Randomised clinical trial: safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple oral doses of tegoprazan (CJ‐12420), a novel potassium‐competitive acid blocker, in healthy male subjects
Summary Background Tegoprazan (CJ‐12420) is a potassium‐competitive acid blocker (P‐CAB) with therapeutic potential for gastro‐oesophageal reflux disease (GERD) by reversibly suppressing gastric H+/K+‐ATPase. Aims To investigate the safety, tolerability, pharmacokinetics and pharmacodynamics of tego...
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| Veröffentlicht in: | Alimentary pharmacology & therapeutics 2019-10, Vol.50 (7), p.751-759 |
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| container_title | Alimentary pharmacology & therapeutics |
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| creator | Han, Sungpil Choi, Hee Youn Kim, Yo Han Nam, Ji Yeon Kim, Bongtae Song, Geun Seog Lim, Hyeong‐Seok Bae, Kyun‐Seop |
| description | Summary
Background
Tegoprazan (CJ‐12420) is a potassium‐competitive acid blocker (P‐CAB) with therapeutic potential for gastro‐oesophageal reflux disease (GERD) by reversibly suppressing gastric H+/K+‐ATPase.
Aims
To investigate the safety, tolerability, pharmacokinetics and pharmacodynamics of tegoprazan
Methods
A phase I, randomised, double‐blind and placebo‐controlled clinical trial was conducted in 56 healthy male subjects without Helicobacter pylori infection. In the single ascending dose study, 50, 100, 200 and 400 mg tegoprazan were administered to 32 subjects. In the multiple ascending dose study, 100 and 200 mg tegoprazan were administered every 24 hours to each of the eight subjects for 7 days. In the comparative pharmacodynamics study, 40 mg esomeprazole was administered to eight subjects every 24 hours for 7 days. The assessment included safety, tolerability, pharmacodynamics through monitoring of 24‐hour gastric pH and pharmacokinetics of tegoprazan in plasma and urine.
Results
Tegoprazan was generally well tolerated. Most adverse events reported in the study were mild in intensity and resolved without any sequelae. Exposure to tegoprazan increased in a dose‐proportional manner. Multiple dosing with tegoprazan showed no accumulation in plasma on day 7. The pharmacodynamic analysis revealed that tegoprazan showed rapid, dose‐dependent gastric acid suppression.
Conclusions
Tegoprazan was well tolerated and showed rapid and potent gastric acid suppression. This supports the further development of tegoprazan as a treatment for acid‐related disorders. |
| doi_str_mv | 10.1111/apt.15438 |
| format | Article |
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Background
Tegoprazan (CJ‐12420) is a potassium‐competitive acid blocker (P‐CAB) with therapeutic potential for gastro‐oesophageal reflux disease (GERD) by reversibly suppressing gastric H+/K+‐ATPase.
Aims
To investigate the safety, tolerability, pharmacokinetics and pharmacodynamics of tegoprazan
Methods
A phase I, randomised, double‐blind and placebo‐controlled clinical trial was conducted in 56 healthy male subjects without Helicobacter pylori infection. In the single ascending dose study, 50, 100, 200 and 400 mg tegoprazan were administered to 32 subjects. In the multiple ascending dose study, 100 and 200 mg tegoprazan were administered every 24 hours to each of the eight subjects for 7 days. In the comparative pharmacodynamics study, 40 mg esomeprazole was administered to eight subjects every 24 hours for 7 days. The assessment included safety, tolerability, pharmacodynamics through monitoring of 24‐hour gastric pH and pharmacokinetics of tegoprazan in plasma and urine.
Results
Tegoprazan was generally well tolerated. Most adverse events reported in the study were mild in intensity and resolved without any sequelae. Exposure to tegoprazan increased in a dose‐proportional manner. Multiple dosing with tegoprazan showed no accumulation in plasma on day 7. The pharmacodynamic analysis revealed that tegoprazan showed rapid, dose‐dependent gastric acid suppression.
