A sensitive method using RIA was developed for determination of newly synthesized anti-allergic agent DS-4574 in human plasma.The method was applied to clin. study and the pharmacokinetic properties in human after a single oral administration od DS-4574 were elucidated.

01 Feb 1995·European Journal of PharmacologyQ3 · MEDICINE

Protective effect of DS-4574, a peptidoleukotriene receptor antagonist, against endotoxin-induced intestinal injury in rats

Q3 · MEDICINE

Article

Author: Kazuhisa Furuhama ; Yoshiaki Tabuchi

We evaluated the protective effect of DS-4574 (6-(2-cyclohexylethyl)-[1,3,4]thiadiazolo[3,2-a]-1,2,3- triazolo[4,5-d]pyrimidin-9(3H)-one), a peptidoleukotriene receptor antagonist, against intestinal mucosal injury evoked by endotoxin in rats by exploring changes in hematocrit and plasma leakage along with morphological features. Treatment with Escherichia coli endotoxin (5 mg/kg i.v.) alone elicited hemoconcentration, vasocongestion and a marked mucosal necrosis. DS-4574 (10-50 mg/kg) effectively prevented these changes on either oral or intraduodenal administration. These results demonstrate that peptidoleukotrienes may be key mediators in the intestinal injury induced by endotoxin in rats.

01 Nov 1994·Journal of Pharmaceutical SciencesQ3 · MEDICINE

Radioimmunoassay for DS‐4574, an Antiallergic Agent: Development, Evaluation, and Application to Human Plasma Samples

Q3 · MEDICINE

Article

Author: Nobuyuki Murayama ; Hisashi Nomura ; Hideo Hakusui ; Minoru Nakaoka

A sensitive radioimmunoassay (RIA) method for DS-4574, an antiallergic drug, in plasma has been developed. As the three major metabolites have a hydroxyl group on the cyclohexyl ring, the triazole ring in the terminal part of molecule was attached to ovalbumin with a spacer of beta-chloropropionic acid succinimido ester to prepare an immunogen. Anti-DS-4574 antisera was obtained in rabbits immunized with the immunogen emulsified in Freund's complete adjuvant. The detection limit of the present RIA method was 1 mg/mL of plasma, which was 100-fold more sensitive than the HPLC method developed previously. Cross-reactivities with three major metabolites were less than 3%. The precision of the assay based on triplicate samples showed intra- and inter-assay coefficients of variations of less than 5% and 4%, respectively. This RIA method was applied to plasma samples of six volunteers who had received a single oral 10 mg dose of DS-4574. Plasma concentrations increased rapidly and reached 60 ng/mL at 0.5 h after administration. The concentration decreased to near the detection limit at 4 h postdose. The present RIA method was shown to possess adequate sensitivity to evaluate pharmacokinetic properties of the drug for clinical study, which was not possible by the HPLC method.

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Phase 2	DE	-	-
Asthma	Phase 2	US	-	-
Asthma	Phase 2	-	Daiichi Sankyo Co., Ltd.	-
Asthma	Phase 2	GB	-	-
Peptic Ulcer	Phase 2	-	Daiichi Sankyo Co., Ltd.	-
Peptic Ulcer	Phase 2	JP	Daiichi Pharmaceutical Co., Ltd.	-

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