A Phase 2b, Randomized, Double-Blind, Active-Controlled Study to Evaluate the Safety and Efficacy of Rifalazil (25 Milligram) Compared With Azithromycin (1 Gram) for the Treatment of Uncomplicated Genital Chlamydia Trachomatis Infection in Women

This study will test the safety and effectiveness of an investigational antibiotic drug, rifalazil for the treatment of uncomplicated genital Chlamydia trachomatis infection. This study will examine the effects of 25 milligram of rifalazil compared with azithromycin 1 gram, which will be given as a single dose to women who have genital chlamydial infection.

Start Date01 Jul 2012

Sponsor / Collaborator

ActivBiotics Pharma LLC

NCT00385385 / Unknown statusPhase 2

Randomized Evaluation of Short-Term Rifalazil Treatment on Carotid Atherosclerosis and Intima Media Thickness

The objective of this study is to evaluate an antibiotic therapy called Rifalazil to determine its effect on hardening of the carotid arteries.

Start Date01 Oct 2006

Sponsor / Collaborator

ActivBiotics, Inc.

NCT00251849 / Unknown statusPhase 3

Prospective Evaluation of Rifalazil Effect On Vascular Symptoms of Intermittent Claudication and Other Endpoints in Chlamydia Seropositive Patients

The objective of this study is to determine whether rifalazil can significantly increase peak walking time (PWT) in patients with peripheral arterial disease (PAD).

Start Date01 Nov 2005

Sponsor / Collaborator

ActivBiotics, Inc.

100 Clinical Results associated with Rifalazil

100 Translational Medicine associated with Rifalazil

100 Patents (Medical) associated with Rifalazil

170

Literatures (Medical) associated with Rifalazil

15 Jun 2023·Microbiology spectrum

CRISPR Interference-Based Inhibition of MAB_0055c Expression Alters Drug Sensitivity in Mycobacterium abscessus.

Article

Author: Nguyen, Thanh Quang ; Choudhary, Arunima ; Jeon, Seunghyeon ; Jang, Jichan ; Park, Yujin ; Heo, Bo Eun ; Moon, Cheol

There is an unmet medical need for effective treatments against Mycobacterium abscessus infections. Although advanced molecular genetic tools to validate drug targets and resistance of M. abscessus exist, the practical design and construction of plasmids are relatively laborious and time-consuming. Thus, for this purpose, we used CRISPR interference (CRISPRi) combined with catalytically deactivated Cas9 to inhibit the gene expression of a predicted LysR-type transcriptional regulator gene, MAB_0055c, in M. abscessus and evaluated its contribution to the development of drug resistance. Our results showed that silencing the MAB_0055c gene lead to increased rifamycin susceptibility depending on the hydroquinone moiety. These results demonstrate that CRISPRi is an excellent approach for studying drug resistance in M. abscessus. IMPORTANCE In this study, we utilized CRISPR interference (CRISPRi) to specifically target the MAB_0055c gene in M. abscessus, a bacterium that causes difficult-to-treat infections. The study found that silencing the gene lead to increased rifabutin and rifalazil susceptibility. This study is the first to establish a link between the predicted LysR-type transcriptional regulator gene and antibiotic resistance in mycobacteria. These findings underscore the potential of using CRISPRi as a tool for elucidating resistance mechanisms, essential drug targets, and drug mechanisms of action, which could pave the way for more effective treatments for M. abscessus infections. The results of this study could have important implications for the development of new therapeutic options for this challenging-to-treat bacterial infection.

29 Apr 2023·International journal of molecular sciences

Riluzole-Loaded Nanostructured Lipid Carriers for Hyperproliferative Skin Diseases.

