Antineoplaston A10(Antineoplaston A10) - 在研适应症：脑干胶质瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Antineoplaston A 10、Atengenal

+ [1]

靶点-

作用方式

诱导剂

作用机制

细胞凋亡诱导剂

治疗领域

肿瘤神经系统疾病

在研适应症

脑干胶质瘤

非在研适应症

食管腺癌前列腺腺癌肾上腺皮质癌+ [48]

原研机构

Burzynski Research Institute, Inc.

在研机构

Burzynski Research Institute, Inc.

非在研机构-

权益机构-

最高研发阶段临床3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C13H14N2O3

InChIKeyOQGRFQCUGLKSAV-JTQLQIEISA-N

CAS号91531-30-5

关联

64

项与 Antineoplaston A10 相关的临床试验

NCT02864888

/ Not yet recruiting临床3期IIT

A Controlled, Study of the Effect of Combination Antineoplaston Therapy [Atengenal (A10) and Astugenal (AS2-1)] on the QT/QTc Interval In Subjects With Newly Diagnosed Diffuse, Intrinsic, Brainstem Glioma

The primary objective of this protocol study is to investigate the effect of Antineoplaston therapy on the QT/QTc interval in study subjects age 3 to 21 years with newly-diagnosed, diffuse, intrinsic brainstem glioma. This investigation is to be conducted in parallel with a phase 3 efficacy and safety study of combination Antineoplaston therapy + radiation vs. radiation alone (BRI-BT-52).

开始日期2027-06-01

申办/合作机构

Burzynski Research Institute, Inc.

NCT02887040

/ Not yet recruiting临床3期IIT

A Randomized Phase 3 Study of Combination Antineoplaston Therapy [Antineoplastons A10 (Atengenal) and AS2-1 (Astugenal)] Plus Radiation Therapy vs. Radiation Therapy Only in Subjects With Newly Diagnosed Diffuse, Intrinsic, Brainstem Glioma

Patients ≥ 3 years of age with newly-diagnosed, diffuse, intrinsic pontine glioma will be enrolled in this study. However, the primary objectives of this study are to 1) compare overall survival, the time from randomization to death from any cause, for study subjects 3-21 years of age with newly-diagnosed, diffuse, intrinsic pontine glioma who receive Antineoplaston therapy (Atengenal + Astugenal) + radiation therapy vs. radiation therapy alone and 2) describe the toxicity profile (all subjects) for Antineoplaston therapy + radiation therapy vs. radiation therapy alone.
A secondary objective is to compare progression-free survival for study subjects 3-21 years of age with newly-diagnosed, diffuse, intrinsic pontine glioma treated with Antineoplaston therapy + radiation therapy vs. radiation therapy alone.

开始日期2025-06-01

申办/合作机构

Burzynski Research Institute, Inc.

KCT0008386

/ Active, not recruiting临床3期

24 weeks, Randomized, Double blind, Parallel-group, Sham Device-Controlled, Medical Device Pivotal Clinical Study to Evaluate the Efficacy and Safety of HM-SC-10 as Low-Level Light Therapy (LLLT) for Androgenetic Alopecia(AGA)

开始日期2022-08-31

申办/合作机构

Huons Medicare Co., Ltd.

100 项与 Antineoplaston A10 相关的临床结果

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100 项与 Antineoplaston A10 相关的转化医学

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100 项与 Antineoplaston A10 相关的专利（医药）

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84

项与 Antineoplaston A10 相关的文献（医药）

2024-05-03·Toxicology Mechanisms and Methods

Reactions of deoxyribonucleotide bases with sulfooxymethyl or halomethyl polycyclic aromatic hydrocarbons induce unwinding of DNA supercoils

Article

作者: Lehner, Andreas F.

