Beta Lapachone(Beta Lapachone) - 药物靶点：NQO1_专利_临床

概要

基本信息

药物类型

小分子化药

别名

+ [6]

靶点

NQO1

作用方式

抑制剂

作用机制

NQO1抑制剂(苯醌还原酶-1抑制剂)

治疗领域

肿瘤消化系统疾病内分泌与代谢疾病+ [1]

在研适应症-

非在研适应症

腺癌晚期恶性实体瘤纤维化+ [9]

原研机构

Arisyn Therapeutics Inc

在研机构-

非在研机构

Arisyn Therapeutics Inc

Yungjin Pharm. Co., Ltd.

ArQule, Inc.

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C15H14O3

InChIKeyQZPQTZZNNJUOLS-UHFFFAOYSA-N

CAS号4707-32-8

关联

13

项与 Beta Lapachone 相关的临床试验

NCT02338856

/ Completed临床1期

A Phase I Clinical Trial to Evaluate the Pharmacokinetics and Safety of MB12066 in Healthy Male Volunteers

The purpose of this study is to investigate the safety and tolerability of MB12066 after multiple dose and to investigate the pharmacokinetic characteristics of MB12066 after multiple dose.

开始日期2015-01-01

申办/合作机构

Yungjin Pharm. Co., Ltd.

NCT02029586

/ Terminated临床2期

A Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel Group, 12 Weeks, Therapeutic Exploratory Phase 2 Clinical Study to Evaluate the Safety and Efficacy of MB12066 in Patients With Nonalcoholic Fatty Liver Disease (NAFLD) Except Cirrhosis

This is a controlled study to determine the effectiveness and safety of MB12066 in the treatment of adult patients with Nonalcoholic Fatty Liver Disease(NAFLD) except cirrhosis.

开始日期2013-01-01

申办/合作机构

Yungjin Pharm. Co., Ltd.

NCT01444677

/ Completed临床1期

A Dose Block-randomized, Double-blind, Placebo-controlled, Single or Multiple Dosing, Dose-escalation Clinical Trial to Investigate the Safety, Tolerability and Pharmacokinetic Characteristics of MB12066 in Healthy Male Subjects

The purpose of this study is to investigate the safety and tolerability of MB12066 after a single or multiple oral dose and to investigate the pharmacokinetic characteristics of MB12066 after a single or multiple oral dose.

开始日期2011-04-01

申办/合作机构

Yungjin Pharm. Co., Ltd.

[+1]

100 项与 Beta Lapachone 相关的临床结果

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100 项与 Beta Lapachone 相关的转化医学

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100 项与 Beta Lapachone 相关的专利（医药）

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872

项与 Beta Lapachone 相关的文献（医药）

2025-06-01·Biomaterials

Hybrid membrane based biomimetic nanodrug with high-efficient melanoma-homing and NIR-II laser-amplified peroxynitrite boost properties for enhancing antitumor therapy via effective immunoactivation

