Delving into the Latest Updates on Henagliflozein Proline with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Henagliflozin, 瑞沁

Target

SGLT2

Mechanism

SGLT2 inhibitors(Sodium/glucose cotransporter 2 inhibitors)

Therapeutic Areas

Endocrinology and Metabolic DiseaseUrogenital Diseases

Active Indication

Diabetes Mellitus, Type 2Chronic Kidney Diseases

Inactive Indication

Diabetes Mellitus, Noninsulin-Dependent, 2Liver Diseases

Originator Organization

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Active Organization

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

CN (31 Dec 2021),

Diabetes Mellitus, Type 2

RegulationSpecial Review Project (CN)

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Structure/Sequence

Molecular FormulaC22H24ClFO7

InChIKeyHYTPDMFFHVZBOR-VNXMGFANSA-N

CAS Registry1623804-44-3

The prevalence of metabolic dysfunction-associated steatotic liver disease (MASLD) is increasing due to changes in economic conditions and lifestyle, and it is anticipated to become a significant liver disease burden in the future. This is particularly true for patients with MASLD who also have type 2 diabetes mellitus (T2DM), as the rate of comorbidity between these conditions has risen in recent years due to their shared mechanisms, necessitating careful management of both. Liver fibrosis is a critical concern, as poor blood glucose control can worsen liver fibrosis, which in turn complicates blood sugar management. Therefore, addressing liver fibrosis in patients with MASLD and T2DM is urgent, yet there are currently no targeted therapies to reverse its progression. SGLT2 inhibitors, have shown promise in potentially reversing liver fibrosis, but existing research is limited and has not adequately focused on liver fibrosis improvement, highlighting the need for more robust evidence-based studies.

Start Date31 Dec 2024

Sponsor / Collaborator

Jiangsu Province Hospital of Traditional Chinese Medicine

[+1]

ChiCTR2400087295

/ SuspendedPhase 4IIT

Henagliflozin for the overweight or obese patients with type 2 diabetes and heart failure: a multicenter, randomized, double-blind, controlled trial

Start Date01 Aug 2024

Sponsor / Collaborator-

ChiCTR2400085789

/ SuspendedPhase 4IIT

Effect of Henagliflozin Proline Tablets on visceral fat area in type 2 diabetic patients

Start Date01 Jul 2024

Sponsor / Collaborator-

100 Clinical Results associated with Henagliflozein Proline

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100 Translational Medicine associated with Henagliflozein Proline

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100 Patents (Medical) associated with Henagliflozein Proline

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13

Literatures (Medical) associated with Henagliflozein Proline

01 Nov 2024·Journal of Diabetes Investigation

Sodium–glucose cotransporter 2 inhibition through henagliflozin ameliorates cognitive impairment in patients with type 2 diabetes

Article

Author: Wang, Fen ; Xu, Jialu ; Yang, Yan ; Ma, Delin ; Chen, Juan ; Song, Xiaoqing ; Zhang, Shujun ; Tao, Jing ; Yu, Xuefeng ; Shi, Xiaoli ; Xie, Lei

AbstractAims/IntroductionTo assess whether the sodium–glucose cotransporter 2 inhibitor, henagliflozin, improves cognitive impairment in patients with type 2 diabetes.Materials and MethodsWe carried out a prospective study on 290 patients with type 2 diabetes and cognitive impairment. Montreal Cognitive Assessment scores and plasma phosphorylated tau181 levels were used to assess cognition. The association between henagliflozin use and changes in cognition was examined using multivariable logistic regression analysis.ResultsMontreal Cognitive Assessment scores at enrollment and after 6 months were 21 (interquartile range [IQR]19–23) versus 22 (IQR 20–25; P < 0.0001) in all patients, 21 (IQR 19–23) versus 24 (IQR 22–26; P < 0.0001) in the henagliflozin group and 21 (IQR 19–22) versus 21 (IQR 19–23; P > 0.05) in the non‐sodium–glucose cotransporter 2 inhibitor group. Logistic regression analysis showed that henagliflozin treatment was associated with Montreal Cognitive Assessment score improvement independent of potential confounders (odds ratio [OR] 3.670, 95% confidence interval [CI] 2.224–6.056, P < 0.0001). Additionally, plasma phosphorylated tau181 levels significantly decreased at 6‐month follow up in all patients (OR 11.5, 95% CI 9.9–13.7 vs OR 10.1, 95% CI 7.8–12.9, P < 0.0001) and in the henagliflozin group (OR 11.5, 95% CI 10.3–13.0 vs OR 9.2, 95% CI 7.1–10.7, P < 0.0001), but not in the non‐sodium–glucose cotransporter 2 inhibitor group. Henagliflozin treatment was independently associated with decreased phosphorylated tau181 levels (OR 3.670, 95% CI 1.598–4.213, P < 0.0001).ConclusionsHenagliflozin treatment was independently associated with improvements in Montreal Cognitive Assessment scores and plasma phosphorylated tau181 levels, indicating significant beneficial effects on cognitive impairment in patients with type 2 diabetes.

