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A mass balance study of [14C] TAS-303 in healthy adult male subjects

A mass balance study of [14C] TAS-303 in healthy adult male subjects

6

Healthy adult males (mean age: 25.8 years)

The number of subjects in this study was 6, and the subjects were enrolled at the study sites in Japan. Six subjects who were considered eligible by the screening test received a single oral dose of the investigational product. All 6 subjects completed the study.

Safety was evaluated in All Treated Subjects (6 subjects). All subjects received a single oral administration of the investigational product. No adverse events occurred, and no clinically significant changes or abnormal values were observed in laboratory test values, vital signs, and 12-lead electrocardiogram.

After single administration of TAS-303 18 mg containing [14C] TAS-303 (approximately 1 MBq) to 6 healthy adult male subjects, 91.73% (mean) of the cumulative amount of radioactivity administered was excreted in urine and feces by 504 hours after administration. Since 66.98% (mean) and 24.77% (mean) of the administered radioactivity were excreted in urine and feces, respectively, it was shown that the major excretion route of radioactivity after administration of [14C] TAS-303 was via urine followed by feces. Radioactivity excreted in urine indicated that the fraction absorbed after a single dose of TAS-303 18 mg was at least approximately 67%.

The major route of excretion was via urine, followed by feces. The fraction absorbed was estimated to be at least approximately 67%. Unchanged TAS-303 represented the largest percentage out of the plasma radioactivity, and none of the metabolized via multiple pathways, including oxidation, dealkylation, glucuronidation, and combinations of these pathways. While 9.0% of the dose was excreted unchanged in urine, but scarcely detected in feces. It was thought that there were no safety concerns in this study.

No

Data will not be shared according to the Sponsor policy on data sharing. Taiho policy on data sharing may be found at https://www.taiho.co.jp/en/science/policy/clinical_trial_information_disclosure_policy/index.html.

https://jrct.mhlw.go.jp/latest-detail/jRCT2071220056

Jinhong Huang

Taiho Pharmaceutical Co., Ltd.

1-27 Kandanishiki-cho, Chiyoda-ku, Tokyo

k-tsukamoto@taiho.co.jp

Ken Tsukamoto

Taiho Pharmaceutical Co., Ltd.

1-27 Kandanishiki-cho, Chiyoda-ku, Tokyo

+81-3-3293-2455

k-tsukamoto@taiho.co.jp

Complete

Oct. 06, 2022

Interventional

single arm study

open(masking not used)

uncontrolled control

single assignment

treatment purpose

(1) Healthy adult male subjects who provided written informed consent to participate in the study
(2) Aged 18 years or older and younger than 40 years at the time of informed consent
(3) Capable of oral intake.
(4) Body weight of 50 kg or more and body mass index of 18.5 or more and less than 25.0
(5)Had blood pressure, pulse rate, and body temperature meeting any of the following at screening:
Systolic blood pressure: >=90 mmHg and =<139 mmHg
Diastolic blood pressure: >=40 mmHg and =<89 mmHg
Pulse rate: >=40 beats per minute (bpm) and =<99 bpm
Body temperature: >=35.0 and =<37.4

(1)Had current or previous hypersensitivity or allergy to drugs
(2)Had current or previous drug abuse (including use of illicit drugs) or alcoholism
(3)Had any concurrent disease (including symptoms and signs; however, diseases that do not affect
evaluations in the study such as asymptomatic pollinosis and wart are excluded)
(4) Received a radioisotope-labeled substance or subject to a large quantity of radiation exposure* within 12 months before the first dose of TAS-303.
* A large quantity of radiation exposure includes continuous X-ray irradiation, computed tomography (CT) scan, gastric barium test, and positron emission tomography (PET) scan, excluding tests with low radiation exposure (e.g., chest, bone, or dental X-ray examination, or X-ray examination before boarding an airplane).
(5) Occupationally exposed to radiation within a year before the first dose of TAS-303 (such as operators who are involved in nuclear power or radiation operations).

Male

Healthy adult male volunteer

Orally administer 40 mL of the liquid containing [14C]TAS-303 (approximately 1 MB) and 18 mg of TAS-303 on day 1.

- Concentrations of total radioactivity in blood and plasma, plasma TAS-303 concentrations and the pharmacokinetics parameters of TAS-303
- Radioactivity excretion and excretion rate, cumulative excretion, cumulative excretion rate into urine and feces.
- Radioactivity excretion and excretion rate, cumulative excretion, cumulative excretion rate in all excreta (urine and faeces).
- Plasma, urinary, and fecal metabolite profiles of TAS-303, and structural estimation.

+81-92-283-7701

Aug. 29, 2022

none