Trial Outcomes & Findings for A Study to Evaluate the Pharmacokinetics of PEP005 (Ingenol Mebutate) Gel, 0.05%, When Applied in a Maximal Use Setting to the Dorsal Aspect of the Forearm in Patients With Actinic Keratosis (NCT NCT00852137)

NCT ID: NCT00852137

Last Updated: 2015-03-06

Results Overview

Maximum observed concentration (Cmax) for ingenol mebutate and its two acyl isomers (PEP015 and PEP025) levels over the 24 hour sampling time period based on actual values measured. Blood samples were taken: at 30 minutes, 1, 2, 4, 8, 12 and 24 hours following study medication application on Day 2.

Recruitment status

COMPLETED

Study phase

PHASE2

Target enrollment

16 participants

Primary outcome timeframe

1 day

Results posted on

2015-03-06

Participant Flow

Study Period: First patient randomized: March 18, 2009 Last patient completed Day 57: May 27, 2009 A single site in the US

Participant milestones

Participant milestones
Measure
PEP005 Gel, 0.05%
PEP005 (ingenol mebutate) Gel 0.05% once daily for 2 consecutive days
Vehicle
Vehicle gel once daily for 2 consecutive days
Overall Study
STARTED
13
3
Overall Study
COMPLETED
13
3
Overall Study
NOT COMPLETED
0
0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

A Study to Evaluate the Pharmacokinetics of PEP005 (Ingenol Mebutate) Gel, 0.05%, When Applied in a Maximal Use Setting to the Dorsal Aspect of the Forearm in Patients With Actinic Keratosis

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure
PEP005 Gel, 0.05%
n=13 Participants
PEP005 (ingenol mebutate) Gel 0.05% once daily for 2 consecutive days
Vehicle
n=3 Participants
Vehicle gel once daily for 2 consecutive days
Total
n=16 Participants
Total of all reporting groups
Age, Categorical
<=18 years
0 Participants
n=99 Participants
0 Participants
n=107 Participants
0 Participants
n=206 Participants
Age, Categorical
Between 18 and 65 years
8 Participants
n=99 Participants
2 Participants
n=107 Participants
10 Participants
n=206 Participants
Age, Categorical
>=65 years
5 Participants
n=99 Participants
1 Participants
n=107 Participants
6 Participants
n=206 Participants
Age, Continuous
63 years
STANDARD_DEVIATION 9.7 • n=99 Participants
64.7 years
STANDARD_DEVIATION 12 • n=107 Participants
63.3 years
STANDARD_DEVIATION 9.7 • n=206 Participants
Sex: Female, Male
Female
7 Participants
n=99 Participants
3 Participants
n=107 Participants
10 Participants
n=206 Participants
Sex: Female, Male
Male
6 Participants
n=99 Participants
0 Participants
n=107 Participants
6 Participants
n=206 Participants
Region of Enrollment
United States
13 participants
n=99 Participants
3 participants
n=107 Participants
16 participants
n=206 Participants

PRIMARY outcome

Timeframe: 1 day

Maximum observed concentration (Cmax) for ingenol mebutate and its two acyl isomers (PEP015 and PEP025) levels over the 24 hour sampling time period based on actual values measured. Blood samples were taken: at 30 minutes, 1, 2, 4, 8, 12 and 24 hours following study medication application on Day 2.

Outcome measures

Outcome measures
Measure
PEP005 Gel, 0.05%
n=13 Participants
PEP005 (ingenol mebutate) Gel 0.05% once daily for 2 consecutive days
Vehicle
n=3 Participants
Vehicle gel once daily for 2 consecutive days
Maximum Observed Concentration (Cmax) for Ingenol Mebutate and Its Two Acyl Isomers (PEP015 and PEP025) Levels
NA ng/mL
Standard Deviation NA
The assay results completed for the interim analysis, confirmed that there were no detectable levels of ingenol mebutate or its acyl isomers (PEP015 or PEP025) in any samples assayed.
NA ng/mL
Standard Deviation NA
The assay results completed for the interim analysis, confirmed that there were no detectable levels of ingenol mebutate or its acyl isomers (PEP015 or PEP025) in any samples assayed.

