Delving into the Latest Updates on Tofogliflozin Hydrate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Tofogliflozin, Tofogliflozin (USAN), Tofogliflozin anhydrous

+ [10]

Target

SGLT2

Mechanism

SGLT2 inhibitors(Sodium/glucose cotransporter 2 inhibitors)

Therapeutic Areas

Endocrinology and Metabolic DiseaseDigestive System DisordersUrogenital Diseases+ [1]

Active Indication

Diabetes Mellitus, Type 2Fibrosis, LiverNonalcoholic Steatohepatitis+ [1]

Inactive Indication-

Originator Organization

Chugai Pharmaceutical Co., Ltd.

Active Organization

Kowa Co., Ltd.Kowa Research Institute, Inc.

Inactive Organization

Hoffmann-La Roche, Inc.

Drug Highest PhaseApproved

First Approval Date

JP (24 Mar 2014),

Diabetes Mellitus, Type 2

Regulation-

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Structure

Molecular FormulaC22H26O6

InChIKeyVWVKUNOPTJGDOB-BDHVOXNPSA-N

CAS Registry903565-83-3

View All Structures (2)

A Randomized, Open-Label, Six-Sequence, Three-Period Crossover Study to Demonstrate the Bioequivalence of Single Oral Administration of K-001 Relative to Single Oral Coadministration of Separate Tablets of K-877-ER Plus CSG452 in Healthy Adult Volunteers, and to Characterize the Food Effect on the Pharmacokinetics of K-001

The goal of this clinical trial is to demonstrate the bioequivalence of single oral administration of K-001 relative to single oral co-administration of separate tablets of K-877-ER and CSG452 in healthy adult volunteers, and to characterize the food effect on the Pharmacokinetics(PK) of K-001.

Start Date24 Feb 2023

Sponsor / Collaborator

Kowa Research Institute, Inc.

JPRN-jRCTs051220140 / RecruitingNot ApplicableIIT

The effect of tofogliflozin on cardiac structure focusing on myocardial fibrosis in type 2 diabetes patients with nonalcoholic fatty liver disease at risk for heart failure

Start Date23 Dec 2022

Sponsor / Collaborator-

JPRN-UMIN000049753 / RecruitingNot ApplicableIIT

A study to verify the efficacy of the selective SGLT2 inhibitor tofogliflozin hydrate in reducing nocturia - The VESTITO Study

Start Date19 Dec 2022

Sponsor / Collaborator-

100 Clinical Results associated with Tofogliflozin Hydrate

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100 Translational Medicine associated with Tofogliflozin Hydrate

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100 Patents (Medical) associated with Tofogliflozin Hydrate

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167

Literatures (Medical) associated with Tofogliflozin Hydrate

01 Nov 2024·Journal of Diabetes Investigation

Safety and effectiveness of tofogliflozin in Japanese people with type 2 diabetes: A multicenter prospective observational study in routine clinical practice

Article

Author: Yabe, Daisuke ; Yamada, Yuichiro ; Seino, Yutaka ; Suzuki, Atsushi ; Terauchi, Yasuo ; Sato, Yasunori ; Shihara, Nobuyuki ; Shide, Kenichiro

ABSTRACTAims/IntroductionSodium–glucose cotransporter 2 (SGLT2) inhibitors effectively and safely reduce fasting and postprandial hyperglycemia while promoting weight loss. However, their unique mechanism of action contributes to concerns regarding their safety. We therefore carried out a large‐scale, non‐commercial, investigator‐initiated study on the safety and effectiveness of the SGLT2 inhibitor tofogliflozin.Materials and MethodsThis multicenter, open‐label, uncontrolled, prospective observational study was carried out at hospitals and clinics across Japan in participants aged ≥20 years who were SGLT2 inhibitor‐naïve and had an established diagnosis of type 2 diabetes. The primary endpoint was adverse drug reactions (ADRs) of special interest. Secondary endpoints included all other ADRs and adverse events, glycated hemoglobin (HbA1c), and weight loss.ResultsThe study, carried out from June 2014 through February 2020, enrolled 11,480 participants from 1,103 medical institutions; 6,967 participants completed the 104‐week follow up. The most common ADRs of special interest were urinary and genital tract infections (1.53%), followed by volume depletion (1.25%). Hypoglycemia occurred in 27 participants (0.24%), adverse events in 1,054 (9.18%) and ADRs in 645 (5.62%). HbA1c decreased by 0.85% (95% confidence interval 0.82%–0.88%) and bodyweight decreased by 3.05 kg (95% confidence interval 2.94–3.17 kg). The HbA1c target was achieved by 51.70% of participants for target HbA1c <7.0%, 85.3% for <8.0% and 5.4% for <6.0% at week 104.ConclusionsTofogliflozin was associated with only mild or moderate ADRs characteristic of SGLT2 inhibitors, with no unpredictable, new, serious, or high‐incidence adverse events or ADRs. This independent study confirmed the safety and effectiveness of tofogliflozin in adult type 2 diabetes patients.

