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Entrectinib Test Formulation

Phase 1

Healthy Volunteers | Small molecule | Other |Roche Holding AG|Last Updated: Feb 26, 2020

Target and mechanism

Molecular targetALK, NTRK1, NTRK2, NTRK3, ROS1
Target classInhibitor
ModalitySmall molecule

Also known as Entrectinib

Success Probability

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Market & Valuation

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Trial Design

RandomizedCONTROLLED
Total Trials1
Total Enrollment14

FDA Designations

No designations recorded

Clinical trial landscape

Entrectinib Test Formulation · 1 trial · 1 indication

Phase 1 1
NCT03796260A Study to Investigate the Relative Bioavailability of Entrectinib Capsule Formulations F1 and F06 Under Fed Conditions in Healthy ParticipantsHealthy Volunteers
COMPLETED14 Analytics
PHASE1COMPLETED
A Study to Investigate the Relative Bioavailability of Entrectinib Capsule Formulations F1 and F06 Under Fed Conditions in Healthy Participants
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Study Endpoints

Primary Endpoints

Area Under the Concentration-Time Curve Extrapolated to Infinity (AUC0-inf) of Entrectinib and M5 Metabolite
At pre-defined intervals from study Day 1 through Day 5 of each Period (Periods 1 and 2 = 6 days)

The area under the concentration-time curve extrapolated to infinity is calculated using the formula: AUC0-inf = AUC0-t + (Ct/λz) where Ct is the last measurable concentration and λz is the apparent terminal elimination rate constant. The presented values in the table are based on all 14 participants receiving the F1 formulation in a 2-way crossover pattern.

Area Under the Concentration-Time Curve (AUC0-t) of Entrectinib and M5 Metabolite
At pre-defined intervals from study Day 1 through Day 5 of each Period (Periods 1 and 2 = 6 days)

The area under the concentration-time curve calculated from Hour 0 to the last measurable concentration, calculated using the linear trapezoidal rule for increasing concentrations and the logarithmic rule for decreasing concentrations. The presented values in the table are based on all 14 participants receiving the F1 formulation in a 2-way crossover pattern.

Maximum Observed Concentration (Cmax) of Entrectinib and M5 Metabolite
At pre-defined intervals from study Day 1 through Day 5 of each Period (Periods 1 and 2 = 6 days)

The presented values in the table are based on all 14 participants receiving the F1 formulation in a 2-way crossover pattern.

Secondary Endpoints

Percentage of Participants With Treatment-Emergent Adverse Events (TEAEs)
Baseline through the end of study (up to clinical cut-off date 04 Feb 2019 [27 days])
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelCROSSOVER
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
F1 to F06 CrossoverEXPERIMENTALParticipants first randomized to this arm will receive a single oral dose of entrectinib F1 (test formulation) on Day 1 of Period 1 after a standardized meal. This dose will be followed by a minimum 14-day washout period, after which participants will receive a single oral dose of entrectinib F06 (reference formulation) under fasted conditions on Day 1 of Period 2 (Periods 1 and 2 = 6 days).
F06 to F1 CrossoverEXPERIMENTALParticipants first randomized to this arm will receive a single oral dose of entrectinib F06 (reference formulation) on Day 1 of Period 1 after a standardized meal. This dose will be followed by a minimum 14-day washout period, after which participants will receive a single oral dose of entrectinib F1 (test formulation) under fasted conditions on Day 1 of Period 2 (Periods 1 and 2 = 6 days).

Interventions

NameTypeDescription
Entrectinib Test Formulation (F1)DRUGParticipants will receive a single oral dose of entrectinib F1 after completion of a standardized meal.
Entrectinib Reference Formulation (F06)DRUGParticipants will receive a single oral dose of entrectinib F06 after completion of a standardized meal.
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Eligibility Criteria

Age Range18 Years to 60 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * Healthy in the opinion of the investigator. Healthy is defined by the absence of evidence of any active disease or clinically significant medical condition based on a detailed medical history and examination * Negative test results for Hepatitis B, Hepatitis C, and Human Immun...

Countries:United States
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Frequently asked questions about Entrectinib Test Formulation

What is Entrectinib used for?

Entrectinib is an investigational small molecule being studied for the treatment of various cancers, including locally advanced solid tumors, advanced unresectable or metastatic solid malignancies, solid tumors, carcinoma, and non-small-cell lung cancer. It is also being evaluated in pediatric patients with solid or primary CNS tumors who have no satisfactory treatment options.

Who makes Entrectinib?

Entrectinib is being developed by Roche Holding AG, which trades under the ticker RHHBY. The company is conducting clinical trials to evaluate the drug's safety and efficacy in multiple oncology indications.

What phase is Entrectinib in?

Entrectinib is in clinical development, with trials listed as Phase 1, Phase 2, and Phase 3. It is an investigational drug and has not been approved by the FDA. The ongoing studies include a Phase 1 trial in children and adolescents and a Phase 3 trial in non-small-cell lung cancer.

What clinical trials is Entrectinib in?

Entrectinib is being studied in several clinical trials, including NCT02650401, a Phase 1 study in children and adolescents with solid or CNS tumors; NCT03961100, a completed Phase 1 bioavailability study in healthy volunteers; NCT04589845, a Phase 2 platform study in solid tumors; and NCT04603807, a Phase 3 trial comparing Entrectinib to crizotinib in ROS1-positive NSCLC.

How does Entrectinib work?

Entrectinib is a kinase inhibitor, belonging to the -tinib class of drugs. It works by targeting and inhibiting specific kinases involved in tumor growth. The drug is being evaluated for its ability to block these molecular targets in various solid tumors and non-small-cell lung cancer.

Is Entrectinib the same as RXDX-101?

Yes, Entrectinib is also known as RXDX-101. The Phase 1 clinical trial NCT02650401, which studies the drug in children and adolescents with locally advanced or metastatic solid or primary CNS tumors, refers to Entrectinib as RXDX-101 in its title.