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A Study to Test the Pharmacodynamic, Pharmacokinetic, Safety, and Tolerability of Padsevonil in Healthy Study Participants Receiving Either Ethanol or Cannabidiol

Phase 1
Terminated
Conditions
Healthy Participants
Interventions
Drug: Placebo (PSL)
Registration Number
NCT04039919
Lead Sponsor
UCB Biopharma S.P.R.L.
Brief Summary

The purpose of the study is to evaluate the pharmacodynamic (PD) interaction between steady-steady treatment with padsevonil (PSL) and Ethanol and the pharmacokinetic (PK) interaction between stead-state treatment with PSL and cannabidiol (CBD).

Detailed Description

Not available

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
40
Inclusion Criteria
  • Participant must be 18 to 55 years of age inclusive, at the time of signing the informed consent
  • Participants who are overtly healthy as determined by medical evaluation including medical history, physical examination, laboratory tests, and cardiac monitoring
  • Participant must have previous experience with alcohol consumption and, therefore, must be familiar with the effects and able to tolerate social amounts of alcohol
  • Participant has a body weight of at least 50 kg (males) or 45 kg (females) and body mass index (BMI) within the range 18 to 30 kg/m2 (inclusive)
  • Participants are male or female:
  • A male participant must agree to use contraception as detailed in the protocol during the treatment period and for at least 7 days after the last dose of study treatment and refrain from donating sperm during this period
  • A female participant is eligible to participate if she is not pregnant, not breastfeeding, and at least 1 of the following conditions applies:
  • Not a woman of childbearing potential (WOCBP) as defined n the protocol OR
  • A WOCBP who agrees to follow the contraceptive guidance in the protocol during the Treatment Period and for at least 90 days after the last dose of study treatment
Exclusion Criteria
  • Participant has history or presence of cardiovascular, respiratory, hepatic, renal, gastrointestinal, endocrinological, hematological, or neurological disorders capable of significantly altering the absorption, metabolism, or elimination of drugs; constituting a risk when taking the study intervention; or interfering with the interpretation of data
  • Participant has a history of chronic alcohol or drug abuse within the previous 6 months or the presence of drug or alcohol dependency at Screening or Day -1 or tests positive for alcohol and/or drugs at Screening or Day -1
  • Participant has a known hypersensitivity to any components of the study medication or comparative drugs (and/or an investigational device) as stated in this protocol
  • Participant has a history of unexplained syncope or a family history of sudden death due to long QT syndrome
  • Participant has lymphoma, leukemia, or any malignancy within the past 5 years except for basal cell or squamous epithelial carcinomas of the skin that have been resected with no evidence of metastatic disease for 3 years
  • Participant has past or intended use of over-the-counter or prescription medication including herbal medications within 2 weeks or 5 half-lives prior to dosing
  • Participant has used hepatic enzyme-inducing drugs within 2 months prior to dosing
  • Participant has alanine transaminase (ALT), aspartate aminotransferase (AST), or alkaline phosphatase (ALP) >1.0x upper limit of normal (ULN)
  • Participant has current or chronic history of liver disease or known hepatic or biliary abnormalities (with the exception of Gilbert's syndrome or asymptomatic gallstones)
  • Participant has any clinically relevant electrocardiogram (ECG) finding at the Screening Visit or at Baseline
  • Participant has the presence of hepatitis B surface antigen (HBsAg) at Screening or within 3 months prior to dosing
  • Participant has a positive hepatitis C antibody test result at Screening or within 3 months prior to starting study intervention
  • Participant has a positive human immunodeficiency virus (HIV) antibody test

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Part B: Padsevonil-Placebo and CannabidiolPlacebo (PSL)Subjects will be randomized to receive Padsevonil-Placebo and Cannabidiol.
Part A: Padsevonil and EthanolPadsevonilSubjects will be randomized to receive Padsevonil and Ethanol.
Part A: Padsevonil and Ethanol-PlaceboPadsevonilSubjects will be randomized to receive Padsevonil and Ethanol-Placebo.
Part B: Padsevonil and CannabidiolPadsevonilSubjects will be randomized to receive Padsevonil and Cannabidiol.
Primary Outcome Measures
NameTimeMethod
Area Under the Curve Over a Dosing Interval (AUCtau) of Cannabidiol During Part BPredose up to 12 hours postdose

AUCtau is the area under the curve over a dosing interval of CBD.

