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A Study of the Safety, Tolerability, Pharmacokinetics and Pharmacodynamic Effects of Single and Multiple Ascending Doses of GDC-0334 and the Effect of Food on the Pharmacokinetics of GDC-0334 in Healthy Adult Participants

Phase 1
Terminated
Conditions
Healthy Volunteers
Interventions
Drug: Placebo
Registration Number
NCT03381144
Lead Sponsor
Genentech, Inc.
Brief Summary

This is a randomized, double-blind, placebo-controlled, single-center, three-part study designed to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamic effects of single and multiple ascending doses of GDC-0334 and the effect of food on the pharmacokinetics of GDC-0334 in healthy adult participants.

Detailed Description

Not available

Recruitment & Eligibility

Status
TERMINATED
Sex
All
Target Recruitment
66
Inclusion Criteria
  • Healthy males or non-pregnant, non-lactating healthy females. Females may be of non-childbearing potential or childbearing potential. Healthy females of childbearing potential must agree to use a highly effective method of contraception.
  • Healthy males must agree to use an adequate method of contraception
  • Body mass index of 18.0 to 32.0 kilograms per meter squared (kg/m^2) or, if outside the range, considered not clinically significant by the investigator
  • Must be willing and able to communicate and participate in the whole study
Exclusion Criteria
  • Participants who have received any investigational medicinal product in a clinical research study within the previous 3 months
  • Participants who are study site employees, or immediate family members of a study site or sponsor employee
  • Participants who have previously been enrolled in this study. Participants who have enrolled in Part 1 are not permitted to enrol in Parts 2 or 3, and participants who have enrolled in Part 2 are not permitted to enroll in Part 3
  • History of any drug or alcohol abuse in the past 2 years
  • Regular alcohol consumption >14 units per week (1 unit = ½ pint beer, 25 milliliters (mL) of 40% spirit or a 125-mL glass of wine)
  • Current smokers and those who have smoked within the last 12 months. A breath carbon monoxide reading of greater than 6 parts per million (ppm) at screening or admission
  • Current users of e-cigarettes and nicotine replacement products and those who have used these products within the last 12 months
  • Participants who do not have suitable veins for multiple venepunctures/cannulation as assessed by the investigator at screening
  • Clinically significant abnormal biochemistry, hematology or urinalysis as judged by the investigator
  • Positive drugs-of-abuse test result at screening or admission
  • Positive hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (HCV Ab), or human immunodeficiency virus (HIV) results
  • Evidence of renal impairment at screening, as indicated by an estimated creatinine clearance of <70 milliliters per minute (mL/min) using the Cockcroft-Gault equation
  • History of seizure
  • History of clinically significant cardiovascular, renal, hepatic, chronic respiratory or gastrointestinal disease, or psychiatric disorder, as judged by the investigator
  • Participants with a history of cholecystectomy or gall stones (applies to any regimen where food effect is being explored)
  • History of serious adverse reaction or serious hypersensitivity to any drug or the formulation excipients
  • Presence or history of active allergy requiring treatment, as judged by the investigator. History of hayfever is allowed unless it is active.
  • Donation or loss of greater than 400 mL of blood within the previous 3 months
  • Participants who are taking, or have taken, any prescribed or over-the-counter drug or herbal remedies in the 14 days or 5 half-lives, whichever is longer, before investigational medicinal product administration. Exceptions may apply on a case-by-case basis, if considered not to interfere with the objectives of the study, as agreed by the principal investigator and sponsor's medical monitor.
  • History or presence of an abnormal electrocardiogram (ECG) that is clinically significant in the investigator's opinion, including complete left bundle branch block, second- or third-degree heart block, or evidence of prior myocardial infarction, at screening or admission
  • QT interval corrected using Fridericia's formula (QTcF) > 450 milliseconds (msec) demonstrated by at least two ECGs >30 minutes apart
  • History of ventricular dysrhythmias or risk factors for ventricular dysrhythmias such as structural heart disease, coronary heart disease (symptomatic or with ischemia demonstrated by diagnostic testing), clinically significant electrolyte abnormalities, or family history of sudden unexplained death or long QT syndrome
  • Current treatment with medications that are well known to prolong the QT interval
  • History of dermatographism
  • Presence or history of clinically significant skin disorders, as judged by the investigator (Parts 1 and 3 only)
  • History of trauma or surgery (laceration repair is not excluded) to the arm but not including wrist or hand injury/surgery (Parts 1 and 3 only)
  • Failure to satisfy the investigator of fitness to participate for any other reason

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
Part 1: GDC-0334GDC-0334Participants in up to 7 cohorts will receive single, ascending doses of GDC-0334 under fasting conditions.
Part 1: PlaceboPlaceboParticipants in up to 7 cohorts will receive single doses of placebo under fasting conditions.
Part 2: PlaceboPlaceboParticipants in up to 3 cohorts will receive single doses of placebo under fasting or fed conditions.
Part 3: GDC-0334GDC-0334Participants in up to 4 cohorts will receive multiple, ascending doses of GDC-0334 under fasting or fed conditions.
Part 3: PlaceboPlaceboParticipants in up to 4 cohorts will receive multiple doses of placebo under fasting or fed conditions.
Part 2: GDC-0334GDC-0334Participants in up to 3 cohorts will receive single doses of GDC-0334 under fasting or fed conditions.
Primary Outcome Measures
NameTimeMethod
Severity of Adverse Events, as Graded per the World Health Organization (WHO) Toxicity Grading ScaleFrom signing of informed consent until 30 days after the last dose of study drug (Up to approximately 42 days)
Percentage of Participants with Adverse EventsFrom signing of informed consent until 30 days after the last dose of study drug (Up to approximately 42 days)
Change from Baseline in Blood PressureUp to approximately 42 days
Change from Baseline in Heart RateUp to approximately 42 days
Incidence of Physical Examination AbnormalitiesUp to approximately 42 days
Incidence of Neurological Examination AbnormalitiesUp to approximately 31 days
Incidence of Electrocardiogram (ECG) AbnormalitiesUp to approximately 42 days
Incidence of Clinical Laboratory AbnormalitiesUp to approximately 30 days
Columbia-Suicide Severity Rating Scale (C-SSRS) - Part 3 OnlyUp to approximately 42 days
Secondary Outcome Measures
NameTimeMethod
Concentration at 12 hours Post-dose (C12) for GDC-0334Up to approximately 35 days
Apparent Terminal Elimination Half-Life (t1/2) for GDC-0334Up to approximately 35 days
Elapsed Time from Dosing at Which GDC-0334 is First Quantifiable in a Concentration versus Time profile (Tlag )Up to approximately 35 days
Percentage of AUC0-inf Accounted for by Extrapolation to Infinity (AUC%extrap) for GDC-0334Up to approximately 35 days
Time to Maximum Plasma Concentration (Tmax) for GDC-0334Up to approximately 35 days
Maximum Observed Plasma Concentration (Cmax) for GDC-0334Up to approximately 35 days
Concentration at 24 hours Post-dose (C24) for GDC-0334Up to approximately 35 days
Area Under the Plasma Concentration Curve from Time Zero to the Last Measurable Concentration (AUC0-t) for GDC-0334Up to approximately 35 days
Area Under the Plasma Concentration Curve from Time Zero Extrapolated to Infinity (AUC0-inf) for GDC-0334Up to approximately 35 days

Trial Locations

Locations (1)

Quotient Clinical Ltd, Clinical Research Unit

🇬🇧

Nottingham, United Kingdom

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