A Study of RO5212054 (PLX3603) in Participants With BRAF V600-Mutated Advanced Solid Tumors

Roche

Status and phase: Completed; Phase 1

Conditions: Neoplasms

Treatments: Drug: RO5212054

Study type: Interventional

Funder types: Industry

Identifiers

NCT01143753

NP25247

2010-018330-42 (EudraCT Number)

Details and patient eligibility

About

This open-label, multi-center study will evaluate the safety, tolerability, and pharmacokinetics of RO5212054 [PLX3603] in participants with BRAF V600-mutated advanced solid tumors. Cohorts of participants will receive escalating oral doses of RO5212054. Anticipated time on study treatment is until disease progression or unacceptable toxicity occurs.

Enrollment: 45 patients

Sex: All

Ages: 18+ years old

Volunteers: No Healthy Volunteers

Inclusion criteria

• Advanced solid tumor
• Dose-escalation phase: Histologically confirmed, newly diagnosed or relapsed/ refractory unresectable American Joint Committee on Cancer (AJCC) Stage IIIC or IV disease
• Eastern Cooperative Oncology Group (ECOG) performance status 0-1
• Adequate liver, renal and bone marrow function

Exclusion criteria

• Participants for whom standard therapy exists and is considered appropriate by the investigator
• Prior treatment with an inhibitor of BRAF (sorafenib allowed)
• Active Central nervous system (CNS) lesions, or history of or known carcinomatous meningitis
• Treatment with any chemotherapy, radiotherapy, immunotherapy or investigational agent within 28 days prior to first dose of study drug
• Anticipated or ongoing anti-cancer therapies other than those administered in this study
• Serious cardiovascular illness within the 6 months prior to study drug administration

Trial design

Primary purpose: Treatment

Allocation: Non-Randomized

Interventional model: Parallel Assignment

Masking: None (Open label)

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45 participants in 2 patient groups

RO5212054: Continuous Dosing Cohort

Experimental group

Description:

Participants will receive RO5212054 in escalating dose levels.

Treatment:

Drug: RO5212054

RO5212054: New Formulation (F05) Bridging Cohort

Experimental group

Description:

Participants will receive RO5212054 as a single dose of new formulation (F05-150 mg film-coated tablet with different ratios of ingredients than F03 to increase bioavailability) and a single dose of current clinical Formulation (F03-150 mg film-coated tablet) in a cross-over manner. Participants will be alternately assigned to receive either F05 or F03 as their first dose, followed by the opposite Formulation as their second dose. Dose of RO5212054 will be decided based on the results of continuous dosing cohort.

Treatment:

Drug: RO5212054