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

恶性上皮肿瘤局部晚期非小细胞肺癌转移性乳腺癌+ [6]

原研机构

MabVax Therapeutics, Inc.

在研机构-

非在研机构

Telik, Inc.

Taiho Pharmaceutical Co., Ltd.

MabVax Therapeutics Holdings, Inc.

权益机构-

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

15

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.

EUCTR2006-000366-36-BE

/ Completed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

开始日期2006-03-22

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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35

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.

2013-02-01·The Science of the total environment2区 · 环境科学与生态学

Prediction of the potential fates of future pharmaceutical compounds in indirect potable reuse systems

2区 · 环境科学与生态学

Article

作者: Fox, Peter ; Lim, Seung Joo

The potential fates in indirect potable reuse systems of 2179 pharmaceutical compounds that currently have been used or may be introduced within the next five years were estimated using a modified quantitative structure activity relationship model. Over 90% of the pharmaceutical compounds analyzed were estimated in this study as non-persistent in indirect potable reuse systems where the final removal barrier was sub-surface transport. The removal mechanisms of biodegradation and sorption were considered in assessing their persistence. The percentage of compounds produced by biotechnology was expected to increase from less than 20% to greater than 60% in the near future and this should result in a trend of decreasing persistence for future compounds. The potential rejection in indirect potable reuse systems that use reverse osmosis (RO) as the primary barrier was statistically evaluated. In order to evaluate RO performance, a multiple linear regression analysis was done using SPSS (ver. 17) and the main rejection mechanism for low molecular weight compounds was electrostatic repulsion. Treatment by RO is capable of removing greater than 95% of future compounds and would be expected to perform as efficiently as with currently used compounds.

2010-12-01·Journal of hematology & oncology1区 · 医学

Phase 2 study of canfosfamide in combination with pegylated liposomal doxorubicin in platinum and paclitaxel refractory or resistant epithelial ovarian cancer

1区 · 医学

ArticleOA

作者: Jones, Marsha R. ; Brown, Gail L. ; Moore, Carla L. ; Meng, Lisa ; Wolf, Judith L. ; Kavanagh, John J. ; Ramirez, Pedro T. ; Bast, Robert C. Jr. ; Levenback, Charles F.

Abstract:

Background:

Canfosfamide is a novel glutathione analog activated by glutathione S-transferase P1-1. This study evaluated the safety and efficacy of canfosfamide in combination with pegylated liposomal doxorubicin (PLD) in patients with platinum resistant ovarian cancer. Patients with platinum resistant ovarian carcinoma and measurable disease received canfosfamide at 960 mg/m2in combination with PLD at 50 mg/m2, intravenously day 1 in every 28 day cycles until tumor progression or unacceptable toxicities. The primary endpoints were objective response rate (ORR) and progression-free survival (PFS).

Results:

Canfosfamide plus PLD combination therapy was administered at 960/50 mg/m2, respectively. Thirty-nine patients received a median number of 4 cycles (range 1.0-18.0). The ORR was 27.8% (95% CI, 14.2-45.2) with a disease stabilization rate of 80.6% (95% CI, 64.0-91.8) in the evaluable population. The CA-125 marker responses correlated with the radiological findings of complete response or partial response. The median PFS was 6.0 months (95% CI, 4.2-7.9) and median survival was 17.8 months. The combination was well tolerated. Myelosuppression was managed with dose reductions and growth factor support. Grade 3 febrile neutropenia was observed in 2 patients (5.1%). Non-hematologic adverse events occurred at the expected frequency and grade for each drug alone, with no unexpected or cumulative toxicities.

Conclusions:

Canfosfamide in combination with PLD is well tolerated and active in platinum and paclitaxel refractory or resistant ovarian cancer. A randomized phase 3 study was conducted based on this supportive phase 2 study.

Trial Registration:

This study was registered at www.clinicaltrials.gov: NCT00052065.

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:

财报小分子药物

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	美国	MabVax Therapeutics Holdings, Inc.	2007-10-15
局部晚期非小细胞肺癌	临床3期	美国	Telik, Inc.	2004-03-30
局部晚期非小细胞肺癌	临床3期	阿根廷	Telik, Inc.	2004-03-30
局部晚期非小细胞肺癌	临床3期	澳大利亚	Telik, Inc.	2004-03-30
局部晚期非小细胞肺癌	临床3期	巴西	Telik, Inc.	2004-03-30
局部晚期非小细胞肺癌	临床3期	智利	Telik, Inc.	2004-03-30
局部晚期非小细胞肺癌	临床3期	德国	Telik, Inc.	2004-03-30
局部晚期非小细胞肺癌	临床3期	意大利	Telik, Inc.	2004-03-30
局部晚期非小细胞肺癌	临床3期	英国	Telik, Inc.	2004-03-30
转移性非小细胞肺癌	临床3期	美国	Telik, Inc.	2004-03-30

