CGC-11047(CGC-11047) - _专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点-

作用方式

刺激剂

作用机制

细胞凋亡刺激剂

治疗领域

肿瘤泌尿生殖系统疾病免疫系统疾病+ [6]

在研适应症-

非在研适应症

晚期恶性实体瘤年龄相关性黄斑变性II型糖原贮积病+ [4]

原研机构

Cellgate, Inc.

在研机构-

非在研机构

Progen Pharmaceuticals, Inc.Epi-Cure Pharmaceuticals, 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C14H36Cl4N4

InChIKeyMNJCMBNLXQCNHO-YGGCHVFLSA-N

CAS号206991-64-2

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关联

5

项与 CGC-11047 相关的临床试验

NCT00446654

/ Completed临床1期

A Phase Ib Randomized Open Label Study Between Once-every-two-weeks and Once-every-four-weeks Treatment of CGC-11047 in Patients With CNV Due to Age Related Macular Degeneration

The purpose of this research study is to determine how safe and effective subconjunctival injections of CGC-11047 are in subjects with wet age related macular degeneration at two different dosing intervals.

开始日期2007-04-01

申办/合作机构

Progen Pharmaceuticals, Inc.

NCT00585416

/ Terminated临床2期IIT

A Phase II Study of CGC-11047 in Patients With Metastatic Hormone Refractory Prostate Cancer (47-02-001)

The purpose of this research is to determine the effectiveness of CGC-11047 in subjects with metastatic hormone refractory prostate cancer as measured by changes in PSA.

开始日期2006-06-01

申办/合作机构

University of Wisconsin Madison

[+1]

NCT00705874

/ Completed临床1期

A Phase I Open Label, Multicenter, Dose-Escalation Study to Determine the Maximum Tolerated Dose, Dose Limiting Toxicity, Safety and Pharmacokinetics of CGC-11047 When Used in Individual Combinations With 1) Gemcitabine or 2) Docetaxel or 3) Bevacizumab or 4) Erlotinib or 5) Cisplatin or 6) 5-Flurouracil or 7) Sunitinib in Patients With Advanced Solid Tumors or Lymphoma

This study will aims to determine the maximum tolerated dose of CGC-11047 when used in individual combinations with gemcitabine, or docetaxel, or bevacizumab, or erlotinib or cisplatin or 5-flurouracil or sunitinib in one of 7 treatment arms. The dose of CGC-11047 will be escalated until the maximum tolerated dose is established.

开始日期2006-05-01

申办/合作机构

Progen Pharmaceuticals, Inc.

100 项与 CGC-11047 相关的临床结果

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100 项与 CGC-11047 相关的转化医学

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100 项与 CGC-11047 相关的专利（医药）

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27

项与 CGC-11047 相关的文献（医药）

2021-01-01·Cancer Chemotherapy and Pharmacology4区 · 医学

A Phase Ib multicenter, dose-escalation study of the polyamine analogue PG-11047 in combination with gemcitabine, docetaxel, bevacizumab, erlotinib, cisplatin, 5-fluorouracil, or sunitinib in patients with advanced solid tumors or lymphoma

4区 · 医学

Article

作者: Becerra, Carlos H Roberto ; Garbo, Lawrence E ; Stephenson, Joe J ; Richards, Donald A ; Wu, Hillary H ; Von Hoff, Daniel ; Casero, Robert A ; Vogelzang, Nicholas J ; Murray Stewart, Tracy ; Boyd, Thomas E ; Smith, David A ; Jotte, Robert M ; Fitzgerald, Michael ; Marton, Laurence J ; Conkling, Paul R

