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Safety and Tolerability of the Twice Daily Intra-anal Application of NRL001 Cream for 14 Days

Phase 1
Completed
Conditions
Faecal Incontinence
Interventions
Drug: NRL001 cream 0.5%w/w
Drug: NRL001 cream 0.75%w/w
Drug: NRL001 cream 1.0%w/w
Drug: NRL001 cream 1.5%w/w
Drug: NRL001 cream 2.0%w/w
Drug: NRL001 cream 2.5%w/w
Registration Number
NCT06593730
Lead Sponsor
Norgine
Brief Summary

The study is being conducted to evaluate the safety and tolerability after single and repeated twice daily intra-anal applications of 1mL NRL001 cream in stepwise increasing concentrations.

Detailed Description

Single-centre, randomised, placebo-controlled, double-blind, repeated dose study in healthy male and female volunteers, comprising up to six sequential dose groups receiving 1 mL doses of an investigational cream formulation containing 0.50, 0.75, 1.00, 1.50, 2.00 and 2.50% w/w NRL001. Doses were to be investigated in stepwise increasing fashion. Progression to a higher dose-step required completion of the previous dose-step without safety limiting findings. Each dose-step was to be investigated in 12 subjects; in each dose-group, subjects assigned to active treatment were to be studied in parallel with subjects assigned to placebo in double-blind fashion with random (9:3) treatment assignment. Each subject was to be studied for one study period with double-blind investigational treatment (1 mL of an investigational cream formulation containing NRL001 or matched placebo) twice daily from the morning of D01 to the afternoon of D14; this phase was to be preceded by a single-blind placebo control day (D-1) with administration of placebo in the morning and afternoon.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
72
Inclusion Criteria
  • Males or females (only females of non-child-bearing potential or of child-bearing potential while taking medically appropriate contraception)
  • Caucasian
  • 35 to 60 years of age (included)
  • BMI: between 22 and 26 kg.m-2
  • BW: between 50 and 100 kg
  • Willing and able to provide written informed consent
Exclusion Criteria

General - all subjects

  • Previous participation in the trial
  • Participation in any other trial during the last 90 days
  • Donation of blood or plasma within the last 90 days before recruitment
  • History of any clinically relevant allergy
  • Presence of acute or chronic infection
  • Presence or history of any relevant medical condition or disease (as evaluated on the basis of medical history, physical examination, recumbent and standing blood pressure, treadmill ergometry, clinical laboratory tests [haematology, clinical chemistry, urinalysis, serology])
  • Presence or history of migraine, frequent headaches, Raynaud phenomenon, urinary urge, signs and symptoms of prostatism
  • Presence or history of regular/habitual diarrhoea or constipation; previous anal surgery or trauma, anal fissures, rectal disorders
  • Resting systolic blood pressure > 145 or < 90 mmHg, diastolic blood pressure > 95 or < 50 mmHg
  • Positive treadmill ergometry test
  • Resting pulse (PR) or electrocardiographic heart rate (HR) < 55 bpm
  • ECG: AV-block (AV-block grade I included), QT > 480 msec, QTc > 450 msec, sick-sinus syndrome
  • Positive hepatitis (HBs-Ag or HBc-Ab, HCV-Ab) or HIV serology test
  • History of alcohol or (social) drug abuse
  • Positive alcohol or urine drug test
  • Daily consumption of > 30 g alcohol
  • Smoking more than 15 cigarettes/day or equivalent of other tobacco products
  • Use of prohibited medication
  • Suspicion or evidence that the subject is not reliable
  • Suspicion or evidence that the subject is not able to make a free consent or to understand the information detailed in the Subject Information sheet.

All females

  • Positive pregnancy test
  • Lactating
  • Premenopausal women : not using contraception which is judged adequate and sufficient in the opinion of the clinical investigator

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
NRL001 cream 0.5%w/wNRL001 cream 0.5%w/w0.5%w/w NRL001 (1R,2S-methoxamine) 1 mL, twice daily administration (morning and afternoon) for 14 days (study Days D1 to D14).
NRL001 cream 0.75% w/wNRL001 cream 0.75%w/w0.75%w/w NRL001 (1R,2S-methoxamine) 1 mL, twice daily administration (morning and afternoon) for 14 days (study Days D1 to D14).
NRL001 cream 1.0% w/wNRL001 cream 1.0%w/w1.0%w/w NRL001 (1R,2S-methoxamine) 1 mL, twice daily administration (morning and afternoon) for 14 days (study Days D1 to D14).
NRL001 cream 1.5% w/wNRL001 cream 1.5%w/w1.5%w/w NRL001 (1R,2S-methoxamine) 1 mL, twice daily administration (morning and afternoon) for 14 days (study Days D1 to D14).
NRL001 cream 2.0% w/wNRL001 cream 2.0%w/w2.0%w/w NRL001 (1R,2S-methoxamine) 1 mL, twice daily administration (morning and afternoon) for 14 days (study Days D1 to D14).
NRL001 cream 2.5% w/wNRL001 cream 2.5%w/w2.5%w/w NRL001 (1R,2S-methoxamine) 1 mL, twice daily administration (morning and afternoon) for 14 days (study Days D1 to D14).
Primary Outcome Measures
NameTimeMethod
Recumbent and standing blood pressure and pulse rate17 days

BP and pulse taken lying and standing at screening, on control day and profiling days

Ambulatory 24 hour BP monitoring17 days

Ambulatory 24 hour BP monitoring on control day and profiling days

12-lead digital resting ECG17 days

12-lead digital resting ECG at screening, on control day and profiling days

3-lead ambulatory 24 hour ECG monitoring17 days

24 hour HOLTER monitoring at screening, on control day and profiling days

Secondary Outcome Measures
NameTimeMethod
Plasma concentrations of NRL00117 days

Single and repeat dose pharmacokinetics of NRL001 in plasma

Well being17 days

Any untoward change in health and/or wellbeing

Adverse events17 days

Any unwanted sign or symptom

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