Delving into the Latest Updates on Lafutidine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Lafutidine (JP17/INN), Stogar, loctidine

+ [9]

Target

H2 receptor

Action

antagonists

Mechanism

H2 receptor antagonists(Histamine H2 receptor antagonists)

Therapeutic Areas

Digestive System DisordersMouth and Tooth DiseasesOtorhinolaryngologic Diseases

Active Indication

Esophagitis, PepticGastritisPeptic Ulcer+ [3]

Inactive Indication

Erosive esophagitisInflammatory Bowel Diseases

Originator Organization

UCB SA

Active Organization

Taiho Pharmaceutical Co., Ltd.

Sichuan Kelun Pharmaceutical Co., Ltd.

Boryung Corp.

+ [1]

Inactive Organization

UCB Pharma GmbH

Salix Pharmaceuticals, Inc.

License Organization-

Drug Highest PhaseApproved

First Approval Date

Japan (08 Jan 2000),

Duodenal UlcerGastroesophageal RefluxStomach Ulcer

Regulation-

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Structure/Sequence

Molecular FormulaC22H29N3O4S

InChIKeyKMZQAVXSMUKBPD-DJWKRKHSSA-N

CAS Registry206449-93-6

主要目的：以济川药业集团有限公司提供的拉呋替丁片为受试制剂，按照有关生物等效性试验规定，与大鹏药品工业株式会社生产的拉呋替丁片（Protecadin®，参比制剂）进行空腹及餐后状态下人体生物利用度与生物等效性试验，评估受试制剂和参比制剂在空腹及餐后状态下给药时的生物等效性。次要目的：观察受试制剂拉呋替丁片和参比制剂拉呋替丁片（Protecadin®）在健康受试者中的安全性。

[Translation]

Primary objective: To use Lafutidine Tablets provided by Jichuan Pharmaceutical Group Co., Ltd. as the test preparation, and conduct human bioavailability and bioequivalence tests with Lafutidine Tablets (Protecadin®, reference preparation) produced by Dapeng Pharmaceutical Industry Co., Ltd. in the fasting and fed state, in accordance with relevant bioequivalence test regulations, to evaluate the bioequivalence of the test preparation and the reference preparation when administered in the fasting and fed state. Secondary objective: To observe the safety of the test preparation Lafutidine Tablets and the reference preparation Lafutidine Tablets (Protecadin®) in healthy subjects.

Start Date05 Jul 2022

Sponsor / Collaborator

Hubei Jumpcan Pharmaceutical Co., Ltd.

ChiCTR2200055479

/ RecruitingPhase 4IIT

Efficacy of nocturnal symptoms and esophageal acid exposure in GERD patients: a randomized controlled study of PPI combined with lafutidine versus PPI alone

Start Date20 Jan 2022

Sponsor / Collaborator-

CTR20181930

/ CompletedNot Applicable

拉呋替丁片单中心、随机、开放、双周期、双交叉设计在中国健康受试者空腹和餐后的生物等效性试验

[Translation] A single-center, randomized, open-label, two-period, double-crossover bioequivalence study of lafutidine tablets in Chinese healthy volunteers with fasting and fed diet

主要目的：评价湖北舒邦药业有限公司的拉呋替丁片（规格：5mg/片）与大鹏药业工业株式会社的拉呋替丁片（规格： 5mg/片）在健康成年受试者空腹和餐后状态下单次口服给药的人体生物等效性。次要目的：评价拉呋替丁片在健康成年受试者中的安全性。

[Translation]

Primary objective: To evaluate the bioequivalence of lafutidine tablets (specification: 5 mg/tablet) of Hubei Shubang Pharmaceutical Co., Ltd. and lafutidine tablets (specification: 5 mg/tablet) of Dapeng Pharmaceutical Industry Co., Ltd. in healthy adult subjects after single oral administration in fasting and fed state. Secondary objective: To evaluate the safety of lafutidine tablets in healthy adult subjects.

Start Date15 Oct 2018

Sponsor / Collaborator

Hubei Shubang Pharmaceutical Co Ltd.

100 Clinical Results associated with Lafutidine

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100 Translational Medicine associated with Lafutidine

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100 Patents (Medical) associated with Lafutidine

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298

Literatures (Medical) associated with Lafutidine

01 Nov 2024·Annals of Palliative Medicine

Assessing lafutidine’s potential to protect lung cancer patients from chemotherapy-induced neuropathy

Article

Author: Khan, Saim Mahmood ; Sultan, Ramsha ; Hussain, Jawairya Muhammad

01 Sep 2024·eBioMedicine

Tanomastat exerts multi-targeted inhibitory effects on viral capsid dissociation and RNA replication in human enteroviruses

Article

Author: Jaladanki, Chaitanya K. ; Fan, Hao ; Wong, Yi Hao ; Jaladanki, Chaitanya K ; Yogarajah, Thinesshwary ; Chu, Justin Jang Hann ; Lim, Therese Yien May

