Delving into the Latest Updates on Ipragliflozin L-Proline with Synapse

The primary purpose of this study is to assess the renal protective effect of ipragliflozin in combination with metformin on the percent change of UACR from baseline to 24 weeks against glimepiride in combination with metformin in type 2 diabetes mellitus patients with albuminuria. The secondary purpose of this study is to assess the efficacy, safety and impact on quality of life (QoL) of ipragliflozin in combination with metformin against glimepiride in combination with metformin in type 2 diabetes mellitus patients with albuminuria.

Start Date25 Apr 2017

Sponsor / Collaborator

Astellas Pharma Korea, Inc.

100 Clinical Results associated with Ipragliflozin L-Proline

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100 Translational Medicine associated with Ipragliflozin L-Proline

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100 Patents (Medical) associated with Ipragliflozin L-Proline

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298

Literatures (Medical) associated with Ipragliflozin L-Proline

01 Oct 2024·Journal of Cardiology

Effects of ipragliflozin on left ventricular diastolic function in patients with type 2 diabetes: A sub-analysis of the PROTECT trial

Article

Author: Ohte, Nobuyuki ; Imai, Takumi ; Node, Koichi ; Sata, Masataka ; Teragawa, Hiroki ; Doi, Masaru ; Yamada, Hirotsugu ; Kadokami, Toshiaki ; Ohishi, Mitsuru ; Kusunose, Kenya ; Fukumoto, Kazuo ; Tanaka, Atsushi ; Koide, Yuji

BACKGROUNDWe hypothesized that the beneficial effects of sodium-glucose cotransporter-2 (SGLT2) inhibitors on diastolic function might depend on baseline left ventricular (LV) systolic function.METHODSTo investigate the effects of SGLT2 inhibitors on LV diastolic function in patients with type 2 diabetes mellitus (T2DM), we conducted a post-hoc sub-study of the PROTECT trial, stratifying the data according to LV ejection fraction (LVEF) at baseline. After excluding patients without echocardiographic data at baseline or 24 months into the PROTECT trial, 31 and 38 patients with T2DM from the full analysis dataset of the PROTECT trial who received ipragliflozin or no SGLT2 inhibitor (control), respectively, were included. The primary endpoint was a comparison of the changes in echocardiographic parameters and N-terminal pro-brain natriuretic peptide levels from baseline to 24 months between the two groups stratified according to baseline LVEF.RESULTSDifferences in diastolic functional parameters (e' and E/e') were noted between the two groups. Among the subgroups defined according to median LVEF values, those with higher LVEF (≥60 %) who received ipragliflozin appeared to have a higher e' and lower E/e' than did those who received the standard of care with no SGLT2 inhibitor, indicating longitudinal improvements between baseline and follow up (p = 0.001 and 0.016, respectively).CONCLUSIONSIpragliflozin generally improved LV diastolic function in patients with type 2 diabetes, the extent of this improvement might appear to vary with LV systolic function.

01 Sep 2024·Journal of Diabetes Investigation

Effect of ipragliflozin in MASLD

Article

Author: Sumita, Takashi ; Yanagisawa, Shinnosuke ; Inoue, Kazuyuki ; Saito, Daigo ; Yanagisawa, Morifumi ; Haisa, Akifumi ; Uchida, Yoshihito ; Shimada, Akira ; Inukai, Kouichi ; Shimizu, Satoshi ; Ito, Daisuke

