Clinical trial NCT03492398
Conditions: Atopic Dermatitis
Keywords: atopic dermatitis
Sponsor: Shaperon
Start date: 2018-01-29; Completion date: 2019-05-28
Enrollment: 56 participants; Allocation: RANDOMIZED; Intervention model: PARALLEL

Brief summary:
A randomized, double-blind, placebo-controlled single and multiple dosing, dose escalation phase I clinical trial to investigate the safety/tolerability and pharmacokinetics of HY209 gel after transdermal administration in healthy male volunteers as a possible treatment option for atopic dermatitis

Detailed description:
A composition containing G Protein Coupled Receptor 19(GPCR19) agonist HY209 and a derivative thereof is found to have a considerable effect in the treatment of atopic dermatitis and is proposed as a pharmaceutical ingredient for prevention, treatment and improvement of atopic dermatitis. The GPCR19 agonist, HY209, is superior to conventional steroid ointment and immunosuppressant ointment in the treatment and improvement of allergic dermatitis. It directly reduces the amount of serum immunoglobulin E, which is a major factor of allergic dermatitis, It increases the T helper type 1(TH1) cytokines that alleviate allergic dermatitis pathologies, reduces the T helper type 2(TH2) cytokines that aggravate allergic dermatitis pathologies, and reduces the infiltration of mast cells, eosinophils and neutrophils into the dermal cells. Thus it can be utilized as a therapeutic drug composition for atopic dermatitis.

Arms: arm 1: single dose of HY209 0.05% gel or single dose of placebo arm 2: single dose of HY209 0.1% gel or single dose of placebo arm 3: single dose of HY209 0.3% gel or single dose of placebo arm 4: single dose of HY209 0.5% gel or single dose of placebo arm 5: multiple dose of HY209 0.1% gel or multiple dose of placebo arm 6: multiple dose of HY209 0.3% gel or multiple dose of placebo arm 7: multiple dose of HY209 0.5% gel or multiple dose of placebo
Interventions: intervention 1: HY209
Intervention descriptions: intervention 1: 6 subjects will be assigned to drug (HY209) and 2 subjects will be assigned to placebo.

Protocol documents:
Prot_000.pdf: 
 
 
 
A randomized, double-blind, placebo-controlled single and 
multiple dosing, escalation phase I clinical trial to investigate 
the safety/tolerability and pharmacokinetics of HY209 gel after 
transdermal administration in healthy male volunteers 
 
 
 
 
 
Protocol No. 
HY209-AD (version 1.5 Date: 2019.01.20) 
National Clinical Trial No. 
NCT03492398 
Investigational Product 
HY209 0.05%, 0.1%, 0.3%, 0.5% 
Development phase of study 
Phase I 
Institutes 
Seoul National University Hospital 
Sponsor 
Shaperon, Inc. 
 
 


 
 
Protocol No.: HY209-AD 
 
Shaperon 
 
CONFIDENTIAL 
 
 AD Phase I Synopsis 
Study Title 
A randomized, double-blind, placebo-controlled single and multiple 
dosing, dose escalation phase I clinical trial to investigate the 
safety/tolerability and pharmacokinetics of HY209 gel after transdermal 
administration in healthy male volunteers 
Sponsor 
Shaperon, Inc. 
Institutes 
Seoul National University Hospital. 
Target disease 
Atopic Dermatitis 
Purpose 
The purpose of this study is to evaluate the safety, tolerability and 
pharmacokinetics of HY209 gel as a possible treatment option for atopic 
dermatitis. 
Study Design 
Randomized, double-blind, placebo-controlled (single and multiple 
dosing), dose escalation phase I clinical trial 
Study Method 
(1) Cohort A Single dosing 
Four groups (HY209 0.05%, 0.1%, 0.3%, 0.5%) of subjects, each group 
consisting of control 6 and placebo 2 will be randomly selected. The trial 
drug or placebo will be applied on the back of each subject. Subjects will 
be released after present tests and blood drawing. 
 
 
(2) Cohort B Multiple dosing 
Three groups (HY209 0.05%, 0.1%, 0.3%) of subjects, each group 
consisting of control 6 and placebo 2 will be randomly selected. The trial 
drug or placebo will be applied on the back of each subject at once a day 
for 28 days. Subjects will visit the clinical research center to be tested 
and have their blood drawn, 


 
 
Protocol No.: HY209-AD 
 
Shaperon 
 
CONFIDENTIAL 
 AD Phase I Synopsis 
 
Investigational 
Product 
 Investigational Product: HY209 0.05%, 0.1%, 0.3%, 0.5% 
 Control Product: Placebo (Vehicle) 
Treatment 
(1) Cohort A Single dosing 
 Once at Day 1 
(2) Cohort B Multiple dosing 
 Once daily for 28 days 
Estimated 
Subjects 
(1) Cohort A Single dosing (total 32 subjects) 
 
(2) Cohort B Multiple dosing (total 24 subjects) 
 
