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Effect of Regorafenib on Digoxin and Rosuvastatin in Patients With Advanced Solid Malignant Tumors.

Phase 1
Completed
Conditions
Neoplasms
Interventions
Registration Number
NCT02106845
Lead Sponsor
Bayer
Brief Summary

Evaluate the effect of regorafenib on the pharmacokinetics of digoxin (P-gp substrate : P-glycoprotein) and rosuvastatin (BCRP substrate: Breast cancer resistant protein) by comparing their Area under time curve (AUC(0-24)) and maximum drug concentration (Cmax) on Day -7 and Cycle 1 or Cycle 2 Day 15 of regorafenib in cancer patients

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
42
Inclusion Criteria
  • The following criteria apply to ALL patients starting the study treatment:

    • Patients with histologically confirmed, locally advanced or metastatic solid tumors refractory to standard therapy or in whom regorafenib is considered a standard treatment.
    • Male or Female Caucasian patients >/= 18 years of age
    • Women of childbearing potential and men must agree to use adequate contraception before entering the program until at least 8 weeks after the last study drug administration.
    • Life expectancy of at leat 12 weeks
    • Eastern Cooperative Oncology Group (ECOG) Performance Status of 0 or 1
    • Adequate bone marrow and liver function
    • Estimated creatinine clearance (CLcr) ≥ 30 mL/min as calculated using the Cockroft-Gault (C-G) equation.
    • Thyroid Stimulating Hormone(TSH) within normal ranges.
  • The following inclusion criteria apply to Group A (digoxin + regorafenib) patients ONLY:

    • Potassium, magnesium and calcium blood levels within normal range according to the local laboratory.
  • The following inclusion criteria apply to Group B (rosuvastatin + regorafenib) patients ONLY:

    • Signed genetic informed consent. Patients must be able to understand and willing to sign the written informed consent intended to screen for BCRP and OATP1B1 polymorphisms.
Exclusion Criteria
  • For ALL patients

  • Major surgical procedure, open biopsy, or significant traumatic injury within 28 days before start of study medication.

  • Non-healing wound, skin ulcer, or bone fracture.

  • Ongoing or active infection.

  • Other anticancer treatment.

  • Patients unable to swallow oral medications

  • For Group A (digoxin + regorafenib):

    • Family history of sudden cardiac death.
  • For Group B (rosuvastatin + regorafenib):

    • Patients with porphyria.
    • Patients with intestinal or urinary obstructions.

Study & Design

Study Type
INTERVENTIONAL
Study Design
CROSSOVER
Arm && Interventions
GroupInterventionDescription
Group B: BCRP probe substrate (rosuvastatin) + regorafenibRegorafenib (Stivarga, BAY73-4506)-
P-gp probe substrate(digoxin)+regorafenibRegorafenib (Stivarga, BAY73-4506)-
P-gp probe substrate(digoxin)+regorafenibDigoxin-
Group B: BCRP probe substrate (rosuvastatin) + regorafenibRosuvastatin-
Primary Outcome Measures
NameTimeMethod
Maximum drug concentration (Cmax) in plasma for rosuvastatinOn Pre-Cycle Day -7 and on Cycle 1 Day15 or Cycle 2 Day 15
Maximum drug concentration (Cmax) in plasma for DigoxinOn Pre-Cycle Day -7 and on Cycle 1 Day15 or Cycle 2 Day 15
Area under the plasma concentration-time curve from time zero to 24 hours (AUC(0-24)) for DigoxinOn Pre-Cycle Day -7 and on Cycle 1 Day15 or Cycle 2 Day 15
Area under the plasma concentration-time curve from time zero to 24 hours (AUC(0-24)) for rosuvastatinOn Pre-Cycle Day -7 and on Cycle 1 Day15 or Cycle 2 Day 15
Secondary Outcome Measures
NameTimeMethod
Number of participants with drug related adverse events as a measure of safety and tolerabilityUp to 30 days after last dose
Number of participants with adverse events as a measure of safety and tolerabilityUp to 30 days after last dose
Tumor Response following RECIST criteriaFrom first dose up to 3 months after end of treatment
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