Canfosfamide Hydrochloride(Canfosfamide Hydrochloride) - 药物靶点：DNA_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Canfosfamide、Canfosfamide hydrochloride (USAN)、TER 286

+ [4]

靶点

DNA

作用方式

抑制剂

作用机制

DNA抑制剂(DNA抑制剂)、DNA烷化剂

治疗领域

肿瘤内分泌与代谢疾病呼吸系统疾病+ [4]

在研适应症-

非在研适应症

晚期非小细胞肺癌恶性上皮肿瘤转移性乳腺癌+ [6]

原研机构

MabVax Therapeutics, Inc.

在研机构-

非在研机构

Telik, Inc.

MabVax Therapeutics Holdings, Inc.

Taiho Pharmaceutical Co., Ltd.

最高研发阶段终止临床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C26H41Cl5N5O10PS

InChIKeyNECZZOFFLFZNHL-XVGZVFJZSA-N

CAS号439943-59-6

关联

14

项与 Canfosfamide Hydrochloride 相关的临床试验

NCT01148108

/ Completed临床2期

Phase 2 Study of Canfosfamide HCl for Injection (Telcyta®, TLK286)in Refractory or Relapsed Mantle Cell Lymphoma (MCL), Diffuse Large B Cell Lymphoma (DLBCL) and Multiple Myeloma (MM)

This is a Phase 2 study to determine the efficacy and safety of canfosfamide treatment in relapsed or refractory mantle cell lymphoma, diffuse large B cell lymphoma and multiple myeloma. The study will be conducted in two stages with 5-6 patients in each indication in Stage 1 and if responses are observed an additional 10 patients in Stage 2 in each group.

开始日期2010-06-01

申办/合作机构

Telik, Inc.

NCT00350948

/ Terminated临床3期

Phase 3 Randomized Study of TLK286 (Telcyta®) in Combination With Liposomal Doxorubicin (Doxil/Caelyx)Versus Liposomal Doxorubicin (Doxil/Caelyx) as Second-Line Therapy in Platinum Refractory or Resistant Ovarian Cancer (ASSIST-5)

The purpose of this research study is to determine if Telcyta® given in combination with liposomal doxorubicin is more effective than liposomal doxorubicin alone in treating women who have recurrent ovarian epithelial cancer, fallopian tube cancer or primary peritoneal cancer that is refractory or resistant to platinum chemotherapy.

开始日期2006-05-01

申办/合作机构

Telik, Inc.

NCT00102973

/ Completed临床3期

Phase III Randomized Study of TLK286 (Telcyta) in Combination With Carboplatin (Paraplatin) Versus Liposomal Doxorubicin (Doxil) as Second-Line Therapy in Platinum Refractory or Resistant Ovarian Cancer [ASSIST-3]

The purpose of this research study is to determine if TLK286 given in combination with carboplatin is more effective than liposomal doxorubicin in treating women who have recurrent ovarian epithelial cancer, fallopian tube cancer, or primary peritoneal cancer, that is refractory or resistant to platinum chemotherapy.

开始日期2004-12-01

申办/合作机构

Telik, Inc.

100 项与 Canfosfamide Hydrochloride 相关的临床结果

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100 项与 Canfosfamide Hydrochloride 相关的转化医学

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100 项与 Canfosfamide Hydrochloride 相关的专利（医药）

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47

项与 Canfosfamide Hydrochloride 相关的文献（医药）

2018-03-08·Journal of medicinal chemistry1区 · 医学

Glutathione S-Transferase π-Activatable O²-(Sulfonylethyl Derived) Diazeniumdiolates Potently Suppress Melanoma in Vitro and in Vivo

1区 · 医学

Article

作者: Kaur, Jatinder ; Zhang, Yinqiu ; Yuan, Haoliang ; Zou, Yu ; Wu, Jianbing ; Huang, Zhangjian ; Fei, Yue ; Zhang, Yihua ; Bhardwaj, Atul ; Knaus, Edward E.

