Gosogliptin

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Gosogliptin
INN: Gosogliptin
Gosogliptin.svg
Clinical data
Other namesPF-734200
Identifiers
  • (3,3-Difluoro-1-pyrrolidinyl){(2S,4S)-4-[4-(2-pyrimidinyl)-1-piperazinyl]-2-pyrrolidinyl}methanone
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
Formula C17H24F2N6O
Molar mass 366.417 g·mol−1
3D model (JSmol)
  • c1cnc(nc1)N2CCN(CC2)[C@H]3C[C@H](NC3)C(=O)N4CCC(C4)(F)F
  • InChI=1S/C17H24F2N6O/c18-17(19)2-5-25(12-17)15(26)14-10-13(11-22-14)23-6-8-24(9-7-23)16-20-3-1-4-21-16/h1,3-4,13-14,22H,2,5-12H2/t13-,14-/m0/s1
  • Key:QWEWGXUTRTXFRF-KBPBESRZSA-N

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]

Related Research Articles

Drugs used in diabetes treat diabetes mellitus by decreasing the glucose level in the blood. With the exception of insulin, most GLP receptor agonists, and pramlintide, all are administered orally and are thus also called oral hypoglycemic agents or oral antihyperglycemic agents. There are different classes of hypoglycemic drugs, and their selection depends on the nature of diabetes, age, and situation of the person, as well as other factors.

<span class="mw-page-title-main">Incretin</span> Group of gastrointestinal hormones

Incretins are a group of metabolic hormones that stimulate a decrease in blood glucose levels. Incretins are released after eating and augment the secretion of insulin released from pancreatic beta cells of the islets of Langerhans by a blood-glucose–dependent mechanism.

<span class="mw-page-title-main">Vildagliptin</span> Chemical compound

Vildagliptin, sold under the brand name Galvus and others, is an oral anti-hyperglycemic agent of the dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Vildagliptin inhibits the inactivation of GLP-1 and GIP by DPP-4, allowing GLP-1 and GIP to potentiate the secretion of insulin in the beta cells and suppress glucagon release by the alpha cells of the islets of Langerhans in the pancreas.

<span class="mw-page-title-main">Dipeptidyl peptidase-4 inhibitor</span> Enzyme blocker and diabetes treatment drug

Inhibitors of dipeptidyl peptidase 4 are a class of oral hypoglycemics that block the enzyme dipeptidyl peptidase-4 (DPP-4). They can be used to treat diabetes mellitus type 2.

<span class="mw-page-title-main">Sitagliptin</span> Diabetes medication

Sitagliptin, sold under the brand name Januvia among others, is an anti-diabetic medication used to treat type 2 diabetes. In the United Kingdom it is listed as less preferred than metformin or a sulfonylurea. It is taken by mouth. It is also available in the fixed-dose combination medication sitagliptin/metformin.

<span class="mw-page-title-main">Dipeptidyl peptidase-4</span> Mammalian protein found in Homo sapiens

Dipeptidyl peptidase-4, also known as adenosine deaminase complexing protein 2 or CD26 is a protein that, in humans, is encoded by the DPP4 gene. DPP4 is related to FAP, DPP8, and DPP9. The enzyme was discovered in 1966 by Hopsu-Havu and Glenner, and as a result of various studies on chemism, was called dipeptidyl peptidase IV [DP IV].

<span class="mw-page-title-main">Saxagliptin</span> Chemical compound

Saxagliptin, sold under the brand name Onglyza, is an oral hypoglycemic of the dipeptidyl peptidase-4 (DPP-4) inhibitor class. Early development was solely by Bristol-Myers Squibb; in 2007 AstraZeneca joined with Bristol-Myers Squibb to co-develop the final compound and collaborate on the marketing of the drug.

<span class="mw-page-title-main">Alogliptin</span> Chemical compound

Alogliptin, sold under the brand names Nesina and Vipidia,) is an oral anti-diabetic drug in the DPP-4 inhibitor (gliptin) class. Alogliptin does not decrease the risk of heart attack and stroke. Like other members of the gliptin class, it causes little or no weight gain, exhibits relatively little risk of hypoglycemia, and has relatively modest glucose-lowering activity. Alogliptin and other gliptins are commonly used in combination with metformin in people whose diabetes cannot adequately be controlled with metformin alone.

