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-

License Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (24 Mar 2014),

Diabetes Mellitus, Type 2

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC23H30O6S

InChIKeyWHSOLWOTCHFFBK-ZQGJOIPISA-N

CAS Registry898537-18-3

AbstractAimsAnti‐vascular endothelial growth factor (VEGF) therapy is the standard treatment for diabetic macular oedema (DMO); however, unmet needs remain. This study aimed to assess the effectiveness of sodium‐glucose cotransporter 2 inhibitors (SGLT2i) in treating DMO.Materials and MethodsThis multicentre randomised open‐label trial included 60 patients with DMO who were eligible for anti‐VEGF therapy. Patients were randomised to receive luseogliflozin or glimepiride. Ranibizumab was administered initially to the target eye, with additional doses per protocol. The number of ranibizumab doses up to week 48, and re‐admission rates were evaluated. Fellow eye injections were also assessed.ResultsSixty participants, mostly with diabetic retinopathy and half previously treated with anti‐VEGF therapy, were included. SGLT2i and sulfonylurea (SU) groups achieved equivalent glycated haemoglobin, central retinal thickness (CRT), and best‐corrected visual acuity improvements. Injection frequency for the target eye was similar between groups (SGLT2i vs. SU: 3.9 ± 0.7 vs. 4.7 ± 0.7 times, p = 0.36). Re‐administration rates were decreased significantly after the fourth injection in the SGLT2i group (p = 0.030, hazard ratio: 0.45, 95% confidence interval: 0.22–0.92). Fellow eyes in the SGLT2i group showed significant CRT reduction and fewer injections compared with those in the SU group (1.3 ± 0.6 vs. 3.4 ± 0.8, p = 0.016).ConclusionsAlthough the overall number of anti‐VEGF injections in the target eye showed no significant difference, some patients responded favourably to SGLT2i and required fewer injections. The reduction in fellow eye injections suggests SGLT2i's efficacy in treating early‐stage DMO.Trial RegistrationUniversity Hospital Medical Information Network Clinical Trial Registry (UMIN000033961); Japan Registry of Clinical Trials (jRCTs031180210).

04 Feb 2025·Cureus

Luseogliflozin Persistently Lowers Glycemia and Body Weight Over a Period of Two Years in Patients With Type 2 Diabetes

Article

Author: Yamashita, Koh ; Aizawa, Toru ; Mori, Jun-Ichirou

INTRODUCTIONSodium-glucose co-transporter-2 inhibitor (SGLT2i) was introduced as an oral hypoglycemic agent. Thereafter, it was revealed that SGLT2i had multifaced effects, such as renal function and heart failure. Luseogliflozin is one of the SGLT2i. However, the long-term effects of luseogliflozin on glycemic control, body weight, and body mass index have not yet been established.AIMSThis study aimed to determine the long-term effects of luseogliflozin, an SGLT2i, on plasma glucose (PG), body weight (BW), body mass index (BMI), and blood pressure (BP) in patients with type 2 diabetes.METHODSLuseogliflozin was administered continuously in an outpatient clinic for at least two years to 35 SGLT2i-naive patients. Random plasma glucose (RPG), hemoglobin A1c (HbA1c) level, BW, BMI, and BP were measured every six months.RESULTSAt baseline, the patients had a median age of 63 years and a median diabetes duration of seven years. The mean RPG levels at the initiation of luseogliflozin and after 1 and 2 years were 213.5, 155.7, and 164.4 mg/dL, respectively. The reductions from baseline at both 1 year (p<0.001) and 2 years (p=0.012) were statistically significant. Compared with the baseline, the mean HbA1c level significantly decreased by 0.98% after 1 year (p<0.001) and by 1.08% after 2 years (p<0.001), respectively. The mean BMI significantly decreased from 27.41 kg/m² at baseline to 26.53 kg/m² after 1 year (p<0.001) and 26.37 kg/m² after 2 years (p<0.001). Systolic/diastolic blood pressure, initially (138.2/79.2 mmHg), was reduced to 132.9/74.5 mmHg after 1 year, with statistically significant declines in both systolic (p=0.035) and diastolic (p=0.016) pressure compared to baseline.CONCLUSIONSThe effects of luseogliflozin on glucose and BW reduction were sustained for at least two years, indicating similarity to other SGLT2 inhibitors.