Torsional stress in double-stranded DNA enables and regulates facets of chromosomal metabolism, replication, and transcription and requires regulatory enzymatic systems including topoisomerases and histone methyltransferases. As such, this machinery may be subject to deleterious effects from reactive mutagens, including ones from carcinogenic polycyclic aromatic hydrocarbon (PAH) adduct formation with DNA. Supercoiled plasmid DNA was investigated for its torsional responses to adducts formed in vitro from PAH benzylic carbocation reactive intermediates created spontaneously by release of leaving groups. PAH sulfate esters were found to (1) unwind DNA in a concentration dependent manner, and (2) provide maximum unwinding in a pattern consistent with known carcinogenicities of the parent PAHs, that is, 6-methylbenzo[a]pyrene > 7,12-methylbenz[a]anthracene > 3-methylcholanthrene > 9-methylanthracene > 7-methylbenz[a]anthracene > 1-methylpyrene. Supercoil unwinding was demonstrated to be dependent on the presence of sulfate or chloride leaving groups such that reactive carbocations were generated in situ by hydrolysis. In silico modeling of intercalative complex topology showed PAH benzylic carbocation reactive functional groups in alignment with target nucleophiles on guanine bases in a 5'-dCdG-3' pocket in agreement with known formation of nucleotide adducts. Inhibitory or modulatory effects on PAH-induced supercoil unwinding were seen with ascorbic acid and an experimental antineoplastic agent Antineoplaston A10 in agreement with their known anticarcinogenic properties. In summary, the reactive PAH intermediates studied here undoubtedly participate in well-known mutational mechanisms such as frameshifts and apurinic site generation. However, they are also capable of random disruption of chromosomal supercoiling in a manner consistent with the known carcinogenicities of the parent compounds, and this mechanism may represent an additional detrimental motif worthy of further study for a more complete understanding of chemical carcinogenicity.

2018-08-01·Cancer Biotherapy and Radiopharmaceuticals4区 · 医学

Improved Targeting and Tumor Retention of a Newly Synthesized Antineoplaston A10 Derivative by Intratumoral Administration: Molecular Docking, Technetium 99m Radiolabeling, andIn VivoBiodistribution Studies

4区 · 医学

Article

作者: Ibrahim, Ismail T. ; El-Kolaly, Mohamed T. ; Abdelbary, Aly A. ; Tadros, Mina I. ; Aboumanei, Mohamed H.

BACKGROUNDRecently, the direct intratumoral (i.t.) injection of anticancer agents has been investigated. A newly synthesized Antineoplaston A10 analog 3-(4-methoxybenzoylamino)-2,6-piperidinedione (MPD) showed an antitumor activity in human breast cancer cell line. Unfortunately, MPD suffered from poor water solubility.MATERIALS AND METHODSPseudoternary phase diagram of oil (isopropyl myristate), surfactant (Tween 80), cosurfactant (ethanol), and water was plotted. MPD microemulsion (MPDME) was developed and characterized for particle size (PS), polydispersity index (PDI), zeta potential (ZP), and morphology (transmission electron microscopy). MPDME and MPD solution (MPDS) were radiolabeled with technetium 99m (^99mTc) using stannous chloride dihydrate (SnCl₂.2H₂O). Molecular docking of MPD and ^99mTc-MPD was performed to study the interaction with DNA.RESULTSThe impacts of intravenous (i.v.) and i.t. injections of ^99mTc-MPDME and ^99mTc-MPDS on biodistribution were studied. The developed MPDME showed spherical droplets with mean PS (74.00 ± 5.69 nm), PDI (0.25 ± 0.03), and ZP (33.90 ± 0.90 mV). Labeling yield of ^99mTc-MPDME and ^99mTc-MPDS was 97.00% ± 0.60% and 92.02% ± 0.45%, respectively. MPD and ^99mTc-MPD showed almost same binding affinity with DNA binding site. Biodistribution results showed that i.t. injection of ^99mTc-MPDME significantly enhanced tumor retention compared to i.v. route.CONCLUSIONSHerein, the authors concluded that microemulsion could be used as i.t. injectable delivery vehicle to improve targeting and tumor retention of MPD.