Maximum Observed Plasma Concentration at Steady State (Cmax,ss) of Cannabidiol During Part BPredose up to 12 hours postdose

Cmax is maximum observed plasma concentration at steady state of CBD.

Area Under the Curve Over a Dosing Interval (AUCtau) of Padsevonil During Part BPredose up to 12 hours post dose

AUCtau is the area under the curve over a dosing interval of padsevonil.

Percentage of Smooth Pursuit Eye Movements on Day 1 of Period 1 or Day 3 of Period 2 During Part APredose, 0.5, 1, 2, 3, 4, 5, 6, 8 and 10 hours postdose on Day 1 of Period 1 or Day 3 of Period 2

Smooth pursuit to assess eye movement coordination and attention to evaluate the ethanol effect. The average percentage of smooth pursuit for all stimulus frequencies was used as a parameter. Participants received either ethanol or placebo on Day 1 of Period 1 or on Day 3 of Period 2. Therefore, the results were summarized by treatment.

Maximum Observed Plasma Concentration at Steady State (Cmax,ss) of Padsevonil During Part BPredose up to 12 hours postdose

Cmax is maximum observed plasma concentration at steady state of padsevonil.

Percentage of Smooth Pursuit Eye Movements on Day 5 of Period 4 or Day 7 of Period 5 During Part APredose, 0.5, 1, 2, 3, 4, 5, 6, 8 and 10 hours postdose on Day 5 of Period 4 or Day 7 of Period 5

Smooth pursuit to assess eye movement coordination and attention to evaluate the ethanol effect. The average percentage of smooth pursuit for all stimulus frequencies was used as a parameter. Participants received either ethanol or placebo on Day 5 of Period 4 or Day 7 of Period 5. Therefore, the results were summarized by treatment.

Secondary Outcome Measures
NameTimeMethod
Area Under the Curve Over a Dosing Interval (AUCtau) of Padsevonil During Part APredose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8 and 12 hours postdose on Day 5

AUC0-tau is the area under the curve over a dosing interval of padsevonil.

Breath Concentration of Ethanol Over Time on Day 5 of Period 4 or Day 7 of Period 5 During Part A-0.4, -0.3, -0.2, -0.16, -0.08, Predose, 0.16, 0.3, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 7 and 8 hours postdose on Day 5 of Period 4 or Day 7 of Period 5

Continuous infusion of ethanol began with a 30 minute loading phase (prior to 0 hours) and was continued for 5 hours with adjustments during the infusion. Participants received either ethanol on Day 5 of Period 4 or Day 7 of Period 5. Therefore, the results were summarized by treatment.

Body Sway to Assess Postural Stability During Part BTreatment Period 1: Screening, Day 1 and Day 2

Body Sway test measured the study participant's body movements in a single direction. Body sway was measured by CHCR NeuroCart. Study participants were asked to stand erect and motionless with their eyes closed. The amplitude and direction of any Body Sway was recorded for 1 minute.

Apparent Total Body Clearance at Steady State (CLss/F) of Padsevonil During Part BPredose up to 12 hours postdose

CLss/F is the apparent total body clearance at steady state following extravascular administration of padsevonil.

Breath Concentration of Ethanol Over Time on Day 1 of Period 1 or Day 3 of Period 2 During Part A-0.4, -0.3, -0.2, -0.16, -0.08, Predose, 0.16, 0.3, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 6, 7 and 8 hours postdose on Day 1 of Period 1 or on Day 3 of Period 2

Continuous infusion of ethanol began with a 30 minute loading phase (prior to 0 hours) and was continued for 5 hours with adjustments during the infusion. Participants received either ethanol on Day 1 of Period 1 or on Day 3 of Period 2. Therefore, the results were summarized by treatment.

Maximum Observed Plasma Concentration at Steady State (Cmax,ss) of Padsevonil During Part APredose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8 and 12 hours postdose on Day 5

Cmax,ss is the maximum observed plasma concentration at steady state of padsevonil.

