RS-130830(RS-130830) - 药物靶点：MMPs_专利_临床

概要

基本信息

药物类型

小分子化药

别名

CTS-1027、RO-1130830

靶点

MMPs

作用机制

MMPs抑制剂(基质金属蛋白酶家族抑制剂)

治疗领域

感染消化系统疾病皮肤和肌肉骨骼疾病

在研适应症-

非在研适应症

关节炎丙型肝炎慢性丙型肝炎

原研机构

F. Hoffmann-La Roche Ltd.

在研机构-

非在研机构

Conatus Pharmaceuticals, Inc.F. Hoffmann-La Roche Ltd.

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-

结构

分子式C19H20ClNO6S

InChIKeyROSNVSQTEGHUKU-UHFFFAOYSA-N

CAS号193022-04-7

关联

4

项与 RS-130830 相关的临床试验

NCT01273064 / Terminated临床2期

A Placebo-Controlled, Multicenter, Double-Blind, Randomized Trial of Pegylated Interferon Plus Ribavirin With or Without CTS-1027 in HCV Null-Responders

Placebo controlled, double-blind, multicenter study utilizing standard of care (SOC) treatment (ribavirin plus pegylated interferon) in combination with CTS-1027 in genotype 1 chronic Hepatitis C (HCV) patients who were null-responders to previous SOC therapy(ies).
Null-responders are defined as patients who failed to achieve a greater than 2 log drop in HCV-RNA (Hepatitis C Ribonucleic acid, also known as "viral load") levels after 12 weeks of treatment (know as an "early virologic response", or EVR) during previous SOC therapy.
If, during previous SOC treatment, a patient had a less than 2 log decline in HCV-RNA at Week 12 but greater than 2 log decline in HCV-RNA at any time from Week 12 to Week 24, that patient is not a null-responder, and is excluded from study participation. If, during previous SOC treatment, a Week 12 HCV-RNA was not obtained, the post Week 12 response must have been < 2 log decline (and still HCV-RNA positive) in order for the patient to be defined as a null-responder.
Patients will be screened and have up to 4 weeks to qualify for study entry. During this screening period, clinical and laboratory tests will be performed. At Week 0/Day 1, patients will undergo centralized, stratified (based on ethnicity), randomization to one of four treatment arms: SOC + one of three doses of CTS-1027 or SOC + placebo. Study treatment will last 24, 48, or 60 weeks, based on each patient's response to study treatment. SOC + placebo patients who do not show a virologic response after 12 weeks of therapy will be rolled onto SOC + 15mg CTS-1027, while maintaining the study blind.

开始日期2011-01-01

申办/合作机构

Conatus Pharmaceuticals, Inc.

NCT01051921 / Completed临床2期

An Open-Label Trial of Pegylated Interferon Plus Ribavirin in Combination With CTS-1027 in HCV Null-Responders

The purpose of this study is to determine if the combination treatment of CTS-1027, pegylated interferon and ribavirin can improve the response rates in HCV patients who did not previously respond to pegylated interferon and ribavirin therapy.

开始日期2010-01-01

申办/合作机构

Conatus Pharmaceuticals, Inc.

NCT00925990 / Completed临床2期

A Trial of CTS-1027 in Interferon-Naive Hepatitis C Patients

The study is intended to determine whether CTS-1027 either alone or in combination with ribavirin is safe and effective in Hepatitis C patients who have not previously been treated with interferon.

开始日期2009-06-01

申办/合作机构

Conatus Pharmaceuticals, Inc.

100 项与 RS-130830 相关的临床结果

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100 项与 RS-130830 相关的转化医学

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100 项与 RS-130830 相关的专利（医药）

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7

项与 RS-130830 相关的文献（医药）

2015-12-01·Journal of neuroinflammation1区 · 医学

The matrix metalloproteinase inhibitor RS-130830 attenuates brain injury in experimental pneumococcal meningitis

1区 · 医学

ArticleOA

作者: Leib, Stephen L ; Leppert, David ; Grandgirard, Denis ; Bächtold, Fabian ; Liechti, Fabian D

BACKGROUND:

Pneumococcal meningitis (PM) is characterized by high mortality and morbidity including long-term neurofunctional deficits. Neuropathological correlates of these sequelae are apoptosis in the hippocampal dentate gyrus and necrosis in the cortex. Matrix metalloproteinases (MMPs) play a critical role in the pathophysiology of PM. RS-130830 (Ro-1130830, CTS-1027) is a potent partially selective inhibitor of MMPs of a second generation and has been evaluated in clinical trials as an anti-arthritis drug. It inhibits MMPs involved in acute inflammation but has low activity against MMP-1 (interstitial collagenase), MMP-7 (matrilysin) and tumour necrosis factor α converting enzyme (TACE).