PURPOSEPolyamines are absolutely essential for maintaining tumor cell proliferation. PG-11047, a polyamine analogue, is a nonfunctional competitor of the natural polyamine spermine that has demonstrated anticancer activity in cells and animal models of multiple cancer types. Preclinical investigations into the effects of common chemotherapeutic agents have revealed overlap with components of the polyamine metabolic pathway also affected by PG-11047. This report describes a Phase Ib clinical trial investigating PG-11047 in combination with cytotoxic and anti-angiogenic chemotherapeutic agents in patients with advanced refractory metastatic solid tumors or lymphoma.METHODSA total of 172 patients were assigned to treatment arms based on cancer type to receive the appropriate standard-of-care therapy (gemcitabine, docetaxel, bevacizumab, erlotinib, cisplatin, 5-fluorouracil (5-FU), or sunitinib as directed) along with once weekly intravenous infusions of PG-11047. PG-11047 dose escalation ranged from 50 to 590 mg.RESULTSThe maximum tolerated dose (MTD) of PG-11047 in combination with bevacizumab, erlotinib, cisplatin, and 5-FU was 590 mg. Dose-limiting toxicities (DLTs) in these groups were rare (5 of 148 patients). Overall partial responses (PR) were observed in 12% of patients treated with PG-11047 and bevacizumab, with stable disease documented in an additional 40%. Stable disease occurred in 71.4% of patients in the 5-FU arm, 54.1% in the cisplatin arm, and 33.3% in the erlotinib arm. Four of the patients receiving cisplatin + PG-11047 (20%) had unconfirmed PRs. MTDs for gemcitabine, docetaxel, and sunitinib could not be determined due to DLTs at low doses of PG-11047 and small sample size.CONCLUSIONSResults of this Phase Ib trial indicate that PG-11047 can be safely administered to patients in combination with bevacizumab, erlotinib, cisplatin, and 5-FU on the once weekly dosing schedule described and may provide therapeutic benefit. The manageable toxicity profile and high MTD determination provide a safety profile for further clinical studies.

2020-06-01·Cancer Chemotherapy and Pharmacology4区 · 医学

A phase I dose-escalation study of the polyamine analog PG-11047 in patients with advanced solid tumors

4区 · 医学

Article

作者: Casero, Robert A ; Desai, Apurva A ; Fitzgerald, Michael L ; Marton, Laurence J ; Murray Stewart, Tracy

PURPOSEPolyamines are essential for the sustained proliferation and biomass required by tumor cells. Bis-alkylated polyamine analogs are nonfunctional competitors of natural polyamines. Of these, PG-11047, a second-generation unsaturated analog of the polyamine spermine, has demonstrated anticancer activity in cell lines and animal models of multiple cancer types. This report describes the first phase I clinical trial to investigate PG-11047 in patients with advanced refractory metastatic solid tumors.METHODSForty-six patients were treated with 60-min intravenous infusions of PG-11047 using a 28-day dosing cycle with treatments on days 1, 8, and 15. Doses ranged from 50 to 750 mg. The treatment period consisted of at least two cycles.RESULTSThe maximum tolerated dose of PG-11047 administered at this dosing schedule was 610 mg. Dose-limiting toxicities (DLT) were mainly gastrointestinal, including oral/anal mucositis and diarrhea; other DLTs included one case each of angioedema and a grade 3 alanine aminotransferase (ALT) increase. The most common adverse effects were fatigue and anorexia. Stable disease was documented in 30% of patients.CONCLUSIONResults of this phase I trial suggest that PG-11047 can be safely administered to patients on the once weekly dosing schedule described. The manageable toxicity profile and high MTD determination provide a safety profile for further clinical studies, including those in combination with current chemotherapeutic agents.

2018-09-04·Molecular Pharmaceutics2区 · 医学

Polymeric Prodrugs Targeting Polyamine Metabolism Inhibit Zika Virus Replication

2区 · 医学

Article

作者: Xie, Ying ; Dunworth, Matthew ; Casero, Robert A. ; Oupicky, David ; Routhu, Nanda Kishore ; Byrareddy, Siddappa N.

The Zika virus (ZIKV) is primarily transmitted via an infected mosquito bite, during sexual intercourse, or in utero mother to child transmission. When a fetus is infected, both neurological malformations and deficits in brain development are frequently manifested. As such, there is a need for vaccines or drugs that may be used to cure ZIKV infections. Metabolic pathways play a crucial role in cell differentiation and development. More importantly, polyamines play a key role in replication and translation of several RNA viruses, including ZIKV, Dengue virus, and Chikungunya virus. Here, we present polyamine analogues (BENSpm and PG11047) and their corresponding polymer prodrug derivatives for inhibiting ZIKV infection by intersecting with polyamine catabolism pathways. We tested the compounds against ZIKV African (MR766) and Asian (PRVABC59) strains in human kidney epithelial (Vero) and glioblastoma derived (SNB-19) cell lines. Our results demonstrate potent inhibition of ZIKV viral replication in both cell lines tested. This antiviral effect was mediated by the upregulation of two polyamine catabolic enzymes, spermine oxidase, and spermidine (SMOX)/spermine N1-acetyltransferase (SAT1) as apparent reduction of the ZIKV infection following heterologous expression of SMOX and SAT1. On the basis of these observations, we infer potential use of these polyamine analogues to treat ZIKV infections.