Conclusions
Tegoprazan was well tolerated and showed rapid and potent gastric acid suppression. This supports the further development of tegoprazan as a treatment for acid‐related disorders.</description><identifier>ISSN: 0269-2813</identifier><identifier>EISSN: 1365-2036</identifier><identifier>DOI: 10.1111/apt.15438</identifier><identifier>PMID: 31437865</identifier><language>eng</language><publisher>England: Wiley Subscription Services, Inc</publisher><subject>Acids ; Administration, Oral ; Adult ; Benzene Derivatives - administration & dosage ; Clinical trials ; Complications ; Dosage ; Dose-Response Relationship, Drug ; Double-Blind Method ; Esomeprazole - administration & dosage ; Esophagus ; Gastric Acid - metabolism ; Gastric juice ; Gastroesophageal reflux ; H(+)-K(+)-Exchanging ATPase - metabolism ; Health risk assessment ; Helicobacter pylori ; Humans ; Imidazoles - administration & dosage ; Male ; Middle Aged ; Omeprazole ; Pharmacodynamics ; Pharmacokinetics ; Potassium ; Randomization ; Safety ; Urine ; Young Adult</subject><ispartof>Alimentary pharmacology & therapeutics, 2019-10, Vol.50 (7), p.751-759</ispartof><rights>2019 John Wiley & Sons Ltd</rights><rights>2019 John Wiley & Sons Ltd.</rights><rights>Copyright © 2019 John Wiley & Sons Ltd</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c3538-5a9483b3b17de917933784631bc7f04c5ad8c16834cf36b1d3b28f60a5a76f083</citedby><cites>FETCH-LOGICAL-c3538-5a9483b3b17de917933784631bc7f04c5ad8c16834cf36b1d3b28f60a5a76f083</cites><orcidid>0000-0002-4674-7682</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1111%2Fapt.15438$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1111%2Fapt.15438$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,776,780,1411,1427,27901,27902,45550,45551,46384,46808</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/31437865$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Han, Sungpil</creatorcontrib><creatorcontrib>Choi, Hee Youn</creatorcontrib><creatorcontrib>Kim, Yo Han</creatorcontrib><creatorcontrib>Nam, Ji Yeon</creatorcontrib><creatorcontrib>Kim, Bongtae</creatorcontrib><creatorcontrib>Song, Geun Seog</creatorcontrib><creatorcontrib>Lim, Hyeong‐Seok</creatorcontrib><creatorcontrib>Bae, Kyun‐Seop</creatorcontrib><title>Randomised clinical trial: safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple oral doses of tegoprazan (CJ‐12420), a novel potassium‐competitive acid blocker, in healthy male subjects</title><title>Alimentary pharmacology & therapeutics</title><addtitle>Aliment Pharmacol Ther</addtitle><description>Summary
Background
Tegoprazan (CJ‐12420) is a potassium‐competitive acid blocker (P‐CAB) with therapeutic potential for gastro‐oesophageal reflux disease (GERD) by reversibly suppressing gastric H+/K+‐ATPase.
Aims
To investigate the safety, tolerability, pharmacokinetics and pharmacodynamics of tegoprazan
Methods
A phase I, randomised, double‐blind and placebo‐controlled clinical trial was conducted in 56 healthy male subjects without Helicobacter pylori infection. In the single ascending dose study, 50, 100, 200 and 400 mg tegoprazan were administered to 32 subjects. In the multiple ascending dose study, 100 and 200 mg tegoprazan were administered every 24 hours to each of the eight subjects for 7 days. In the comparative pharmacodynamics study, 40 mg esomeprazole was administered to eight subjects every 24 hours for 7 days. The assessment included safety, tolerability, pharmacodynamics through monitoring of 24‐hour gastric pH and pharmacokinetics of tegoprazan in plasma and urine.
Results
Tegoprazan was generally well tolerated. Most adverse events reported in the study were mild in intensity and resolved without any sequelae. Exposure to tegoprazan increased in a dose‐proportional manner. Multiple dosing with tegoprazan showed no accumulation in plasma on day 7. The pharmacodynamic analysis revealed that tegoprazan showed rapid, dose‐dependent gastric acid suppression.
