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A Phase 1 Study of CS-3150 Evaluation of Safety, Pharmacokinetics, and Pharmacodynamics after Multiple Oral Administration in Japanese Healthy Adult Male Subjects

A Phase 1 Study of CS-3150 Evaluation of Safety, Pharmacokinetics, and Pharmacodynamics after Multiple Oral Administration in Japanese Healthy Adult Male Subjects

40

The mean age was 24.8 years to 28.0 years, mean height was 168.93 cm to 173.00 cm, mean body weight was 59.01 kg to 65.98 kg, and mean BMI was 20.64 to 22.00 in each administration group. No notable difference was found between the administration groups.

After obtaining informed consent for the study, a total of 40 subjects who were confirmed to be eligible were enrolled in the study. One subject withdrew from the study.

- Adverse events occurred in 12 of the 32 subjects (37.5%) in the overall esaxerenone group, nine of which (28.1%) were considered to be related to the study drug. No AEs were reported in the placebo group. - TEAE leading to study discontinuation occurred in 1 subject, TEAE which were considered unrelated to study drug. - No deaths and other serious adverse events were reported in the study. - In the esaxerenone groups, serum potassium concentrations increased in a dose-dependent manner from Day 2 to 72 hours after completion of study drug administration, and they decreased to similar levels to those in the placebo group in the follow-up examination. No other particular concerns were noted in other safety endpoints.

Please refer to "adverse events" section since primary outcome measures in the study are safety.

Pharmacokinetic endpoints - The results of pharmacokinetic assessment showed that plasma esaxerenone trough concentrations were almost constant and considered to reach the steady state on and after Day 4. - Systemic exposure (AUCtau and Cmax) of esaxerenone on Day 10 was larger than those on Day 1. Pharmacodynamic endpoints - Plasma renin activity, active renin concentration, and plasma aldosterone concentration increased in a dose-dependent manner. Angiotensin II concentrations increased in the 50 mg and 100 mg groups. In the esaxerenone groups, the urinary Na+/K+ ratio increased on Day 1 or 2 and decreased to the baseline level or lower on Day 10. No obvious relationship was found between these changes and any of the esaxerenone doses.

Esaxerenone was well tolerated in multiple oral administration of the drug at doses of 10 mg to 100 mg once daily for 10 days in Japanese healthy male subjects.

June. 07, 2018

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6046505/

No

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DAIICHI SANKYO Co.,Ltd.

dsclinicaltrial@daiichisankyo.co.jp

DAIICHI SANKYO Co.,Ltd.

dsclinicaltrial@daiichisankyo.co.jp

completed

Aug. 04, 2011

Interventional

A single-center, randomized, double-blind, placebo-controlled study

other

1

1) Japanese male
2) Persons >= 20 years and =< 45 years of age at the time of informed consent
3) Persons with a body mass index (BMI; calculated by body weight [kg]/height [m]2) of >= 18.5 kg/m2 and < 25.0 kg/m2 at the screening examination

1) Persons with hypersensitivity or idiosyncratic reactions to a drug, (such as penicillin allergy)
2) Persons with drug or alcohol dependence

Male

Healthy volunteers

investigational material(s)
Generic name etc : CS-3150
INN of investigational material : esaxerenone
Therapeutic category code : 214 Antihypertensives
Dosage and Administration for Investigational material : Oral

control material(s)
Generic name etc : -
INN of investigational material : -
Therapeutic category code :
Dosage and Administration for Investigational material : -

safety
Safety, pharmacokinetics and Pharmacodynamics

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July. 21, 2011