<span class="mw-page-title-main">Remogliflozin etabonate</span> Chemical compound

Remogliflozin etabonate (INN/USAN) is a drug of the gliflozin class for the treatment of non-alcoholic steatohepatitis ("NASH") and type 2 diabetes. Remogliflozin was discovered by the Japanese company Kissei Pharmaceutical and is currently being developed by BHV Pharma, a wholly owned subsidiary of North Carolina, US-based Avolynt, and Glenmark Pharmaceuticals through a collaboration with BHV. In 2002, GlaxoSmithKline (GSK) received a license to use it. From 2002 to 2009, GSK carried out a significant clinical development program for the treatment of type-2 diabetes mellitus in various nations across the world and obesity in the UK. Remogliflozin etabonate's pharmacokinetics, pharmacodynamics, and clinical dose regimens were characterized in 18 Phase I and 2 Phase II investigations. Due to financial concerns, GSK stopped working on remogliflozin and sergliflozin, two further SGLT2 inhibitors that were licensed to the company, in 2009. Remogliflozin was commercially launched first in India by Glenmark in May 2019.

Dipeptidyl peptidase-4 inhibitors are enzyme inhibitors that inhibit the enzyme dipeptidyl peptidase-4 (DPP-4). They are used in the treatment of type 2 diabetes mellitus. Inhibition of the DPP-4 enzyme prolongs and enhances the activity of incretins that play an important role in insulin secretion and blood glucose control regulation. Type 2 diabetes mellitus is a chronic metabolic disease that results from inability of the β-cells in the pancreas to secrete sufficient amounts of insulin to meet the body's needs. Insulin resistance and increased hepatic glucose production can also play a role by increasing the body's demand for insulin. Current treatments, other than insulin supplementation, are sometimes not sufficient to achieve control and may cause undesirable side effects, such as weight gain and hypoglycemia. In recent years, new drugs have been developed, based on continuing research into the mechanism of insulin production and regulation of the metabolism of sugar in the body. The enzyme DPP-4 has been found to play a significant role.

<span class="mw-page-title-main">Gemigliptin</span> Chemical compound

Gemigliptin (rINN), sold under the brand name Zemiglo, is an oral anti-hyperglycemic agent of the dipeptidyl peptidase-4 inhibitor class of drugs. Glucose lowering effects of DPP-4 inhibitors are mainly mediated by GLP-1 and gastric inhibitory polypeptide (GIP) incretin hormones which are inactivated by DPP-4.

<span class="mw-page-title-main">Anagliptin</span> Chemical compound

Anagliptin is a pharmaceutical drug for the treatment of type 2 diabetes mellitus. It is approved for use in Japan. It belongs to the class of anti-diabetic drugs known as dipeptidyl peptidase-4 inhibitors or "gliptins".

<span class="mw-page-title-main">Teneligliptin</span> Chemical compound

Teneligliptin is a pharmaceutical drug for the treatment of type 2 diabetes mellitus. It belongs to the class of anti-diabetic drugs known as dipeptidyl peptidase-4 inhibitors or "gliptins".

<span class="mw-page-title-main">Trelagliptin</span> Chemical compound

Trelagliptin is a pharmaceutical drug used for the treatment of type 2 diabetes.

<span class="mw-page-title-main">Omarigliptin</span> Chemical compound

Omarigliptin (MK-3102) is a potent, long-acting oral antidiabetic drug of the DPP-4 inhibitor class used for once-weekly treatment of type 2 diabetes and currently under development by Merck & Co. It inhibits DPP-4 to increase incretin levels, which inhibit glucagon release, which in turn increases insulin secretion, decreases gastric emptying and decreases blood glucose levels.

<span class="mw-page-title-main">Evogliptin</span> Chemical compound

Evogliptin is an antidiabetic drug in the dipeptidyl peptidase-4 (DPP-4) inhibitor or "gliptin" class of drugs. It was developed by the South Korean pharmaceutical company Dong-A ST and is approved for use in South Korea and Russia. In a meta-analysis involving data from 6 randomized controlled trials, Dutta et. al. demonstrated the good glycaemic efficacy and safety of this medicine as compared to other DPP4 inhibitors like sitagliptin and linagliptin.

