Delving into the Latest Updates on Topiroxostat with Synapse

Primary objective: To evaluate the efficacy and safety of 160 mg, 200 mg, and 240 mg maintenance doses of topiramate tablets in the treatment of gout with hyperuricemia compared with allopurinol tablets. Secondary objective: To evaluate the protective effect of topiramate tablets on renal function in the treatment of gout with hyperuricemia compared with allopurinol tablets.

Start Date22 Aug 2024

Sponsor / Collaborator

Hunan Jiudian Pharmaceutical Co., Ltd.

[+1]

CTR20234213 / CompletedNot Applicable

托吡司特片在中国健康受试者中进行的单中心、随机、开放、单次（空腹/餐后）口服给药、两制剂、两序列、四周期重复交叉的人体生物等效性试验

[Translation] A single-center, randomized, open-label, single-dose (fasting/postprandial) oral bioequivalence study of topiramate tablets in healthy Chinese subjects using two formulations, two sequences, and four-period repeated crossover

主要目的：观察中国健康受试者在空腹/餐后状态下单次口服受试制剂托吡司特片（规格：60mg；生产企业：河北华晨药业集团有限公司）和参比制剂托吡司特片（商品名：Topiloric®；规格：60mg；持证商：株式会社富士薬品）后的药代动力学特征，评价空腹/餐后状态下两种制剂的生物等效性。次要目的：观察受试制剂托吡司特片和参比制剂托吡司特片（Topiloric®）在中国健康受试者中的安全性。

[Translation]

Primary objective: To observe the pharmacokinetic characteristics of the test preparation Topiramate Tablets (Specification: 60 mg; Manufacturer: Hebei Huachen Pharmaceutical Group Co., Ltd.) and the reference preparation Topiramate Tablets (Trade name: Topiloric®; Specification: 60 mg; Licensee: Fuji Pharmaceutical Co., Ltd.) after a single oral administration in the fasting/postprandial state in healthy Chinese subjects, and to evaluate the bioequivalence of the two preparations in the fasting/postprandial state. Secondary objective: To observe the safety of the test preparation Topiramate Tablets and the reference preparation Topiramate Tablets (Topiloric®) in healthy Chinese subjects.

Start Date13 Jun 2024

Sponsor / Collaborator

Hebei Huachen Pharmaceutical Co. Ltd.

CTR20240506 / CompletedNot Applicable

托匹司他片人体生物等效性研究（餐后）

[Translation] Bioequivalence study of topinostat tablets in humans (after meal)

主要研究目的：按有关生物等效性试验的规定，选择株式会社富士薬品持证的托匹司他片（商品名：トピロリック®，规格：40mg）为参比制剂，对长春海悦药业股份有限公司持证的受试制剂托匹司他片（规格：40mg）进行餐后给药人体生物等效性试验，比较受试制剂中药物的吸收速度和吸收程度与参比制剂的差异是否在可接受的范围内，评估两种制剂在餐后给药条件下的生物等效性。次要研究目的：观察健康志愿受试者口服受试制剂托匹司他片（40mg）和参比制剂托匹司他片（商品名：トピロリック®，规格：40mg）的安全性。

[Translation]

Main research purpose: According to the relevant provisions of bioequivalence test, Fuji Pharmaceutical Co., Ltd.'s certified topinostat tablets (trade name: Topirolic®, specification: 40 mg) were selected as the reference preparation, and the test preparation topinostat tablets (specification: 40 mg) certified by Changchun Haiyue Pharmaceutical Co., Ltd. were used for postprandial human bioequivalence test, to compare whether the absorption rate and degree of the drug in the test preparation were within the acceptable range with the reference preparation, and to evaluate the bioequivalence of the two preparations under postprandial administration conditions. Secondary research purpose: To observe the safety of oral administration of the test preparation topinostat tablets (40 mg) and the reference preparation topinostat tablets (trade name: Topirolic®, specification: 40 mg) by healthy volunteers.

Start Date13 May 2024

Sponsor / Collaborator

Changchun Haiyue Pharmaceutical Co., Ltd

100 Clinical Results associated with Topiroxostat

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100 Translational Medicine associated with Topiroxostat

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100 Patents (Medical) associated with Topiroxostat

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417

Literatures (Medical) associated with Topiroxostat

01 Jan 2025·European Journal of Medicinal Chemistry

Design, synthesis, and evaluation of 4-(4-methyl-4H-1,2,4-triazol-3-yl)piperidine derivatives as potential glutaminyl cyclase isoenzyme inhibitors for the treatment of cancer

Article

Author: He, Pan ; Wang, Zhuoran ; Zhou, Qingqing ; Zhu, Fangyi ; Qin, Feixia ; Wu, Haiqiang ; Gao, Ying ; Li, Chenyang ; Wu, Zhenxin ; Xiong, Wei

Upregulated glutaminyl cyclase isoenzyme (isoQC) contributes to cancer development by catalyzing pE-CD47 generation and thus enhancing CD47-SIRPα binding and subsequent "don't eat me" signals. We thus consider that isoQC could represent a novel target for cancer therapy. We previously prepared a series of diphenyl conjugated imidazole derivatives (DPCIs) and evaluated their use as glutaminyl cyclase (QC) inhibitors. Here, a new series of DPCIs was rationally designed and synthesized. As anticipated, the analogues exhibited considerably improved inhibitory potency against both QC and isoQC. Crucially, these chemicals exhibited marked selectivity toward isoQC. Further assessments established that one selected compound (27) did not affect the viability of A549, H1299, PC9, or HEK293T cells or the body weight of mice. This compound did, however, reduce pE-CD47 levels in infected A549 cells (isoQC_OE and isoQC_KD) and exhibited apparent anti-cancer effects in vivo by downregulating the level of pE-CD47 via the inhibition of isoQC activity. Taken together, these findings indicated that the compounds synthesized in this study could represent potential QC/isoQC inhibitors for the treatment of cancers.

