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- Lusefi (luseogliflozin) / Taisho
[VIRTUAL] Luseogliflozin protects pancreatic beta cells via improving mitochondrial metabolism (Poster Hall) - Jul 2, 2020 - Abstract #EASD2020EASD_370;
Relief of glucotoxicity by luseogliflozin may reduce ROS generation and increase gene expression related to beta cell proliferation and maturation, including Nkx6.1. Elevated expressions of these genes represent to improve glucose uptake and metabolism, resulting in protection of beta cells.
- || Jardiance (empagliflozin) / Eli Lilly, Boehringer Ingelheim, Farxiga (dapagliflozin) / Ono Pharma, AstraZeneca
Clinical, Observational data, Journal, Real-World Evidence: Kidney outcomes associated with use of SGLT2 inhibitors in real-world clinical practice (CVD-REAL 3): a multinational observational cohort study. (Pubmed Central) - Jul 2, 2020
In this large, international, real-world study of patients with type 2 diabetes, initiation of SGLT2 inhibitor therapy was associated with a slower rate of kidney function decline and lower risk of major kidney events compared with initiation of other glucose-lowering drugs. These data suggest that the benefits of SGLT2 inhibitors on kidney function identified in clinical trials seem to be largely generalisable to clinical practice.
- || glimepiride / Generic mfg., Lusefi (luseogliflozin) / Taisho, Lucentis (ranibizumab) / Roche, Novartis
Clinical, Journal, Combination therapy: Safety and Efficacy of Ranibizumab and Luseogliflozin Combination Therapy in Patients with Diabetic Macular Edema: Protocol for a Multicenter, Open-Label Randomized Controlled Trial. (Pubmed Central) - Jun 17, 2020
Secondary and exploratory endpoints include safety and ophthalmologic and internal medical clinical parameters. This study is registered at the University Hospital Medical Information Network Clinical Trial Registry (UMIN000033961) and Japan Registry of Clinical Trials (jRCTs031180210).
- | Lusefi (luseogliflozin) / Taisho
Preclinical, Journal: Luseogliflozin attenuates neointimal hyperplasia after wire injury in high-fat diet-fed mice via inhibition of perivascular adipose tissue remodeling. (Pubmed Central) - May 27, 2020
Our present study suggests that luseogliflozin could attenuate neointimal hyperplasia after wire injury in HFD-fed mice partly via suppression of macrophage PDGF-B expression in PVAT. Inhibition of PVAT remodeling by luseogliflozin may be a novel therapeutic target for vascular remodeling after angioplasty.
- Lusefi (luseogliflozin) / Taisho
[VIRTUAL] Anti–Skeletal Muscle Atrophy Effect of Luseogliflozin via Lipidome Modification in db/db Mice () - May 18, 2020 - Abstract #ADA2020ADA_1911;
Stearate acids in blood increased in Db/Db mice, which increased stearate acids in skeletal muscle. Increased stearate acid concentration in skeletal muscle stimulates the expression of scd1, on the other hand, the administration of luseogliflozin decreased stearate acids in blood and skeletal muscle, which decreased the expression of scd1 in skeletal muscle.
- || Lusefi (luseogliflozin) / Taisho
Clinical, Journal: The effect of luseogliflozin and alpha-glucosidase inhibitor on heart failure with preserved ejection fraction in diabetic patients: rationale and design of the MUSCAT-HF randomised controlled trial. (Pubmed Central) - Apr 5, 2020
The results will be submitted for publication in peer-reviewed journals. UMIN000018395.