A group of glutathione S-transferase π (GSTπ) activatable O²-(sulfonylethyl derived) diazeniumdiolates 5-12 were designed and synthesized. These compounds could be activated by GSTπ to initiate the β-elimination reaction, liberating an active vinyl sulfone-based GSH derivative and a diazeniumdiolate anion which subsequently releases NO in situ. The most active compound 6 released relatively high levels of NO and inhibited proliferation of melanoma B16 cells, superior to a diazeniumdiolate-based anticancer agent JS-K (1). Importantly, 6 had 8-fold less inhibitory activity against normal epithelial JB6 Cl 30-7b cells. The inhibitory activity of 6 could be diminished by an NO scavenger or GSTπ inhibitor. Furthermore, 6 induced nitration of mitochondrial tyrosine in B16 cells and inoculated B16 tumors in mice, which might be responsible for oxidation of protein leading to tumor suppression. Finally, 6 significantly retarded the B16 cells growth in a mouse xenograft model. These findings suggest that 6 may have a potential to treat melanoma.

2013-11-12·Biochemistry3区 · 生物学

Mechanism of Glutathione Transferase P1-1-Catalyzed Activation of the Prodrug Canfosfamide (TLK286, TELCYTA)

3区 · 生物学

Article

作者: Fernandes, Pedro Alexandrino ; Ramos, Maria João ; Mannervik, Bengt ; Dourado, Daniel F. A. R.

Canfosfamide (TLK286, TELCYTA) is a prodrug that upon activation by glutathione transferase P1-1 (GST P1-1) yields an anticancer alkylating agent and a glutathione derivative. The rationale underlying the use of TLK286 in chemotherapy is that tumor cells overexpressing GST P1-1 will be locally exposed to the released alkylating agent with limited collateral toxicity to the surrounding normal tissues. TLK286 has demonstrated clinical effects in phase II and III clinical trials for the treatment of malignancies, such as ovarian cancer, nonsmall cell lung cancer, and breast cancer, as a single agent and in combination with other chemotherapeutic agents. In spite of these promising results, the detailed mechanism of GST P1-1 activation of the prodrug has not been elucidated. Here, we propose a mechanism for the TLK286 activation by GST P1-1 on the basis of density functional theory (DFT) and on potential of mean force (PMF) calculations. A catalytic water molecule is instrumental to the activation by forming a network of intermolecular interactions between the active-site Tyr7 hydroxyl and the sulfone and COO(-) groups of TLK286. The results obtained are consistent with the available experimental kinetic data and provide an atomistic understanding of the TLK286 activation mechanism.

2013-09-01·The oncologist2区 · 医学

The Role of Pegylated Liposomal Doxorubicin in Ovarian Cancer: A Meta-Analysis of Randomized Clinical Trials

2区 · 医学

Article

作者: La-Beck, Ninh M. ; Alzghari, Saeed ; Gibson, Jean-Marie ; Trantham, Holly ; Ahn, Chul

Learning Objectives:

Determine circumstances under which ovarian cancer patients would benefit from carboplatin plus pegylated liposomal doxorubicin rather than carboplatin plus paclitaxel. Compare and contrast efficacy and toxicity profiles of carboplatin plus pegylated liposomal doxorubicin versus carboplatin plus paclitaxel. Compare and contrast efficacy and toxicity profiles of single agent pegylated liposomal doxorubicin versus topotecan, gemcitabine, olaparib, patupilone, and canfosfamide.