METHODS:

A well-established infant rat model of PM was used where live Streptococcus pneumoniae were injected intracisternally and antibiotic treatment with ceftriaxone was initiated 18 h post infection (hpi). Treatment with RS-130830 (75 mg/kg bis in die (bid) i.p., n = 40) was started at 3 hpi while control littermates received the vehicle (succinylated gelatine, n = 42).

RESULTS:

Cortical necrosis was significantly attenuated in animals treated with RS-130830, while the extent of hippocampal apoptosis was not influenced. At 18 hpi, concentrations of interleukin (IL)-1β and IL-10 were significantly lower in the cerebrospinal fluid of treated animals compared to controls. RS-130830 significantly reduced weight loss and leukocyte counts in the cerebrospinal fluid of survivors of PM.

CONCLUSION:

This study identifies MMP inhibition, specifically with RS-130830, as an efficient strategy to attenuate disease severity and cortical brain injury in PM.

2010-01-01·Methods and findings in experimental and clinical pharmacology

Gateways to clinical trials

作者: Moral, M A ; Tomillero, A

Aclidinium bromide, AE-37, Alemtuzumab, AMA1-C1/ISA 720, Amlodipine besylate/atorvastatin calcium, Arachidonic acid, Arbaclofen placarbil, Aripiprazole, ARQ-621, Azelnidipine, Azilsartan medoxomil potassium; Bevacizumab, Biphasic insulin aspart, Bortezomib; Choriogonadotropin alfa, CTS-1027; Dapagliflozin, Dasatinib, Deforolimus, Degarelix acetate, Denufosol tetrasodium, Desvenlafaxine succinate, Dronedarone hydrochloride, Duloxetine hydrochloride, Dutasteride; Enfuvirtide, Entecavir, Etaracizumab, Everolimus, Exenatide, Ezetimibe; Ferric carboxymaltose, Fludarabine, Foretinib; Gefitinib, GFT-505, GSK-256066; HPV-6/11/16/18, HuM195/rGel, HyperAcute-Lung cancer vaccine; I5NP, Imatinib mesylate, Imexon, Insulin detemir, Insulin glargine, Ivabradine hydrochloride; L2G7, Lacosamide, Lapatinib ditosylate, Lenalidomide, Lidocaine/prilocaine, Liposomal vincristine, Liraglutide, Lixivaptan; Meningococcal (groups A, C, Y and W-135) oligosaccharide diphtheria CRM197 conjugate vaccine, Methoxy polyethylene glycol-epoetin-β, Mirabegron, Morphine/oxycodone, MR Vaccine, MSC-1936369B, Mycophenolic acid sodium salt; Narlaprevir, N-Desmethylclozapine; Ocriplasmin, Olaparib, Olmesartan medoxomil, Olmesartan medoxomil/azelnidipine, ONO-5334, ONO-8539; Palifermin, Panitumumab, Pardoprunox hydrochloride, PCV7, Peginterferon alfa-2a, Peginterferon alfa-2b, Pemetrexed disodium, Pexelizumab, PF-337210, Pitavastatin calcium; Raltegravir potassium, Recombinant interleukin-7, Regadenoson, Reniale, Roflumilast, Rosuvastatin calcium; Safinamide mesilate, SB-1518, SCH-527123, Selumetinib, Sipuleucel-T, Solifenacin succinate, Sorafenib, Sunitinib malate; Tadalafil, Talaporfin sodium, Tanespimycin, Technosphere/Insulin, Telaprevir, Telatinib, Telcagepant, Telmisartan/hydrochlorothiazide, Teriparatide, Testosterone transdermal gel, TH-302, Tiotropium bromide, Tocilizumab, Trabedersen, Tremelimumab; Valsartan/amlodipine besylate, Vernakalant hydrochloride, Visilizumab, Voreloxin, Vorinostat.

