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OpenTrials
Completed

NCT Number: NCT03961100

A Performance and Bioavailability Study of Entrectinib in Healthy Volunteers.

This study will evaluate the bioavailability, palatability, safety and tolerability of entrectinib in healthy volunteers. Part 1 of the study will explore the performance of entrectinib multi-particle formulation. Part 2 will evaluate the effect of drug substance particle size on entrectinib bioavailability.

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Key information

Conditions

Age range

18 year–60 year

Sex eligibility

All sexes

Study type

Interventional

Phase

Phase 1

Primary location

Quotient Clinical Ltd, Clinical Research Unit

Nottingham, NG11 6JS, United Kingdom

Who can participate

Healthy volunteers accepted: Yes

Only the study team can determine whether someone qualifies for participation.

Inclusion criteria

  • A body mass index (BMI) between 18.0 and 32.0 kilogram per square meter (kg/m2), inclusive, and weighing >/=50 kg.
  • Agreement to comply with measures to prevent pregnancy and restrictions on egg and sperm donation

Exclusion criteria

  • Women of childbearing potential, women who are pregnant or breastfeeding, or intending to become pregnant during the study or within 14 days after the final dose of entrectinib or have a pregnant partner
  • A clinical significant medical history of gastrointestinal surgery (e.g., gastric bypass) or other gastrointestinal disorder (e.g., malabsorption syndrome) that might affect absorption of medicines from the gastrointestinal tract
  • Presence of a clinically significant disease, illness, medical condition or disorder, or any other medical history determined by the investigator to be clinically significant and relevant
  • Clinically significant change in health status, or any major illness, or clinically significant acute infection or febrile illness
  • Use of moderate or potent inhibitors or inducers of CYP P450 3A4 enzyme or P-gp transporter, or use of other prohibited medications
  • Participation in any other clinical study involving an investigational medicinal product (IMP) or device
  • A positive test result for hepatitis B, hepatitis C (HCV), or human immunodeficiency virus (HIV)
  • Current smokers and those who have smoked, or users of e-cigarettes and nicotine replacement products within the last 12 months
  • Known history of clinically significant hypersensitivity, or severe allergic reaction, to entrectinib or related compounds

Treatment and study plan

Entrectinib 600 mg (T1)

Drug

Test formulation 1 (T1): Multi-particulate formulation 1: entrectinib film-coated mini-tablets

Entrectinib 600 mg (T2)

Drug

Test formulation 2 (T2): Multi-particulate formulation 2: entrectinib film-coated mini-tablets

Entrectinib 200 mg (R)

Drug

Reference formulation (R): entrectinib hard capsules

Entrectinib 200 mg (T)

Drug

Test formulation (T): entrectinib HPMC capsules

Primary outcomes

  1. Area Under the Concentration-Time Curve From Time 0 to Infinity (AUC0-inf) of Entrectinib

    Time frame: At pre-defined intervals from study Day 1 to Day 5 of each periods (each period=7 days)

  2. AUC0-inf of Entrectinib Active Metabolite M5

    Time frame: At pre-defined intervals from study Day 1 to Day 5 of each periods (each period=7 days)

  3. Maximum Plasma Concentration (Cmax) of Entrectinib

    Time frame: At pre-defined intervals from study Day 1 to Day 5 of each periods (each period=7 days)

  4. Cmax of Entrectinib Active Metabolite M5

    Time frame: At pre-defined intervals from study Day 1 to Day 5 of each periods (each period=7 days)

Secondary outcomes

  1. Percentage of Participants With Treatment-Emergent Adverse Events (TEAEs)

    Time frame: From Day -1 to Day 5 of each periods (each period=7 days)

    An adverse event (AE) is any untoward medical occurrence in a subject administered a pharmaceutical product and which does not necessarily have to have a causal relationship with the treatment. An adverse event can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding, for example), symptom, or disease temporally associated with the use of a pharmaceutical product, whether or not considered related to the pharmaceutical product. Preexisting conditions which worsen during a study are also considered as adverse events. Treatment-emergent adverse events (TEAEs) are AEs that were not present before the first dose of study drug or that were present before the first dose of study drug but worsened in intensity during exposure to study drug.

Sponsors and collaborators

Lead sponsor

Genentech, Inc.

Industry

Registry information

Official study title

A Randomized, Open-Label, Two Part Study to Explore the Performance of Entrectinib Prototype Mini-Tablet Formulations and the Effect of Drug Substance Particle Size On Entrectinib Bioavailability in Healthy Volunteers

Important dates

Study start
2019
Primary completion
2019
Study completion
2019
First posted
May 23, 2019
Registry last updated
Sep 7, 2020

OpenTrials presents study information sourced from ClinicalTrials.gov. The official registry record should be consulted for the latest information.

View the official ClinicalTrials.gov record (opens in a new tab)

This listing is for discovery and informational purposes only. It is not medical advice, does not guarantee that a study is recruiting, and does not determine eligibility. Contact the study team and a qualified healthcare professional when considering participation.

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