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A Study of the Safety, Tolerability, and Effects of Cobimetinib and GDC-0994 in Patients With Locally Advanced or Metastatic Solid Tumors

Phase 1
Completed
Conditions
Non-Small Cell Lung Cancer, Metastatic Colorectal Cancer, Metastatic Non Small Cell Lung Cancer, Metastatic Cancers, Melanoma
Interventions
Registration Number
NCT02457793
Lead Sponsor
Genentech, Inc.
Brief Summary

This is a two-stage dose-escalation study to assess the safety, tolerability and effects of oral dosing of cobimetinib and GDC-0994 administered in combination in patients with histologically confirmed, locally advanced, or metastatic solid tumors for which standard therapies either do not exist or have proven ineffective or intolerable.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
24
Inclusion Criteria
  • Eastern Cooperative Oncology Group (ECOG) performance status of 0 or 1
  • Histologically or cytologically documented, locally advanced or metastatic solid tumors for which standard therapy either does not exist or has proven ineffective or intolerable
  • Evaluable disease or disease measurable
  • Life expectancy > or = 12 weeks
  • Adequate hematologic and end organ function
  • For female patients of childbearing potential and male patients with partners of childbearing potential, use of an effective form of contraception with continued use for study duration and up to 3 months or more following discontinuation of treatment drug
  • Fluorodeoxyglucose positron emission tomography (FDG-PET) avid disease on baseline scan

For enrollment in part 2, patients must meet all of the following:

  • Measurable disease
  • No more than four prior systemic therapies for locally advanced or metastatic cancer
Exclusion Criteria
  • History of prior significant toxicity from another MEK inhibitor or ERK inhibitor requiring discontinuation of treatment
  • Evidence of visible retinal pathology as assessed by ophthalmologic examination that is considered a risk factor for retinal vein thrombosis
  • History of glaucoma
  • Intraocular pressure > 21 mmHg as measured by tonometry
  • Predisposing factors to retinal vein occlusion (RVO)
  • History of RVO, neurosensory retinal detachment, or neovascular macular degeneration
  • Allergy or hypersensitivity to components of the cobimetinib or GDC-0994 formulation
  • Palliative radiotherapy within 2 weeks prior to first dose of study-drug treatment in Cycle 1
  • Experimental therapy within 4 weeks prior to first dose of study-drug treatment in Cycle 1
  • Major surgical procedure or significant traumatic injury within 4 weeks prior to the first dose of study-drug treatment in Cycle 1, or anticipation of the need for major surgery during the course of study treatment
  • Anti-cancer therapy within 28 days prior to the first dose of study-drug treatment in Cycle 1
  • Current severe, uncontrolled systemic disease
  • History of clinically significant cardiac dysfunction
  • History of symptomatic congestive heart failure or serious cardiac arrhythmia requiring treatment
  • History of myocardial infarction within 6 months prior to the first dose of study-drug treatment in Cycle 1
  • History of congenital long QT syndrome or QTc > 470 msec
  • LVEF
  • History of malabsorption or other condition that would interfere with enteral absorption
  • Clinically significant history of liver disease, current alcohol abuse, or current known active infection with HIV, hepatitis B virus, or hepatitis C virus
  • Any condition requiring warfarin or thrombolytic anticoagulants
  • Active autoimmune disease
  • Uncontrolled ascites requiring weekly large volume paracentesis for 3 consecutive weeks prior to enrollment
  • Pregnancy, lactation, or breastfeeding
  • Known brain metastases that are untreated, symptomatic, or require therapy to control symptoms
  • No other history of or ongoing malignancy that would potentially interfere with the interpretation of the Pharmacodynamic (PD) or efficacy assays

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
COB 40 mg + GDC 200 mgGDC-0994Concurrent or intermittent dosing of cobimetinib 40 mg, concurrent with GDC-0994 200 mg for 21 consecutive days, followed by 7 days off.
COB 80 mg + GDC 400 mgGDC-0994Concurrent or intermittent dosing of cobimetinib 80 mg, concurrent with GDC-0994 400 mg for 21 consecutive days, followed by 7 days off.
COB 20 mg + GDC 200 mgGDC-0994Concurrent or intermittent dosing of cobimetinib 20 mg, concurrent with GDC-0994 200 mg for 21 consecutive days, followed by 7 days off.
COB 80 mg + GDC 200 mgGDC-0994Concurrent or intermittent dosing of cobimetinib 80 mg, concurrent with GDC-0994 200 mg for 21 consecutive days, followed by 7 days off.
COB 100 mg + GDC 200 mgGDC-0994Concurrent or intermittent dosing of cobimetinib 100 mg, concurrent with GDC-0994 200 mg for 21 consecutive days, followed by 7 days off.
Not assignedGDC-0994One participant was assigned to receive intermittent cobimetinib 80 milligrams (mg) + GDC 0994 200 mg) and did receive study drug. However, the participant diary was not returned, and the site was unable to document study dose administration.
Not assignedCobimetinibOne participant was assigned to receive intermittent cobimetinib 80 milligrams (mg) + GDC 0994 200 mg) and did receive study drug. However, the participant diary was not returned, and the site was unable to document study dose administration.
COB 20 mg + GDC 200 mgCobimetinibConcurrent or intermittent dosing of cobimetinib 20 mg, concurrent with GDC-0994 200 mg for 21 consecutive days, followed by 7 days off.
COB 40 mg + GDC 200 mgCobimetinibConcurrent or intermittent dosing of cobimetinib 40 mg, concurrent with GDC-0994 200 mg for 21 consecutive days, followed by 7 days off.
COB 80 mg + GDC 200 mgCobimetinibConcurrent or intermittent dosing of cobimetinib 80 mg, concurrent with GDC-0994 200 mg for 21 consecutive days, followed by 7 days off.
COB 80 mg + GDC 400 mgCobimetinibConcurrent or intermittent dosing of cobimetinib 80 mg, concurrent with GDC-0994 400 mg for 21 consecutive days, followed by 7 days off.
COB 100 mg + GDC 200 mgCobimetinibConcurrent or intermittent dosing of cobimetinib 100 mg, concurrent with GDC-0994 200 mg for 21 consecutive days, followed by 7 days off.
Primary Outcome Measures
NameTimeMethod
Percentage of Participants With at Least One Serious Adverse Event (SAE)Up to 15 months

