Delving into the Latest Updates on OPS-2071 with Synapse

This is a A Multicenter, Randomized, Double-blind, Placebo-controlled, Clinical Trial to Evaluate the Efficacy and Safety of Different Doses of OPS-2071 in the Treatment of Irritable Bowel Syndrome of Diarrhea type (IBS-D).The trial is mainly divided into three periods: screening period, treatment period and follow-up period.

Start Date02 Aug 2023

Sponsor / Collaborator

Otsuka Beijing Research Institute

NCT03850509

/ TerminatedPhase 2

A Phase 2, Multicenter, Randomized, Double-blind, Placebo-controlled, Proof-of-Concept Trial to Assess the Efficacy and Safety of Orally Administered OPS-2071 for 12 Weeks in Subjects With Crohn's Disease Showing Symptoms of Active Inflammation Despite Ongoing Treatment

The purpose of this study is to evaluate the effects and safety of OPS-2071 (150, 300, or 600 mg twice a day [BID]) versus placebo, as add-on therapy in participants with Crohn's disease who show symptoms of active inflammation despite being on ongoing treatment.

Start Date25 Feb 2020

Sponsor / Collaborator

Otsuka Pharmaceutical Development & Commercialization, Inc.

[+1]

NCT02473393

/ CompletedPhase 2

A Clinical Trial to Assess Three Different Doses of OPS-2071 in Patients With Bacterial Enteritis

To assess safety, efficacy and pharmacokinetics of multiple dosesin patients with Bacterial Enteritis caused by Clostridium difficile infection(CDI) or Enteric infection.

Start Date20 Aug 2015

Sponsor / Collaborator

Otsuka Pharmaceutical Co., Ltd.

100 Clinical Results associated with OPS-2071

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100 Translational Medicine associated with OPS-2071

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100 Patents (Medical) associated with OPS-2071

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6

Literatures (Medical) associated with OPS-2071

28 Nov 2022·The Journal of antimicrobial chemotherapy

In vitro antibacterial activity of OPS-2071 against Gram-positive and Gram-negative enteropathogenic bacteria

Article

Author: Matsumoto, Makoto ; Suzuki, Yasuhiko ; Changkwanyeun, Ruchirada ; Yamaguchi, Tomoyuki ; Oka, Daisuke ; Nakajima, Chie

Abstract:

Background:

Enteric infections are a major public health issue in developing countries. Antimicrobial resistance is also a problem for enteric infection. OPS-2071 is a novel quinolone antibiotic with low oral absorption and potent antibacterial activity against Clostridioides difficile.

Objectives:

This study was conducted to confirm the antimicrobial activity of OPS-2071 against major enteropathogenic bacteria and to evaluate the risk of emergence of drug resistance.

Methods:

The antibacterial activity was evaluated by the agar dilution method. The inhibitory activity against DNA gyrase and topoisomerase IV was determined by supercoiling assay and decatenation assay, respectively. The mutant prevention concentration and frequency of spontaneous resistance were determined by inoculation on drug-containing agar.

Results:

Compared with the reference drugs, the antibacterial activity of OPS-2071 was more potent against Gram-positive bacteria and Campylobacter jejuni, including quinolone-resistant strains. Against other Gram-negative bacteria, OPS-2071 was comparable to existing quinolones. The inhibitory activities against DNA gyrase with quinolone-resistant mutations closely correlated with the antibacterial activity. Spontaneous resistance to OPS-2071 was not observed in Staphylococcus aureus and Escherichia coli and was lower than that of existing quinolones and higher than that of azithromycin in C. jejuni. The mutant prevention concentration of OPS-2071 was lower than that of tested compounds in S. aureus and C. jejuni and slightly higher than that of existing quinolones in E. coli.

Conclusions:

The broad and potent in vitro antibacterial activity and lower risk of drug resistance suggested that OPS-2071 may be useful for enteric infections caused by major pathogens including quinolone-resistant Campylobacter.

01 Aug 2022·Digestive diseases and sciencesQ3 · MEDICINE

Antibacterial and Immunosuppressive Effects of OPS-2071, a Candidate Therapy for Inflammatory Bowel Disease

Q3 · MEDICINE

Article

Author: Yamaya, Naomitsu ; Sato, Masayoshi ; Hagita, Hiraku ; Inagaki, Katsuya ; Matsumoto, Makoto ; Shibuya, Isao ; Takagi, Hiroko ; Fujii, Kazuyuki ; Oka, Daisuke

BACKGROUND:

Inflammatory bowel disease (IBD) is a chronic inflammatory disease of the gastrointestinal tract. Although many types of drug are used, clinical outcomes are still unsatisfactory. Previous studies have suggested that intestinal bacteria are involved in the pathogenesis of IBD. Accordingly, in an IBD model we evaluated the therapeutic effects of OPS-2071, a low-absorption quinolone antibacterial agent indicated for intestinal infection, and investigated its mechanism of action.

METHODS:

The therapeutic effects of OPS-2071 and comparison therapies were evaluated using naive CD4 + T cell-transfer IBD model mice. In vitro inhibition of LPS-induced TNF-α production and inhibitory effects on T cell responses stimulated using anti-CD3/CD28 antibody-loaded beads were evaluated using mouse splenocytes and human peripheral blood mononuclear cells. In addition, in vitro activities against bacteria implicated in IBD pathogenesis were tested.