- Efficacy of Semaglutide by Background Sodium-glucose Co-transporter-2 Inhibitor: a Post Hoc Analysis of SUSTAIN 9 (poster area 3) - Mar 22, 2020 - Abstract #DDG2020DDG_335;
SUSTAIN 9 investigated semaglutide 1.0 mg vs placebo as add-on to a stable dose of sodium – glucose co transporter-2 inhibitor (SGLT-2i) therapy, with or without metformin or a sulfonylurea...In this post hoc analysis, SUSTAIN 9 data were analyzed by background SGLT-2i (empagliflozin, canagliflozin, dapagliflozin or other [ipragliflozin, luseogliflozin and tofogliflozin; drugs available only in Japan])...No diabetic ketoacidosis or lower limb amputation events occurred. In conclusion, in subjects with T2D already receiving an SGLT-2i, semaglutide generally resulted in superior HbA1c and body weight reductions vs placebo, regardless of background SGLT-2i therapy.
- Efficacy of Semaglutide by Background Sodium-Glucose Cotransporter 2 Inhibitor: A Post Hoc Analysis of SUSTAIN 9 () - Feb 2, 2020 - Abstract #QDEM42020QDEM_42;
In this post hoc analysis, SUSTAIN 9 data were analysed by background SGLT2is (empagliflozin, canagliflozin, dapagliflozin or other [ipragliflozin, luseogliflozin and tofogliflozin; drugs available only in Japan])... InsubjectswithT2Dalready receivinganSGLT2i,semaglutide generallyresultedin superior HbA1c and body weightreductions vs. placebo,regardless of background SGLT2i Therapy.
- || Lusefi (luseogliflozin) / Taisho, Januvia (sitagliptin) / Merck (MSD)
Clinical, Journal: The efficacy and safety of luseogliflozin and sitagliptin depending on the sequence of administration in patients with type 2 diabetes mellitus: a randomized controlled pilot study. (Pubmed Central) - Jan 10, 2020
No drug-related adverse events were reported. Over the 24-week period, LS was more effective in reducing HbA1c levels than SL in Japanese T2DM patients.
- Steglatro (ertugliflozin) / Pfizer, Merck (MSD), Jardiance (empagliflozin) / Eli Lilly, Boehringer Ingelheim, Farxiga (dapagliflozin) / Ono Pharma, AstraZeneca
Use of SGLT-2 inhibitors in patients with T2DM and kidney disease: An Asian perspective and expert recommendations (Poster Area) - Nov 20, 2019 - Abstract #IDF2019IDF_1347;
Given its consistent benefits on the CV and renal outcomes, SGLT-2i represent an essential therapy for the management of Asian T2DM patients with kidney or CV disease or those with multiple risk factors. Based on the currently available evidence and experts’ clinical opinion, a series of recommendations have been developed for the use of SGLT-2i in this population.
- | Lusefi (luseogliflozin) / Taisho
Preclinical, Journal: Effect of the sodium-glucose cotransporter 2 inhibitor luseogliflozin on pancreatic beta cell mass in db/db mice of different ages. (Pubmed Central) - Oct 31, 2019
Luseogliflozin preserved beta cell mass in db/db mice. The protective effect was more evident in the earlier phase of diabetes.
- | Lusefi (luseogliflozin) / Taisho
Clinical, PK/PD data, Journal: Pharmacokinetics and Pharmacodynamics of Luseogliflozin, a Selective SGLT2 Inhibitor, in Japanese Patients With Type 2 Diabetes With Mild to Severe Renal Impairment. (Pubmed Central) - Oct 29, 2019
No clear trends were observed between eGFR and incidence, type, or severity of adverse events. Thus, luseogliflozin administration should be carefully considered, as patients with renal impairment may show an insufficient response to treatment.
- Lusefi (luseogliflozin) / Taisho
Clarification of the Mechanism of Acute GFR Change by SGLT2 Inhibition with In Vivo Imaging Technique (Exhibit Hall, Walter E. Washington Convention Center) - Oct 14, 2019 - Abstract #KIDNEYWEEK2019KIDNEY_WEEK_2701;
Both rats were divided to the following groups; luseogliflozin (10mg/kg, gavage) group, luseogliflozin + adenosine A1 receptor (A1aR) antagonist (8-cyclopentyl-1,3-dipropylxanthine, 1mg/kg) group, and insulin group...The A1aR-antagonist group showed similar urinary excretion pattern, but initial decline of SNGFR was not observed. Conclusion Adenosine/ A1aR pathways play an important role in the regulation of GFR and is involved in the acute decline of GFR by SGLT2i treatment.
- Lusefi (luseogliflozin) / Taisho
Acute Changes in Estimated Glomerular Filtration Rate and Related Factors and Subsequent Renal Function in Type 2 Diabetes Mellitus After Initiating Luseogliflozin (Exhibit Hall, Walter E. Washington Convention Center) - Oct 14, 2019 - Abstract #KIDNEYWEEK2019KIDNEY_WEEK_2665;
State of basal glomerular filtration rate and interaction of diuretics may relate to acute changes in eGFR after initiating SGLT2 inhibitor. Funding Commercial Support
- | Lusefi (luseogliflozin) / Taisho
Clinical, Journal: Efficacy and safety of luseogliflozin added to insulin therapy in Japanese patients with type 2 diabetes: a multicenter, 52-week, clinical study with a 16-week, double-blind period and a 36-week, open-label period. (Pubmed Central) - Sep 12, 2019
Funding Commercial Support Luseogliflozin added to insulin therapy significantly improved glycemic control with bodyweight reduction and was well tolerated in Japanese patients with T2D.
- Jardiance (empagliflozin) / Eli Lilly, Boehringer Ingelheim
Sodium-Glucose Cotransporter 2 Inhibitors Reduce Residual Cardiovascular Risk in Heart Failure With Preserved Ejection Fraction (Zone 2, Science and Technology Hall) - Aug 21, 2019 - Abstract #AHA2019AHA_2590;
We selected T2DM subjects with HFpEF; 201 received empagliflozin, canagliflozin, luseogliflozin, or tofogliflozin (SGLT2i), and 198 did not (non-SGLT2i). These findings showed that SGLT2i treatment can reduce the potential impact of TG-rich lipoproteins on residual risk and suggest potential applications in pharmacological targeting of HFpEF by reducing TG-rich lipoproteins, perhaps through nitric oxide production from lower insulin resistance.
- | Jardiance (empagliflozin) / Eli Lilly, Boehringer Ingelheim
Clinical, Journal: Lower Cardiovascular Risk Associated with SGLT-2i in >400,000 Patients: The CVD-REAL 2 Study. (Pubmed Central) - Aug 15, 2019
P=N/A
These findings showed that SGLT2i treatment can reduce the potential impact of TG-rich lipoproteins on residual risk and suggest potential applications in pharmacological targeting of HFpEF by reducing TG-rich lipoproteins, perhaps through nitric oxide production from lower insulin resistance. In this large, international study of patients with T2D from the Asia-Pacific, Middle East and North America, initiation of SGLT-2i was associated with a lower risk of CV events, across a broad range of outcomes and patient characteristics.
- | Lusefi (luseogliflozin) / Taisho
Journal: The sodium-glucose cotransporter 2 inhibitor luseogliflozin can suppress muscle atrophy in Db/Db mice by suppressing the expression of foxo1. (Pubmed Central) - Aug 6, 2019
The fluorescence intensity of foxo1 in the Db/Db mice fed SGLT-2i was significantly lower than that in the Db/Db mice without SGLT-2i. The administration of luseogliflozin resulted in the suppression of both the increased foxo1 expression and the reduced muscle cross-sectional area in the soleus muscle of Db/Db mice.