The objective of this study is an exploratory study to evaluate the safety, 
tolerability, and pharmacokinetics of HY209, the number of subjects was 
not determined based on statistical considerations. 
Group 
Dose 
Number of subjects 
1 
HY209 0.05% 
8 (HY209; 6, placebo; 2) 
2 
HY209 0.1% 
8 (HY209; 6, placebo; 2) 
3 
HY209 0.3% 
8 (HY209; 6, placebo; 2) 
4 
HY209 0.5% 
8 (HY209; 6, placebo; 2) 
Group 
Dose 
Number of subjects 
5 
HY209 0.05% 
8 (HY209; 6, placebo; 2) 
6 
HY209 0.1% 
8 (HY209; 6, placebo; 2) 
7 
HY209 0.3% 
8 (HY209; 6, placebo; 2) 
Inclusion 
Criteria 
1) 
Healthy male aged from 20 to 50 
2) 
Weight minimum 45 kg, maximum 90 kg with BMI minimum 17 
kg/m2 maximum 27 kg/m2 
➢ 
BMI (kg/m2) = weight (kg) / [height (m)]2 


 
 
Protocol No.: HY209-AD 
 
Shaperon 
 
CONFIDENTIAL 
 AD Phase I Synopsis 
3) 
No skin diseases, no skin damages (scars, tattoo, etc.), no hairy 
skin in drug-applied area which may cause the alteration of drug 
absorption 
4) 
Those who must be capable of giving informed consent and willing 
to comply with all clinic visits and study-related procedures until 
study completion 
Exclusion 
Criteria 
1)  Those who have a history of hypersensitivity or clinically significant 
hypersensitivity reactions to drugs (containing Taurodeoxycholate 
component, aspirin, antibiotics, etc.) 
2)  Those who have clinically significant liver, kidney, respiratory, 
endocrine, neurologic diseases or hematologic diseases, mental 
diseases, especially hemorrhagic diseases (hemophilia, von 
Willebrand disease, etc.), cardiovascular diseases (coronary artery 
diseases, congestive heart failure, arrhythmia, cerebrovascular 
diseases, etc.) or who have a history of those diseases 
3)  Those who have clinical symptoms suspected of acute infectious 
disease within 2 weeks before the schedule date of the first 
administration, or whose temperature measured by the screening 
test was 38℃ or higher 
4)  Those who have taken any ETC medicines, herbal medicines, crude 
drugs within 2 weeks before the scheduled date of administration of 
medicines for clinical trials, or OTC medicines or vitamin 
preparations within 1 week (if all other selection / exclusion criteria 
are met. The researcher should consult with the sponsor to 
determine whether it is appropriate to take the subject into the trials, 
considering the safety of the subject or the effect on overall clinical 
trial results.) 
5)  Those who have a history of substance abuse, or positive urine 
screening tests (cannabinoid, opiates, amphetamine, cocaine, 
barbiturate, benzodiazepine) 
6)  Those who have a history of smoking within 3 months (However, if 
they quit smoking three months before the first scheduled 
medication, they are eligible for selection) 
7)  Those who have been found to be positive in serological tests (HBs 


 
 
Protocol No.: HY209-AD 
 
Shaperon 
 
CONFIDENTIAL 
 AD Phase I Synopsis 
antigen, HCV antibody and HIV antibody) 
8)  Those who drink continuously (above 21 units / week, 1 unit = 10 g 
of pure alcohol) 
9)  Those who have been taking medicines by participating in other 
clinical trials or bioequivalence studies within 3 months prior to the 
date of first dosing (the time from the date of the previous clinical 
trial will be based on the date of administration of each relevant 
clinical trial drug, If the half-life of a test drug taken in a clinical trial 
is more than two weeks, it may be attained more than five times the 
expected half-life of the test drug.) 
10) Those who have been bleeding, blood drawings or blood donation of 
400mL or more within 8 weeks before the scheduled date of 
administration of the drug for clinical trials 
11) Those who have vital signs measured at sitting postion after the 
break for more than 3 minutes,  
➢ 
Low blood pressure (systolic blood pressure < 90 mmHg, 
diastolic blood pressure < 50 mmHg)  
➢ 
High blood pressure (systolic blood pressure greater than 150 
mmHg, diastolic blood pressure greater than 100 mmHg) 
12) Test subjects who are deemed unsuitable for participating in clinical 
trials due to clinical laboratory tests, ECG results, or other reasons 
Outcome 
Measures 
 Primary Outcome Measures 
1) 
Safety and tolerability assessment 
➢ Adverse events, physical symptoms, vital signs, physical test, 
electrocardiography, clinical laboratory test, local stimulation 
assessment, numerical plan rating scale 
 Secondary Outcome Measures 
1) 
Pharmacokinetics 
➢ Cmax, ss, Cmin, ss, AUCinf, T, ss, Tmax, ss, t1/2, ss, CL/F