Conclusions
Tegoprazan was well tolerated and showed rapid and potent gastric acid suppression. This supports the further development of tegoprazan as a treatment for acid‐related disorders.</description><subject>Acids</subject><subject>Administration, Oral</subject><subject>Adult</subject><subject>Benzene Derivatives - administration & dosage</subject><subject>Clinical trials</subject><subject>Complications</subject><subject>Dosage</subject><subject>Dose-Response Relationship, Drug</subject><subject>Double-Blind Method</subject><subject>Esomeprazole - administration & dosage</subject><subject>Esophagus</subject><subject>Gastric Acid - metabolism</subject><subject>Gastric juice</subject><subject>Gastroesophageal reflux</subject><subject>H(+)-K(+)-Exchanging ATPase - metabolism</subject><subject>Health risk assessment</subject><subject>Helicobacter pylori</subject><subject>Humans</subject><subject>Imidazoles - administration & dosage</subject><subject>Male</subject><subject>Middle Aged</subject><subject>Omeprazole</subject><subject>Pharmacodynamics</subject><subject>Pharmacokinetics</subject><subject>Potassium</subject><subject>Randomization</subject><subject>Safety</subject><subject>Urine</subject><subject>Young Adult</subject><issn>0269-2813</issn><issn>1365-2036</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2019</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp1kc9u1DAQhy0EosvCgRdAlrhQadP6T-Ik3KoVFFClIlTO0cRxut46drCdovTUR-ABe-JJcHfb3vDFmplP30jzQ-gtJUc0vWMY4xEtcl49QwvKRZExwsVztCBM1BmrKD9Ar0LYEkJESdhLdMBpzstKFAt09wNs5wYdVIel0VZLMDh6DeYjDtCrOK9wdEZ5aLXR99W4AT-AdFfaqqhlWOFkeOp2s4UhdbHrcdD20qjdeJhM1GMqnE_-zgW1I6K6dKOHG7D4w_rb39s_lOWMHCYltu5aGTy6CCHoaUgz6YYxbYz6Ojml7nBrnLxSfoW1xRsFJm5mPEBaEqZ2q2QMr9GLHkxQbx7-Jfr5-dPF-kt2dn76dX1ylkle8CoroM4r3vKWlp2qaVnzdJxccNrKsie5LKCrJBUVz2XPRUs73rKqFwQKKEVPKr5E7_fe0btfkwqx2brJ27SyYaxmJCFJt0SHe0p6F4JXfTN6PYCfG0qa-xyblGOzyzGx7x6MUzuo7ol8DC4Bx3vgtzZq_r-pOfl-sVf-A0ZjrIM</recordid><startdate>201910</startdate><enddate>201910</enddate><creator>Han, Sungpil</creator><creator>Choi, Hee Youn</creator><creator>Kim, Yo Han</creator><creator>Nam, Ji Yeon</creator><creator>Kim, Bongtae</creator><creator>Song, Geun Seog</creator><creator>Lim, Hyeong‐Seok</creator><creator>Bae, Kyun‐Seop</creator><general>Wiley Subscription Services, Inc</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>7T5</scope><scope>7TK</scope><scope>7U9</scope><scope>H94</scope><scope>M7N</scope><orcidid>https://orcid.org/0000-0002-4674-7682</orcidid></search><sort><creationdate>201910</creationdate><title>Randomised clinical trial: safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple oral doses of tegoprazan (CJ‐12420), a novel potassium‐competitive acid blocker, in healthy male subjects</title><author>Han, Sungpil ; Choi, Hee Youn ; Kim, Yo Han ; Nam, Ji Yeon ; Kim, Bongtae ; Song, Geun Seog ; Lim, Hyeong‐Seok ; Bae, Kyun‐Seop</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3538-5a9483b3b17de917933784631bc7f04c5ad8c16834cf36b1d3b28f60a5a76f083</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2019</creationdate><topic>Acids</topic><topic>Administration, Oral</topic><topic>Adult</topic><topic>Benzene Derivatives - administration & dosage</topic><topic>Clinical trials</topic><topic>Complications</topic><topic>Dosage</topic><topic>Dose-Response Relationship, Drug</topic><topic>Double-Blind Method</topic><topic>Esomeprazole - administration & dosage</topic><topic>Esophagus</topic><topic>Gastric Acid - metabolism</topic><topic>Gastric juice</topic><topic>Gastroesophageal reflux</topic><topic>H(+)-K(+)-Exchanging ATPase - metabolism</topic><topic>Health risk assessment</topic><topic>Helicobacter pylori</topic><topic>Humans</topic><topic>Imidazoles - administration & dosage</topic><topic>Male</topic><topic>Middle Aged</topic><topic>Omeprazole</topic><topic>Pharmacodynamics</topic><topic>Pharmacokinetics</topic><topic>Potassium</topic><topic>Randomization</topic><topic>Safety</topic><topic>Urine</topic><topic>Young Adult</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Han, Sungpil</creatorcontrib><creatorcontrib>Choi, Hee Youn</creatorcontrib><creatorcontrib>Kim, Yo Han</creatorcontrib><creatorcontrib>Nam, Ji