2009-08-01·Hepatology research : the official journal of the Japan Society of Hepatology3区 · 医学

Anti‐fibrotic therapy: Are matrix metalloproteinases friends or foes?

3区 · 医学

Article

作者: Yoshiji, Hitoshi

A review.The research of Kahraman at al. (2009) entitled, 'The Matrix metalloproteinase inhibitor, CTS-1027, attenuates liver injury and fibrosis in the bile duct-ligated mouse' is reviewed with commentary and referencesThe authors showed that the matrix metalloproteinase (MMP) inhibitor, CTS-1027, improves the development of bile duct ligation (BDL)-induced liver fibrosis, along with suppression of liver injury and apoptosis of the hepatocytes.They also observed that overall survival improved in the CTS-1027-treated animals.Despite of having a few shortcomings, this study provides further support for the MMP/tissue inhibitors of metalloproteinase (TIMP) complex as being an attractive therapeutic target for liver fibrosis.

100 项与 RS-130830 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
丙型肝炎	临床2期	美国	Conatus Pharmaceuticals, Inc.	2009-06-01
丙型肝炎	临床2期	波多黎各	Conatus Pharmaceuticals, Inc.	2009-06-01
慢性丙型肝炎	临床2期	美国	Conatus Pharmaceuticals, Inc.	2007-12-01
关节炎	临床2期	-	F. Hoffmann-La Roche Ltd.	-
关节炎	临床2期	-	Conatus 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


NCT01273064 (CTgov)	临床2期	丙型肝炎	114	CTS-1027+ribavirin+pegylated interferon (CTS-1027 60 mg + Ribavirin + Peglyated Interferon)	簾餘壓窪構構鑰築獵範(夢衊繭積繭衊鑰簾顧夢) = 網鏇鏇餘製憲鏇膚網觸鹽憲廠願糧鏇蓋築廠繭 (壓觸艱鑰簾壓築製艱蓋, 觸鏇窪襯壓範遞構獵窪 ~ 鑰蓋餘鑰網鏇遞構顧觸) 更多	-	2012-05-30
				Placebo+CTS-1027+ribavirin+pegylated interferon (CTS-1027 30 mg + Ribavirin + Pegylated Interferon)	簾餘壓窪構構鑰築獵範(夢衊繭積繭衊鑰簾顧夢) = 憲構廠廠糧繭艱網窪顧鹽憲廠願糧鏇蓋築廠繭 (壓觸艱鑰簾壓築製艱蓋, 鑰鹽築餘鏇願積鏇選壓 ~ 廠積繭積獵壓網廠範衊) 更多
NCT01051921 (CTS-1027-04, CTgov)	临床2期	丙型肝炎	67	Pegylated Interferon+CTS-1027+Ribavirin	鹹襯憲鹽鏇膚積糧積衊(積糧襯網顧鹹衊齋積積) = 襯鑰鏇築選餘蓋繭鏇夢繭選觸鑰鏇憲憲廠鬱獵 (積夢選觸夢網製遞鏇築, 觸築壓觸餘獵築艱獵願 ~ 獵窪衊鬱鏇鑰窪壓鹹範) 更多	-	2012-04-10
NCT00925990 (CTgov)	临床2期	丙型肝炎	70	CTS-1027+ribavirin (CTS-1027 + Ribavirin)	醖簾構齋襯窪簾獵構蓋(夢壓憲廠壓淵糧廠獵廠) = 淵製淵壓衊襯餘遞構壓簾醖壓淵憲廠積鬱艱積 (築壓網鹽夢齋範窪壓夢, 鏇繭積鹽築顧遞簾憲鑰 ~ 襯艱壓網鬱鬱夢鑰窪範) 更多	-	2012-03-27
				Placebo for ribavirin+CTS-1027 (CTS-1027 + Placebo)	醖簾構齋襯窪簾獵構蓋(夢壓憲廠壓淵糧廠獵廠) = 淵蓋鹹築醖遞襯網鏇襯簾醖壓淵憲廠積鬱艱積 (築壓網鹽夢齋範窪壓夢, 獵選願獵鬱鏇遞鏇蓋築 ~ 鹽網糧壓獵衊簾膚淵遞) 更多