative to 50 mg IR twice daily tablet in India.</description><identifier>ISSN: 1871-4021</identifier><identifier>EISSN: 1878-0334</identifier><identifier>DOI: 10.1016/j.dsx.2022.102438</identifier><identifier>PMID: 35272176</identifier><language>eng</language><publisher>Netherlands: Elsevier Ltd</publisher><subject>Adult ; Cross-Over Studies ; Diabetes Mellitus, Type 2 - drug therapy ; Dipeptidyl-peptidase IV inhibitors ; Dipeptidyl-Peptidase IV Inhibitors - therapeutic use ; Humans ; Hypoglycemic Agents - therapeutic use ; Pharmacodynamic ; Pharmacokinetic ; Therapeutic equivalence ; Treatment adherence and compliance ; Type 2 diabetes mellitus ; Vildagliptin ; Vildagliptin - therapeutic use</subject><ispartof>Diabetes & metabolic syndrome clinical research & reviews, 2022-03, Vol.16 (3), p.102438-102438, Article 102438</ispartof><rights>2022 Diabetes India</rights><rights>Copyright © 2022 Diabetes India. Published by Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c268t-ec1314dd1dc43128f8dbe0869c8e3f9bcb1cf87c5bdf31e332ded7879913c9363</citedby><cites>FETCH-LOGICAL-c268t-ec1314dd1dc43128f8dbe0869c8e3f9bcb1cf87c5bdf31e332ded7879913c9363</cites><orcidid>0000-0002-4446-5200 ; 0000-0003-3772-0370</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>315,786,790,27957,27958</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/35272176$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Sangana, Ramachandra</creatorcontrib><creatorcontrib>Mittal, Hemant</creatorcontrib><creatorcontrib>Barsainya, Sarita</creatorcontrib><creatorcontrib>Hoermann, Aldo</creatorcontrib><creatorcontrib>Borde, Parag</creatorcontrib><creatorcontrib>Naik, Sachin</creatorcontrib><creatorcontrib>Thorat, Anup Vilas</creatorcontrib><creatorcontrib>Zhang, Jie</creatorcontrib><creatorcontrib>Valentin, Marie-Anne</creatorcontrib><creatorcontrib>Kalluri, Sampath</creatorcontrib><title>Therapeutic equivalence of vildagliptin 100 mg once daily modified release to 50 mg twice daily immediate release formulation: An open-label, randomized, two-period, single- and multiple-dose, 6-day crossover study</title><title>Diabetes & metabolic syndrome clinical research & reviews</title><addtitle>Diabetes Metab Syndr</addtitle><description>Vildagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor to treat type 2 diabetes mellitus, is available as immediate release (IR) tablets administered at 50 mg twice daily (BID). A 100 mg modified release (MR) formulation was developed for once daily (QD) dosing. This study aimed to compare the therapeutic equivalence of vildagliptin 100 mg MR QD (test) and 50 mg IR BID (reference) formulations at steady state under fasting conditions.
This was an open-label, randomized, two-period, single- and multiple-dose, two-way crossover, steady state study conducted in healthy adult subjects. Both vildagliptin formulations were administered for six days. Endpoints included pharmacodynamic equivalence, pharmacokinetic parameters, and tolerability of both formulations.
Thirty subjects were enrolled and 26 completed both treatments. Maximum plasma concentration and exposure achieved with test was lower than reference formulation on day 1 and 6. The DPP-4 enzyme inhibition over time (DPP-4-AUEC0-24) was comparable between the formulations. Both formulations were well tolerated.
This study confirms the therapeutic equivalence of vildagliptin IR and MR formulations for DPP-4 enzyme inhibition over time. The study supports vildagliptin 100 mg MR QD as a useful therapeutic alternative to 50 mg IR BID formulation to possibly improve treatment adherence and patient compliance. Long-term safety of the vildagliptin 100 mg MR QD formulation is not evaluated in this study.
