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A Phase 1, Single and Multiple Ascending Dose Study to Assess the Safety, Tolerability and Pharmacokinetics of TO-210 5% in Japanese Subjects With Acne Vulgaris

TO-210 Phase 1 Study

34

No notable differences were observed between the cohorts and between subjects who received the active treatment and those who received the placebo treatment in any of demographic and other baseline. The main demographic characteristics in the safety analysis population were as follows. 1. Age (mean) (1) Part 1 (Cohort 1 to 3) -TO-210; 23.6 years -Placebo; 22.3 years (2) Part 2 (Cohort 4) -TO-210; 23.1 years -Placebo; 27.0 years 2. Sex (Male%) (1) Part 1 (Cohort 1 to 3) -TO-210; 72.2% -Placebo; 83.3% (2) Part 2 (Cohort 4) -TO-210; 62.5% -Placebo; 50.0% 3. Total lesions count (mean) (1) Part 1 (Cohort 1 to 3) -TO-210; 17.2 -Placebo; 14.5 (2) Part 2 (Cohort 4) -TO-210 8g; 18.4 -Placebo; 14.0

Part 1 In Cohort 1, of 38 subjects who signed the informed consent, 8 were randomized to receive the study drug (6 to the active treatment and 2 to the placebo treatment) and subsequently received the study drug. In Cohort 2, of 35 subjects who signed the informed consent, 8 were randomized to receive the study drug (6 to the active treatment and 2 to the placebo treatment) and subsequently received the study drug. In Cohort 3, of 46 subjects who signed the informed consent, 8 were randomized to receive the study drug (6 to the active treatment and 2 to the placebo treatment) and subsequently received the study drug. All subjects who received the study drug completed the assessments and no subjects discontinued the study in either cohort. Part 2 Of 41 subjects who signed the informed consent, 10 were randomized to receive the study drug (8 to the active treatment and 2 to the placebo treatment) and subsequently received the study drug. All 10 subjects who received the study drug completed the assessments and no subjects discontinued the study.

Part 1 No deaths, serious treatment-emergent adverse events (TEAEs), or TEAEs leading to study discontinuation were reported. TEAEs were reported in 1 (5.6%) of 18 subjects for active treatment group and 1 (16.7%) of 6 subjects for placebo treatment group. All reported TEAEs were mild in severity. Part 2 No deaths, serious TEAEs, or TEAEs leading to study discontinuation were reported. TEAEs were reported in 3 (37.5%) of 8 subjects for active treatment group and 1 (50.0%) of 2 subjects for placebo treatment group. All reported TEAEs were mild in severity.

Part 1 The mean plasma concentrations of the unchanged compound rapidly increased following the administration of TO-210 5%, decreased after 0.5 or 2 hours post-dose, and remained stable thereafter across all cohorts. At 48 hours post dose, the final blood sampling point, all subjects had concentrations below lower limit of quantification. Part 2 Following the first administration of approximately 8 g of TO-210 5%, the mean plasma concentrations of the unchanged compound rapidly increased and decreased over time from 2 to 24 hours post-dose. At 24, 72, 120, and 144 hours after the first administration, when samples were collected prior to the administration of TO-210 5%, the mean plasma concentrations of the unchanged compound were close to the lower limit of quantitation. Time courses of the mean plasma concentrations of the unchanged compound on Day 7 were comparable to those observed on Day 1. No increase in the Ctrough was observed following 7-day repeated doses of approximately 8 g once daily of TO 210-5%.

TO-210 5% were tolerated up to the highest dose of approximately 8 g. Additionally, the plasma concentrations of the unchanged compound were either below lower limit of quantification or low across all doses and time points.

Oct. 20, 2025

No

https://jrct.mhlw.go.jp/latest-detail/jRCT2071230128

Natsui Kensuke

Torii Pharmaceutical Co.,Ltd.

4-1, Nihonbashi-Honcho 3-chome, Chuo-ku, Tokyo 103-8439, Japan

kensuke.natsui@torii.co.jp

Natsui Kensuke

Torii Pharmaceutical Co.,Ltd.

4-1, Nihonbashi-Honcho 3-chome, Chuo-ku, Tokyo 103-8439, Japan

+81-3-3231-6583

kensuke.natsui@torii.co.jp

Complete

Mar. 29, 2024

Interventional

randomized controlled trial

double blind

placebo control

parallel assignment

other

-Japanese patients aged between 18 and 49 years at informed consent
-Patients with facial acne valgaris with an Investigator's Global Assessment (IGA) score of 2-4
-Patients with 5-100 inflammatory lesions (papules, pustules) on the face (including the nose)

-Patients with a history of serious diseases such as brain, liver, kidney, heart, lung, digestive system, blood, endocrine system, metabolic system and mental system, or those currently under treatment
-Patients whose acne symptoms suddenly changed within at least 12 weeks before screening
-Patients with other skin diseases (e.g., urticaria, atopic dermatitis) or skin infections (bacterial, fungal, or viral) that might interfere with the evaluation of acne or TO-210 safety, except for tinea pedis

Both

Acne Vulgaris

Cohort 1-3
Single dose application of TO-210 5% or Placebo
Cohort 4
Multiple dose application of TO-210 5% or Placebo once daily for 7 days

Safety, Pharmacokinetics

+81-92-283-7701

Mar. 22, 2024

none