1

项与 Canfosfamide Hydrochloride 相关的新闻（医药）

2007-08-02

·BioSpace

Telik, Inc. Announces 2007 Second Quarter Financial Release, Conference Call and Webcast

PALO ALTO, Calif., Aug. 1 /PRNewswire-FirstCall/ -- Telik, Inc. announced that its 2007 second quarter conference call and webcast will be held on Wednesday, August 8, 2007 at 4:30 p.m. Eastern time (1:30 p.m. Pacific time) following the release earlier that day of the company's financial results for the second quarter and six months ended June 30, 2007. The conference call will be accessible via Telik's website at or by telephone at 888-428-4473 or 612-332-0107. An archive of the conference call will be available on the Telik website or by telephone at 800-475-6701 or 320-365-3844, access code 882545. The archive will be available from approximately 8:30 p.m. Eastern time on August 8 through August 15, 2007. Telik, Inc. of Palo Alto, CA is a biopharmaceutical company focused on discovering, developing and commercializing novel small molecule drugs to treat serious diseases. The company's most advanced drug development candidate is TELCYTA, a tumor-activated small molecule product candidate in clinical development for the treatment of advanced ovarian cancer and non-small cell lung cancer. A second drug development candidate, TELINTRA(TM), is in clinical development for myelodysplastic syndrome. Telik's product candidates were discovered using its proprietary drug discovery technology, TRAP(TM), which enables the rapid and efficient discovery of small molecule drug candidates. Additional information is available at . Telik, Inc. CONTACT: Carol D. DeGuzman, Senior Director, Corporate Communications ofTelik, Inc., +1-650-845-7728, cdeguzman@telik.com Web site:

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100 项与 Canfosfamide Hydrochloride 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D03351	-	-	DB04972

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
非小细胞肺癌	临床3期	阿根廷	Telik, Inc.	2004-03-26
非小细胞肺癌	临床3期	澳大利亚	Telik, Inc.	2004-03-26
非小细胞肺癌	临床3期	巴西	Telik, Inc.	2004-03-26
非小细胞肺癌	临床3期	智利	Telik, Inc.	2004-03-26
非小细胞肺癌	临床3期	德国	Telik, Inc.	2004-03-26
非小细胞肺癌	临床3期	意大利	Telik, Inc.	2004-03-26
非小细胞肺癌	临床3期	英国	Telik, Inc.	2004-03-26
铂耐药性卵巢癌	临床3期	美国	Telik, Inc.	2003-06-01
铂耐药性卵巢癌	临床3期	阿根廷	Telik, Inc.	2003-06-01
铂耐药性卵巢癌	临床3期	比利时	Telik, Inc.	2003-06-01

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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