- | Lusefi (luseogliflozin) / Taisho, Sutent (sunitinib) / Pfizer
Preclinical, Journal: A sodium-glucose transporter 2 inhibitor attenuates renal capillary injury and fibrosis by a vascular endothelial growth factor-dependent pathway after renal injury in mice. (Pubmed Central) - Jun 7, 2019
Withdrawal of glucose from cultured medium, to halt glucose uptake, remarkably increased VEGF-A expression and reversed the luseogliflozin-induced increase in VEGF-A expression in the proximal tubular cells. Thus, luseogliflozin prevented endothelial rarefaction and subsequent renal fibrosis after renal ischemia/reperfusion injury through a VEGF-dependent pathway induced by the dysfunction of proximal tubular glucose uptake in tubules with injury-induced GLUT2 downregulation.
- | Lusefi (luseogliflozin) / Taisho
Clinical, Journal: Correction: The effect of luseogliflozin and alpha-glucosidase inhibitor on heart failure with preserved ejection fraction in diabetic patients: rationale and design of the MUSCAT-HF randomised controlled trial. (Pubmed Central) - Jun 4, 2019
Thus, luseogliflozin prevented endothelial rarefaction and subsequent renal fibrosis after renal ischemia/reperfusion injury through a VEGF-dependent pathway induced by the dysfunction of proximal tubular glucose uptake in tubules with injury-induced GLUT2 downregulation. No abstract available
- | Lusefi (luseogliflozin) / Taisho
Journal: Responses of renal hemodynamics and tubular functions to acute sodium-glucose cotransporter 2 inhibitor administration in non-diabetic anesthetized rats. (Pubmed Central) - Apr 19, 2019
Luseogliflozin did not elicit any significant effects on the other urinary parameters in Nx SD rats. These data indicate that SGLT2 inhibitor elicits direct tubular effects in non-diabetic rats with normal renal functions.
- | Clinical, Journal: Effects of Concomitant Administration of a Dipeptidyl Peptidase-4 Inhibitor in Japanese Patients with Type 2 Diabetes Showing Relatively Good Glycemic Control Under Treatment with a Sodium Glucose Co-Transporter 2 Inhibitor. (Pubmed Central) - Apr 7, 2019
Then, the therapeutic responses to concurrent administration with SGLT2 inhibitor of each of the 5 individual DPP-4 inhibitors used in this study were analyzed. The results showed that concomitant administration of sitagliptin, a DPP-4 inhibitor, with the SGLT2 inhibitor yielded the best results in terms of the lowering of the HbA1c and improvement of the serum lipid profile.
- Lusefi (luseogliflozin) / Taisho
Trial completion: The Clinical Study to Assess the Effect of the Amount of Carbohydrate Intake and Meals Differing in Glycemic Index (GI) in Patients Treated With a Sodium-dependent Glucose Cotransporter 2 (SGLT2) Inhibitor (clinicaltrials.gov) - Sep 1, 2016
P=N/A, N=24, Completed, Sponsor: Kansai Electric Power Hospital
The results showed that concomitant administration of sitagliptin, a DPP-4 inhibitor, with the SGLT2 inhibitor yielded the best results in terms of the lowering of the HbA1c and improvement of the serum lipid profile. Active, not recruiting --> Completed
- | Apleway (tofogliflozin) / Kowa, Takeda, Tradjenta (linagliptin) / Boehringer Ingelheim, Eli Lilly, Lusefi (luseogliflozin) / Taisho
New P4 trial: Metabolic and Cardiovascular Effects of Dipeptidyl Peptidase-4 (DPP-4) or Sodium-glucose Co-transporter Type 2 (SGLT2) Inhibitors (clinicaltrials.gov) - Aug 19, 2015
P4, N=100, Recruiting, Sponsor: Kurume University
- Lusefi (luseogliflozin) / Taisho
New trial: The Clinical Study to Assess the Effect of the Amount of Carbohydrate Intake and Meals Differing in Glycemic Index (GI) in Patients Treated With a Sodium-dependent Glucose Cotransporter 2 (SGLT2) Inhibitor (clinicaltrials.gov) - Jul 16, 2015
P=N/A, N=24, Active, not recruiting, Sponsor: Kansai Electric Power Hospital