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5-HT3 receptor(Serotonin 3 (5-HT3) receptor)	1

Sterols are widely and abundantly distributed in nature. It is convenient to utilize them for the preparation of useful compounds such as pharmaceuticals with steroid and secosteroid skeletons. This paper describes the synthesis and structure-activity relationships of naturally occurring active forms of vitamin D analogues, sterols having neurite outgrowth activity, and liver X receptor agonist. The active form of vitamin D(4) showed similar biological activities but had higher affinity to the vitamin D-binding protein compared with the corresponding vitamins D(2) and D(3). This shows that the active form of vitamin D(4) is a good candidate for an agent to replace the active forms of vitamins D(2) and D(3). In the course of screening for low molecular-weight compounds that exhibit neurite outgrowth activity in the culture broth, we found that the natural product dictyosterol showed strong activity. From screening of the analogues, it was found that the double bond between C22 and C23 in the side chain of the sterol is essential for its activity. Ergost-22-ene-1alpha,3beta-diol was found to serve as a stronger liver X receptor agonist than 24(S), 25-epoxycholesterol, which regulates the expression of genes involved in lipid metabolism. Structure-function study showed that the 1alpha-hydroxyl group, the saturated steroid structure, and the double bond between C22 and C23 are needed to function as a liver X receptor agonist.

01 Jan 2006·Journal of Nutritional Science and VitaminologyQ4 · MEDICINE

Comparative Oral Toxicity of Coenzyme Q10 and Its (2Z)-Isomer in Rats: Single and Four-Week Repeated Dose Toxicity Studies

Q4 · MEDICINE

Article

Author: Hatakeyama, Shigeki ; Kawase, Shigeo ; Yoshimura, Ikuo

It has been reported that coenzyme Q10 (CoQ10) functions as an electron transfer carrier in mitochondria, and can produce an improvement in heart diseases such as congestive heart failure. Its (2Z)-isomer contains a cis-double bond at the 2-position of the decaprenyl side chain. As the original organic industrial synthesis of CoQ10 resulted in a product that contained a small amount of this isomer, the efficacy and safety of CoQ10 was determined using CoQ10 containing this isomer; however, no toxicity data have been reported for the (2Z)-isomer itself. Thus, we conducted single (2,000 mg/kg) and 4-wk repeated (1,000 mg/kg) oral dose toxicity studies in rats to compare the toxicological profiles of CoQ10 and its (2Z)-isomer. The two compounds displayed similar toxicological profiles, and it was concluded that neither CoQ10 nor its (2Z)-isomer produce toxic effects in rats in single or repeated doses.

Japanese Pharmacology & Therapeutics

Pharmacokinetics and safety of indisetron tablets in healthy subjects: multiple-oral dose study

Author: Yamada, Tadashi ; Nakata, Fumihisa ; Tadokoro, Toyohiro ; Yonezawa, Katsunobu

Indisetron is a 5-hydroxytryptamine 3 receptor antagonist and an anti-emetic agent.It shows also 5-hydroxytryptamine 4 antagonistic activity in pharmacol. profiles.A multiple-oral dose study as phase I trial for healthy male volunteers was performed to show the tolerability and the pharmacokinetic profiles at a dose of 16 mg twice a day for 7 consecutive days (once a day on Day 1 and Day 7).Subjects were assigned randomly to Indisetron group and placebo group, and the trial was performed under single blind.They were administered the Indisetron tablets orally at 30min before morning and evening meals.As for pharmacokinetics, the plasma and urinary concentrations of indisetron and its metabolites were measured, and then pharmacokinetic parameters were evaluated.The safety was estimated by laboratory test, vital signs, signs and symptoms.Nine healthy male adult volunteers were enrolled and 6 subjects were administered indisetron in this study.As for adverse drug reactions, 2 subjects were presented with constipation and increase in serum amylase resp., and not significant problems clin.The plasma concentrations of indisetron were suggested to be achieved in steady state by Day 3.No changes of the pharmacokinetics and accumulation of indisetron by the repeated administration were indicated.And it was revealed that plasma protein binding, urinary excretion, renal clearance of the unchanged drug, the plasma concentration, urinary excretion ratio of the metabolites were not affected by the repeated administration.It showed no clin. problem of pharmacokinetic profiles in administration of 1 6mg multiple-oral dose of indisetron tablets in pre-prandial.

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Pipeline Snapshot as of 11 Feb 2025

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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