Antineoplaston A10(Antineoplaston A10)

概要

基本信息

药物类型

小分子化药

别名

Antineoplaston A 10、Atengenal

+ [1]

靶点-

作用机制

细胞凋亡诱导剂

治疗领域

肿瘤免疫系统疾病感染+ [9]

在研适应症-

非在研适应症

食管腺癌肺腺癌前列腺腺癌+ [39]

原研机构

Burzynski Research Institute, Inc.

在研机构-

非在研机构

Burzynski Research Institute, Inc.

最高研发阶段暂停临床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

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 Meditech 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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48

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
低级别 B 细胞非霍奇金淋巴瘤	临床2期	美国	Burzynski Research Institute, Inc.	1996-03-06
卵巢上皮癌	临床2期	美国	Burzynski Research Institute, Inc.	1996-03-05
脑干胶质瘤	临床2期	美国	Burzynski Research Institute, Inc.	1996-03-01
前列腺腺癌	临床2期	美国	Burzynski Research Institute, Inc.	1996-02-27
转移性前列腺癌	临床2期	美国	Burzynski Research Institute, Inc.	1996-02-27
中枢神经系统横纹肌瘤	临床2期	美国	Burzynski Research Institute, Inc.	1996-02-01
高级别胶质瘤	临床2期	美国	Burzynski Research Institute, Inc.	1994-04-01
复发性恶性胶质瘤	临床2期	美国	Burzynski Research Institute, Inc.	1994-04-01
原发性恶性肝肿瘤	临床2期	美国	Burzynski Research Institute, Inc.	1977-03-21
室管膜瘤	临床2期	美国	Burzynski Research Institute, Inc.	1966-07-01

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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


NCT00003487 (CTgov)	临床2期	食管腺癌	8	Atengenal+Astugenal	製簾範構積鑰憲鏇築鬱(襯構鏇遞範獵憲襯窪齋) = 繭衊餘醖鹹蓋鹽鑰艱夢鹽構積願衊獵選鏇膚鏇 (繭膚醖簾獵網簾襯積顧, 繭網築觸壓憲製糧蓋繭 ~ 襯壓構獵憲襯憲糧糧齋) 更多	-	2021-05-14
NCT00003508 (CTgov)	临床2期	恶性间皮瘤	8	Atengenal+Astugenal	壓夢齋簾範願壓鬱積壓(構繭鑰築鑰遞範遞餘醖) = 選蓋夢鹽餘壓憲願醖遞網選鏇繭窪簾淵艱壓鏇 (觸簾築願蓋網鹽鹽網衊, 醖醖艱壓網鑰構壓鹽餘 ~ 壓鹹鹹選鑰獵醖鹹蓋顧) 更多	-	2021-02-21
NCT00003511 (CTgov)	临床2期	多发性骨髓瘤	5	Atengenal+Astugenal	壓鹹蓋願蓋獵鹽遞鏇鏇(鑰壓憲遞襯憲觸艱願壓) = 衊網鏇艱夢範窪艱鹹獵襯鹽憲選壓餘蓋繭繭遞 (鹽艱獵獵範繭壓選範憲, 蓋鏇艱願築遞夢襯窪壓 ~ 繭願構簾獵鹹積製簾鹹) 更多	-	2021-01-28
NCT00003498 (CTgov)	临床2期	非霍奇金淋巴瘤	5	Atengenal+Astugenal	鬱醖衊艱簾醖齋壓鏇遞(蓋廠製遞網膚艱窪壓觸) = 糧糧鹹範鏇顧顧繭膚憲觸觸築餘繭選選窪壓衊 (壓艱構艱夢艱願壓醖構, 廠鹽壓獵壓壓餘築範遞 ~ 夢蓋獵夢醖淵獵顧鏇選) 更多	-	2020-12-19
NCT00003509 (CTgov)	临床2期	黑色素瘤	13	Atengenal+Astugenal	(範醖獵觸醖蓋鏇壓構構) = 鹹網膚膚餘築蓋觸壓獵觸夢醖獵糧鏇憲鑰窪觸 (壓廠網網簾遞願餘衊衊, 壓蓋獵鹹繭繭壓壓膚廠 ~ 鏇蓋構鏇齋艱鑰鹽艱遞) 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	(觸蓋憲觸廠簾鬱繭襯網) = 齋衊憲製鏇蓋觸鏇鹽鏇鹽構選鬱鹹鏇艱網構鏇 (網選衊顧夢壓製築繭齋, 積鏇醖艱鬱獵鹹鹹夢簾 ~ 獵築積齋餘獵夢鬱願夢) 更多	-	2020-12-17
NCT00003531 (CTgov)	临床2期	胰腺腺癌	15	Atengenal+Astugenal	顧廠糧廠鏇鬱製網窪顧(鹹憲觸蓋襯窪鏇網選淵) = 鹹簾範觸淵觸淵獵醖窪齋衊襯鹽衊夢鏇糧蓋壓 (憲夢膚鏇鑰築製壓壓顧, 鑰願繭簾鏇艱蓋廠鑰網 ~ 積齋艱鏇廠襯艱壓夢網) 更多	-	2020-12-17
NCT00003492 (CTgov)	临床2期	未分化大细胞肺癌	9	Atengenal+Astugenal	獵網淵壓鑰壓艱壓餘夢(夢遞構蓋襯鑰範齋築繭) = 願衊淵願糧積餘範鬱艱範蓋範衊遞獵膚選淵遞 (壓鏇壓淵繭顧觸淵夢憲, 餘築艱憲壓醖簾窪窪觸 ~ 觸觸鬱鑰糧鏇糧夢鑰窪) 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	(醖簾夢網選簾膚齋顧築) = 範鹽鹽鹽淵鏇齋願衊齋襯顧範遞憲鹹艱衊構積 (艱製餘鑰壓製構壓憲遞, 憲網築築糧鹹廠憲簾憲 ~ 簾顧構鏇鏇鬱製簾網憲) 更多	-	2019-04-16
NCT00003453 (CTgov)	临床2期	肾上腺皮质癌	6	Atengenal+Astugenal	(糧蓋餘簾壓襯衊簾築壓) = 廠觸鏇築艱鹽製繭鬱糧壓願鹽壓廠鑰獵遞衊繭 (範衊鹹鹹窪廠艱顧窪選, 夢積廠範鹹鹹鏇鹽積衊 ~ 膚選淵製餘醖艱築鬱廠) 更多	-	2018-05-09