Pharmacokinetics and Pharmacodynamics of Tofogliflozin (a Selective SGLT2 Inhibitor) in Healthy Male Subjects

Drug Research

Volumn 67, Issue 6, 2017, Pages 349-357

  Kasahara Ito, Nahoko ^a   Fukase, Hiroyuki ^b   Ogama, Yoichiro ^c   Saito, Tomohisa ^a   Ohba, Yasuhiro ^a   Shimada, Sumire ^a   Takano, Yasuki ^a   Ichihara, Tomoko ^d   Terao, Kimio ^a   Nakamichi, Noboru ^e   Kumagai, Yuji ^f   Ikeda, Sachiya ^a  

^a CHUGAI PHARMACEUTICAL CO LTD   (Japan)

^b CPC Clinical Trial Hospital   (Japan)

^c Sumida Hospital   (Japan)

^d Chugai Clinical Research Center Co Ltd   (Japan)

^e Medical Co Shintokai   (Japan)

^f KITASATO UNIVERSITY SCHOOL OF MEDICINE   (Japan)

Author keywords

food effect; healthy male subject; Japanese and Caucasian; tofogliflozin; type 2 diabetes mellitus; urinary glucose excretion

Indexed keywords

ALDOSTERONE; KETONE BODY; RENIN; TOFOGLIFLOZIN; 6-((4-ETHYLPHENYL)METHYL)-3',4',5',6'-TETRAHYDRO-6'-(HYDROXYMETHYL)SPIRO(ISOBENZOFURAN-1(3H),2'-(2H)PYRAN)-3',4',5'-TRIOL; ANTIDIABETIC AGENT; BENZHYDRYL DERIVATIVE; GLUCOSE; GLUCOSIDE; SLC5A2 PROTEIN, HUMAN; SODIUM GLUCOSE COTRANSPORTER 2;

ADULT; AREA UNDER THE CURVE; ARTICLE; BODY MASS; CAUCASIAN; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DOSE ESCALATION; DRUG EXCRETION; DRUG SAFETY; DRUG TOLERABILITY; ELECTROCARDIOGRAPHY; FOOD INTAKE; GLUCOSE URINE LEVEL; HUMAN; HUMAN EXPERIMENT; HYPOGLYCEMIA; JAPANESE (PEOPLE); MALE; NORMAL HUMAN; OPEN STUDY; PHASE 1 CLINICAL TRIAL; RANDOMIZED CONTROLLED TRIAL; SINGLE DRUG DOSE; STEADY STATE; SYSTEMIC CIRCULATION; TIME TO MAXIMUM PLASMA CONCENTRATION; URINARY EXCRETION; ANTAGONISTS AND INHIBITORS; ASIAN CONTINENTAL ANCESTRY GROUP; CLINICAL TRIAL; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; HALF LIFE TIME; JAPAN; METABOLISM; YOUNG ADULT;

ADULT; AREA UNDER CURVE; ASIAN CONTINENTAL ANCESTRY GROUP; BENZHYDRYL COMPOUNDS; DOSE-RESPONSE RELATIONSHIP, DRUG; DOUBLE-BLIND METHOD; EUROPEAN CONTINENTAL ANCESTRY GROUP; GLUCOSE; GLUCOSIDES; HALF-LIFE; HUMANS; HYPOGLYCEMIC AGENTS; JAPAN; MALE; SODIUM-GLUCOSE TRANSPORTER 2; YOUNG ADULT;

EID: 85018818422     PISSN: 21949379     EISSN: 21949387     Source Type: Journal    
DOI: 10.1055/s-0043-104779     Document Type: Article

References (20)