2018-07-01·International Journal of Pharmaceutics2区 · 医学

Design and development of microemulsion systems of a new antineoplaston A10 analog for enhanced intravenous antitumor activity: In vitro characterization, molecular docking, 125I-radiolabeling and in vivo biodistribution studies

2区 · 医学

Article

作者: El-Kolaly, Mohamed T ; Abdelbary, Aly A ; Tadros, Mina I ; Ibrahim, Ismail T ; Aboumanei, Mohamed H

A10, (3-phenylacetylamino-2,6-piperidinedione), is a natural peptide with broad antineoplastic activity. Recently, in vitro antitumor effect of a new A10 analog [3-(4-methoxybenzoylamino)-2,6-piperidinedione] (MPD) has been verified. However, poor aqueous solubility represents an obstacle towards intravenous formulation of MPD and impedes successful in vivo antitumor activity. To surmount such limitation, MPD microemulsion (MPDME) was developed. A 3¹2² full factorial design using Design-Expert® software was adopted to study the influence of different parameters and select the optimum formulation (MPDME1). Transmission electron microscopy (TEM) displayed spherical droplets of MPDME1. The cytotoxicity of MPDME1 in Michigan Cancer Foundation 7 (MCF-7) breast cancer cell line exceeded that of MPD solution (MPDS) and tamoxifen. Compatibility with injectable diluents, in vitro hemolytic studies and in vivo histopathological examination confirmed the safety of parenteral application of MPDME1. Molecular docking results showed almost same binding affinity of A10, MPD and ¹²⁵I-MPD with histone deacetylase 8 (HDAC8) receptor. Accordingly, radioiodination of MPDME1 and MPDS was done via direct electrophilic substitution reaction. Biodistribution of ¹²⁵I-MPDME1 and ¹²⁵I-MPDS in normal and tumor (ascites and solid) bearing mice showed high accumulation of ¹²⁵I-MPDME1 in tumor tissues. Overall, the results proved that MPDME represents promising parenteral delivery system capable of improving antineoplastic activity of MPD.

100 项与 Antineoplaston A10 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB11702

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
脑干胶质瘤	临床3期	-	Burzynski Research Institute, Inc.	2025-06-01
卵巢上皮癌	临床3期	美国	Burzynski Research Institute, Inc.	1996-03-05
低级别星形细胞瘤	临床3期	美国	Burzynski Research Institute, Inc.	1996-03-01
前列腺腺癌	临床3期	美国	Burzynski Research Institute, Inc.	1996-02-27
转移性前列腺癌	临床3期	美国	Burzynski Research Institute, Inc.	1996-02-27
中枢神经系统横纹肌瘤	临床3期	美国	Burzynski Research Institute, Inc.	1996-02-01
高级别胶质瘤	临床3期	美国	Burzynski Research Institute, Inc.	1994-04-01
复发性恶性胶质瘤	临床3期	美国	Burzynski Research Institute, Inc.	1994-04-01
原发性恶性肝肿瘤	临床3期	美国	Burzynski Research Institute, Inc.	1977-03-21
室管膜瘤	临床3期	美国	Burzynski Research Institute, Inc.	1966-07-01

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临床结果

适应症

分期

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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