ABSTRACTAims/IntroductionWe conducted a 5 year post‐trial monitoring study of our previous randomized 24 week, open‐label, active‐controlled trial that showed beneficial effects of ipragliflozin on metabolic dysfunction‐associated steatotic liver disease (MASLD), identical to those of pioglitazone.Materials and MethodsIn our previous trial, 66 patients with MASLD and type 2 diabetes were randomly assigned to receive either ipragliflozin (n = 32) or pioglitazone (n = 34). Upon its conclusion, 61 patients were monitored for 5 years for outcome measures of MASLD, glycemic, and metabolic parameters. Differences between the two groups were analyzed at baseline, 24 weeks, and 5 years; changes in outcome measures from baseline were also evaluated.ResultsAt 5 years, the mean liver‐to‐spleen attenuation ratio increased by 0.20 (from 0.78 ± 0.24 to 0.98 ± 0.20) in the ipragliflozin group and by 0.26 (from 0.76 ± 0.26 to 1.02 ± 0.20) in the pioglitazone group (P = 0.363). Similarly, ipragliflozin and pioglitazone significantly improved serum aminotransferase, HbA1c, and fasting plasma glucose levels over 5 years. In the ipragliflozin group, significant reductions in body weight and visceral fat area observed at 24 weeks were sustained throughout the 5 years (−4.0%, P = 0.0075 and −7.6%, P = 0.045, respectively). Moreover, ipragliflozin significantly reduced the values of fibrosis markers (serum ferritin and FIB‐4 index), was well tolerated, and had a higher continuation rate for 5 years compared with pioglitazone.ConclusionsIpragliflozin and pioglitazone improved MASLD and glycemic parameters over 5 years. In the ipragliflozin group, significant reductions in body weight and visceral fat mass persisted for 5 years.

01 Jul 2024·Diabetes

The Early Pathogenesis of Diabetic Retinopathy and Its Attenuation by Sodium–Glucose Transporter 2 Inhibitors

Article

Author: Yamada, Ken-Ichi ; Yamato, Mayumi ; Kato, Nao ; Inoguchi, Toyoshi

The early pathogenetic mechanism of diabetic retinopathy (DR) and its treatment remain unclear. Therefore, we used streptozotocin-induced diabetic mice to investigate the early pathogenic alterations in DR and the protective effect of sodium–glucose cotransporter 2 (SGLT2) inhibitors against these alterations. Retinal vascular leakage was assessed by dextran fluorescence angiography. Retinal thickness and vascular leakage were increased 2 and 4 weeks after onset of diabetes, respectively. Immunostaining showed that morphological change of microglia (amoeboid form) was observed at 2 weeks. Subsequently, increased angiopoietin-2 expression, simultaneous loss of pericytes and endothelial cells, decreased vessel density, retinal hypoxia, and increased vascular endothelial growth factor (VEGF)-A/VEGF receptor system occurred at 4 weeks. SGLT2 inhibitors (luseogliflozin and ipragliflozin) had a significant protective effect on retinal vascular leakage and retinal thickness at a low dose that did not show glucose-lowering effects. Furthermore, both inhibitors at this dose attenuated microglia morphological changes and these early pathogenic alterations in DR. In vitro study showed both inhibitors attenuated the lipopolysaccharide-induced activation of primary microglia, along with morphological changes toward an inactive form, suggesting the direct inhibitory effect of SGLT2 inhibitors on microglia. In summary, SGLT2 inhibitors may directly prevent early pathogenic mechanisms, thereby potentially playing a role in preventing DR.Article Highlights

100 Deals associated with Ipragliflozin L-Proline

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KEGG	Wiki	ATC	Drug Bank
D10200	Ipragliflozin L-Proline	A10BK05	DB11698

R&D Status

Approved

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 1	JP	-	17 Jan 2014
Diabetes Mellitus, Type 2	JP	-	17 Jan 2014

Developing

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	Phase 1	TW	Astellas Pharma, Inc.	28 Nov 2011
Diabetes Mellitus, Noninsulin-Dependent, 2	Phase 1	JP	Astellas Pharma, Inc.	15 May 2010
Liver Diseases	Phase 1	US	Astellas Pharma, Inc.	01 May 2010
Diabetes Mellitus, Type 2	Discovery	TW	Astellas Pharma, Inc.	28 Nov 2011