Article

Author: Lopez-Ramajo, Daniel ; Esteruelas, Gerard ; Filgaira, Ingrid ; Agudelo, Mariana Garnica ; Espina, Marta ; García, Maria Luisa ; Sánchez-López, Elena ; Soler, Concepció ; Llorente, Xavier ; Bonilla, Lorena ; Pujol, Montserrat ; Gong, Ruoyi C ; Manils, Joan

Nanocarriers, and especially nanostructured lipid carriers (NLC), represent one of the most effective systems for topical drug administration. NLCs are biodegradable, biocompatible and provide a prolonged drug release. The glutamate release inhibitor Riluzole (RLZ) is a drug currently used for amyotrophic lateral sclerosis (ALS), with anti-proliferative effects potentially beneficial for diseases with excessive cell turnover. However, RLZ possesses low water solubility and high light-sensibility. We present here optimized NLCs loaded with RLZ (RLZ-NLCs) as a potential topical treatment. RLZ-NLCs were prepared by the hot-pressure homogenization method using active essential oils as liquid lipids, and optimized using the design of experiments approach. RLZ-NLCs were developed obtaining optimal properties for dermal application (mean size below 200 nm, negative surface charge and high RLZ entrapment efficacy). In vitro release study demonstrates that RLZ-NLCs allow the successful delivery of RLZ in a sustained manner. Moreover, RLZ-NLCs are not angiogenic and are able to inhibit keratinocyte cell proliferation. Hence, a NLCs delivery system loading RLZ in combination with natural essential oils constitutes a promising strategy against keratinocyte hyperproliferative conditions.

07 Nov 2022·Molecular pharmaceutics

A Colon-Targeted Prodrug of Riluzole Improves Therapeutic Effectiveness and Safety upon Drug Repositioning of Riluzole to an Anti-Colitic Drug

Article

Author: Yoon, In-Soo ; Yoo, Jin-Wook ; Lee, Jaewon ; Kang, Changyu ; Ju, Sanghyun ; Park, Sohee ; Kim, Jaejeong ; Kim, Min-Soo ; Jung, Yunjin

Riluzole (RLZ) is a neuroprotective drug indicated for amyotrophic lateral sclerosis. To examine the feasibility of RLZ for repositioning as an anti-inflammatory bowel disease (IBD) drug, RLZ (2, 5, and 10 mg/kg) was administered orally to rats with colitis induced by 2,4-dinitrobenzenesulfonic acid. Oral RLZ was effective against rat colitis in a dose-dependent manner, which was statistically significant at doses over 5 mg/kg. To address safety issues upon repositioning and further improve anti-colitic effectiveness, RLZ was coupled with salicylic acid (SA) via an azo-bond to yield RLZ-azo-SA (RAS) for the targeted colonic delivery of RLZ. Upon oral gavage, RAS (oral RAS) was efficiently delivered to and activated to RLZ in the large intestine, and systemic absorption of RLZ was substantially reduced. Oral RAS ameliorated colonic damage and inflammation in rat colitis and was more effective than oral RLZ and sulfasalazine, a current anti-IBD drug. Moreover, oral RAS potently inhibited glycogen synthase kinase 3β (GSK3β) in the inflamed distal colon, leading to the suppression of NFκB activity and an increase in the level of the anti-inflammatory cytokine interleukin-10. Taken together, RAS, which enables RLZ to be delivered to and inhibit GSK3β in the inflamed colon, may facilitate repositioning of RLZ as an anti-IBD drug.

News (Medical) associated with Rifalazil

10 Mar 2006

·www.biospace.com

ActivBiotics To Sponsor Satellite Symposium At 2006 American College of Cardiology Meeting