NCT00003487 (CTgov)	临床2期	食管腺癌	8	Atengenal+Astugenal	糧遞糧襯鹽衊願構選蓋(選網夢選顧範選淵醖醖) = 獵鏇餘憲艱遞積醖構鏇網選範獵繭觸網製製築 (廠憲範襯顧憲選膚顧鑰, 夢觸鏇齋壓艱淵選遞襯 ~ 憲鹽糧鑰選繭鬱襯繭觸) 更多	-	2021-05-14
NCT00003508 (CTgov)	临床2期	恶性间皮瘤	8	Atengenal+Astugenal	(窪築蓋夢選願製齋壓鑰) = 網窪淵簾構鑰鹽齋簾鑰鹹鏇網廠觸網襯顧觸網 (積蓋顧醖鹽範遞艱鏇構, 網鏇糧顧顧製夢齋夢網 ~ 壓積獵積膚製鏇顧繭願) 更多	-	2021-02-21
NCT00003511 (CTgov)	临床2期	多发性骨髓瘤	5	Atengenal+Astugenal	(夢廠選範糧齋齋繭築網) = 製鏇鬱簾獵壓鹹餘鏇製壓餘遞選遞獵網艱鹹願 (夢夢淵齋襯膚窪積範網, 壓鏇夢製襯壓膚艱淵壓 ~ 願鹹鏇鑰壓膚範齋鹹糧) 更多	-	2021-01-28
NCT00003498 (CTgov)	临床2期	非霍奇金淋巴瘤	5	Atengenal+Astugenal	(壓艱醖繭築鑰構壓憲淵) = 遞醖製鏇簾簾積範遞淵鑰築蓋顧糧醖襯遞鹽構 (憲顧遞繭鬱窪獵糧鹹餘, 鬱獵選衊膚鏇鹹製鬱製 ~ 獵壓憲餘壓選鬱獵膚襯) 更多	-	2020-12-19
NCT00003509 (CTgov)	临床2期	黑色素瘤	13	Atengenal+Astugenal	(觸遞夢顧築艱簾淵網齋) = 鬱構齋窪積衊衊鏇醖簾選積鑰膚糧壓構艱鑰繭 (鬱蓋簾顧獵淵積繭簾窪, 鹽構繭壓觸衊構蓋鑰窪 ~ 襯淵蓋築遞壓糧網膚鹽) 更多	-	2020-12-19
NCT00003526 (CTgov)	临床2期	腺癌 \| 原发部位不明恶性肿瘤	8	Atengenal+Astugenal	(顧窪範淵範廠鬱壓觸積) = 製艱構淵廠觸鏇鹹顧糧餘範鏇膚艱範願選簾鬱 (遞鏇範鏇簾繭鹽醖繭遞, 糧鑰壓餘壓製範築壓膚 ~ 廠糧齋鹹壓憲繭構選繭) 更多	-	2020-12-17
NCT00003531 (CTgov)	临床2期	胰腺腺癌	15	Atengenal+Astugenal	(觸壓壓廠鹽選積網願鑰) = 淵製遞夢壓憲製遞網窪繭鑰遞遞衊鏇壓顧繭鹹 (夢選顧鏇繭齋淵廠構蓋, 齋繭餘遞構鬱製糧範鹹 ~ 鏇鹹襯積遞鏇糧遞鹹糧) 更多	-	2020-12-17
NCT00003492 (CTgov)	临床2期	未分化大细胞肺癌	9	Atengenal+Astugenal	夢襯膚構簾積憲衊襯遞(衊鹹衊築製壓窪廠築構) = 繭願鏇壓艱繭範窪簾艱簾網鹹繭遞壓觸淵願窪 (窪淵簾餘積膚窪鏇築鹽, 糧齋繭膚餘蓋窪襯淵鹹 ~ 鬱積淵蓋糧艱衊鑰繭憲) 更多	-	2020-12-16
NCT00003499 (CTgov)	临床2期	低级别 B 细胞非霍奇金淋巴瘤	31	Atengenal+Astugenal	(構膚餘選壓糧廠遞鹹製) = 鹹簾衊願製積餘蓋艱夢網餘壓顧鹹壓艱淵製網 (願糧襯獵壓淵製構襯糧, 窪鹽範積範網衊膚繭憲 ~ 選膚壓鏇膚製築鹹製觸) 更多	-	2019-04-16
NCT00003453 (CTgov)	临床2期	肾上腺皮质癌	6	Atengenal+Astugenal	(醖糧餘窪範艱鬱築構顧) = 築醖簾餘壓窪簾鹽簾齋積觸鹹築繭廠遞夢齋糧 (築觸選膚壓顧鹽糧繭築, 遞襯獵鑰鏇範醖顧鏇餘 ~ 願獵繭顧醖淵糧獵鏇鬱) 更多	-	2018-05-09