PRIMARY outcome

Timeframe: 1 day

Time at which Cmax is attained (Tmax) for ingenol mebutate, and its two acyl isomers (PEP015 and PEP025) levels measured at 30 min, 1, 2, 4, 8, 12 and 24 hours following study medication application on Day 2. If a maximum value occured at more than one timepoint Tmax is defined as the first timepoint with this value.

Outcome measures

Outcome measures
Measure
PEP005 Gel, 0.05%
n=13 Participants
PEP005 (ingenol mebutate) Gel 0.05% once daily for 2 consecutive days
Vehicle
n=3 Participants
Vehicle gel once daily for 2 consecutive days
Time at Which Cmax is Attained (Tmax) for Ingenol Mebutate, and Its Two Acyl Isomers (PEP015 and PEP025) Levels.
NA hours
NA
The assay results completed for the interim analysis, confirmed that there were no detectable levels of ingenol mebutate or its acyl isomers (PEP015 or PEP025) in any samples assayed.
NA hours
NA
The assay results completed for the interim analysis, confirmed that there were no detectable levels of ingenol mebutate or its acyl isomers (PEP015 or PEP025) in any samples assayed.

PRIMARY outcome

Timeframe: 1 day

Area under the blood conc. versus time curve was calculated for time 0-24 hours (AUC(0-24)) for ingenol mebutate and its two acyl isomers (PEP015 and PEP025) levels measured at 30 min, 1, 2, 4, 8, 12 and 24 hours following study medication application on Day 2.

Outcome measures

Outcome measures
Measure
PEP005 Gel, 0.05%
n=13 Participants
PEP005 (ingenol mebutate) Gel 0.05% once daily for 2 consecutive days
Vehicle
n=3 Participants
Vehicle gel once daily for 2 consecutive days
Area Under the Blood Conc. Versus Time Curve for Time 0-24 Hours (AUC(0-24)) for Ingenol Mebutate and Its Two Acyl Isomers (PEP015 and PEP025) Levels
NA ng/mL x h
Standard Deviation NA
The assay results completed for the interim analysis, confirmed that there were no detectable levels of ingenol mebutate or its acyl isomers (PEP015 or PEP025) in any samples assayed.
NA ng/mL x h
Standard Deviation NA
The assay results completed for the interim analysis, confirmed that there were no detectable levels of ingenol mebutate or its acyl isomers (PEP015 or PEP025) in any samples assayed.

SECONDARY outcome

Timeframe: baseline and day 57

Number of participants with complete clearence. Complete clearance rate is defined as no clinically visible actinic keratosis (AK) lesions in a 25 cm\^2 area within the selected treatment area at Day 57 compared to baseline

Outcome measures

Outcome measures
Measure
PEP005 Gel, 0.05%
n=13 Participants
PEP005 (ingenol mebutate) Gel 0.05% once daily for 2 consecutive days
Vehicle
n=3 Participants
Vehicle gel once daily for 2 consecutive days
Complete Clearance Rate in a 25 cm^2 Area Within the Selected Treatment Area
10 participants
0 participants

SECONDARY outcome

Timeframe: Baseline and Day 57

Percentage (%) change in actinic keratosis (AK) lesions count at Day 57, compared to baseline, in a 25 cm\^2 area within the selected treatment area.

Outcome measures

Outcome measures
Measure
PEP005 Gel, 0.05%
n=13 Participants
PEP005 (ingenol mebutate) Gel 0.05% once daily for 2 consecutive days
Vehicle
n=3 Participants
Vehicle gel once daily for 2 consecutive days
Percentage (%) Change in Actinic Keratosis (AK) Lesions in a 25 cm^2 Area Within the Selected Treatment Area
-96 change from baseline lesion count (%)
Standard Deviation 8
33 change from baseline lesion count (%)
Standard Deviation 58

SECONDARY outcome

Timeframe: baseline and Day 2, 3, 8, 15, 29 and 57

Number of patients with LSR at any time point during the study above 0. The treatment area was assessed at baseline and at each subsequent study visit for the presence and grade of the following Local Skin Responses (LSRs): erythema, flaking/scaling, crusting, swelling, vesiculation/pustulation, and erosion/ulceration using the Local Skin Response Grading Scale (version 5). Each LSR was graded from 0 (best outcome) to 4 (worst outcome). A composite LSR score was calculated as the sum of each individual LSR grade, giving a possible range of 0-24.

