Delving into the Latest Updates on MCI-225 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

+ [1]

Target

HTR3 x NET

Action

antagonists, inhibitors

Mechanism

5-HT3 receptor antagonists(5-hydroxytryptamine receptors, ionotropic (HTR3) antagonists), NET inhibitors(Norepinephrine transporter inhibitors)

Therapeutic Areas

Nervous System DiseasesDigestive System DisordersOther Diseases

Active Indication-

Inactive Indication

Depressive DisorderDiarrheaGastrointestinal Diseases+ [2]

Originator Organization

Mitsubishi Tanabe Pharma Corp.

Active Organization-

Inactive Organization

Dynogen Pharmaceuticals, Inc.

EDUSA Corp.

Mitsubishi Tanabe Pharma Corp.

+ [1]

License Organization-

Drug Highest PhaseDiscontinuedPhase 2

First Approval Date-

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC17H20ClFN4OS

InChIKeySAURKKOJWIFYSR-UHFFFAOYSA-N

CAS Registry476148-82-0

View All Structures (2)

This is a randomized, double blind, placebo controlled, multicenter study designed to assess the safety and efficacy of DDP225 in patients with chronic functional vomiting. Male or female patients from 18 to 65 years of age with a functional vomiting history for at least 12 weeks in the preceding 12 months or cyclic vomiting history with at least 3 episodes in the previous 12 months are eligible. A total of 30 eligible patients with chronic functional vomiting will be enrolled.
The total duration of study participation for an individual patient is approximately 15 weeks (105 days) from the initial screening visit to final study evaluations. The total duration of dosing with study medication (either DDP225 or placebo) is 12 weeks.
Patients who satisfy all of the inclusion criteria and none of the exclusion criteria are eligible to enter the Treatment Period and will be randomly assigned to one of three treatment groups.
After a patient is randomized and enters the Treatment Period, he/she will take the appropriate study medication once a day for 84 days and return to the clinic at two week intervals for a total of six visits during the Treatment Period. During the Treatment Period, patients will maintain a daily diary and complete questionnaires. One week after completing the 84-day Treatment Period, patients return to the clinic for final safety evaluations which include a physical examination, electrocardiogram, and clinical laboratory testing.

Start Date01 Nov 2005

Sponsor / Collaborator

Dynogen Pharmaceuticals, Inc.

NCT00230581

/ CompletedPhase 2

A Phase 2, Randomized, Double Blind, Placebo Controlled Study to Evaluate the Safety, Tolerability, and Pharmacodynamics of Multiple Doses and Dose Levels of DDP225 in Female Patients With Irritable Bowel Syndrome With Diarrhea

In this study, female patients with IBS-d will be treated for 8 weeks to assess the safety and effectiveness of DDP225 on GI transit and in reducing IBS symptoms.

Start Date01 Sep 2005

Sponsor / Collaborator

Dynogen Pharmaceuticals, Inc.

100 Clinical Results associated with MCI-225

Login to view more data

100 Translational Medicine associated with MCI-225

Login to view more data

100 Patents (Medical) associated with MCI-225

Login to view more data

8

Literatures (Medical) associated with MCI-225

01 Aug 2001·Nihon rinsho. Japanese journal of clinical medicine

[Serotonin-noradrenaline reuptake inhibitors(SNRIs)].

Review

Author: Ishigooka, J

Pharmacology, clinical efficacy and tolerability of serotonin noradrenaline reuptake inhibitors(SNRIs) are overviewed. They include milnacipran, venlafaxine, duloxetine, MCI-225 and nefazodone, however, only milnacipran is currently used in Japan. Pharmacology of SNRIs is characterized by inhibition of both serotonin and noradrenaline at the presynaptic membrane and by weak affinity with receptors at the postsynaptic membrane, which expects the same efficacy on major depressive disorder(MDD) as tricyclic antidepressant drugs(TCAs) with less adverse effects in clinical use. Currently available evidences show that SNRIs possess antidepressant effects on MDD at least similar potencies to TCAs with more potencies than selective serotonin reuptake inhibitors. SNRIs are well tolerated in general and safer than TCAs. SNRIs can be considered to be first-line antidepressant drugs.

