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

171

Literatures (Medical) associated with Rifalazil

01 Oct 2024·Journal of Pharmaceutical Sciences

Correlation of surface properties with dissolution behavior of amorphous solid dispersion of Riluzole and its pharmacodynamic evaluation

Article

Author: Bharti, Kanchan ; Jha, Abhishek ; Satpute, Amol Parasram ; Mishra, Brahmeshwar ; Akhilesh ; Manjit ; Kumar, Manish ; Tiwari, Vinod

Formulation of amorphous solid dispersion (ASD) of any poorly water-soluble drug is among the most promising techniques to increase the dissolution profile of drug and hence its bioavailability. Various literatures give evidences of the role of drug-polymer interactions in the ASD systems, very little information is available about the surface properties of the drug molecule and their ASDs which contributes to a higher dissolution profile. Current work focuses on exploring the surface behavior of a poorly water-soluble drug Riluzole (RLZ) and its ASDs prepared with two highly hydrophilic polymers, polyacrylic acid (PAA), and polyvinylpyrrolidone vinyl acetate (PVP VA). Initial characterization using X-ray diffraction (XRD) revealed about the weight fraction of drug required to prepare a single-phase homogenous system with both the polymers. The saturation solubility and the dissolution studies showed an increase in RLZ solubility as well as the dissolution profile due to the presence of polymers. The role of polymers in changing the surface properties in terms of wettability and polarity were explored using contact angle method and X-ray photon spectroscopy (XPS). Additionally, the neuroprotective efficacy and dose dependent hepatotoxicity were also evaluated in male wistar rats. These studies confirmed the increase in the surface polarity and hence the enhanced ability of ASD formulations to interact with water. The in vivo studies indicated that at the current recommended dose the efficacy as well as toxicity is increased for the ASD formulation. Hence, this formulation can be given at a lower dose to achieve same therapeutic effect with lower toxicity.

15 Jun 2023·Microbiology spectrum

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

Article

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

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

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.

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.

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Indication	Highest Phase	Country/Location	Organization	Date
Peripheral Arterial Disease	Phase 3	-	Kaneka Corp.	-
Peripheral Arterial Disease	Phase 3	-	ActivBiotics, Inc.	-
Chlamydia Infections	Phase 2	-	ActivBiotics, Inc.	-
Chlamydia Infections	Phase 2	-	Kaneka Corp.	-
Intermittent Claudication	Discovery	RU	ActivBiotics, Inc.	01 Nov 2005
Intermittent Claudication	Discovery	BR	ActivBiotics, Inc.	01 Nov 2005
Intermittent Claudication	Discovery	US	ActivBiotics, Inc.	01 Nov 2005
Peripheral Vascular Diseases	Discovery	RU	ActivBiotics, Inc.	01 Nov 2005
Peripheral Vascular Diseases	Discovery	US	ActivBiotics, Inc.	01 Nov 2005
Peripheral Vascular Diseases	Discovery	BR	ActivBiotics, Inc.	01 Nov 2005

Clinical Result

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT01631201 (Pubmed \| Antimicrob Agents Chemother)	Phase 2	Chlamydia trachomatis infection	82	Rifalazil (25 mg)	ahumxgznue(vjjvcrvlsc) = eiggwfxmqc gmijbteego (avjfgxnbbd ) View more	Negative	01 Jul 2014
				Azithromycin (1 g)	ahumxgznue(vjjvcrvlsc) = kdrxgcgqft gmijbteego (avjfgxnbbd ) View more

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