•To address patients' treatment adherence needs, vildagliptin 100 mg once daily modified release formulation was developed.•Study confirms therapeutic equivalence (DPP4 enzyme inhibition over time) between IR and MR formulations of vildagliptin.•Vildagliptin 100 mg MR once daily formulation can be used as therapeutic alternative to 50 mg IR twice daily tablet in India.</description><subject>Adult</subject><subject>Cross-Over Studies</subject><subject>Diabetes Mellitus, Type 2 - drug therapy</subject><subject>Dipeptidyl-peptidase IV inhibitors</subject><subject>Dipeptidyl-Peptidase IV Inhibitors - therapeutic use</subject><subject>Humans</subject><subject>Hypoglycemic Agents - therapeutic use</subject><subject>Pharmacodynamic</subject><subject>Pharmacokinetic</subject><subject>Therapeutic equivalence</subject><subject>Treatment adherence and compliance</subject><subject>Type 2 diabetes mellitus</subject><subject>Vildagliptin</subject><subject>Vildagliptin - therapeutic use</subject><issn>1871-4021</issn><issn>1878-0334</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2022</creationdate><recordtype>article</recordtype><recordid>eNp9kUtuFDEQhlsIRELgAGyQlyymBz_64YZVFIWHFIlNWFtuu3qokbvdsd0Dw2k4S07BcfBkwixZuUr11S_bX1G8ZnTNKGvebdc2_lxzynnueSXkk-KcyVaWVIjq6UPNyopydla8iHFLaV13vHtenImat5y1zXnx5_Y7BD3DktAQuFtwpx1MBogfyA6d1RuHc8KJMErvf48b4g9Dq9HtyegtDgiWBHCgI5DkSX2k0g88YTiOYFEnOHGDD-PidEI_vSeXE_EzTKXTPbgVCXqyfsRfYFc5xZczBPS5jjhtHJQkj0leTjjnzvoIK9KUVu-JCT5Gv4NAYlrs_mXxbNAuwqvH86L49vH69upzefP105ery5vS8EamEgwTrLKWWVMJxuUgbQ9UNp2RIIauNz0zg2xN3dtBMBCCW7CtbLuOCdOJRlwUb4-5c_B3C8SkRowGnNMT-CUq3gjZ8qpu24yyI_pw1QCDmgOOOuwVo-ogVG1VFqoOQtVRaN558xi_9PkbTxv_DGbgwxGA_MgdQlDR4MGgxQAmKevxP_F_AW8Mtrw</recordid><startdate>202203</startdate><enddate>202203</enddate><creator>Sangana, Ramachandra</creator><creator>Mittal, Hemant</creator><creator>Barsainya, Sarita</creator><creator>Hoermann, Aldo</creator><creator>Borde, Parag</creator><creator>Naik, Sachin</creator><creator>Thorat, Anup Vilas</creator><creator>Zhang, Jie</creator><creator>Valentin, Marie-Anne</creator><creator>Kalluri, Sampath</creator><general>Elsevier Ltd</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>7X8</scope><orcidid>https://orcid.org/0000-0002-4446-5200</orcidid><orcidid>https://orcid.org/0000-0003-3772-0370</orcidid></search><sort><creationdate>202203</creationdate><title>Therapeutic equivalence of vildagliptin 100 mg once daily modified release to 50 mg twice daily immediate release formulation: An open-label, randomized, two-period, single- and multiple-dose, 6-day crossover study</title><author>Sangana, Ramachandra ; Mittal, Hemant ; Barsainya, Sarita ; Hoermann, Aldo ; Borde, Parag ; Naik, Sachin ; Thorat, Anup Vilas ; Zhang, Jie ; Valentin, Marie-Anne ; Kalluri, Sampath</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c268t-ec1314dd1dc43128f8dbe0869c8e3f9bcb1cf87c5bdf31e332ded7879913c9363</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2022</creationdate><topic>Adult</topic><topic>Cross-Over Studies</topic><topic>Diabetes Mellitus, Type 2 - drug therapy</topic><topic>Dipeptidyl-peptidase IV inhibitors</topic><topic>Dipeptidyl-Peptidase IV Inhibitors - therapeutic use</topic><topic>Humans</topic><topic>Hypoglycemic Agents - therapeutic use</topic><topic>Pharmacodynamic</topic><topic>Pharmacokinetic</topic><topic>Therapeutic equivalence</topic><topic>Treatment adherence and compliance</topic><topic>Type 2 diabetes mellitus</topic><topic>Vildagliptin</topic><topic>Vildagliptin - therapeutic use</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Sangana, Ramachandra</creatorcontrib><creatorcontrib>Mittal, Hemant</creatorcontrib><creatorcontrib>Barsainya, Sarita</creatorcontrib><creatorcontrib>Hoermann, Aldo</creatorcontrib><creatorcontrib>Borde, Parag</creatorcontrib><creatorcontrib>Naik, Sachin</creatorcontrib><creatorcontrib>Thorat, Anup Vilas</creatorcontrib><creatorcontrib>Zhang, Jie</creatorcontrib><creatorcontrib>Valentin, Marie-Anne</creatorcontrib><creatorcontrib>Kalluri, Sampath</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Diabetes & metabolic syndrome clinical research & reviews</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Sangana, Ramachandra</au><au>Mittal, Hemant</au><au>Barsainya, Sarita</au><au>Hoermann, Aldo</au><au>Borde, Parag</au><au>Naik, Sachin</au><au>Thorat, Anup Vilas</au><au>Zhang, Jie</au><au>Valentin, Marie-Anne</au><au>Kalluri, Sampath</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Therapeutic equivalence of vildagliptin 100 mg once daily modified release to 50 mg twice daily immediate release formulation: An open-label, randomized, two-period, single- and multiple-dose, 6-day crossover study</atitle><jtitle>Diabetes & metabolic syndrome clinical research & reviews</jtitle><addtitle>Diabetes Metab Syndr</addtitle><date>2022-03</date><risdate>2022</risdate><volume>16</volume><issue>3</issue><spage>102438</spage><epage>102438</epage><pages>102438-102438</pages><artnum>102438</artnum><issn>1871-4021</issn><eissn>1878-0334</eissn><notes>ObjectType-Article-1</notes><notes>SourceType-Scholarly Journals-1</notes><notes>ObjectType-Feature-2</notes><notes>ObjectType-News-3</notes><notes>content type line 23</notes><abstract>Vildagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor to treat type 2 diabetes mellitus, is available as immediate release (IR) tablets administered at 50 mg twice daily (BID). A 100 mg modified release (MR) formulation was developed for once daily (QD) dosing. This study aimed to compare the therapeutic equivalence of vildagliptin 100 mg MR QD (test) and 50 mg IR BID (reference) formulations at steady state under fasting conditions.
This was an open-label, randomized, two-period, single- and multiple-dose, two-way crossover, steady state study conducted in healthy adult subjects. Both vildagliptin formulations were administered for six days. Endpoints included pharmacodynamic equivalence, pharmacokinetic parameters, and tolerability of both formulations.
Thirty subjects were enrolled and 26 completed both treatments. Maximum plasma concentration and exposure achieved with test was lower than reference formulation on day 1 and 6. The DPP-4 enzyme inhibition over time (DPP-4-AUEC0-24) was comparable between the formulations. Both formulations were well tolerated.
This study confirms the therapeutic equivalence of vildagliptin IR and MR formulations for DPP-4 enzyme inhibition over time. The study supports vildagliptin 100 mg MR QD as a useful therapeutic alternative to 50 mg IR BID formulation to possibly improve treatment adherence and patient compliance. Long-term safety of the vildagliptin 100 mg MR QD formulation is not evaluated in this study.
•To address patients' treatment adherence needs, vildagliptin 100 mg once daily modified release formulation was developed.•Study confirms therapeutic equivalence (DPP4 enzyme inhibition over time) between IR and MR formulations of vildagliptin.•Vildagliptin 100 mg MR once daily formulation can be used as therapeutic alternative to 50 mg IR twice daily tablet in India.</abstract><cop>Netherlands</cop><pub>Elsevier Ltd</pub><pmid>35272176</pmid><doi>10.1016/j.dsx.2022.102438</doi><tpages>1</tpages><orcidid>https://orcid.org/0000-0002-4446-5200</orcidid><orcidid>https://orcid.org/0000-0003-3772-0370</orcidid></addata></record> |
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| ispartof | Diabetes & metabolic syndrome clinical research & reviews, 2022-03, Vol.16 (3), p.102438-102438, Article 102438 |
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| language | eng |
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| source | Elsevier |
| subjects | Adult Cross-Over Studies Diabetes Mellitus, Type 2 - drug therapy Dipeptidyl-peptidase IV inhibitors Dipeptidyl-Peptidase IV Inhibitors - therapeutic use Humans Hypoglycemic Agents - therapeutic use Pharmacodynamic Pharmacokinetic Therapeutic equivalence Treatment adherence and compliance Type 2 diabetes mellitus Vildagliptin Vildagliptin - therapeutic use |
| title | Therapeutic equivalence of vildagliptin 100 mg once daily modified release to 50 mg twice daily immediate release formulation: An open-label, randomized, two-period, single- and multiple-dose, 6-day crossover study |
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