A SAE is any experience that: results in death, is life-threatening, requires in-patient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect, or is medically significant.

Percentage of Participants With at Least One Adverse EventUp to 15 months

An adverse event is any untoward medical occurrence in a clinical investigation participant administered a pharmaceutical product, regardless of causal attribution.

Percentage of Participants With at Least One Adverse Event of Special InterestUp to 15 months

AESIs were graded per the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE), v4.0. AESIs included the following: Grade ≥ 1 retinal vein occlusion; Grade ≥ 2 visual disturbances (including events suggestive of serous retinopathy); Grade ≥ 3 rash for \> 7 days; Grade ≥ 3 diarrhea for \> 3 days; Grade ≥ 2 left ventricular ejection fraction (LVEF) decrease; Grade 3 hepatotoxicity; any dose-limiting toxicity (DLT); cases of potential drug-induced liver injury that include an elevated alanine aminotransferase (ALT) or aspartate aminotransferase (AST) (AST \> 3 × baseline value \[and above the upper limit of normal, ULN\]) in combination with either an elevated bilirubin ( \> 2 × ULN) or clinical jaundice; or suspected transmission of an infectious agent by either study drug.

Mean Change From Baseline in Pulse RateBaseline, up to 15 months
Mean Change From Baseline in Systolic Blood PressureBaseline, up to 15 months
Mean Change From Baseline in TemperatureBaseline, up to 15 months
Mean Change From Baseline in WeightBaseline, up to 15 months
Mean Change From Baseline in Diastolic Blood PressureBaseline, up to 15 months
Number of Participants With Dose-Limiting Toxicities (DLTs)28 days (Cycle 1)

DLTs include symptoms considered by the investigator to be possibly related to study drug.

Percentage of Participants With Laboratory AbnormalitiesUp to 15 months

Laboratory abnormalities were graded per the National Cancer Institute Common Terminology Criteria for Adverse Events (NCI CTCAE), v4.0.

SGPT/ALT - serum glutamic-pyruvic transaminase/alanine aminotransferase; SGOT/AST - serum glutamic oxaloacetic transaminase/aspartate aminotransferase

Mean Change From Baseline in Lean Body MassBaseline, Day 15
Mean Change From Baseline in Respiratory RateBaseline, up to 15 months
Secondary Outcome Measures
NameTimeMethod
Total Exposure (AUC From Time 0 to 24 Hour After Dose) for GDC-09940 to 24 hours post-dose (Up to Day 22)

Data are reported for evaluable participants.

Total Exposure (AUC From Time 0 to 24 Hour After Dose) for Cobimetinib0 to 24 hours post-dose (Up to Day 22)
Maximum Serum Concentration (Cmax) for GDC-0994Up to Day 22
Median Time to Maximum Serum Concentration (Tmax) for CobimetinibUp to Day 22
Mean Accumulation RatioPre-dose Day 1 Cycle 1, 2, 3, Day 18, 21 Cycle 1; post-dose 0.5, 1, 2, 3, 4, 6 hours Day 1, 18, 21 Cycle 1; Day 2, 15, 19, 22, Cycle 1
Maximum Serum Concentration (Cmax) for CobimetinibUp to Day 22
Mean Terminal Half-life (t1/2)Up to day 22 of study
Change From Baseline in Fluorodeoxyglucose Positron Emission Tomography (FDG-PET)Baseline, Day 15
Change From Baseline in Tumor Tissue BiomarkersUp to 15 months
Median Time to Maximum Serum Concentration (Tmax) for GDC-0994Up to Day 22

Trial Locations

Locations (5)

University of Colorado

🇺🇸

Aurora, Colorado, United States

Yale Cancer Center

🇺🇸

New Haven, Connecticut, United States

Sarah Cannon Research Institute

🇺🇸

Nashville, Tennessee, United States

Dana Farber Cancer Institute

🇺🇸

Boston, Massachusetts, United States

Washington University School of Medicine

🇺🇸

Saint Louis, Missouri, United States

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