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A First-in-human Study to Evaluate the Safety, Tolerability and Pharmacokinetics of LFX453

Phase 1
Completed
Conditions
Healthy
Interventions
Drug: LFX453 H1
Drug: LFX453 L1
Drug: LFX453 H2
Drug: LFX453 L2
Drug: Placebo 1
Drug: Placebo 2
Registration Number
NCT02052687
Lead Sponsor
Novartis Pharmaceuticals
Brief Summary

The purpose of this first-in human study is to demonstrate systemic and local tolerability and investigate pharmacokinetics of LFX453 after multiple topical applications in healthy subjects.

The current study has been designed with three distinct parts. Part 1 focuses on safety and tolerability of once daily application on the back, prior to moving forward and assessing the safety and tolerability in more sensitive treatment areas in Part 2 or twice daily application in Part 3.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
41
Inclusion Criteria
  • Healthy male and female subjects of non-childbearing potential, 18 to 65 years of age inclusive (at the time of the screening visit), and in good health as determined by past medical history, physical examination, vital signs, electrocardiogram, and laboratory tests at screening.
  • Male subjects must agree to total abstinence from male:female intercourse or agree to use a condom during drug dosing and for four weeks after dosing has stopped.
Exclusion Criteria
  • History of serious allergic reaction to any drug.

  • History of hypersensitivity to any of the study drugs or to drugs of similar chemical classes.

  • History of any atopic dermatitis (only within the last 2 years), autoimmune disease, psoriasis or erythema multiforme.

  • Presence of skin disease (e.g. warts) or skin features on treatment areas that may affect local tolerability or the ability of the investigator to evaluate local tolerability.

  • History of heart failure, left ventricular dysfunction or known family history or known presence of long QT syndrome.

  • A history of clinically significant ECG abnormalities, or any of the following ECG abnormalities at screening or baseline:

    • 2nd or 3rd degree AV-block
    • PR > 200 msec
    • QRS complex > 120 msec
    • QTcF > 450 msec (males)
    • QTcF > 460 msec (females)
  • Pregnant or nursing (lactating) women, where pregnancy is defined as the state of a female after conception and until the termination of gestation, confirmed by a positive hCG laboratory test.

  • Women of child-bearing potential, defined as all women physiologically capable of becoming pregnant.

