Yajima K

References (3)

Title : Efficacy and safety of teneligliptin in addition to insulin therapy in type 2 diabetes mellitus patients on hemodialysis evaluated by continuous glucose monitoring - Yajima_2016_Diabetes.Res.Clin.Pract_122_78
Author(s) : Yajima T , Yajima K , Hayashi M , Takahashi H , Yasuda K
Ref : Diabetes Res Clin Pract , 122 :78 , 2016
Abstract : AIMS: Appropriate glycemic control without hypoglycemia is important in patients with type 2 diabetes on hemodialysis. Teneligliptin, a novel dipeptidyl peptidase-4 inhibitor, can be used without dose adjustment for these patients. Using continuous glucose monitoring (CGM), we evaluated the efficacy and safety of adding teneligliptin to insulin therapy. METHODS: Twenty-one type 2 diabetes mellitus patients on hemodialysis treated with insulin were enrolled. After the adjustment of insulin dose, their blood glucose level was monitored by CGM. Insulin dose was reduced after teneligliptin administration. RESULTS: The median total daily insulin dose significantly reduced from 18 (9-24)U to 6 (0-14)U (p<0.0001). Maximum, mean, and standard deviation of blood glucose level on the hemodialysis and non-hemodialysis days did not change after teneligliptin administration. However, minimum blood glucose level was significantly elevated on the hemodialysis day after teneligliptin administration (from 3.9+/-1.0mmol/L to 4.4+/-0.9mmol/L, p=0.040). The incidence of asymptomatic hypoglycemia on the hemodialysis day detected by CGM significantly decreased from 38.1% to 19.0% (p=0.049). CONCLUSIONS: Teneligliptin may contribute toward reducing the total daily insulin dose and preventing hypoglycemic events on the hemodialysis day in type 2 diabetes mellitus patients.
ESTHER : Yajima_2016_Diabetes.Res.Clin.Pract_122_78
PubMedSearch : Yajima_2016_Diabetes.Res.Clin.Pract_122_78
PubMedID: 27810689

Title : Data on Wistar Hannover rats from a general toxicity study - Yamatoya_2012_Exp.Anim_61_467
Author(s) : Yamatoya H , Kawaguchi H , Yajima K , Kadokura H , Yoshikawa T , Yamashita R , Shiraishi M , Miyamoto A , Miyoshi N
Ref : Exp Anim , 61 :467 , 2012
Abstract : The aim of this study was to collect data on chronological changes in clinical laboratory tests, pathological examinations, and hepatic drug-metabolizing enzymes from Wistar Hannover rats at 8, 10, 19, and 32 weeks of age. The serum triglyceride concentration and the serum LDL cholesterol level were higher in males than in females at all ages. In contrast, serum total protein and creatinine concentrations and cholinesterase activity were lower in males than in females. In addition, sex differences were confirmed in pituitary weight and hepatic CYP3A2 and CYP2C11 activities. In conclusion, the general toxicological data noted in clinical laboratory tests, pathological examinations, and hepatic drug-metabolizing enzymes relating to chronological changes and sex differences may be useful in assessing drug-related toxicity in this strain.
ESTHER : Yamatoya_2012_Exp.Anim_61_467
PubMedSearch : Yamatoya_2012_Exp.Anim_61_467
PubMedID: 22850647

Title : Identification of human cytochrome P450 isoforms and esterases involved in the metabolism of mirabegron, a potent and selective beta(3)-adrenoceptor agonist - Takusagawa_2012_Xenobiotica_42_957
Author(s) : Takusagawa S , Yajima K , Miyashita A , Uehara S , Iwatsubo T , Usui T
Ref : Xenobiotica , 42 :957 , 2012
Abstract : Human cytochrome P450 CYP enzymes and esterases involved in the metabolism of mirabegron a potent and selective human beta(3)-adrenoceptor agonist intended for the treatment of overactive bladder were identified in in vitro studies Incubations of mirabegron with recombinant human CYP enzymes showed significant metabolism of mirabegron by CYP2D6 and CYP3A4 only Correlation analyses showed a significant correlation between mirabegron metabolism and testosterone 6beta-hydroxylation CYP3A4/5 marker activity In inhibition studies using antiserum against CYP3A4 a strong inhibition at maximum 80 inhibition of the metabolism of mirabegron was observed whereas the inhibitory effects of monoclonal antibodies against CYP2D6 were small at maximum 10 inhibition These findings suggest that CYP3A4 is the primary CYP enzyme responsible for in vitro oxidative metabolism of mirabegron with a minor role of CYP2D6 Mirabegron hydrolysis was catalyzed in human blood plasma and butyrylcholinesterase BChE solution but not in human liver microsomes intestinal microsomes liver S9 intestinal S9 and recombinant acetylcholinesterase solution K(m values of mirabegron hydrolysis in human blood plasma and BChE solution were all similar 13.4-15.2 muM The inhibition profiles in human blood and plasma were also similar to those in BChE solution suggesting that mirabegron hydrolysis is catalyzed by BChE.
ESTHER : Takusagawa_2012_Xenobiotica_42_957
PubMedSearch : Takusagawa_2012_Xenobiotica_42_957
PubMedID: 22509825