Yeon</creatorcontrib><creatorcontrib>Kim, Bongtae</creatorcontrib><creatorcontrib>Song, Geun Seog</creatorcontrib><creatorcontrib>Lim, Hyeong‐Seok</creatorcontrib><creatorcontrib>Bae, Kyun‐Seop</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Immunology Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><jtitle>Alimentary pharmacology & therapeutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Han, Sungpil</au><au>Choi, Hee Youn</au><au>Kim, Yo Han</au><au>Nam, Ji Yeon</au><au>Kim, Bongtae</au><au>Song, Geun Seog</au><au>Lim, Hyeong‐Seok</au><au>Bae, Kyun‐Seop</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Randomised clinical trial: safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple oral doses of tegoprazan (CJ‐12420), a novel potassium‐competitive acid blocker, in healthy male subjects</atitle><jtitle>Alimentary pharmacology & therapeutics</jtitle><addtitle>Aliment Pharmacol Ther</addtitle><date>2019-10</date><risdate>2019</risdate><volume>50</volume><issue>7</issue><spage>751</spage><epage>759</epage><pages>751-759</pages><issn>0269-2813</issn><eissn>1365-2036</eissn><abstract>Summary
Background
Tegoprazan (CJ‐12420) is a potassium‐competitive acid blocker (P‐CAB) with therapeutic potential for gastro‐oesophageal reflux disease (GERD) by reversibly suppressing gastric H+/K+‐ATPase.
Aims
To investigate the safety, tolerability, pharmacokinetics and pharmacodynamics of tegoprazan
Methods
A phase I, randomised, double‐blind and placebo‐controlled clinical trial was conducted in 56 healthy male subjects without Helicobacter pylori infection. In the single ascending dose study, 50, 100, 200 and 400 mg tegoprazan were administered to 32 subjects. In the multiple ascending dose study, 100 and 200 mg tegoprazan were administered every 24 hours to each of the eight subjects for 7 days. In the comparative pharmacodynamics study, 40 mg esomeprazole was administered to eight subjects every 24 hours for 7 days. The assessment included safety, tolerability, pharmacodynamics through monitoring of 24‐hour gastric pH and pharmacokinetics of tegoprazan in plasma and urine.
Results
Tegoprazan was generally well tolerated. Most adverse events reported in the study were mild in intensity and resolved without any sequelae. Exposure to tegoprazan increased in a dose‐proportional manner. Multiple dosing with tegoprazan showed no accumulation in plasma on day 7. The pharmacodynamic analysis revealed that tegoprazan showed rapid, dose‐dependent gastric acid suppression.
Conclusions
Tegoprazan was well tolerated and showed rapid and potent gastric acid suppression. This supports the further development of tegoprazan as a treatment for acid‐related disorders.</abstract><cop>England</cop><pub>Wiley Subscription Services, Inc</pub><pmid>31437865</pmid><doi>10.1111/apt.15438</doi><tpages>9</tpages><orcidid>https://orcid.org/0000-0002-4674-7682</orcidid></addata></record> |
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| ispartof | Alimentary pharmacology & therapeutics, 2019-10, Vol.50 (7), p.751-759 |
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| language | eng |
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| source | MEDLINE; Wiley Online Library Journals Frontfile Complete; Wiley Online Library Free Content; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals |
| subjects | Acids Administration, Oral Adult Benzene Derivatives - administration & dosage Clinical trials Complications Dosage Dose-Response Relationship, Drug Double-Blind Method Esomeprazole - administration & dosage Esophagus Gastric Acid - metabolism Gastric juice Gastroesophageal reflux H(+)-K(+)-Exchanging ATPase - metabolism Health risk assessment Helicobacter pylori Humans Imidazoles - administration & dosage Male Middle Aged Omeprazole Pharmacodynamics Pharmacokinetics Potassium Randomization Safety Urine Young Adult |
| title | Randomised clinical trial: safety, tolerability, pharmacokinetics, and pharmacodynamics of single and multiple oral doses of tegoprazan (CJ‐12420), a novel potassium‐competitive acid blocker, in healthy male subjects |
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