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
Part 2 groupA: LFX453/placeboLFX453 H1once daily: LFX453 cream 1 / Placebo 1
Part 2 groupA: LFX453/placeboLFX453 L1once daily: LFX453 cream 1 / Placebo 1
Part 2 groupA: LFX453/placeboLFX453 H2once daily: LFX453 cream 1 / Placebo 1
Part 2 groupB: LFX453/placeboLFX453 H1once daily: LFX453 cream 2 / Placebo 2
Part 2 groupB: LFX453/placeboLFX453 L2once daily: LFX453 cream 2 / Placebo 2
Part 2 groupB: LFX453/placeboPlacebo 2once daily: LFX453 cream 2 / Placebo 2
Part 1: LFX453/placeboLFX453 H1once daily: LFX453 cream 1 high dose / LFX453 cream 1 low dose /Placebo 1 / LFX453 cream 2 high dose / LFX453 cream 2 low dose / Placebo 2
Part 1: LFX453/placeboLFX453 L1once daily: LFX453 cream 1 high dose / LFX453 cream 1 low dose /Placebo 1 / LFX453 cream 2 high dose / LFX453 cream 2 low dose / Placebo 2
Part 2 groupB: LFX453/placeboLFX453 H2once daily: LFX453 cream 2 / Placebo 2
Part 2 groupC: LFX453/LFX453LFX453 L1once daily: LFX453 cream 1 / LFX453 cream 2
Part 2 groupC: LFX453/LFX453LFX453 H2once daily: LFX453 cream 1 / LFX453 cream 2
Part 3: LFX453/placeboPlacebo 2twice daily: LFX453 cream 1 high dose / LFX453 cream 1 low dose /Placebo 1 / LFX453 cream 2 high dose / LFX453 cream 2 low dose / Placebo 2
Part 1: LFX453/placeboLFX453 H2once daily: LFX453 cream 1 high dose / LFX453 cream 1 low dose /Placebo 1 / LFX453 cream 2 high dose / LFX453 cream 2 low dose / Placebo 2
Part 2 groupA: LFX453/placeboLFX453 L2once daily: LFX453 cream 1 / Placebo 1
Part 3: LFX453/placeboLFX453 H2twice daily: LFX453 cream 1 high dose / LFX453 cream 1 low dose /Placebo 1 / LFX453 cream 2 high dose / LFX453 cream 2 low dose / Placebo 2
Part 3: LFX453/placeboLFX453 L1twice daily: LFX453 cream 1 high dose / LFX453 cream 1 low dose /Placebo 1 / LFX453 cream 2 high dose / LFX453 cream 2 low dose / Placebo 2
Part 1: LFX453/placeboLFX453 L2once daily: LFX453 cream 1 high dose / LFX453 cream 1 low dose /Placebo 1 / LFX453 cream 2 high dose / LFX453 cream 2 low dose / Placebo 2
Part 1: LFX453/placeboPlacebo 1once daily: LFX453 cream 1 high dose / LFX453 cream 1 low dose /Placebo 1 / LFX453 cream 2 high dose / LFX453 cream 2 low dose / Placebo 2
Part 1: LFX453/placeboPlacebo 2once daily: LFX453 cream 1 high dose / LFX453 cream 1 low dose /Placebo 1 / LFX453 cream 2 high dose / LFX453 cream 2 low dose / Placebo 2
Part 2 groupA: LFX453/placeboPlacebo 1once daily: LFX453 cream 1 / Placebo 1
Part 2 groupB: LFX453/placeboLFX453 L1once daily: LFX453 cream 2 / Placebo 2
Part 2 groupA: LFX453/placeboPlacebo 2once daily: LFX453 cream 1 / Placebo 1
Part 2 groupB: LFX453/placeboPlacebo 1once daily: LFX453 cream 2 / Placebo 2
Part 2 groupC: LFX453/LFX453LFX453 H1once daily: LFX453 cream 1 / LFX453 cream 2
Part 2 groupC: LFX453/LFX453LFX453 L2once daily: LFX453 cream 1 / LFX453 cream 2
Part 3: LFX453/placeboLFX453 H1twice daily: LFX453 cream 1 high dose / LFX453 cream 1 low dose /Placebo 1 / LFX453 cream 2 high dose / LFX453 cream 2 low dose / Placebo 2
Part 3: LFX453/placeboLFX453 L2twice daily: LFX453 cream 1 high dose / LFX453 cream 1 low dose /Placebo 1 / LFX453 cream 2 high dose / LFX453 cream 2 low dose / Placebo 2
Part 3: LFX453/placeboPlacebo 1twice daily: LFX453 cream 1 high dose / LFX453 cream 1 low dose /Placebo 1 / LFX453 cream 2 high dose / LFX453 cream 2 low dose / Placebo 2
Part 2 groupD: ImiquimodImiquimodonce daily: imiquimod cream
Primary Outcome Measures
NameTimeMethod
General safety (number of subjects with adverse events)14 days

Summarized statistics on adverse events will be reported under categories such as total adverse events, serious adverse events and death.

Local skin tolerability (tolerability score)14 days

Summarized statistics on 5-point scale tolerability scores over 14 days of treatment.

Secondary Outcome Measures
NameTimeMethod
All parts: Amount (ng/mL) of LFX453 in plasma14 days

Evaluate systemic steady state pharmacokinetics in human after topical administration of LFX453.

Part 1 and 2: LFX453 concentrations (ng/g) in the skinDay 14 and between days 18-21

LFX453 analyzed in skin.

All parts: LFX453 concentration (ng/mL) in urineDay 14

LFX453 analyzed in urine.

Trial Locations

Locations (1)

Novartis Investigative Site

🇬🇧

Mid Glamorgan, United Kingdom

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