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A Phase 1,randomized,placebo-controlled,double-blind, single ascending dose and multiple ascending dose study of M132101 in healthy subjects.

Single ascending dose and multiple ascending dose study of M132101 in healthy subjects.

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The participants of this study were healthy adult males. In both Period I (single dose) and Period II (multiple dose), no apparent differences were observed between the 0.15%, 0.3%, 0.45%, and placebo groups in terms of demographic and other baseline characteristics of the participants. The mean age and BMI (standard deviation) were 25.9 (6.6) years and 21.45 (1.99) for Period I (24 participants), and 28.6 (6.7) years and 22.37 (1.75) for Period II (24 participants), respectively.

In both Period I (single dose) and Period II (multiple dose), among the participants who consented to participate in this study, 24 participants were randomized, and all of them received the investigational medicinal product (IMP). In Period I, all 24 participants completed the study. In Period II, 23 participants completed the study, and 1 participant from the placebo group withdrew from the study. The reason for withdrawal was "subject's request for study discontinuation." For both Period I and Period II, out of the 24 participants, 18 participants (6 in each group) excluding the 6 from the placebo group were included in pharmacokinetic analysis set. Furthermore, in both Period I and II, all 24 participants (6 in each group) were included in safety analysis set.

In Period I (single dose), adverse events were arthropod sting in 1 participant in the 0.45% group, and C-reactive protein increased and monocyte count increased in 1 participant (the same participant) in the placebo group. In Period II (multiple dose), adverse events were contusion in 1 participant in the 0.15% group, application site erythema and application site acne in 1 each participant in the 0.45% group, and application site erythema and alanine aminotransferase increased in 1 each participant in the placebo group. None of these events were related to the IMP, all were mild in severity, and resolved without treatment. There were no deaths, other serious adverse events, or adverse events leading to discontinuation of the IMP. As adverse events of special interest, adverse events related to local findings at the application site were observed in 3 participants who received M132101 and 1 participant received placebo, however, there were no noteworthy adverse events. No clinically significant changes were observed in laboratory parameters, vital signs, electrocardiograms, or skin safety evaluations.

In Period I (single dose), the concentrations of the drug and its major metabolite in plasma were below the lower limit of quantification (LOQ) at all measurement points for all participants. In Period II (multiple dose), the plasma concentration of the drug was detected only at 4 time points in 1 participant (the same participant) in the 0.45% group, and all values were near the LOQ of 0.5 ng/mL. The plasma concentration of the major metabolite was below the LOQ at all measurement points for all participants.

In healthy adult males, the administration of M132101 at concentrations of 0.15% (1.5 mg/g), 0.3% (3 mg/g), 0.45% (4.5 mg/g), or M132101 placebo either as a single dose or twice daily for 7 days (total of 13 doses) was found to be safe and well-tolerated. Furthermore, it was suggested that the systemic absorption of M132101 at concentrations up to 0.45% was extremely low.

Oct. 31, 2025

No

https://jrct.mhlw.go.jp/latest-detail/jRCT2071230113

Nishiura Tomoyuki

Maruho Co.,Ltd. Kyoto R&D Center

93 chudoji Awatacho, Shimogyo-ku, Kyoto

ctinfo@mii.maruho.co.jp

- Clinical Trials Information

Maruho Co.,Ltd. Kyoto R&D Center

93 chudoji Awatacho, Shimogyo-ku, Kyoto

+81-75-325-3279

ctinfo@mii.maruho.co.jp

Complete

Feb. 08, 2024

Interventional

randomized controlled trial

double blind

placebo control

parallel assignment

treatment purpose

Males who are 18 to 44 years of age at the time of informed consent

(1)Individuals with a history or complications with liver, kidney, or heart disease, etc. considered inappropriate for participation in the clinical study
(2)Individuals with abnormal findings (eczema/dermatitis, pigment abnormalities, inflammation due to sunburn, wounds, scars, skin infections, etc.) at the administration site.
(3)Individuals who are judged to be unsuitable as subject by the principal (sub) investigator

Male

infantile hemangioma

M132101 or placebo will be topically applied once or twice a day for 7 days

Tolerability, Safety, PK

+81-92-283-7701

Feb. 29, 2024

none