Biology:Gosogliptin
From HandWiki
Short description: Chemical compound
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| Other names | PF-734200 |
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| Formula | C17H24F2N6O |
| Molar mass | 366.417 g·mol−1 |
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Gosogliptin (INN; trade name Saterex) is a drug for the treatment of type II diabetes. It is in the class of dipeptidyl peptidase-4 (DPP-4) inhibitors (also called gliptins). It was discovered[1] and developed through Phase 1[2][3][4] and Phase 2[5][6][7] by Pfizer. The crystal structure of DPP-4 in complex with gosogliptin is available.[8] Its metabolism, excretion and pharmacokinetics in rat, dog and human have been described.[9] A cost efficient route has been published.[10] Other studies[11] including Phase 3 studies were conducted in Russia.[12][13] It is approved for use in Russia.[14]
References
- ↑ "(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor". Bioorganic & Medicinal Chemistry Letters 19 (7): 1991–1995. April 2009. doi:10.1016/j.bmcl.2009.02.041. PMID 19275964.
- ↑ "Non-linear increase in GLP-1 levels in response to DPP-IV inhibition in healthy adult subjects". Diabetes, Obesity and Metabolism 10 (6): 506–513. 2008. doi:10.1111/j.1463-1326.2007.00742.x. PMID 18284437.
- ↑ "The pharmacokinetics of PF-734200, a DPP-IV inhibitor, in subjects with renal insufficiency". British Journal of Clinical Pharmacology 72 (1): 85–91. July 2011. doi:10.1111/j.1365-2125.2011.03954.x. PMID 21366665.
- ↑ "The pharmacokinetics and pharmacodynamics of PF-00734200, a DPP-IV inhibitor, in healthy Japanese subjects". International Journal of Clinical Pharmacology and Therapeutics 50 (7): 505–509. 2012. doi:10.5414/CP201614. PMID 22541754.
- ↑ "Efficacy and safety of the dipeptidyl peptidase‐4 inhibitor PF‐734200 added to metformin in Type 2 diabetes". Diabetic Medicine 28 (4): 464–469. 2011. doi:10.1111/j.1464-5491.2010.03181.x. PMID 21392067.
- ↑ "A Phase 2, Randomized, Double-Blind, Placebo-Controlled, Parallel Group Study to Evaluate the Efficacy and Safety of 12-Week Administration of PF-00734200 to Subjects with Type 2 Diabetes Mellitus and Insufficient Glycemic Control on Metformin Treatment". 9 June 2011. https://clinicaltrials.gov/ct2/show/NCT00618007.
- ↑ "A Phase 2a, Randomized, Placebo-Controlled, Parallel Group, Multiple-Dose Study to Evaluate the Efficacy, Safety, and Tolerability of 12-Week Oral Administration of PF-00734200 Tablets to Subjects with Type 2 Diabetes Mellitus on Stable Treatment with Metformin". 22 June 2010. https://clinicaltrials.gov/ct2/show/NCT00473525.
- ↑ "RCSB PDB - 3F8S: Crystal structure of dipeptidyl peptidase IV in complex with inhibitor". https://www.rcsb.org/structure/3F8S.
- ↑ "Metabolism, Excretion, and Pharmacokinetics of ((3,3-Difluoropyrrolidin-1-yl)((2 S ,4 S )-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a Dipeptidyl Peptidase Inhibitor, in Rat, Dog and Human" (in en). Drug Metabolism and Disposition 40 (11): 2143–2161. November 2012. doi:10.1124/dmd.112.047316. ISSN 0090-9556. PMID 22896728.
- ↑ "New Synthetic Route to a Dipeptidyl Peptidase-4 Inhibitor". Organic Process Research & Development 16 (3): 409–14. January 2012. doi:10.1021/op200309z.
- ↑ "Initial investigation of efficacy and safety of a new dipeptidyl peptidase-4 inhibitor, gosogliptin, for type 2 diabetes in Russia". Diabetes Mellitus 17 (4): 81–86. 2014. doi:10.14341/DM2014481-86.
- ↑ "Comparison of the novel Russian DPP-4 inhibitor gosogliptin with vildagliptin in patients with type 2 diabetes mellitus". Diabetes Mellitus 19 (1): 89‐96. April 2016. doi:10.14341/DM7233.
- ↑ "Evaluate Efficacy and Safety of Gosogliptin as Monotherapy and in Combination with Metformin vs. Vildagliptin as Monotherapy and in Combination with Metformin in Drug-naive Type 2 Diabetic Patients". 18 March 2017. https://clinicaltrials.gov/ct2/show/NCT03088670.
- ↑ "SatRx LLC Announces First Registration in Russia of SatRx (gosogliptin), an Innovative Drug for Treatment of Type 2 Diabetes" (Press release). SatRx LLC.
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