09 Aug 2024·Medicine

Effects of 6-month administration of tofogliflozin on cardiac function in elderly patients with heart failure with preserved ejection fraction: A retrospective study of a patient cohort

Article

Author: Nakahashi, Takeshi ; Ishigami, Keiichirou ; Kiyosawa, Jun ; Kasamaki, Yuji ; Higashikawa, Toshihiro ; Haraguchi, Takatoshi ; Iguchi, Masaharu ; Kuroki, Kengo ; Okuro, Masashi ; Yamada, Shinya ; Kanda, Tsugiyasu ; Sangen, Ryusho ; Fukuda, Akihiro ; Mizuno, Takuro ; Saito, Atsushi ; Ito, Tomohiko

Patients with type 2 diabetes mellitus are frequently hospitalized for heart failure. The ratio of early diastolic mitral inflow velocity to early diastolic mitral annulus velocity (E/e’), measured by echocardiography, is a simple and convenient indicator of diastolic dysfunction. Various large clinical trials have reported that sodium glucose transporter-2 inhibitor therapy reduced cardiovascular events and hospitalizations in heart failure patients. We examined the effect of tofogliflozin on various physiological and cardiac function. A retrospective analysis was performed on elderly patients aged 65 years or older with type 2 diabetes mellitus attending Himi Municipal Hospital who were taking oral tofogliflozin 20 mg/day. Measurement of physiological and hormonal variables, blood sampling, and echocardiographic evaluations at 0, 1, 3, and 6 months were performed on those with ejection fraction (EF) of 40% or greater at the time of treatment. Statistical analysis was performed using t-tests and mixed-effects models, with brain natriuretic peptide less than or not less than 100 pg/mL, estimated glomerular filtration rate (eGFR) less than or not less than 50 mL/min/1.73 m2, and diuretics administered or not. Hypoglycemic effects were observed at 0, 1, 3, and 6 months. At each time point, EF was retained and E/e’ was significantly reduced. On the other hand, most physiological parameters and laboratory results showed no clinical abnormalities. Mixed-effects models showed time-dependent reduction of E/e’ in high/low brain natriuretic peptide, high/low eGFR, with or without diuretics between baseline and at 6 months. The interaction with time was significant in high/low eGFR. Tofogliflozin was shown to improve E/e’, a measure of diastolic function, while maintaining EF, with hypoglycemic effects and no clinical side effects.

01 Jul 2024·Diabetology International

Changes in serum levels of liver-related parameters, uric acid, and hemoglobin in patients with type 2 diabetes mellitus under treatment with tofogliflozin—a post-hoc analysis of the UTOPIA study

Article

Author: Katakami, Naoto ; Watada, Hirotaka ; Mita, Tomoya ; Sato, Yasunori ; Shimomura, Iichiro

Aims/IntroductionThe aim of the study was to evaluate the effects of tofogliflozin, a selective sodium-glucose cotransporter 2 inhibitor, on circulating levels of hepatic enzymes, uric acid and hemoglobin levels in patients with type 2 diabetes mellitus (T2DM).Materials and methodsWe evaluated longitudinal changes in circulating aspartate aminotransferase (AST), alanine aminotransferase (ALT), gamma-glutamyl transpeptidase (γ-GTP), uric acid, and hemoglobin levels in tofogliflozin (n = 169) and conventional treatment groups (n = 170) using data obtained from the UTOPIA trial, a randomized prospective study conducted to evaluate the efficacy of tofogliflozin in preventing atherosclerosis.ResultsWithin 104 weeks, tofogliflozin treatment, but not conventional treatment, significantly reduced AST, ALT, and γ-GTP levels. This reduction was significantly greater in the tofogliflozin group than in the conventional group. Stratified analysis showed that, in patients with obesity (defined as body mass index (BMI) ≥ 25.0 kg/m²), significant differences were observed in AST, ALT, and γ-GTP changes from baseline to 104 weeks between treatment groups. However, in patients without obesity, there were no significant differences in AST and γ-GTP changes from baseline to 104 weeks between treatment groups. Multivariable regression analysis showed that changes in BMI and HbA1c levels were independently associated with changes in AST, ALT, and γ-GTP levels. The reduction of uric acid and the increase of hemoglobin from baseline to 104 weeks were significantly greater in the tofogliflozin group than in the conventional group.ConclusionsThe beneficial effects of tofogliflozin on circulating levels of hepatic enzymes, uric acid, and Hb lasted for 2 years in patients with T2DM.Clinical trial registrationUMIN000017607 (https://www.umin.ac.jp/icdr/index.html).Supplementary InformationThe online version contains supplementary material available at 10.1007/s13340-024-00693-x.