<span class="mw-page-title-main">Fotagliptin</span> Chemical compound

Fotagliptin (SAL067) is a DPP-4 inhibitor under development for the treatment of type 2 diabetes. Like other DPP-4 inhibitors, it works by increasing endogenously produced GLP-1 and GIP. In a phase 3 trial it showed similar results as alogliptin.

<span class="mw-page-title-main">Cofrogliptin</span> Chemical compound

Cofrogliptin is a long-acting DPP4 inhibitor dosed once every two weeks.

<span class="mw-page-title-main">Prusogliptin</span> Chemical compound

Prusogliptin (DBPR108) is an experimental DPP-4 inhibitor developed by CSPC Pharmaceutical Group to treat type 2 diabetes.

<span class="mw-page-title-main">Janagliflozin</span> Chemical compound

Janagliflozin is an experimental SGLT2 inhibitor developed by Sihuan Pharmaceutical.

References

  1. ↑ Ammirati MJ, Andrews KM, Boyer DD, Brodeur AM, Danley DE, Doran SD, Hulin B, Liu S, McPherson RK, Orena SJ, Parker JC, Polivkova J, Qiu X, Soglia CB, Treadway JL, VanVolkenburg MA, Wilder DC, Piotrowski DW (April 2009). "(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. doi:10.1016/j.bmcl.2009.02.041. PMID   19275964.
  2. ↑ Dai H, Gustavson SM, Preston GM, Eskra JD, Calle R, Hirshberg B (2008). "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. doi:10.1111/j.1463-1326.2007.00742.x. PMID   18284437. S2CID   13417601.
  3. ↑ Dai H, Johnson SL, Terra SG, Marbury TC, Smith WB, Alcorn H, Boyd RA, Wang R, Nguyen TT (July 2011). "The pharmacokinetics of PF-734200, a DPP-IV inhibitor, in subjects with renal insufficiency". British Journal of Clinical Pharmacology. 72 (1): 85–91. doi:10.1111/j.1365-2125.2011.03954.x. PMC   3141189 . PMID   21366665.
  4. ↑ Muto C, Dai H, Teeter JG, Johnson S, Cropp AB, Chiba K, Suwa T (2012). "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. doi:10.5414/CP201614. PMID   22541754.
  5. ↑ Rosenstock J, Lewin AJ, Norwood P, Somayaji V, Nguyen TT, Teeter JG, Johnson SL, Dai H, Terra SG (2011). "Efficacy and safety of the dipeptidyl peptidase‐4 inhibitor PF‐734200 added to metformin in Type 2 diabetes". Diabetic Medicine. 28 (4): 464–469. doi:10.1111/j.1464-5491.2010.03181.x. PMID   21392067. S2CID   205550845.
  6. ↑ "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.
  7. ↑ "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.
  8. ↑ "RCSB PDB - 3F8S: Crystal structure of dipeptidyl peptidase IV in complex with inhibitor".
  9. ↑ Sharma R, Sun H, Piotrowski DW, Ryder TF, Doran SD, Dai H, Prakash C (November 2012). "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". Drug Metabolism and Disposition. 40 (11): 2143–2161. doi:10.1124/dmd.112.047316. ISSN   0090-9556. PMID   22896728. S2CID   14277073.
  10. ↑ Lafrance D, Caron S (January 2012). "New Synthetic Route to a Dipeptidyl Peptidase-4 Inhibitor". Organic Process Research & Development. 16 (3): 409–14. doi:10.1021/op200309z.
  11. ↑ Nedosugova LV, Petunina NA, Galstyan KO (2014). "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. doi: 10.14341/DM2014481-86 .
  12. ↑ Galstyan KO, Nedosugova LV, Petunina NA, Trakhtenberg JA, Vostokova NV, Karavaeva OV, Chasovskaya TE (April 2016). "Comparison of the novel Russian DPP-4 inhibitor gosogliptin with vildagliptin in patients with type 2 diabetes mellitus". Diabetes Mellitus. 19 (1): 89‐96. doi: 10.14341/DM7233 .
  13. ↑ "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.
  14. ↑ "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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