ATLANTA, March 10 /PRNewswire/ -- The 55th Annual Scientific Session of the American College of Cardiology (ACC) in Atlanta will feature an educational symposium supported by ActivBiotics, Inc. entitled "Infectious Contributions to Atherosclerosis and Vascular Disease: Do we really know the answer?" From 12 noon till 2 pm on Saturday, March 11th, 2006 in room 6-10 at the Atlanta Marriott Marquis, key opinion leaders will discuss new perspectives on clinical trials using antibacterial therapy in vascular disease. Chairing the event is J. Thomas Grayston, MD, Professor Emeritus of Epidemiology at the University of Washington in Seattle, and the principal investigator on the completed ACES (Azithromycin and Coronary Events Study) trial. Joining Dr. Grayston on the panel will be William Hiatt, MD, Professor of Cardiovascular Research at the University of Colorado Health Sciences Center in Denver, J. Robert Crouse III, MD, Professor of Medicine and Public Health Sciences at Wake Forest University School of Medicine in Winston-Salem, David Gilbert, MD, Professor of Medicine at Oregon Health Science University in Portland, and Lee Ann Campbell, PhD, Professor of Pathobiology at the University of Washington Medical Center in Seattle. "We are delighted with the interest generated in this symposium, and especially grateful to this expert faculty who will discuss new evidence into the potential contributory role Chlamydia pneumoniae, a ubiquitous bacterial pathogen, may play in accelerating atherosclerotic disease," said Steve Gilman, PhD, President and CEO of ActivBiotics, Inc. This activity is sponsored by the North American Center for Continuing Medical Education (NACCME). NACCME is accredited by the Accreditation Council for Continuing Medical Education to provide continuing medical education for physicians. The event is not part of the official ACC Annual Scientific Session as planned by the Annual Scientific Session Program Committee (ASSPC). To register for this symposium, please go to . ActivBiotics, Inc. is a private biopharmaceutical company focused on the discovery, development and commercialization of breakthrough therapies for the treatment of vascular disease, inflammation, and other high-value chronic and infectious diseases. The Company's lead product candidate, rifalazil, is currently being developed for multiple indications, including intermittent claudication (leg pain) resulting from peripheral arterial disease (PAD), a serious complication of atherosclerosis that affects over 14 million Americans. Based on its experience with rifalazil, the Company has amassed a library of over 1,500 biologically active compounds from the rifamycin class of antibiotics. ABI-0043, the lead candidate in this series of compounds, is in preclinical development as a novel antibacterial agent. In additional to antibacterial programs, the Company has a second platform of anti-inflammatory oxygen free radical scavenging agents, which are small molecule mimetics of human superoxide dismutase. M-40403, the lead candidate among these, has been in Phase 2 trials. The Company is headquartered in Lexington, Massachusetts and has additional operations in Toronto, Canada. For more information on ActivBiotics, please visit . Contact details: Andrew Sternlicht, MD Glenn Kazo VP, Medical Affairs and Corp. Development Chief Business Officer ActivBiotics, Inc. ActivBiotics, Inc. (781) 372-4854 (781) 372-4864 asternlicht@activbiotics.comgkazo@activbiotics.com ActivBiotics, Inc. CONTACT: Andrew Sternlicht, MD, VP, Medical Affairs and Corp. Development,+1-781-372-4854, asternlicht@activbiotics.com, or Glenn Kazo, ChiefBusiness Officer, +1-781-372-4864, gkazo@activbiotics.com both ofActivBiotics, Inc. Web site:

Small molecular drug

100 Deals associated with Rifalazil

External Link

KEGG	Wiki	ATC	Drug Bank
D02550	Rifalazil	-	DB04934

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Intermittent Claudication	Phase 3	US	ActivBiotics, Inc.	01 Nov 2005
Intermittent Claudication	Phase 3	BR	ActivBiotics, Inc.	01 Nov 2005
Intermittent Claudication	Phase 3	RU	ActivBiotics, Inc.	01 Nov 2005
Peripheral Vascular Diseases	Phase 3	US	ActivBiotics, Inc.	01 Nov 2005
Peripheral Vascular Diseases	Phase 3	BR	ActivBiotics, Inc.	01 Nov 2005
Peripheral Vascular Diseases	Phase 3	RU	ActivBiotics, Inc.	01 Nov 2005
Peripheral Arterial Disease	Phase 3	-	ActivBiotics, Inc.	-
Peripheral Arterial Disease	Phase 3	-	Kaneka Corp.	-
Chlamydia trachomatis infection	Phase 2	US	ActivBiotics Pharma LLC	01 Jul 2012
Carotid Artery Diseases	Phase 2	US	ActivBiotics, Inc.	01 Oct 2006

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01631201 (Pubmed \| Antimicrob Agents Chemother)	Phase 2	Chlamydia trachomatis infection	82	Rifalazil (25 mg)	mybijnumnr(jpwebpcwmh) = ttcgbcqbjj hswbedfaaw (uavitsrblq ) View more	Negative	01 Jul 2014
				Azithromycin (1 g)	mybijnumnr(jpwebpcwmh) = hmcmohphcd hswbedfaaw (uavitsrblq ) View more

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis