Delving into the Latest Updates on Luseogliflozin Hydrate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Luseogliflozin, Luseogliflozin hydrate (JAN)

+ [3]

Target

SGLT2

Action

inhibitors

Mechanism

SGLT2 inhibitors(Sodium/glucose cotransporter 2 inhibitors)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Diabetes Mellitus, Type 2

Inactive Indication-

Originator Organization

Taisho Pharmaceutical Co., Ltd.

Active Organization

Taisho Pharmaceutical Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (24 Mar 2014),

Diabetes Mellitus, Type 2

Regulation-

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Structure/Sequence

Molecular FormulaC23H30O6S

InChIKeyWHSOLWOTCHFFBK-ZQGJOIPISA-N

CAS Registry898537-18-3

Several sodium-glucose cotransporter 2 (SGLT2) inhibitors are known to have beneficial effects on renal function in patients with type 2 diabetes. However, the long-term effects of luseogliflozin, an SGLT2 inhibitor, remain uncertain in real-world settings. This multicenter, open-label, prospective observational study evaluated the long-term effects of luseogliflozin on renal function in Japanese patients with type 2 diabetes. Fifty-four outpatients initiated on luseogliflozin at Fukuoka University Chikushi Hospital or associated clinics were enrolled from April 2018 to December 2019, with 46 patients included in the final analysis set. The primary outcome was the change in estimated glomerular filtration rate (eGFR) from baseline to 104 weeks, and secondary outcomes included the change in eGFR at week 52 and changes in body weight and blood and urinary parameters at 52 and 104 weeks. The mean duration of diabetes was 8.1 years. Baseline eGFR was 75.8 ± 17.4 mL/min/1.73m², and no decline in eGFR was observed from baseline to 104 weeks. Decline in eGFR was suppressed in the two groups stratified by baseline eGFR (< 60 and ≥ 60 mL/min/1.73m²). No changes were noted in urinary albumin excretion rate. Blood glucose, body weight, blood pressure, liver function, and uric acid levels showed significant improvements. There were four adverse events, but no serious adverse events closely related to luseogliflozin treatment. In type 2 diabetes patients, 2-year treatment with luseogliflozin provided beneficial metabolic effects and improved the rate of decline in eGFR, suggesting a renal protective effect.

01 Dec 2024·European Journal of Internal Medicine

Sodium–Glucose Co-transporter 2 Inhibitors treatment improve pancreatic β-cells function and insulin resistance in patients with Type 2 diabetes

Letter

Author: Shi, Fang-Hong ; Li, Hao ; Xu, Li ; Cao, Min-Jia ; Shen, Long

This study is about Sodium Glucose Co-transporter 2 Inhibitors treatment improve pancreatic β -cells function and insulin resistance in patients with Type 2 diabetes .Diabetes is a leading cause of death and disability .Approx., more than 1.31 billion people will have diabetes by 2050 .Insulin resistance in target tissues and insufficient insulin secretion from pancreatic β -cell are the main characteristics of type 2 diabetes mellitus (T2DM) .Prolonged exposure to hyperglycemia induces insulin biosynthesis and secretion, resulting in the deterioration of β -cell function, known as β -cell glucose toxicity.Sodium-glucose co-transporter 2 (SGLT2) inhibitors are highly recommended in clin. setting because they safely lower blood glucose levels by enhancing urinary glucose excretion in an insulin-independent manner.Thirty-two RCTs were included in the quant. synthesis, involving 9157 adults, with 6132 receiving SGLT2 inhibitors and 3025 receiving non-SGLT2 inhibitor treatments.Seven SGLT2 inhibitors, canagliflozin, dapaglflozin, empagliflozin, ertugliflozin, lusegliflozin, ipragliflozin, and tofogliflozin were included in this meta-anal.Thus, this meta-anal. results suggested that empagliflozin treatment did not significantly improve insulin resistance; however, this does not mean that empagliflozin has no effect on improving insulin resistance.The control group included other hypoglycemic drugs that may have weakened the effect of SGLT2 inhibitors on β -cell function.In conclusion, our study suggests that SGLT2 inhibitors improve insulin sensitivity and resistance in patients with T2DM, as evidenced by a significant increase in HOMA- β levels and decrease in HOMA-IR levels.This study highlights a possible strategy in which SGLT2 inhibitors may be a good choice for patients with high insulin resistance as insulin sensitizers after metformin and pioglitazone treatment.SGLT2 inhibitor treatment should be administered to these patients for at least 24 wk.

01 Nov 2024·In Vivo

Retrospective Analysis of Factors Influencing the Hemoglobin Level-increasing Effect of Sodium-glucose Co-transporter-2 Inhibitors

Article

Author: YOSHIDA, YUKI ; Yamada, Harumi ; Sato, Junya ; Yoshida, Yuki ; SATO, JUNYA ; YAMADA, HARUMI