Outcome measures

Outcome measures
Measure
PEP005 Gel, 0.05%
n=13 Participants
PEP005 (ingenol mebutate) Gel 0.05% once daily for 2 consecutive days
Vehicle
n=3 Participants
Vehicle gel once daily for 2 consecutive days
Number of Patients With Local Skin Responses (LSRs) Above 0 at Any Time Point During the Study.
13 participants
1 participants

SECONDARY outcome

Timeframe: Baseline, Day 2, 3, 8, 15, 29 and 57

Patients with Incidence of pigmentation and scarring, and grade of pigmentation and scarring, following study treatment through Day 57

Outcome measures

Outcome measures
Measure
PEP005 Gel, 0.05%
n=13 Participants
PEP005 (ingenol mebutate) Gel 0.05% once daily for 2 consecutive days
Vehicle
n=3 Participants
Vehicle gel once daily for 2 consecutive days
Patients With Incidence of Pigmentation and Scarring
0 participants
0 participants

SECONDARY outcome

Timeframe: Day 3

Max composite Local Skin Response (LSR) score on day 3 only . The treatment area was assessed at baseline and at each subsequent study visit for the presence and grade of the following Local Skin Responses (LSRs): erythema, flaking/scaling, crusting, swelling, vesiculation/pustulation, and erosion/ulceration using the Local Skin Response Grading Scale (version 5). Each LSR was graded from 0 (best outcome) to 4 (worst outcome). A composite LSR score was calculated as the sum of each individual LSR grade, giving a possible range of 0-24. (One vehicle treated patent had a LSR on day 1 only).

Outcome measures

Outcome measures
Measure
PEP005 Gel, 0.05%
n=13 Participants
PEP005 (ingenol mebutate) Gel 0.05% once daily for 2 consecutive days
Vehicle
n=3 Participants
Vehicle gel once daily for 2 consecutive days
Max Composite Local Skin Response (LSR) Score
6.6 local skin response score
Standard Deviation 3.1
0 local skin response score
Standard Deviation 0

Adverse Events

PEP005 Gel, 0.05%

Serious events: 0 serious events
Other events: 3 other events
Deaths: 0 deaths

Vehicle

Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Other adverse events
Measure
PEP005 Gel, 0.05%
n=13 participants at risk
PEP005 (ingenol mebutate) Gel 0.05% once daily for 2 consecutive days
Vehicle
n=3 participants at risk
Vehicle gel once daily for 2 consecutive days
Gastrointestinal disorders
Toothache
7.7%
1/13 • 57 days
0.00%
0/3 • 57 days
Infections and infestations
Sinusitis
7.7%
1/13 • 57 days
0.00%
0/3 • 57 days
Injury, poisoning and procedural complications
Arthropod bite
7.7%
1/13 • 57 days
0.00%
0/3 • 57 days
Injury, poisoning and procedural complications
Joint sprain
7.7%
1/13 • 57 days
0.00%
0/3 • 57 days
Investigations
Gamma-glutamyltransferase increased
7.7%
1/13 • 57 days
0.00%
0/3 • 57 days
Gastrointestinal disorders
Diarrhoea
0.00%
0/13 • 57 days
33.3%
1/3 • 57 days
Infections and infestations
Upper respiratory tract infection
0.00%
0/13 • 57 days
33.3%
1/3 • 57 days

Additional Information

Dr. Torsten Skov

LEO Pharma

Phone: +4520736294

Results disclosure agreements

  • Principal investigator is a sponsor employee Evaluator and Principal Investigator agree not to individually publish the result of the study, but rather, to participate in a joint publication of the Study results coordinated by sponsor, who shall have the first righ to publish. If such joint publication is not submitted for publication within 1 year of study completion at all sites Evaluator and Principal Investigator have the right to individually produce and submit a proposed publication, subject to the prior review of sponsor.
  • Publication restrictions are in place

Restriction type: OTHER