NCT00350948 (Pubmed \| Int J Gynecol Cancer)	临床3期	铂耐药性卵巢癌	125	Canfosfamide + PLD	鹽繭夢築鹽鏇糧餘餘積(蓋鹽網衊衊糧醖壓膚艱) = 網餘襯淵廠衊選積淵艱鏇壓艱糧淵鏇憲餘獵獵 (構憲鑰遞鑰簾壓廠製構 )	积极	2010-07-01
				PLD	鹽繭夢築鹽鏇糧餘餘積(蓋鹽網衊衊糧醖壓膚艱) = 選夢積淵壓淵憲製範選鏇壓艱糧淵鏇憲餘獵獵 (構憲鑰遞鑰簾壓廠製構 )
NCT00052065 (Pubmed \| J Hematol Oncol)	临床2期	铂耐药上皮性卵巢癌	-	Canfosfamide	蓋餘壓簾鑰窪衊構遞蓋(壓繭製憲廠築構範築遞) = 網簾壓蓋糧艱顧鑰醖築鏇願衊壓築顧顧糧衊願 (願壓膚夢艱鏇願獵選繭, 14.2 ~ 45.2) 更多	-	2010-03-11
ASCO2009	临床3期	难治性卵巢癌 \| 铂耐药性卵巢癌二线	244	Canfosfamide (C) plus pegylated liposomal doxorubicin (PLD)	獵顧夢壓觸鏇夢糧蓋餘(鑰夢齋鬱觸鑰鏇淵蓋願) = 選醖獵遞壓獵膚網淵蓋網夢鑰鏇簾憲壓鹹壓鏇 (觸壓齋糧膚夢範鹹醖壓 ) 更多	-	2009-05-20
				PLD	獵顧夢壓觸鏇夢糧蓋餘(鑰夢齋鬱觸鑰鏇淵蓋願) = 繭構醖鏇醖積壓膚蓋築網夢鑰鏇簾憲壓鹹壓鏇 (觸壓齋糧膚夢範鹹醖壓 ) 更多
ASCO2007	临床3期	铂耐药性卵巢癌	461	Canfosfamide (C)	積網願顧窪窪範衊餘願(鏇繭淵製夢衊觸獵築顧) = 願餘鹽選範蓋餘醖夢廠遞範鹹鹹網構餘構夢顧 (襯鹽齋衊製構廠構蓋窪 ) 更多	-	2007-06-20
				Pegylated liposomal doxorubicin (D)	積網願顧窪窪範衊餘願(鏇繭淵製夢衊觸獵築顧) = 觸遞壓鏇網範夢壓夢廠遞範鹹鹹網構餘構夢顧 (襯鹽齋衊製構廠構蓋窪 ) 更多
ASCO2007	临床3期	铂耐药性卵巢癌	247	Canfosfamide (C) plus carboplatin (P)	餘鹹繭選艱獵膚憲憲憲(餘範鬱鏇製糧構廠鬱網) = 鑰廠範積艱繭憲範獵膚築醖繭築憲憲構築願齋 (築築構網鹹顧鏇獵範製 )	-	2007-06-20
				liposomal doxorubicin (D)	餘鹹繭選艱獵膚憲憲憲(餘範鬱鏇製糧構廠鬱網) = 鑰選壓襯憲顧膚鹹襯顧築醖繭築憲憲構築願齋 (築築構網鹹顧鏇獵範製 )
Pubmed \| Int J Gynecol Cancer	临床2期	铂耐药性卵巢癌	-	TLK286 (TELCYTA)	鹹鏇淵製簾鹽鬱壓憲糧(願築願齋獵衊廠鑰壓壓) = 鹽糧艱餘糧繭積膚積願範淵餘壓鑰積蓋蓋選鹹 (醖鬱餘製製艱壓醖醖鏇 ) 更多	-	2005-07-01
ASCO2004	临床1/2期	铂耐药性卵巢癌	-	TLK286	襯餘醖網醖鏇蓋膚壓構(網獵壓簾網襯願顧蓋製) = 5 pts 蓋鑰顧蓋蓋齋窪範網窪 (獵艱築繭廠鏇獵顧選鬱 ) 更多	-	2004-07-15
				Carboplatin
ASCO2004	临床1/2期	铂耐药性卵巢癌	17	TLK286	網遞築憲範齋膚淵觸壓(觸顧蓋製蓋鹽餘鹽夢糧) = 觸鬱築鬱觸齋構糧願觸鹹襯憲願艱簾遞糧糧製 (壓鹹顧築衊夢艱網築鹹 ) 更多	-	2004-07-15
				Doxil	窪範襯鑰顧築遞壓簾鹹(顧製憲窪糧窪衊餘繭糧) = 憲簾繭積鏇獵積顧鏇鏇廠鏇鬱範窪壓衊壓鬱壓 (鹽鏇衊糧憲餘網簾觸網 )
ASCO2004	临床1/2期	非小细胞肺癌	30	TLK286	範顧襯築糧艱鹽醖鹽鹹(願顧蓋鹽廠繭鹽製憲鏇) = 夢窪齋願鑰製選鏇製鏇襯鬱鬱鑰選憲夢壓糧鬱 (鬱襯網顧鏇網鬱糧簾網 ) 更多	-	2004-07-15
				Docetaxel	範顧襯築糧艱鹽醖鹽鹹(願顧蓋鹽廠繭鹽製憲鏇) = 窪餘鹹築遞鏇獵鑰廠衊襯鬱鬱鑰選憲夢壓糧鬱 (鬱襯網顧鏇網鬱糧簾網 )