01 Jan 2025·Journal of Inorganic Biochemistry

Anticancer dinuclear Ir(III) complex activates Nrf2 and interferes with NAD(H) in cancer cells

Article

Author: Kryštof, Vladimír ; Bárta, Ondřej ; Řezníčková, Eva ; Štarha, Pavel ; Milde, David

Dinuclear complex [Ir₂(μ-L1)(η⁵-Cp*)₂Cl₂](PF₆)₂ (1) exhibits low micromolar cytotoxic activity in vitro in various human cancer cells (GI₅₀ = 1.7-3.0 μM) and outperformed its mononuclear analogue [Ir(η⁵-Cp*)Cl(L2)]PF₆ (2; GI₅₀ > 40.0 μM); Cp* = pentamethylcyclopentadienyl, L1 = 4-chloro-2,6-bis[5-(pyridin-2-yl)-1,3,4-thiadiazol-2-yl]pyridine, L2 = 5-(pyridin-2-yl)-1,3,4-thiadiazol-2-amine. Compound 1 upregulated the Keap1/Nrf2 oxidative stress-protective pathway in the treated MV4-11 acute myeloid leukemia cells. In connection with the redox-mediated mode of action of 1, its NADH-oxidizing activity was detected in solution (¹H NMR), while NAD⁺ remained intact (with formate as a hydride source). Surprisingly, only negligible NADH oxidation was detected in the presence of the reduced glutathione and ascorbate. Following the results of in-solution experiments, NAD(H) concentration was assessed in 1-treated MV4-11 cancer cells. Besides the intracellular NADH oxidation in the presence of 1, the induced oxidative stress also led to a decrease of NAD⁺, resulting in depletion of both NAD⁺/NADH coenzymes. The discussed findings provide new insight into the biochemical effects of catalytic anticancer compounds that induce cell death via a redox-mediated mode of action.

01 Dec 2024·Computational Biology and Chemistry

Molecular descriptors and in silico studies of 4-((5-(decylthio)-4-methyl-4n-1,2,4-triazol-3-yl)methyl)morpholine as a potential drug for the treatment of fungal pathologies

Article

Author: Inna, Bushuieva ; Gutyj, Bogdan ; Myroslava, Ohloblina ; Poustforoosh, Alireza ; Tüzün, Burak ; Parchenko, Volodymyr

The article explores the polypharmacological profiling of 4-((5-(decylthio)-4-methyl-4H-1,2,4-triazole-3-yl)methyl)morpholine as a potential antimicrobial agent. The study utilized 15148 electronic pharmacophore models of organisms, ranked by the Tversky index. Detailed analysis revealed classical bonding patterns with selected enzymes, identifying key amino acid residues involved in complex formation. Protein target prediction was conducted through various stages using the Galaxy web service, including ligand structure creation, pharmacophore alignment, and target ranking. The activities of the molecules against 1G6C, 2W6O, 3G7F, 3OWU, 4IVR, and 4TZT proteins were compared. Docking studies with PyMOL and Discovery Studio Visualizer revealed binding to thymidine kinase, thiamine phosphate synthase, and biotin carboxylase with promising binding affinities. These interactions suggest potential antibacterial and antiviral effects, warranting further virtual screening and in-depth studies for the development of effective antimicrobial drugs. Calculations of the molecules were made with the gaussian package program. Calculations were made on the 6-31++g** basis set at B3LYP, HF, and M062X levels with Gaussian software. Afterwards, the 0-100 ns interaction of the molecule with the highest activity was examined.

100 Deals associated with Topiroxostat

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External Link

KEGG	Wiki	ATC	Drug Bank
D09786	Topiroxostat	M04	DB01685

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Gout	JP	Sanwa Kagaku Kenkyusho Co., Ltd.	28 Jun 2013
Gout	JP	Fuji Yakuhin Co., Ltd.	28 Jun 2013
Gout	JP	Fuji Pharma Co., Ltd.	28 Jun 2013
Hyperuricemia	JP	Fuji Pharma Co., Ltd.	28 Jun 2013
Hyperuricemia	JP	Sanwa Kagaku Kenkyusho Co., Ltd.	28 Jun 2013
Hyperuricemia	JP	Fuji Yakuhin Co., Ltd.	28 Jun 2013

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Gout	Phase 3	CN	-	23 Mar 2018
Hyperuricemia	Phase 3	CN	-	23 Mar 2018
Diabetic Nephropathies	Discovery	JP	Sanwa Kagaku Kenkyusho Co., Ltd.	30 Dec 2014
Diabetic Nephropathies	Discovery	JP	Fuji Yakuhin Co., Ltd.	30 Dec 2014

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Clinical Result

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Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


FP275 (ERA2015)	Not Applicable	Chronic Kidney Diseases serum urate levels \| urinary albumin excretion	-	Topiroxostat 160 mg/day	peiurxnowj(gucjiedvwu) = rbedboycoa yuvqbwdzip (lodeshwram )	Positive	21 May 2015
				Placebo	peiurxnowj(gucjiedvwu) = svnaikamor yuvqbwdzip (lodeshwram )