RESULTS:

OPS-2071 dose-dependently decreased both colonic weight/length ratio and the colitis histological score as compared with the vehicle group. The therapeutic effect of OPS-2071 was equivalent to that of anti-IL-12/23 (p40) antibody. In vitro, OPS-2071 suppressed TNF-α production induced by LPS stimulation and T cell responses in a dose-dependent manner. At high concentrations, these effects were comparable to those of existing immunosuppressive agents, such as prednisolone, in both mouse and human cells. OPS-2071 also showed antibacterial activity against IBD-related bacteria.

CONCLUSIONS:

Our results suggest that OPS-2071 had both immunosuppressive and antibacterial effects. This dual effect makes OPS-2071 a unique and promising candidate for IBD.

01 Jul 2022·Digestive diseases and sciencesQ3 · MEDICINE

Novel Gut Microbiota Modulator, Which Markedly Increases Akkermansia muciniphila Occupancy, Ameliorates Experimental Colitis in Rats

Q3 · MEDICINE

Article

Author: Nakashima, Takako ; Seki, Toyokazu ; Kawasome, Hideki ; Fujii, Kazuyuki ; Aoyama, Masashi ; Azuma, Atsushi

BACKGROUND:

Since gut microbiota is involved in the pathogenesis of inflammatory bowel disease (IBD), antibiotics or probiotics may be attractive options for the treatment of IBD. Akkermansia muciniphila is expected as a next-generation probiotic for IBD, and OPS-2071 is a novel quinolone with potent antibacterial activity against Clostridioides difficile.

AIMS:

The aim of this study is to assess the potential of OPS-2071 as a gut microbiota modulator for IBD.

METHODS:

Minimum inhibitory concentrations of several bacteria in the human intestinal microbiota were determined. Microbiota changes in the feces were typed using metagenomic analysis after oral administration of OPS-2071 (100 mg/kg) twice a day to normal rats. The amounts of mucin were determined using the Fecal Mucin Assay Kit. The effects of OPS-2071 (1, 3, 10 mg/kg) twice a day on fecal symptoms and fecal microbiota were evaluated in a colitis rat model induced by free access to drinking water containing 3% dextran sulfate sodium for 10 days.

RESULTS:

OPS-2071 showed notably low antibacterial activity against only A. muciniphila in spite of higher antimicrobial activity against other strains of intestinal bacteria. OPS-2071 rapidly and dramatically increased the occupancy of A. muciniphila as well as the amount of mucin in the feces of normal rats. OPS-2071 (10 mg/kg) significantly suppressed the exacerbation of stool scores, especially the bloody stool score, with the increase in A. muciniphila occupancy.

CONCLUSIONS:

OPS-2071 is expected to be a new therapeutic option for IBD as a gut microbiota modulator by significantly increasing A. muciniphila occupancy.

100 Deals associated with OPS-2071

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Irritable bowel syndrome with diarrhea	Phase 2	China	Otsuka Pharmaceutical Co., Ltd.	27 Jun 2023
Crohn Disease	Phase 2	United States	Otsuka Pharmaceutical Development & Commercialization, Inc.	25 Feb 2020
Crohn Disease	Phase 2	Poland	Otsuka Pharmaceutical Development & Commercialization, Inc.	25 Feb 2020
Inflammation	Phase 2	United States	Otsuka Pharmaceutical Development & Commercialization, Inc.	25 Feb 2020
Inflammation	Phase 2	Poland	Otsuka Pharmaceutical Development & Commercialization, Inc.	25 Feb 2020
Bacterial enteritis	Phase 2	United States	Otsuka Pharmaceutical Co., Ltd.	20 Aug 2015
Bacterial enteritis	Phase 2	Japan	Otsuka Pharmaceutical Co., Ltd.	20 Aug 2015
Bacterial enteritis	Phase 2	Singapore	Otsuka Pharmaceutical Co., Ltd.	20 Aug 2015
Clostridium difficile infection	Preclinical	China	Otsuka Shanghai Research Institute	18 Mar 2021
Clostridium difficile infection	Preclinical	Japan	Otsuka Pharmaceutical Co., Ltd.	18 Mar 2021

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Clinical Result

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03850509 (CTgov)	Phase 2	Inflammation \| Crohn Disease	3	OPS-2071 (OPS-2071 300 mg BID)	tpdzfgoamr = txconhfuwd jggawddhdh (ggyxrggrih, hbgecoixwp - bvyyvigfxn) View more	-	15 Jun 2021
				Placebo (Placebo)	tpdzfgoamr = irqvfigsla jggawddhdh (ggyxrggrih, abcrvndypx - mtmiqlitfa) View more
NCT02473393 (CTgov)	Phase 2	Bacterial enteritis	43	OPS-2071 (CDI Group)	yoaqlvraje = vuwuirtfdi gihdanupju (ptaixqczpb, sasrgvasbx - bdmmvmisvy) View more	-	24 Mar 2021
				EI (EI Group (50 mg))	yoaqlvraje = qnslosmtzv gihdanupju (ptaixqczpb, ikunjkrkvb - ripqbgmzka) View more