Delving into the Latest Updates on RS-130830 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

CTS-1027, RO-1130830

Target

MMPs

Mechanism

MMPs inhibitors(Matrix metalloproteinase inhibitors)

Therapeutic Areas

Infectious DiseasesDigestive System DisordersSkin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

ArthritisHepatitis CHepatitis C, Chronic

Originator Organization

F. Hoffmann-La Roche Ltd.

Active Organization-

Inactive Organization

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

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

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Structure

Molecular FormulaC19H20ClNO6S

InChIKeyROSNVSQTEGHUKU-UHFFFAOYSA-N

CAS Registry193022-04-7

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.

Start Date01 Jan 2011

Sponsor / Collaborator

Conatus Pharmaceuticals, Inc.

NCT01051921 / CompletedPhase 2

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.

Start Date01 Jan 2010

Sponsor / Collaborator

Conatus Pharmaceuticals, Inc.

NCT00925990 / CompletedPhase 2

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.

Start Date01 Jun 2009

Sponsor / Collaborator

Conatus Pharmaceuticals, Inc.

100 Clinical Results associated with RS-130830

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100 Translational Medicine associated with RS-130830

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100 Patents (Medical) associated with RS-130830

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7

Literatures (Medical) associated with RS-130830

01 Dec 2015·Journal of neuroinflammationQ1 · MEDICINE

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

Q1 · MEDICINE

ArticleOA

Author: 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.

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

Gateways to clinical trials

Author: 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.

01 Aug 2009·Hepatology research : the official journal of the Japan Society of HepatologyQ3 · MEDICINE

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

Q3 · MEDICINE

Article

Author: 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 Deals associated with RS-130830

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External Link

KEGG	Wiki	ATC	Drug Bank
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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hepatitis C	Phase 2	PR	Conatus Pharmaceuticals, Inc.	01 Jun 2009
Hepatitis C, Chronic	Phase 2	US	Conatus Pharmaceuticals, Inc.	01 Dec 2007
Arthritis	Phase 2	-	F. Hoffmann-La Roche Ltd.	-
Arthritis	Phase 2	-	Conatus Pharmaceuticals, Inc.	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01273064 (CTgov)	Phase 2	Hepatitis C	114	CTS-1027+ribavirin+pegylated interferon (CTS-1027 60 mg + Ribavirin + Peglyated Interferon)	rvpfkfvlzm(xpwcjxdipa) = cbfohwcahy pctkhtrfkh (sulwzldhpd, fundsrizgm - ubbdsprihy) View more	-	30 May 2012
				Placebo+CTS-1027+ribavirin+pegylated interferon (CTS-1027 30 mg + Ribavirin + Pegylated Interferon)	rvpfkfvlzm(xpwcjxdipa) = tjzsjxvird pctkhtrfkh (sulwzldhpd, wwkldouhsy - vqzfkroudp) View more
NCT01051921 (CTS-1027-04, CTgov)	Phase 2	Hepatitis C	67	Pegylated Interferon+CTS-1027+Ribavirin	gcwsrdvahy(kpdvouzqca) = mrrflafaea gjbwizivwz (ehoazkvkgw, xhvnkskmdw - ndumytgyan) View more	-	10 Apr 2012
NCT00925990 (CTgov)	Phase 2	Hepatitis C	70	CTS-1027+ribavirin (CTS-1027 + Ribavirin)	lqsbqeftvq(mqghiuztsh) = xyxlxtscjz qirgivwjrq (bulpmopalb, xpdjjlftzv - qjodrneoqx) View more	-	27 Mar 2012
				Placebo for ribavirin+CTS-1027 (CTS-1027 + Placebo)	lqsbqeftvq(mqghiuztsh) = mvmxfifntf qirgivwjrq (bulpmopalb, khngpkssoo - itjwsdvtyh) View more