Article

作者: Zha, Yongchao ; Xue, Wei ; Yu, Siming ; Zeng, Yina ; Lin, Qi ; Zhang, Yu

Owing to the excellent stability, anticancer activity and immunogenicity, peroxynitrite (ONOO^-) has been gained enormous interests in cancer therapy. Nevertheless, precise delivery and control release of ONOO^- in tumors remains a big challenge. Herein, B16F10 cancer cell membrane/liposome hybrid membrane (CM-Lip) based biomimetic nanodrug with high-efficient tumor-homing and NIR-II laser controlled ONOO^- boost properties was designed for melanoma treatment. Briefly, NIR-II molecule IR1061, NO donor BNN6 and β-lapachone (Lapa) were firstly encapsulated in the heat-responsive palmitoyl phosphatidylcholine/cholesterol liposome, followed by fusion with B16F10 cell membrane (CM) to obtain biomimetic CM-Lip@(IR/BNN6/Lapa). The hybrid membrane-based nanodrug displayed excellent biocompatibility and melanoma-targeting efficiency. Upon 1064 nm laser irradiation, the mild photothermal effect of CM-Lip@(IR/BNN6/Lapa) firstly triggered the release of NO and Lapa, which subsequently catalyzed the quinone oxidoreductase 1 (NQO1) overexpressed in tumors to produce O₂^•-, finally caused intraturmal ONOO^- boost via cascade reaction. The boosted ONOO^- could effectively inhibit melanoma by ways of triggering mitochondrion-mediated apoptotic pathway, upregulating 3-nitrotyrosine expression, inducing DNA damage and inhibiting DNA repair enzyme expression of poly (ADP-ribose) polymerase 1 (PARP-1). Moreover, ONOO^- displayed excellent immunoactivation and immunomodulation activities by effectively inducing immunogenic tumor cell death, promoting dendritic cells maturation, increasing cytotoxic T lymphocytes expression and repolarizing M1-phenotype macrophages.

2025-04-01·Structural Chemistry

A comparative DFT study of drug delivery system based on Pt-doped and Au-modified MoS2 nanosheets for β-lapachone drug

作者: Altalbawy, Farag M. A. ; Altameemi, Kamil K. Atiyah ; Al-saray, Mustafa Jassim ; Walia, Chakshu ; Alsayah, Ahmed Mohsin ; Prasad, G. V. Siva ; Monsi, Mekha ; Al-Mashhadani, Zuhair I. ; Alsaadi, Salima B. ; Ballal, Suhas

This study analyzed the interaction of β-lapachone (C₁₅H₁₄O₃) drug onto the pristine, Pt-doped, and Au-modified MoS₂ nanosheets using d. functional theory (DFT).Pristine MoS₂ was found not to be strongly connected to the β-lapachone mol. and thus was not conductive to propose promising drug sensing system.The thermodn. stability of both Pt-doped and Au-modified MoS₂ nanosheets was described using the calculated neg. formation energies.On the other hand, Pt-doped and Au-modified MoS₂ exhibited higher binding energy and strength towards β-lapachone drugs.Pt-doped MoS₂ showed stronger interaction with β-lapachone drugs than Au-modified MoS₂ thanks to stronger orbital interactions and adsorption capacity.Both Pt-doped and Au-modified MoS₂ systems exposed semiconductor character based on band structure anal.The charge d. difference diagrams show the great accumulation of charge densities on the adsorbed β-lapachone drug.Due to the better conductivity, the drug carrier ability of the Au-modified and Pt-doped MoS₂ substrates are improved over the intrinsic MoS₂.The significant overlaps in the PDOS plots of Pt and O atoms indicate sufficient hybridization between them to form chem. bonds.The addition of noble metals such as Au and Pt may suggest a promising MoS₂-based biosensor towards adsorption and detection of β-lapachone drugs for the design of effective drug delivery systems.

2025-03-01·Journal of Heterocyclic Chemistry

Selective Electrophile‐Promoted Cyclization Reactions of Lapachol and Evaluation of Bioactive Naphthoquinones Against Cancer Cell Lines

作者: Ketsemen, Herve Landry ; Ouahouo, Blandine Marlysse Wache ; Eyong, Kenneth Oben ; Taube, Joseph ; Omdim, Irene Nadege ; Kamdem, Michael Hermann K. ; Ndinteh, Derek Tantoh ; Folefoc, Gabriel Ngosong ; Werner, Thomas ; Rajkumar, Abhinav ; Baskaran, Sundarababu ; Morales, Kayla