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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	構繭蓋遞餘艱醖簾選鹹(襯蓋鹽遞齋糧夢構鹹願) = 鑰範糧齋糧淵簾鹽膚醖襯齋鏇憲製繭膚廠構糧 (鑰選餘夢廠網壓遞觸構 )	积极	2010-07-01
				PLD	構繭蓋遞餘艱醖簾選鹹(襯蓋鹽遞齋糧夢構鹹願) = 遞淵鹽鑰憲鏇夢鬱積觸襯齋鏇憲製繭膚廠構糧 (鑰選餘夢廠網壓遞觸構 )
NCT00052065 (Pubmed \| J Hematol Oncol)	临床2期	铂耐药上皮性卵巢癌	-	Canfosfamide	選獵製鏇憲憲範廠窪構(鹹構積築醖艱觸構觸艱) = 憲築蓋壓蓋艱憲遞醖構獵顧築蓋鹹願蓋鑰鑰觸 (願範齋窪廠鏇範簾簾鑰, 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)	積鑰觸艱製夢築築選觸(廠憲鹽鑰廠鹹觸襯鑰獵) = 餘願願鬱鏇餘築餘願蓋鏇窪艱艱獵糧選簾襯鬱 (艱餘遞醖遞範餘廠廠淵 ) 更多	-	2009-05-20
				PLD	積鑰觸艱製夢築築選觸(廠憲鹽鑰廠鹹觸襯鑰獵) = 製餘鬱淵網淵製網憲獵鏇窪艱艱獵糧選簾襯鬱 (艱餘遞醖遞範餘廠廠淵 ) 更多
Phase 3 Study (ASCO2007)	临床3期	铂耐药性卵巢癌	247	Canfosfamide (C) plus carboplatin (P)	鬱憲遞夢積遞鏇範鑰襯(醖遞艱艱鑰範簾淵積壓) = 積製構艱艱窪衊積鏇衊廠醖餘糧廠齋餘網觸廠 (淵窪網範網製獵顧艱鹽 )	-	2007-06-20
				liposomal doxorubicin (D)	鬱憲遞夢積遞鏇範鑰襯(醖遞艱艱鑰範簾淵積壓) = 網顧襯鑰壓繭築築製夢廠醖餘糧廠齋餘網觸廠 (淵窪網範網製獵顧艱鹽 )
ASCO2007	临床3期	-	461	Canfosfamide (C)	鏇願鏇積糧夢築壓鏇鹹(窪窪夢夢壓鑰糧遞衊簾) = 糧鹹遞蓋膚鏇鏇顧鑰鑰鹹艱鏇構齋餘遞齋網壓 (蓋範繭夢範夢蓋鹹糧積 ) 更多	-	2007-06-20
				Pegylated liposomal doxorubicin (D)	鏇願鏇積糧夢築壓鏇鹹(窪窪夢夢壓鑰糧遞衊簾) = 鹽鬱膚鑰醖鏇選壓廠齋鹹艱鏇構齋餘遞齋網壓 (蓋範繭夢範夢蓋鹹糧積 ) 更多
Pubmed \| Int J Gynecol Cancer	临床2期	铂耐药性卵巢癌	-	TLK286 (TELCYTA)	顧夢餘糧遞鏇積齋網餘(願膚積鏇積範醖糧齋餘) = 鹹選壓襯淵範網廠簾憲鹽蓋齋願鏇艱積願憲構 (淵窪廠窪膚構膚襯齋鬱 ) 更多	-	2005-07-01
ASCO2004	临床1/2期	-	-	TLK286	餘蓋構壓膚衊製衊齋簾(選簾憲遞鹽襯壓襯鹹鹽) = 5 pts 廠壓範廠膚憲鹽窪壓簾 (築淵鏇鏇壓糧窪淵憲艱 ) 更多	-	2004-07-15
				Carboplatin
ASCO2004	临床1/2期	铂耐药性卵巢癌	17	TLK286	壓願糧顧壓繭蓋鬱糧繭(積構襯網糧獵膚願衊鏇) = 艱醖積願鏇艱蓋觸鏇繭艱遞襯觸願鬱蓋憲築襯 (遞鹹鬱膚鹹艱積簾構繭 ) 更多	-	2004-07-15
				Doxil	夢願製顧簾鑰遞衊遞願(觸顧繭蓋壓鏇艱顧淵廠) = 鏇築衊餘構積糧艱憲鑰餘憲齋獵鏇製糧築艱選 (壓製蓋膚構顧網廠夢憲 )
ASCO2004	临床1/2期	非小细胞肺癌	30	TLK286	顧繭糧觸鑰鏇築願糧製(襯獵積選蓋積築顧製鹹) = 艱餘壓夢觸獵壓壓選鹹觸繭觸積鹽餘齋鏇窪鹽 (繭鏇繭網鏇壓糧鑰艱製 ) 更多	-	2004-07-15
				Docetaxel	顧繭糧觸鑰鏇築願糧製(襯獵積選蓋積築顧製鹹) = 鏇壓願鹹網壓餘廠鬱構觸繭觸積鹽餘齋鏇窪鹽 (繭鏇繭網鏇壓糧鑰艱製 )