31 Dec 2024·Drug Discoveries & Therapeutics

Long-term renoprotective effect of luseogliflozin in type 2 diabetes patients: CHikushi Anti-diabetes mellitus Trial-Lusefi (CHAT-Lu)

Article

Author: Imanaga, Chiyori ; Urata, Hidenori ; Kawamura, Akira ; Abe, Ichiro ; Takamiya, Yosuke ; Ike, Amane ; Kobayashi, Kunihisa

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.

100 Deals associated with Luseogliflozin Hydrate

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D10195	Luseogliflozin Hydrate	A10BH	DB12214

R&D Status

10 top approved records.

Login

to view more data

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

Login to view more data

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	ktngtzgnkc(hezuuejeja) = ekxnxkixde fwisbfycxf (aqrnfydnsx )	Positive	30 Sep 2021
				DPP-4i	ktngtzgnkc(hezuuejeja) = ehvuwuxlhm fwisbfycxf (aqrnfydnsx ) View more
EASD2020	Not Applicable	Insulinoma	-	Luseogliflozin 0.01%	eknwqgtjny(rvgaqurzkc) = hsujzypajd eootqyggdp (ggzllycjyt ) View more	-	22 Sep 2020
				Luseogliflozin (Standard Chow)	upbuoismbg(uhmrafaovr) = dfpqbbnqen fvllpekmdf (rwjvdgzmbr )
ASN2019	Phase 3	Diabetes Mellitus, Type 2	941	Luseogliflozin 2.5 mg daily	(knjndpvdbj) = ubgxaumejy jpfsrdstsa (iejpknzzyy )	Positive	05 Nov 2019
ISC2018	Not Applicable	Hyperglycemia	-	Luseogliflozin 2.5mg	poxebbpejk(unvdowiuwy) = umedbqgzni iewipdiidw (fwfbqxtmib )	-	22 Jan 2018
EASD2016	Not Applicable	Insulinoma	6	Luseogliflozin	xshrkmwfsg(ddqyxkfzde) = elevated relative to Controls jnxnyucska (yznqfbnokj ) View more	Positive	13 Sep 2016
				luseogliflozin (Control group)
EASD2015	Not Applicable	Fatty Liver	16	Luseogliflozin	(dwakdvfqjp) = mxilfsnhgi ddiuezbmzc (jpwrhxxkok, 58.8 - 76.2) View more	Positive	17 Sep 2015
				Sitagliptin	(dwakdvfqjp) = zlgtvwevnj ddiuezbmzc (jpwrhxxkok, 59.6 - 76.3) View more
JPRN-JapicCTI-111507 (EASD2013)	Not Applicable	Diabetes Mellitus, Type 2 Add-on	221	Luseogliflozin 2.5 mg	(nwhrtxuork) = 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. glmlnlhbmx (ghjbhwlkua )	Positive	26 Sep 2013
JPRN-JapicCTI-111661 \| JPRN-JapicCTI-111509 (EASD2013)	Phase 3	Diabetes Mellitus, Type 2	-	Luseogliflozin 2.5 mg	(gdjiajzcgl) = 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. wadrxwkaok (lswnoqmcku )	Positive	25 Sep 2013
JPRN-JapicCTI-111508 (EASD2013)	Phase 3	Diabetes Mellitus, Type 2 Add-on	487	Luseogliflozin 2.5 mg	gugcccgsxi(efmdkpogaf) = observed in all groups, but most of these events were mild in severity zvotpalsjl (butdlhygfw ) View more	Positive	25 Sep 2013
				Luseogliflozin 5 mg