01 Oct 2024·BMJ Open

Efficacy and safety of henagliflozin combined with continuous subcutaneous insulin infusion in the treatment of Chinese inpatients with type 2 diabetes mellitus based on a continuous glucose monitoring system: protocol of a multicentre, open-label, inpatient, randomised, controlled trial

Article

Author: Huang, Zhenxing ; Wu, Yingling ; Qin, Yingfen

IntroductionThe role of sodium-glucose cotransporter 2 inhibitors (SGLT2is) in diabetes treatment is expanding; however, few studies have investigated the efficacy and safety of combining SGLT2is with insulin pump therapy. Notably, there is a scarcity of high-quality, multicentre, clinical trials. Therefore, we aim to conduct a prospective multicentre, randomised, controlled, study to investigate whether treatment of type 2 diabetes patients with continuous subcutaneous insulin infusion (CSII) combined with henagliflozin can reduce the time required for blood glucose control, decrease total insulin requirements, mitigate blood glucose fluctuations and enhance beta-cell function.Methods and analysisIn this inpatient, open-label, multicentre, randomised, controlled trial, 200 patients with type 2 diabetes who have not received hypoglycaemic drugs will be randomly allocated at a 1:1 ratio to either the henagliflozin combined with CSII group or the CSII group. The efficacy and safety of treatment in both groups will be compared. We will use a real-time continuous glucose monitoring system for blood glucose monitoring. The primary aim of this study is to compare the time (% time in range (TIR)) in the range of 3.9~10.0 mmol/L blood glucose between the two treatment groups. The secondary outcome measures will include comparisons of the two treatment groups with respect to the (a) time at TIR >70%; (b) mean amplitude of glycaemic excursions; (c) time below range; (d) total insulin dosage; and (e) time above range.Ethics and disseminationThis study was approved by the Ethics Committee of the First Affiliated Hospital of Guangxi Medical University and is to be conducted in accordance with the Declaration of Helsinki and Good Clinical Practice. The study will be disseminated through peer-reviewed publications and conference presentations.Trial registration numberNCT05677334.

01 Aug 2024·The Journal of Clinical Pharmacology

Pharmacokinetic, Pharmacodynamic, and Safety Profiles of Proline Henagliflozin in Chinese Subjects with Varying Degrees of Liver Dysfunction

Article

Author: Liu, Meiyou ; Diao, Qingbo ; Ding, Likun ; Feng, Sheng ; Sun, Li ; Ren, Danjun ; Zhang, Juanli ; Yang, Lin ; Wen, Aidong ; Wang, Jingwen ; Gao, Xiaohua

AbstractProline henagliflozin, a novel selective inhibitor of sodium glucose cotransporter 2, is a treatment for type 2 diabetes mellitus. We designed a parallel‐group, open‐label, and multicenter study to evaluate the pharmacokinetic (PK), pharmacodynamic (PD), and safety profiles of henagliflozin in Chinese subjects with varying degrees of liver dysfunction. Thirty‐two subjects were enrolled and divided into four groups based on liver function (normal liver function, mild, moderate, or severe liver dysfunction). The area under the plasma concentration from time zero to infinity of henagliflozin in subjects with mild liver dysfunction, moderate liver dysfunction, and severe liver dysfunction compared with normal liver function was increased by 137%, 197%, and 204%, respectively. The maximum plasma concentration was also increased by 123%, 129%, and 139%, respectively. PK parameters of three metabolites varied to different degrees in the liver dysfunction groups than in the normal liver function group. The mean accumulative excretion amounts and fraction of dose excreted in urine expressed as a percentage were all increased with the decrease of liver function. The PD parameters were significantly higher in liver dysfunction groups than those in the normal liver function group. However, the urine creatinine (UCr) was not significantly different among the groups. No notable adverse events or adverse drug reactions were observed. Due to the higher exposures in subjects with liver dysfunction, the benefit: risk ratio should be individually assessed because the long‐term safety profile and efficacy have not been specifically studied in this population.

100 Deals associated with Henagliflozein Proline

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB11939

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	CN	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	31 Dec 2021

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Chronic Kidney Diseases	IND Approval	CN	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	27 Nov 2023
Liver Diseases	Preclinical	CN	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	01 Jun 2015
Diabetes Mellitus, Noninsulin-Dependent, 2	Discovery	CN	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	02 Nov 2017

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


Corporate Publications Manual	Phase 3	Diabetes Mellitus, Type 2	-	恒格列净+二甲双胍 (恒格列净5 mg联合组)	(ocvrhgbtcj) = kgspiyydpx miukxyrvfb (bhxkdsmlnq ) View more	Positive	08 Jan 2024
				恒格列净+二甲双胍 (恒格列净10 mg联合组)	(ocvrhgbtcj) = ukyyhttdbv miukxyrvfb (bhxkdsmlnq ) View more
ChiCTR2200062872 (not available, Pubmed \| Clin Pharmacokinet)	Phase 4	Diabetes Mellitus	20	Henagliflozin 5 mg/day	(foswhzbtfi) = xqhqfjvbkv vuyfejqgyq (ppwcsqacen ) View more	Positive	01 Nov 2023
				Henagliflozin 10 mg/day	(foswhzbtfi) = wedfrahjsq vuyfejqgyq (ppwcsqacen ) View more