01 Apr 2001·Pharmacology Biochemistry and BehaviorQ4 · PSYCHOLOGY

The anxiolytic-like effect of MCI-225, a selective NA reuptake inhibitor with 5-HT3 receptor antagonism

Q4 · PSYCHOLOGY

Article

Author: Saito, K.-I. ; Inomata, Y. ; Eguchi, J.

We have previously reported that MCI-225, a selective noradrenaline (NA) reuptake inhibitor with serotonin (5-HT)3 receptor antagonism, shows antidepressant-like properties in experiments using rodents. In this study, we investigated the effect of MCI-225 in anxiety models in comparison with diazepam, ondansetron, maprotiline, imipramine, and trazodone. In social interaction (SI) test in rats, MCI-225 (10 and 30 mg/kg, p.o.), diazepam (1-10 mg/kg, p.o.), and a selective 5-HT3 receptor antagonist ondansetron (1 mg/kg, p.o.) significantly increas

01 Jan 2000·The Japanese Journal of Pharmacology

Effects of Acute and Chronic Administration of MCI-225, a New Selective Noradrenaline Reuptake Inhibitor With 5-HT3 Receptor Blocking Action, on Extracellular Noradrenaline Levels in the Hypothalamus of Stressed Rats.

Article

Author: Yoshida, M ; Ishii, H ; Tanaka, M ; Wu, Y L ; Koga, K ; Emoto, H

In the present study, we investigated the effects of acute and chronic systemic administration of MCI-225 (4-(2-fluorophenyl)-6-methyl-2-(1-piperazinyl)thieno[2,3-d]pyrimidine monohydrate hydrochloride), a newly-developed selective noradrenaline (NA) reuptake inhibitor with 5-HT3-receptor-blocking action, on extracellular NA levels in the hypothalamus of stressed and non-stressed rats by utilizing intracerebral microdialysis. Acute administration of MCI-225 (3 and 10 mg/kg, p.o.) significantly and dose-dependently increased extracellular NA levels in the hypothalamus in non-stressed rats. Footshock for 20 min also significantly increased NA levels in the hypothalamus of both groups of rats pretreated with vehicle and MCI-225. Although chronic administration of MCI-225 (3 or 10 mg/kg, p.o. for 14 days) did not alter the basal extracellular NA levels in the hypothalamus, the stress-induced increases in extracellular NA levels were significantly lower in rats chronically treated with MCI-225 (10 mg/kg) than those of rats pretreated with vehicle for the same period. The increase in extracellular NA levels induced by MCI-225 challenge (3 or 10 mg/kg, p.o.) were not different between rats chronically treated with MCI-225 or vehicle. These results suggest that MCI-225 enhances extracellular NA levels in the hypothalamus in both non-stressed and stressed rats by inhibiting NA uptake and that chronic systemic administration of MCI-225 did not alter basal extracellular NA levels, but reduced the increase in NA release caused by footshock stress. These data suggest the possibility that MCI-225 might possess anxiolytic and/or antidepressant properties.

100 Deals associated with MCI-225

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB05642

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Gastrointestinal Diseases	Phase 2	United States	Dynogen Pharmaceuticals, Inc.	01 Nov 2005
Vomiting	Phase 2	United States	Dynogen Pharmaceuticals, Inc.	01 Nov 2005
Diarrhea	Phase 2	Canada	Dynogen Pharmaceuticals, Inc.	01 Sep 2005
Diarrhea	Phase 2	United States	Dynogen Pharmaceuticals, Inc.	01 Sep 2005
Irritable Bowel Syndrome	Phase 2	Canada	Dynogen Pharmaceuticals, Inc.	01 Sep 2005
Irritable Bowel Syndrome	Phase 2	United States	Dynogen Pharmaceuticals, Inc.	01 Sep 2005
Depressive Disorder	Phase 2	-	Mitsubishi Tanabe Pharma Corp.	-
Depressive Disorder	Phase 2	-	EDUSA Corp.	-
Depressive Disorder	Phase 2	-	Arachnova	-