Clinical trial · Interventional
A Performance and Bioavailability Study of Entrectinib in Healthy Volunteers.
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
NCT03961100CI-TRIAL-00046995completedPhase 1Results postedClinicalTrials.gov clinicaltrialsProvenance
- Source
- ClinicalTrials.gov
- Retrieved
- Sep 8, 2026
- Layer
- normalized (units and labels harmonized; values unchanged)
- Run
- ING-CLINICALTRIALS-20260908-000001
Summary
Brief summary (as posted)
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.
Conditions
Conditions (1)
Free-text conditions as registered, with the CancerIndex entity they were reconciled to and the match type.
| Condition (as posted) | Mapped entity | Match | Confidence |
|---|---|---|---|
| Solid Tumor | Solid Neoplasm | CURATED_BROADER | 0.80 |
Interventions
Interventions (4)
| Intervention | Type | Mapped drug | Match |
|---|---|---|---|
| Entrectinib 200 mg (R) | Drug | Entrectinib | ALIAS |
| Entrectinib 200 mg (T) | Drug | Entrectinib | ALIAS |
| Entrectinib 600 mg (T1) | Drug | Entrectinib | ALIAS |
| Entrectinib 600 mg (T2) | Drug | Entrectinib | ALIAS |
Design
Arms and outcomes
Arms (2)
- type
- EXPERIMENTAL
- label
- Part 1
- description
- Participants will be randomly assigned to one of the three treatment sequences (T1T2R, T2RT1, RT1T2). In each treatment sequences, participants will cross-over to three periods taking different formulations of entrectinib. Entrectinib will be administered as a single 600 milligram (mg) oral dose under fed condition in three different formulations. Test formulation 1 (T1): film-coated mini-tablet; Test formulation 2 (T2): film-coated mini-tablet; Reference formulation (R): hard capsule.
- interventionNames
- Drug: Entrectinib 600 mg (T1)
- Drug: Entrectinib 600 mg (T2)
- Drug: Entrectinib 200 mg (R)
- type
- EXPERIMENTAL
- label
- Part 2
- description
- Participants will be randomly assigned to one of the two treatment sequences (TR, RT). In each treatment sequences, participants will cross-over to two periods taking different formulations of entrectinib. Entrectinib will be administered as a single 200 mg oral dose under fasted condition in two different formulations. Test formulation (T): hydroxypropyl methylcellulose (HPMC) capsule; Reference formulation (R): hard capsule.
- interventionNames
Eligibility
Eligibility (as posted)
- Sex
- All
- Minimum age
- 18 Years
- Maximum age
- 60 Years
Show eligibility criteria text
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
References
Publications (0)
Data not yet available
No reference posted for this study.