100 Deals associated with Tofogliflozin Hydrate

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External Link

KEGG	Wiki	ATC	Drug Bank
D09978	Tofogliflozin Hydrate	A10BH	DB11824

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	JP	Kowa Co., Ltd.	24 Mar 2014

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	Preclinical	US	Hoffmann-La Roche, Inc.	22 Jan 2009
Diabetes Mellitus, Type 2	Preclinical	CA	Hoffmann-La Roche, Inc.	22 Jan 2009
Diabetes Mellitus, Type 2	Preclinical	AU	Hoffmann-La Roche, Inc.	22 Jan 2009
Diabetes Mellitus, Type 2	Preclinical	JP	Hoffmann-La Roche, Inc.	22 Jan 2009
Diabetes Mellitus, Type 2	Preclinical	LV	Hoffmann-La Roche, Inc.	22 Jan 2009
Diabetes Mellitus, Type 2	Preclinical	MX	Hoffmann-La Roche, Inc.	22 Jan 2009
Diabetes Mellitus, Type 2	Preclinical	ES	Hoffmann-La Roche, Inc.	22 Jan 2009
Diabetes Mellitus, Type 2	Preclinical	BR	Hoffmann-La Roche, Inc.	22 Jan 2009
Diabetes Mellitus, Type 2	Preclinical	HK	Hoffmann-La Roche, Inc.	22 Jan 2009
Diabetes Mellitus, Type 2	Preclinical	DE	Hoffmann-La Roche, Inc.	22 Jan 2009

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02649465 (Pubmed) Manual	Phase 4	Diabetes Mellitus, Type 2 \| Metabolic dysfunction-associated steatotic liver disease	40	Tofogliflozin	(alicitoqoy) = The histological variables of steatosis (65%, P = 0.001), hepatocellular ballooning (55%, P = 0.002), and lobular inflammation (50%, P = 0.003) were improved in the tofogliflozin group, whereas only hepatocellular ballooning was improved in the glimepiride group (25%, P = 0.025). cljhfskeqo (pxgoqrchtj )	Positive	27 Jul 2022
				Glimepiride
ADA2021	Not Applicable	Anemia \| Polycythemia	774	Tofogliflozin (Anemia group)	plgzecojvi(uzuhfqqkmf) = ahlxdboxuz ytgzzffvfd (fbafukmwfr )	-	01 Jun 2021
				Tofogliflozin (Polycythemia group)	plgzecojvi(uzuhfqqkmf) = ezdvmoyzjh ytgzzffvfd (fbafukmwfr )
NCT00800176 (CTgov)	Phase 2	Diabetes Mellitus, Type 2	394	Placebo (Placebo)	mcaivfgqqc(qkppqfqkbx) = eqsnlllgxl zcgubspqow (gieoejybjp, ufegeafstl - jcteatfnfz) View more	-	18 Nov 2020
				RO4998452 (RO4998452 5mg)	mcaivfgqqc(qkppqfqkbx) = xhdwykhqso zcgubspqow (gieoejybjp, kmvposbxnr - dhshwqyjrm) View more
UTOPIA Trial (ADA2020)	Not Applicable	Diabetes Mellitus, Type 2	340	Tofogliflozin treatment group	sdpseobluv(etjzlihlkj) = mwcjjtlgcp fkmqctmcdb (fzxvdaiwlb ) View more	-	01 Jun 2020
ADA2020	Not Applicable	Diabetes Mellitus, Type 2	12	Tofogliflozin	(nhinboufsh) = ejoehyhnco immhymtisj (lzoyugxuip )	-	01 Jun 2020
				Tofogliflozin (No administration of drugs)	(nhinboufsh) = spbkofxxqq immhymtisj (lzoyugxuip )
ADA2020	Not Applicable	Diabetes Mellitus, Type 2 Add-on	774	Tofogliflozin (Quartiles 1-3)	ohvyifikoy(iufjmqpyws) = lanhzrmgkm mizgxmmkls (xgbjieyhsn ) View more	-	01 Jun 2020
				Tofogliflozin (Quartile 4)	ohvyifikoy(iufjmqpyws) = ucqbjpunxe mizgxmmkls (xgbjieyhsn ) View more
ADA2020	Not Applicable	-	166	Tofogliflozin	ikcjtikavf(jaqjhhjnku) = mxpnacdozj gtscobsprl (mjmeonelxi ) View more	-	01 Jun 2020
NCT02537834 (Pubmed \| J Diabetes Investig)	Phase 4	Diabetes Mellitus, Type 2 Add-on	67	Tofogliflozin 20 mg + GLP-1 receptor agonist	(rygclqcdye) = pdssmicaah tfzthmhikd (kainnqakvn )	Positive	01 Nov 2019
JPRN-UMIN000026161 (EASD2019)	Not Applicable	Third line	-	Tofogliflozin 20 mg/day	(scyoivdkof) = Adverse events were observed in 27.3% patients in Tofogliflozin 20 mg/day and 29.0% in Glimepiride 0.5 mg/day. None of them were severe. There was one patient experienced hypoglycemia in Glimepiride 0.5 mg/day but none in Tofogliflozin 20 mg/day. mbulzwyjhv (tkewuvhuhf )	Positive	19 Sep 2019
				Glimepiride 0.5 mg/day
EASD2018	Not Applicable	-	-	Tofogliflozin 10 mg	uplfvkuiie(gjsdgnzads) = vggwzerttw rphutjrjoa (wknypwavgo ) View more	-	02 Oct 2018
				Tofogliflozin 20 mg	uplfvkuiie(gjsdgnzads) = zasfcxuwox rphutjrjoa (wknypwavgo ) View more