100 项与 CGC-11047 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB05722

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
年龄相关性黄斑变性	临床2期	美国	Progen Pharmaceuticals, Inc.	2007-04-01
年龄相关性黄斑变性	临床2期	墨西哥	Progen Pharmaceuticals, Inc.	2007-04-01
II型糖原贮积病	临床2期	美国	Progen Pharmaceuticals, Inc.	2007-04-01
II型糖原贮积病	临床2期	墨西哥	Progen Pharmaceuticals, Inc.	2007-04-01
II型糖原贮积病	临床2期	俄罗斯	Progen Pharmaceuticals, Inc.	2007-04-01
转移性去势抵抗性前列腺癌	临床2期	美国	Progen Pharmaceuticals, Inc.	2006-06-01
晚期恶性实体瘤	临床2期	美国	Progen Pharmaceuticals, Inc.	2006-05-01
复发性淋巴瘤	临床2期	美国	Progen Pharmaceuticals, Inc.	2006-01-01
难治性淋巴瘤	临床2期	美国	Progen Pharmaceuticals, Inc.	2006-01-01
实体瘤	临床2期	美国	Epi-Cure Pharmaceuticals, 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


NCT00705653 (Pubmed \| Cancer Chemother Pharmacol)	临床1期	晚期恶性实体瘤	46	PG-11047	(蓋獵獵範鹽顧顧窪膚選) = 鏇願襯衊蓋願鏇膚壓遞積膚醖遞鹹積醖憲醖獵 (襯構鑰鑰憲獵蓋獵繭膚 ) 更多	-	2020-06-01
NCT00446654 (CTgov)	临床1期	年龄相关性黄斑变性 \| II型糖原贮积病	43	CGC-11047 (CGC-11047 Once Every 2 Weeks)	簾襯艱獵選襯鑰壓齋鹽(糧廠願繭鑰築壓窪鏇網) = 鬱衊淵膚窪襯觸願鬱獵築夢繭顧範獵鏇遞願築 (築齋艱鹹膚襯醖觸製蓋, 壓醖構鑰夢願蓋醖廠廠 ~ 鹹製淵製膚餘築淵壓壓) 更多	-	2012-08-06
NCT00446654 (CTgov)	临床1期	年龄相关性黄斑变性 \| II型糖原贮积病	43	CGC-11047 (CGC-11047 Once Every Four Weeks)	簾襯艱獵選襯鑰壓齋鹽(糧廠願繭鑰築壓窪鏇網) = 築鹽願蓋鹹醖襯繭遞願築夢繭顧範獵鏇遞願築 (築齋艱鹹膚襯醖觸製蓋, 選襯襯艱窪窪積網淵夢 ~ 觸糧夢遞網簾鹹網繭廠) 更多	-	2012-08-06
NCT00705653 (CTgov)	临床1期	实体瘤	46	PG-11047	淵願齋憲製築觸築繭窪(醖鹽繭膚製憲淵獵廠範) = 餘獵鹽鏇鹽衊願淵衊齋願構廠獵選構顧願餘憲 (憲網襯淵衊鹹廠艱選鏇, 廠顧鹹憲顧艱蓋選餘鬱 ~ 顧齋餘觸遞廠夢選糧構) 更多	-	2012-02-27
NCT00705874 (CTgov)	临床1期	晚期恶性实体瘤 \| 淋巴瘤	172	Gemcitabine+PG-11047 (PG11047/Gemcitabine)	(構壓觸醖鹽鬱餘鬱壓蓋) = 顧襯願夢鏇繭憲淵獵選繭壓衊襯夢夢簾襯鏇鏇 (積繭鏇積築齋築願壓選, 觸選鏇廠襯鹹鑰獵衊願 ~ 鹽醖繭簾壓製齋鏇廠繭) 更多	-	2012-02-27
NCT00705874 (CTgov)	临床1期	晚期恶性实体瘤 \| 淋巴瘤	172	Docetaxel (PG11047/Docetaxel)	(構壓觸醖鹽鬱餘鬱壓蓋) = 糧壓獵繭廠窪積鬱鹹構繭壓衊襯夢夢簾襯鏇鏇 (積繭鏇積築齋築願壓選, 範窪鏇淵廠齋積願願廠 ~ 繭窪鏇觸鬱憲積鹹鬱憲) 更多	-	2012-02-27