BACKGROUND/AIMIn several studies, Sodium-glucose co-transporter-2 inhibitors (SGLT2i) have been reported to increase hemoglobin (Hb) levels. In a study in which Hb levels were compared between patients who received SGLT2i and dipeptidyl peptidase-4 inhibitors, some patients exhibited increased Hb levels (>1.0 g/dl), whereas some exhibited unchanged Hb levels. Notably, several factors may influence the Hb-increasing effect of SGLT2i. This study aimed to analyze the factors influencing the Hb-increasing effect of SGLT2i.PATIENTS AND METHODSType 2 diabetes patients were divided into three groups: SGLT2i (SGLT2i only group, n=36), those receiving a combination of SGLT2i and angiotensin-converting enzyme inhibitors (ACEi) or angiotensin receptor blockers (ARBs) (SGLT2i+ACEi/ARBs group, n=32), and those not receiving these drugs (control group, n=49). We retrospectively analyzed Hb changes in these groups. Kaplan-Meier curves compared Hb changes from SGLT2i initiation to day 63, with an Hb increase defined as ≥0.5 g/dl. In addition, sex, age, ACEi/ARBs, estimated glomerular filtration rate, and hematocrit levels were analyzed using Cox proportional hazards as factors influencing Hb-increasing events.RESULTSHb-increasing event rates were 61%, 41%, and 20% in the SGLT2i only, SGLT2i+ACEi/ARBs, and control groups, respectively. The Kaplan-Meier curves showed significantly higher Hb-increasing event rates in the SGLT2i only group than in the control and SGLT2i+ACEi/ARBs groups. In the Cox proportional hazards model, ACEi/ARBs use was associated with a 39% reduction in the incidence of Hb-increasing events.CONCLUSIONSGLT2i exhibit a Hb-increasing effect, which may be reduced by ACEi/ARBs.

100 Deals associated with Luseogliflozin Hydrate

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External Link

KEGG	Wiki	ATC	Drug Bank
D10195	Luseogliflozin Hydrate	A10BH	DB12214

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	Japan	Taisho Pharmaceutical Co., Ltd.	24 Mar 2014

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Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


JPRN-jRCTs011180019 \| JPRN-UMIN000031451 (EASD2021)	Phase 4	Diabetes Mellitus, Type 2 \| Hypertension	56	Luseogliflozin 2.5 mg/day	midrznhsri(kenedendeh) = jrzfxlpkta pwhkibiknk (tmmumdjxfv )	Positive	30 Sep 2021
				DPP-4i	midrznhsri(kenedendeh) = tdcusxneoc pwhkibiknk (tmmumdjxfv ) View more
EASD2020	Not Applicable	Insulinoma	-	Luseogliflozin 0.01%	esawudsoar(pnlfmiyilp) = grmdnlbpgo yhdriocenu (ntjpaqxweq ) View more	-	22 Sep 2020
				Luseogliflozin (Standard Chow)	oshbvymffo(rwsqkujdzk) = ppclsegboo jrvdblhycn (plkyldherv )
ASN2019	Phase 3	Diabetes Mellitus, Type 2	941	Luseogliflozin 2.5 mg daily	(vvmlcxveql) = wqcnncfddh kbvcaakxsa (auclgtfzql )	Positive	05 Nov 2019
ISC2018	Not Applicable	Hyperglycemia	-	Luseogliflozin 2.5mg	crpephgxts(qcetfgvwnc) = custiptebv ufusqqhcto (mtoiibrnkn )	-	22 Jan 2018
EASD2016	Not Applicable	Insulinoma	6	Luseogliflozin	jurxiwimgc(ckuvcxbcaq) = elevated relative to Controls ofvbaclnuu (trkctuzhtn ) View more	Positive	13 Sep 2016
				luseogliflozin (Control group)
EASD2015	Not Applicable	Fatty Liver	16	Luseogliflozin	(pnjliixkau) = pzxusfxync nhqcalcfvi (nnoduauhth, 58.8 - 76.2) View more	Positive	17 Sep 2015
				Sitagliptin	(pnjliixkau) = eqexfdykti nhqcalcfvi (nnoduauhth, 59.6 - 76.3) View more
JPRN-JapicCTI-111507 (EASD2013)	Not Applicable	Diabetes Mellitus, Type 2 Add-on	221	Luseogliflozin 2.5 mg	(fqabwllyab) = Incidence of hypoglycemia with patients who received luseogliflozin for 52 weeks was 10.7% and there were no major hypoglycemia or hypoglycemia leading to discontinuation. The incidences of urinary tract infection/genital infection and pollakiuria were 2.7% and 2.8%, and every event was mild in severity. suubhklokn (sasjsauely )	Positive	26 Sep 2013
JPRN-JapicCTI-111661 \| JPRN-JapicCTI-111509 (EASD2013)	Phase 3	Diabetes Mellitus, Type 2	-	Luseogliflozin 2.5 mg	(cxiekaengg) = Frequencies of adverse events were similar across groups (Luseogliflozin 2.5mg, 59.5%; placebo, 57.0%) in Study-1 and 75.3% in Study-2. Most adverse events were mild in severity. There were no major changes in clinical laboratory tests. Luseogliflozin was well tolerated throughout both studies. wvyehzhxgf (aptzckibjx )	Positive	25 Sep 2013
JPRN-JapicCTI-111508 (EASD2013)	Phase 3	Diabetes Mellitus, Type 2 Add-on	487	Luseogliflozin 2.5 mg	qvsakpjtth(bffntfgoht) = observed in all groups, but most of these events were mild in severity wmwdjcsjiz (yrwtysjmak ) View more	Positive	25 Sep 2013
				Luseogliflozin 5 mg