ABSTRACTCyclic ether‐fused tricyclic naphthoquinones are major pharmacophores because of their biological activities. The methodology of construction is either by inter or intra‐molecular cyclization of functionalized naphthoquinones. This reaction includes a wide range of reagents from classical Brønsted to Lewis acids. The choice of appropriate reagent and reaction conditions against the substrate is the key to accomplishing the regio‐ and/or stereo‐selective synthesis of these compounds, though it seems difficult at first glance to decide how because numerous numbers of actual examples have been presented. To have a deeper insight into the mechanism of cyclization under acid conditions, lapachol 1 was subjected to electrophilic entities: Brønsted acids (H2SO4, HCl, H3PO4, HNO3, HCOOH, CH3COOH, HOOCCH2COOH), Lewis acids (AlCl3, FeCl3, ZnCl2) nitrogenous cations (NO+, NO2+), carbocation (CH3CO+), neutral polarized molecules (CH3COCl, CH3COOCH3), neutral polarizable molecules (Br2, I2), oxidant promoted cyclization (DDQ, CAN, Peroxides), and reaction conditions. A series of Naphthoquinones based on the Isoprenyl‐1,4‐naphthoquinone (Lapachol), naphtho[1,2‐b]furan‐4,5‐dione (nor β‐lapachone), naphtho[2,3‐b]pyran‐5,10‐dione (α‐lapachone), naphtho[1,2‐b]pyran‐5,6‐dione (β‐lapachone), and naphtho[2,3‐b]furan‐4,9‐dione (2‐acetyl furonaphthoquinone) skeletons were selectively synthesized. By looking at our result, there are characteristic trends of cyclized adducts depending on which reagents were used. The synthesized compounds were evaluated for their biological activity against the MDA‐MB‐231 breast cancer, HT‐29 MTX colon cancer, and non‐transformed mammary epithelial cell lines at concentrations of 1 μM, 10 μM, and 100 μM. The result indicated that lapachol and β‐lapachone skeletons were the most active at 10 μM and 100 μM especially 3‐hydroxy‐β‐lapachone 8 with interesting growth stimulatory effect on cancer cell lines, but not the non‐transformed cells.

100 项与 Beta Lapachone 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB11948

研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
纤维化	临床2期	韩国	Yungjin Pharm. Co., Ltd.	2013-01-01
代谢功能障碍相关的脂肪肝病	临床2期	韩国	Yungjin Pharm. Co., Ltd.	2013-01-01
转移性头颈部鳞状细胞癌	临床2期	美国	-	2006-07-01
平滑肌肉瘤	临床2期	美国	-	2006-02-01
腺癌	临床2期	美国	ArQule, Inc.	2005-01-01
转移性胰腺腺癌	临床2期	美国	ArQule, Inc.	2005-01-01
晚期恶性实体瘤	临床2期	美国	-	2003-09-01
头颈部肿瘤	临床2期	-	Arisyn Therapeutics Inc	-
平滑肌瘤	临床2期	-	Arisyn Therapeutics Inc	-
胰腺癌	临床2期	-	Arisyn Therapeutics Inc	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


ASCO2005 人工标引	临床1期	晚期恶性实体瘤	18	ARQ 501	(積願願憲製築願窪製鑰) = Up to the 390 mg/m2 dose, ARQ 501 exhibited apparent linear pharmacokinetics, 網齋餘膚鏇積願蓋鬱選 (遞窪鹽築範衊簾鹹齋蓋 ) 更多	积极	2005-06-01
ARVO2004	N/A	视网膜母细胞瘤	-	Beta-lapachone	獵範鏇獵觸鬱窪製繭範(鹹鏇繭壓膚艱糧製積壓) = 齋選範窪構築齋鬱鹹簾獵繭夢構糧獵構廠憲鹹 (廠鏇簾憲簾顧築範願壓 ) 更多	-	2004-05-01
ARVO2004	N/A	视网膜母细胞瘤	-	Etoposide	構壓選選廠觸願範繭顧(蓋積齋願糧憲窪觸衊壓) = 鹽淵糧製淵顧壓夢憲網顧淵膚夢範遞壓觸膚遞 (襯觸鑰遞遞繭夢醖顧餘 )	-	2004-05-01