Determination of the Relative Bioavailability of ARQ 197 Tablet Formulation With Capsule C Formulation as a Reference in Subjects With Advanced Solid Tumors

An Open-Label, Phase 1, Randomized, Two-Treatment, Two-Period, Two-Way Crossover, Relative Bioavailability Study Of A Capsule And A Tablet Formulation Of ARQ 197 In Subjects With Advanced Solid Tumors

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT01149720

Enrollment

Registered

2010-06-23

Start date

2010-07-31

Completion date

2011-03-31

Last updated

2019-02-12

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Solid Tumors

Keywords

Relative bioavailability, ARQ 197

Brief summary

This is a Phase 1, randomized, open label, 2 treatment, 2 period, 2-way crossover study, with an extension phase design in which the steady state PK of ARQ 197 will be investigated using the tablet administered in fed state (test treatment) and capsule administered at least 1 hour before or 2 hours after a meal (reference treatment) in subjects with advanced solid tumors.

Interventions

DRUGTivantinib (ARQ 197) Capsule

Oral BID 360 mg dose (Capsule C: 6 X 60 mg) of ARQ 197 at least 1 hour before or 2 hours after a meal for 7 days

DRUGTivantinib (ARQ 197) Tablet

Oral BID 360 mg dose (Tablet: 3 x 120 mg) of ARQ 197 under fed conditions for 7 days

DRUGTivantinib (ARQ 197) Capsule D, oral

Oral BID 360 mg dose (Capsule D: 3 x 120 mg) of ARQ 197 under fed conditions in the extension phase

Study design

Allocation

RANDOMIZED

Intervention model

CROSSOVER

Primary purpose

TREATMENT

Masking

NONE

Eligibility

Sex/Gender

ALL

Age

18 Years to No maximum

Healthy volunteers

Inclusion criteria

* Subjects must have a histologically or cytologically confirmed advanced solid tumor at screening. * Male or female equal or greater than 18 years of age. * All female subjects of childbearing potential must each have a negative serum pregnancy test result before initiating study treatment. * An Eastern Cooperative Oncology Group (ECOG) performance status equal or less than 2 * Adequate bone marrow, liver, and renal function, defined as: * Platelet count equal or greater than 75 x 10(9)/L * Hemoglobin (Hb) equal or greater than 9.0 g/dL * Absolute neutrophil count (ANC) equal or greater than 1.5 x 10(9)/L * Total bilirubin equal or less than 1.5 x upper limit of normal (ULN) * Alanine aminotransferase (ALT) and aspartate aminotransferase (AST) equal or less than 3 x ULN (equal or less than 5 x ULN for subjects with liver metastases) * Serum creatinine equal or less than 1.5 x ULN

Exclusion criteria

* History of cardiac disease: Active coronary artery disease (CAD), defined as myocardial infarction (MI), unstable angina, coronary bypass graft (CABG), or stenting within 6 months prior to study entry (an MI that occurred \> 6 months prior to study entry is permitted) * Evidence of uncontrolled bradycardia or other cardiac arrhythmia defined as equal or greater than Grade 2 according to NCI CTCAE, version 4.0, or uncontrolled hypertension * Active, clinically serious infection(s) defined as equal or greater than Grade 2 according to NCI CTCAE, version 4.0. * Known metastatic brain or meningeal tumors, unless the subject is \> 3 months from definitive therapy and clinically stable (supportive therapy with steroids or anticonvulsant medications is allowed) with respect to the tumor at the time of first dose of study drug. * Prior therapy with mesenchymal-epithelial transition factor (c-MET) inhibitors, including ARQ 197.

Design outcomes

Primary

Measure	Time frame	Description
Determination of the relative bioavailability of ARQ 197 tablet formulation with capsule C formulation	14 days	The primary endpoints are the area under the concentration time curve from time of dosing until 12 hours post-dose (AUC0-12) and maximum observed concentration in plasma (Cmax) of ARQ 197 following the administration of the tablet (fed conditions) and capsule formulation (at least 1 hour before or 2 hours after a meal).

Secondary

Measure	Time frame	Description
Assessment of additional pharmacokinetic parameters of ARQ 197 tablet formulation and capsule C formulation	14 days	Time until Cmax (tmax), apparent oral clearance (CL/F), and apparent volume of distribution (V/F) of ARQ 197, and if possible, minimum observed concentration (Cmin) and average observed concentration (Cavg) following the administration of the tablet (fed conditions) and capsule formulation (at least 1 hour before or 2 hours after a meal)

Countries

United States

Outcome results

None listed

Source: ClinicalTrials.gov · Data processed: Feb 4, 2026