1. Misra M. SGLT2 inhibitors: A promising new therapeutic option for treatment of type 2 diabetes mellitus. J Pharm Pharmacol: 2013; 65 317 327
2. Scheen A. J. Pharmacodynamics, efficacy and safety of sodium-glucose co-transporter type 2 (SGLT2) inhibitors for the treatment of type 2 diabetes mellitus. Drugs: 2015; 75 33 59
3. Suzuki M. Honda K. Fukazawa M. et al Tofogliflozin, a potent and highly specific sodium/glucose cotransporter 2 inhibitor, improves glycemic control in diabetic rats and mice. J Pharmacol Exp Ther: 2012; 341 692 701
4. Kaku K. Watada H. Iwamoto Y. et al Efficacy and safety of monotherapy with the novel sodium/glucose cotransporter-2 inhibitor tofogliflozin in Japanese patients with type 2 diabetes mellitus: A combined Phase 2 and 3 randomized, placebo-controlled, double-blind, parallel-group comparative study. Cardiovasc Diabetol: 2014; 13 65
5. Tanizawa Y. Kaku K. Araki E. et al. Long-term safety and efficacy of tofogliflozin, a selective inhibitor of sodium-glucose cotransporter 2, as monotherapy or in combination with other oral antidiabetic agents in Japanese patients with type 2 diabetes mellitus: Multicenter, open-label, randomized controlled trials. Expert Opin Pharmacother: 2014; 15 749 766
6. Yamane M. Kawashima K. Yamaguchi K. et al. In vitro profiling of the metabolism and drug-drug interaction of tofogliflozin, a potent and highly specific sodium-glucose co-transporter 2 inhibitor, using human liver microsomes, human hepatocytes, and recombinant human CYP. Xenobiotica: 2015; 45 230 238
7. 13 C]tofogliflozin in humans. Clin Pharmacokinet: 2013; 52 463 473
8. Kasahara N. Fukase H. Ohba Y. et al. A pharmacokinetic/pharmacodynamic drug-drug interaction study of tofogliflozin (a new SGLT2 inhibitor) and selected anti-type 2 diabetes mellitus drugs. Drug Res (Stuttg): 2016; 66 74 81
9. World Medical Association. Declaration of Helsinki - Ethical principles for medical research involving human subjects. Available from: http://dl.med.or.jp/dl-med/wma/helsinki2013e.pdf Accessed March 11, 2016
10. U.S. Department of Health and Human Services, Food and Drug Administration. Guidance for Industry: Food-effect bioavailability and fed bioequivalence studies. Available from: http://www.fda.gov/downloads/RegulatoryInformation/Guidances/UCM070241.pdf Accessed March 11, 2016
11. U.S. Department of Health and Human Services, Food and Drug Administration. Guidance for Industry: Safety testing of metabolites. Available from: http://www.fda.gov/OHRMS/DOCKETS/98fr/FDA-2008-D-0065-GDL.pdf Accessed June 24, 2016
12. U.S. Department of Health and Human Services, Food and Drug Administration. Guidance for Industry: Bioanalytical method validation. Available form: http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm070107.pdf Accessed March 11, 2016
13. Zell M. Husser C. Kuhlmann O. et al. Metabolism and mass balance of SGLT2 inhibitor tofogliflozin following oral administration to humans. Xenobiotica: 2014; 44 369 378
14. Tang W. Leil T. A. Johnsson E. et al. Comparison of the pharmacokinetics and pharmacodynamics of dapagliflozin in patients with type 1 versus type 2 diabetes mellitus. Diabetes Obes Metab: 2016; 18 236 240
15. Kasichayanula S. Chang M. Hasegawa M. et al. Pharmacokinetics and pharmacodynamics of dapagliflozin, a novel selective inhibitor of sodium-glucose co-transporter type 2, in Japanese subjects without and with type 2 diabetes mellitus. Diabetes Obes Metab: 2011; 13 357 365
16. Zhang W. Krauwinkel W. J. Keirns J. et al. The effect of moderate hepatic impairment on the pharmacokinetics of ipragliflozin, a novel sodium glucose co-transporter 2 (SGLT2) inhibitor. Clin Drug Investig: 2013; 33 489 496
17. Sasaki T. Seino Y. Fukatsu A. et al. Safety, pharmacokinetics, and pharmacodynamics of single and multiple luseogliflozin dosing in healthy Japanese males: a randomized, single-blind, placebo-controlled trial. Adv Ther: 2014; 31 345 361
18. Devineni D. Vaccaro N. Polidori D. et al. Single- and multiple-dose pharmacokinetics and pharmacodynamics of canagliflozin, a selective inhibitor of sodium glucose co-transporter 2, in healthy participants. Int J. Clin Pharmacol Ther: 2015; 53 129 138
19. Sarashina A. Koiwai K. Seman L. J. et al. Safety, tolerability, pharmacokinetics and pharmacodynamics of single doses of empagliflozin, a sodium glucose cotransporter 2 (SGLT2) inhibitor, in healthy Japanese subjects. Drug Metab Pharmacokinet: 2013; 28 213 219
20. Veltkamp S. A. Kadokura T. Krauwinkel W. J. et al. Effect of ipragliflozin (ASP1941), a novel selective sodium-dependent glucose co-transporter 2 inhibitor, on urinary glucose excretion in healthy subjects. Clin Drug Investig: 2011; 31 839 851