Half-life (t1/2) of Padsevonil During Part BPredose up to 12 hours postdose

t1/2 is the apparent terminal half-life of padsevonil.

Saccadic Peak Velocity to Assess Sedation on Day 5 of Period 4 or Day 7 of Period 5 During Part APredose, 0.5, 1, 2, 3, 4, 5, 6, 8 and 10 hours postdose on Day 5 of Period 4 or Day 7 of Period 5

Sixteen saccades were recorded with interstimulus intervals varying randomly. Average values of latency (reaction time), saccadic peak velocity of all correct saccades, and inaccuracy of all saccades were used as parameters. Participants received either ethanol or placebo on Day 5 of Period 4 or Day 7 of Period 5. Therefore, the results were summarized by treatment.

Adaptive Tracking to Assess Visuo-Motor Control and Vigilance on Day 5 of Period 4 or Day 7 of Period 5 During Part APredose, 0.5, 1, 2, 3, 4, 5, 6, 8 and 10 hours on Day 5 of Period 4 or Day 7 of Period 5

The adaptive tracking test was performed as originally described by Borland and Nicholson (Borland and Nicholson, 1984). Performance was scored after a fixed period of 3.5 minutes and reflected visuo-motor control and vigilance. The average performance scores were used in the analysis. Participants received either ethanol or placebo on Day 5 of Period 4 or Day 7 of Period 5. Therefore, the results were summarized by treatment.

Number of Participants With Serious Adverse Events During Part AFrom Screening up to the Safety Follow-up visit of Part A (up to Day 26)

A serious adverse event (SAE) was any untoward medical occurrence that at any dose resulted in death, is life-threatening, required in patient hospitalization or prolongation of existing hospitalization, is a congenital anomaly or birth defect, is an infection that requires treatment parenteral antibiotics, other important medical events which based on medical or scientific judgement may jeopardize the participants, or may require medical or surgical intervention to prevent any of the above.

Half-life (t1/2) of Cannabidiol During Part BPredose up to 12 hours postdose

t1/2 is the apparent terminal half-life of CBD.

Saccadic Peak Velocity to Assess Sedation During Part BTreatment Period 1: Screening, Day 1 and Day 2

Sixteen saccades were recorded with interstimulus intervals varying randomly. Average values of latency (reaction time), saccadic peak velocity of all correct saccades, and inaccuracy of all saccades were used as parameters.

Adaptive Tracking to Assess Visuo-Motor Control and Vigilance During Part BTreatment Period 1: Screening, Day 1 and Day 2

The adaptive tracking test was performed as originally described by Borland and Nicholson (Borland and Nicholson, 1984). Performance was scored after a fixed period of 3.5 minutes and reflected visuo-motor control and vigilance.

Number of Participants With Adverse Events During Part BFrom Screening up to the Safety Follow-up visit of Part B (up to Day 66)

An AE was any untoward medical occurrence in a participant or trial participant that is administered a drug or biologic (medicinal product) or that is using a medical device. The event does not necessarily have a causal relationship with that treatment or usage.

Number of Participants With Treatment-related Adverse Events During Part BFrom Baseline up to Safety Follow-up visit of Part B (up to Day 66)

Treatment-related adverse event was an adverse event for which a causal relationship between the product and the occurrence is suspected.

Number of Participants With Adverse Events Leading to Discontinuation of the Study During Part BFrom Screening up to Safety Follow-up visit of Part B (up to Day 66)

An AE was any untoward medical occurrence in a participant or clinical investigation participant administered a pharmaceutical product, which does not necessarily have a causal relationship with this treatment. An AE could therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal (investigational) product, whether or not related to the medicinal (investigational) product.

Saccadic Peak Velocity to Assess Sedation on Day 1 of Period 1 or Day 3 of Period 2 During Part APredose, 0.5, 1, 2, 3, 4, 5, 6, 8 and 10 hours postdose on Day 1 of Period 1 or Day 3 of Period 2

Sixteen saccades were recorded with interstimulus intervals varying randomly. Average values of latency (reaction time), saccadic peak velocity of all correct saccades, and inaccuracy of all saccades were used as parameters. Participants received either ethanol or placebo on Day 1 of Period 1 or on Day 3 of Period 2. Therefore, the results were summarized by treatment.