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


Suglat-AID (ADA2023)	Not Applicable	Diabetes Mellitus, Type 1	-	Ipragliflozin 50 mg	efbaqncfst(asprrkjope) = fxafaatvrh cnvlcnfgro (dxvehqrijh )	-	20 Jun 2023
UMIN000015170 (EASD2022)	Not Applicable	HbA1c \| BMI \| visceral fat area ... View more	103	Ipragliflozin 50 mg	kavfokrnfy(qovhzzisgm) = bgdgslgwfq rdepeimscv (rgchrquisq )	Positive	20 Sep 2022
				Metformin 1000 mg	kavfokrnfy(qovhzzisgm) = vuqprfrexl rdepeimscv (rgchrquisq )
NCT02479399 (STELLA-LONG TERM, Pubmed)	Not Applicable	Diabetes Mellitus, Type 2 First line	11,412	ipragliflozin (Treatment-naïve patients)	(ybcmhwqrva) = vowtdcfctu uelolvffkn (sjnewezwzj ) View more	-	01 Oct 2021
				ipragliflozin (Non-naïve patients)	(ybcmhwqrva) = emqyaaoagw uelolvffkn (sjnewezwzj ) View more
NISM Study (ADA2021)	Not Applicable	-	87	Ipragliflozin	resaizrivz(hzhdajykvr) = mjgszduxca kgugtphjlu (kmpaxflqne ) View more	-	01 Jun 2021
				Sitagliptin	resaizrivz(hzhdajykvr) = mpnmnbsvkm kgugtphjlu (kmpaxflqne ) View more
NCT02577003 \| NCT02564211 (Pubmed \| Diabetes Obes Metab)	Not Applicable	Diabetes Mellitus, Type 2	-	Ipragliflozin 50 mg	(ezzjbyisrb) = bgpkvuyeft jvizdtxlny (jmnbqvgucc )	-	25 May 2021
NCT02479399 (STELLA-LONG TERM, Pubmed \| Diabetes Ther)	Not Applicable	Diabetes Mellitus, Type 2	11,412	Ipragliflozin in patients aged <65 years	uqsrcskcee(wwwkvtnjjq) = puktmcurpx vrunbqucbj (cndjpgxmbz ) View more	-	17 Mar 2021
				Ipragliflozin in patients aged ≥65 years	uqsrcskcee(wwwkvtnjjq) = wmywgssbjf vrunbqucbj (cndjpgxmbz ) View more
EASL2020	Not Applicable	Fibrosis, Liver \| Nonalcoholic Steatohepatitis hemoglobin A1c \| visceral fat area	-	Ipragliflozin (50 mg/day)	prvrajkxzb(mttxknpxpo) = tpmqhnkpat samgjzyuip (qafvrvuzxu )	Positive	27 Aug 2020
				Active control treatment (excluding SGLT2, pioglitazone, and/or glucagon-like peptide-1 analogs)	prvrajkxzb(mttxknpxpo) = udjqwoyqfk samgjzyuip (qafvrvuzxu )
JPRN-jRCTs031180205 (ADA2020)	Not Applicable	Diabetes Mellitus, Type 2 Second line	-	Ipragliflozin	nrxrakqnkb(kpyylixtnx) = oanvtunkwi bjcgredzbd (usnugjnpxt ) View more	-	01 Jun 2020
				Sitagliptin	nrxrakqnkb(kpyylixtnx) = wtvkwngbvk bjcgredzbd (usnugjnpxt ) View more
NCT01225081 \| NCT01071850 \| NCT01117584 \| NCT00621868 \| NCT01057628 \| NCT01135433 \| NCT01316094 \| NCT02452632 \| NCT01242215 \| NCT02175784 \| NCT01505426 \| NCT02794792 (Pubmed \| Diabetes Ther)	Not Applicable	Diabetes Mellitus, Type 2	-	Ipragliflozin 50 mg	(pvjixozgmw) = kxjesfebce kbdelhcsqw (bhnouigjml ) View more	-	01 Dec 2019
				Placebo	(pvjixozgmw) = ogapglfjwk kbdelhcsqw (bhnouigjml ) View more
NCT02479399 (STELLA-LONG TERM, Pubmed \| Curr Med Res Opin)	Not Applicable	Diabetes Mellitus, Type 2	11,412	ipragliflozin (Non-elderly patients)	(dwidbtdpxk) = fsgzrwdjdx zuuknsmujx (ylnpxwcksk ) View more	-	01 Nov 2019
				ipragliflozin (Elderly patients)	(dwidbtdpxk) = apwfyonpqu zuuknsmujx (ylnpxwcksk ) View more