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Phase 1 Completed N=20 Randomized Treatment

A Study to Evaluate the Effect of a Proton-Pump Inhibitor (Rabeprazole) on the Relative Bioavailability of Cobimetinib in Healthy Participants

Healthy Volunteer
Source: ClinicalTrials.gov NCT01277718 ↗
Enrolled (actual)
20
Serious AEs
0.0%
Results posted
Jul 2016
Primary outcomePrimary: Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf) of Cobimetinib — 778; 864; 846 nanograms*hours/milliliter (ng*hr/mL)

Summary

This is a Phase 1, single-center, open-label, randomized, 3-period, 2-sequence crossover study of cobimetinib in healthy participants to evaluate the effect of the proton-pump inhibitor (PPI) rabeprazole on the relative bioavailability of cobimetinib in healthy participants when administered in the fed or fasted states.

Outcome Measures

OutcomeResultp-value
PRIMARY
Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf) of Cobimetinib
778; 864; 846
PRIMARY
Maximum Observed Concentration of Cobimetinib
17.0; 17.2; 14.8

Eligibility Criteria

Inclusion Criteria

  • With a body mass index range of 18.5 to 29.9 kilograms per meter square (kg/m^2)
  • In good health, determined by no clinically significant findings from medical history, 12-lead electrocardiogram (ECG), and vital signs
  • Clinical laboratory evaluations within the reference range for the test laboratory
  • Negative test for selected drugs of abuse at Screening (does not include alcohol) and at each Check-in
  • Negative hepatitis panel (including hepatitis B virus surface antigen [HBsAg] and hepatitis C virus antibody [anti-HCV]) and negative human immunodeficiency virus (HIV) antibody screens
  • Healthy males and females of nonchildbearing potential who agree to use effective contraception

Exclusion Criteria

  • Significant history or clinical manifestation of any significant metabolic, allergic, dermatological, hepatic, renal, hematological, pulmonary, cardiovascular, gastrointestinal, neurological, or psychiatric disorder
  • History of significant hypersensitivity, intolerance, or allergy to any drug compound, food, or other substance
  • History of stomach or intestinal surgery or resection that would potentially alter absorption and/or excretion of orally administered drugs, except that appendectomy, hernia repair, and/or cholecystectomy will be allowed
  • History or presence of an abnormal ECG
  • History of alcoholism or drug addiction within 1 year prior to Period 1 Check-in
  • Use of any tobacco- or nicotine-containing products within 6 months prior to Period 1 Check-in
  • Participation in any other investigational study drug trial in which receipt of an investigational study drug occurred within 30 days or 5 half-lives, whichever is longer, prior to Period 1 Check-in
  • Use of any prescription medications/products within 14 days prior to Period 1 Check-in
  • Use of any over-the-counter, non-prescription preparations within 7 days prior to Period 1 Check-in
  • Use of alcohol-, grapefruit-, or caffeine-containing foods or beverages within 72 hours prior to Period 1 Check-in
  • Poor peripheral venous access
  • Any acute or chronic condition that would limit the participant's ability to complete and/or participate in this clinical study
  • Female participant is pregnant, lactating, or breastfeeding
  • Use of PPIs or histamine H2 receptor antagonists within 1 month prior to Period 1 Check-in
  • Known hypersensitivity to rabeprazole or any of its components or to derived products of benzimidazoles
  • Predisposing factors to retinal vein occlusion (RVO)
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT01277718). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.

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