Adaptive Tracking to Assess Visuo-Motor Control and Vigilance on Day 1 of Period 1 or Day 3 of Period 2 During Part APredose, 0.5, 1, 2, 3, 4, 5, 6, 8 and 10 hours postdose on Day 1 of Period 1 or Day 3 of Period 2

The adaptive tracking test was performed as originally described by Borland and Nicholson (Borland and Nicholson, 1984). Performance was scored after a fixed period of 3.5 minutes and reflected visuo-motor control and vigilance. The average performance scores were used in the analysis. Participants received either ethanol or placebo on Day 1 of Period 1 or on Day 3 of Period 2. Therefore, the results were summarized by treatment.

Body Sway to Assess Postural Stability on Day 1 of Period 1 or Day 3 of Period 2 During Part APredose, 0.5, 1, 2, 3, 4, 5, 6, 8 and 10 hours postdose on Day 1 of Period 1 or Day 3 of Period 2

Body Sway test measured the study participant's body movements in a single direction. Body sway was measured by CHCR NeuroCart. Study participants were asked to stand erect and motionless with their eyes closed. The amplitude and direction of any Body Sway was recorded for 1 minute. Participants received either ethanol or placebo on Day 1 of Period 1 or on Day 3 of Period 2. Therefore, the results were summarized by treatment.

Body Sway to Assess Postural Stability on Day 5 of Period 4 or Day 7 of Period 5 During Part APredose, 0.5, 1, 2, 3, 4, 5, 6, 8 and 10 hours on Day 5 of Period 4 or Day 7 of Period 5

Body Sway test measured the study participant's body movements in a single direction. Body sway was measured by CHCR NeuroCart. Study participants were asked to stand erect and motionless with their eyes closed. The amplitude and direction of any Body Sway was recorded for 1 minute. Participants received either ethanol or placebo on Day 5 of Period 4 or Day 7 of Period 5. Therefore, the results were summarized by treatment.

Number of Participants With Adverse Events During Part AFrom Screening up to the Safety Follow-up visit of Part A (up to Day 26)

An adverse event (AE) was any untoward medical occurrence in a participant or trial participant that is administered a drug or biologic (medicinal product) or that is using a medical device. The event does not necessarily have a causal relationship with that treatment or usage.

Number of Participants With Serious Adverse Events During Part BFrom Screening up to the Safety Follow-up visit of Part B (up to Day 66)

A SAE was any untoward medical occurrence that at any dose resulted in death, is life-threatening, required in patient hospitalization or prolongation of existing hospitalization, is a congenital anomaly or birth defect, is an infection that requires treatment parenteral antibiotics, other important medical events which based on medical or scientific judgement may jeopardize the participants, or may require medical or surgical intervention to prevent any of the above.

Number of Participants With Treatment-related Adverse Events During Part AFrom Baseline up to Safety Follow-up visit of Part A (up to Day 26)

Treatment-related adverse event was an adverse event for which a causal relationship between the product and the occurrence is suspected.

Apparent Total Body Clearance at Steady State (CLss/F) of Cannabidiol During Part BPredose up to 12 hours postdose

CLss/F is the apparent total body clearance at steady state following extravascular administration of CBD.

Percentage of Smooth Pursuit Eye Movements During Part BTreatment Period 1: Screening, Day 1 and Day 2

Smooth pursuit to assess eye movement coordination and attention to evaluate the ethanol effect. The average percentage of smooth pursuit for all stimulus frequencies was used as a parameter.

Number of Participants With Adverse Events Leading to Discontinuation of the Study During Part AFrom Screening up to Safety Follow-up visit of Part A (up to Day 26)

An AE was any untoward medical occurrence in a participant or clinical investigation participant administered a pharmaceutical product, which does not necessarily have a causal relationship with this treatment. An AE could therefore be any unfavorable and unintended sign, symptom, or disease temporally associated with the use of a medicinal (investigational) product, whether or not related to the medicinal (investigational) product.

Trial Locations

Locations (1)

Up0071 001

🇳🇱

Leiden, Netherlands

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