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AbstractThe pharmacokinetics of DP-1904, a new potent and selective thromboxane synthetase inhibitor and its effects on ex-vivo prostanoid formation were studied in Japanese normal male volunteers, who received orally a single 10, 20, 50, 100, 200, 400 or 800 mg dose. The drug was well tolerated by all subjects without evidence of any adverse reactions. The absorption of DP-1904 from gastro-intestinal tract was rapid. After oral doses of 10–800 mg of the drug given to volunteers in the fasted state, the mean maximum drug concentrations in plasma (Cmax) (mean ± s.e., n = 5) of 0·215 (± 0·041), 0·399 (± 0·037), 1·47 (± 0·22), 2·86 (±0·22), 4·66 (±0·58), 7·28(±0·72) and 16·9 (±2·6) μgmL−1 were reached within 1 h. DP-1904 concentrations declined monophasically after Cmax with half lives of 30–40 min. These half lives were independent of the administered doses. The mean area under the concentration-time curves (AUCs) increased from 0·398 (±0·038) to 30·0 (±2·7) μgh. mL−1 as the dose increased from 10 to 800 mg. Linear relations between the doses and Cmax and AUCs were observed. The correlation coefficients for Cmax and AUC were 0·930 and 0·960, respectively. The apparent oral clearance (CL/F) and renal clearance (CLR) did not change significantly as dose increased from 10 to 800 mg. The kinetics of DP-1904 proved to be linear in the dose range studied. The urinary excretion of DP-1904 was also independent of the administered dose, and about half of the dose was recovered in urine as unchanged form within 48 h after administration. The elimination of the drug was fast and almost complete within 6 h after dosing. On the other hand, only 0·5% of the dose was excreted into faeces as intact DP-1904 up to 48 h after 400 mg oral dose. Food intake delayed the absorption of DP-1904 but did not significantly modify its pharmacokinetics. Serum thromboxane B2 levels (the stable metabolite of thromboxane A2) were reduced more than 90% within 0·5 h after all doses studied. DP-1904 had a long duration of inhibitory activity and there was still more than 80, 90 and 95% suppression at 12 h after 200, 400, and 800 mg doses, respectively.

01 Jan 1992·Progress in drug research. Fortschritte der Arzneimittelforschung. Progres des recherches pharmaceutiques

Mode of action of new quinolones: the inhibitory activity on DNA gyrase.

Review

Author: Mitsuhashi, S ; Hoshino, K ; Sato, K

01 Jan 1990·The Journal of Japan Atherosclerosis Society

Effect of Pantethine, Soysterol and their Combinations on Serum Lipoprotein Metabolism and the Incidence of Atheromatous Lesions in Cholesterol-fed Rabbits

Author: TOMIKAWA, Munehiro ; IMOTO, Suguki ; HASEGAWA, Kyoko ; MORISHITA, Kumi ; NAKAI, Yoshiaki ; YOSHIDA, Yoji ; ISHIHARA, Masanao ; KANAI, Hideki ; MOGAKI, Masatoshi ; ISHIKAWA, Kaori ; YAMADA, Akimoto ; SASUGA, Motoi

Male New Zealand white rabbits were fed on atherogenic cholesterol diet (0.5% in diet), the cholesterol diets containing pantethine (0.5% in diet), soysterol (1.0% in diet), and these 2 drugs for 8 wk.Vitamin E was also added to cholesterol diet containing 2 drugs.The combined treatment for hypercholesterolemia with 2 or 3 drugs reduced the levels of serum total cholesterol (TC), low d. lipoprotein-cholesterol, phospholipids, triglycerides, apolipoprotein B and apolipoprotein E.Hypocholesterolemic action of pantethine or soysterol was increased incrementally by the combined treatment.Liver TC, aorta TC, aorta surface involvement of lipids were reduced.The combined treatment also lowered atheromatous lesion in aorta and coronary artery.

100 Deals associated with Daiichi Seiyaku Co., Ltd.

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100 Translational Medicine associated with Daiichi Seiyaku Co., Ltd.

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Pipeline

Pipeline Snapshot as of 08 Nov 2024

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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Current Projects

Drug(Targets)	Indications	Global Highest Phase

Levosemotiadil Fumarate ( Potassium channel x SCNA x VDCCs x VGKCs )	Arrhythmias, Cardiac More	Discontinued
Semotiadil ( VDCCs )	Hypertension More	Discontinued
BNP(Daiichi) ( NPRA )	Heart Failure More	Pending
FYK-1352 ( MMPs x TFPI )	Neoplasms More	Pending
D-11-1580 ( Chemokine receptors )	Atherosclerosis More	Pending