BACKGROUNDGlobal cyclical outbreaks of human enterovirus infections has positioned human enterovirus A71 (EV-A71) as a neurotropic virus of clinical importance. However, there remains a scarcity of internationally approved antivirals and vaccines.METHODSIn pursuit of repurposing drugs for combating human enteroviruses, we employed a comprehensive pharmacophore- and molecular docking-based virtual screen targeting EV-A71 capsid protein VP1-4, 3C protease, and 3D polymerase proteins. Among 15 shortlisted ligand candidates, we dissected the inhibitory mechanism of Tanomastat in cell-based studies and evaluated its in vivo efficacy in an EV-A71-infected murine model.FINDINGSWe demonstrated that Tanomastat exerts dose-dependent inhibition on EV-A71 replication, with comparable efficacy profiles in enterovirus species A, B, C, and D in vitro. Time-course studies suggested that Tanomastat predominantly disrupts early process(es) of the EV-A71 replication cycle. Mechanistically, live virus particle tracking and docking predictions revealed that Tanomastat specifically impedes viral capsid dissociation, potentially via VP1 hydrophobic pocket binding. Bypassing its inhibition on entry stages, we utilized EV-A71 replication-competent, 3D^pol replication-defective, and bicistronic IRES reporter replicons to show that Tanomastat also inhibits viral RNA replication, but not viral IRES translation. We further showed that orally administered Tanomastat achieved 85% protective therapeutic effect and alleviated clinical symptoms in EV-A71-infected neonatal mice.INTERPRETATIONOur study establishes Tanomastat as a broad-spectrum anti-enterovirus candidate with promising pre-clinical efficacy, warranting further testing for potential therapeutic application.FUNDINGMOE Tier 2 grants (MOE-T2EP30221-0005, R571-000-068-592, R571-000-076-515, R571-000-074-733) and A∗STARBiomedical Research Council (BMRC).

01 May 2024·Biomedicine & Pharmacotherapy

Utilizing machine learning to identify nifuroxazide as an inhibitor of ubiquitin-specific protease 21 in a drug repositioning strategy

Article

Author: Kim, Sang Geon ; Ahn, Hee-Chul ; Tak, Jihoon ; Lee, Kyeong ; Nguyen, Tan Khanh

Ubiquitin-specific protease (USP), an enzyme catalyzing protein deubiquitination, is involved in biological processes related to metabolic disorders and cancer proliferation. We focused on constructing predictive models tailored to unveil compounds boasting USP21 inhibitory attributes. Six models, Extra Trees Classifier, Random Forest Classifier, LightGBM Classifier, XGBoost Classifier, Bagging Classifier, and a convolutional neural network harnessed from empirical data were selected for the screening process. These models guided our selection of 26 compounds from the FDA-approved drug library for further evaluation. Notably, nifuroxazide emerged as the most potent inhibitor, with a half-maximal inhibitory concentration of 14.9 ± 1.63 μM. The stability of protein-ligand complexes was confirmed using molecular modeling. Furthermore, nifuroxazide treatment of HepG2 cells not only inhibited USP21 and its established substrate ACLY but also elevated p-AMPKα, a downstream functional target of USP21. Intriguingly, we unveiled the previously unknown capacity of nifuroxazide to increase the levels of miR-4458, which was identified as downregulating USP21. This discovery was substantiated by manipulating miR-4458 levels in HepG2 cells, resulting in corresponding changes in USP21 protein levels in line with its predicted interaction with ACLY. Lastly, we confirmed the in vivo efficacy of nifuroxazide in inhibiting USP21 in mice livers, observing concurrent alterations in ACLY and p-AMPKα levels. Collectively, our study establishes nifuroxazide as a promising USP21 inhibitor with potential implications for addressing metabolic disorders and cancer proliferation. This multidimensional investigation sheds light on the intricate regulatory mechanisms involving USP21 and its downstream effects, paving the way for further exploration and therapeutic development.

100 Deals associated with Lafutidine

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External Link

KEGG	Wiki	ATC	Drug Bank
D01131	Lafutidine	A02BA08	DB12770

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Esophagitis, Peptic	Japan	Taiho Pharmaceutical Co., Ltd.	07 Oct 2014
Gastritis	Japan	Taiho Pharmaceutical Co., Ltd.	06 Apr 2000
Peptic Ulcer	Japan	-	18 Jan 2000
Duodenal Ulcer	Japan	Taiho Pharmaceutical Co., Ltd.	08 Jan 2000
Gastroesophageal Reflux	Japan	Taiho Pharmaceutical Co., Ltd.	08 Jan 2000
Stomach Ulcer	Japan	Taiho Pharmaceutical Co., Ltd.	08 Jan 2000

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Peptic Ulcer	Phase 3	United States	Boryung Corp.	01 Aug 2015
Erosive esophagitis	Phase 3	-	Boryung Corp.	01 Nov 2011
Gastroesophageal Reflux	Phase 3	Japan	UCB Pharma GmbH	01 Apr 2005
Gastritis	Phase 3	United States	Salix Pharmaceuticals, Inc.	31 Dec 2000
Esophagitis, Peptic	Phase 3	South Korea	Boryung Corp.	-
Inflammatory Bowel Diseases	Phase 2	Japan	-	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01499368 (CTgov)	Phase 3	Erosive esophagitis	495	Lafutidine (Lafutidine)	xixezznqyx(dgqdufqyaa): P-Value = 0.05 View more	-	16 Sep 2020
				Famotidine (Famotidine)
JPRN-UMIN000002703 (AEOLUS, ASCO_GI2018)	Not Applicable	Stomach Cancer Adjuvant	-	S-1 with lafutidine	acqcldpsfk(nbnyxbihqi) = ahuyhvxnde iaugrshsfg (yibeibklgt ) View more	Positive	26 Feb 2018
				S-1	acqcldpsfk(nbnyxbihqi) = gqyzapoifg iaugrshsfg (yibeibklgt ) View more
NCT00229424 (Pubmed)	Phase 3	Esophagitis, Peptic	-	Lafutidine 20mg	(fnuxonzoqo) = tiytdmymjy tbfvctjdyh (sqovpphdko ) View more	-	01 Apr 2010
				Famotidine 40mg	(fnuxonzoqo) = lphhbisrng tbfvctjdyh (sqovpphdko )