Pharmacokinetic Study Comparing Blood Levels of Dasatinib in Healthy Participants Who Received the Tablet Formulation With Those Who Received Liquid and Tablet-dispersed Formulations

Lead sponsor

Bristol-Myers Squibb is the lead sponsor of 1,538 studies on the registry; 116 are open to participants now.

Of its 429 completed or terminated interventional studies of FDA-regulated products, 223 (52%) have results posted.

Eligibility criteria

Study arms

• Other
  Dasatinib, 100 mg as tablets + water

  Treatment A. Participants were randomized to and received treatment in 1 of 6 sequences (ABC, ACB, BCA, BAC, CAB, or CBA), administered over 3 1-day treatment periods (Days 1, 5, and 9), with treatment changing to next in the sequence at start of each new period. A 3-day washout period followed treatment periods 1 and 2.

  Drug: Dasatinib as tablets

• Other
  Dasatinib, 100 mg as liquid + water

  Treatment B. Participants were randomized to and received treatment in 1 of 6 sequences (ABC, ACB, BCA, BAC, CAB, or CBA), administered over 3 1-day treatment periods (Days 1, 5, and 9), with treatment changing to next in the sequence at start of each new period. A 3-day washout period followed treatment periods 1 and 2.

  Drug: Dasatinib as liquid

• Other
  Dasatinib, 100 mg as tablets in orange juice + water

  Treatment C. Participants were randomized to and received treatment in 1 of 6 sequences (ABC, ACB, BCA, BAC, CAB, or CBA), administered over 3 1-day treatment periods (Days 1, 5, and 9), with treatment changing to next in the sequence at start of each new period. A 3-day washout period followed treatment periods 1 and 2.

  Drug: Dasatinib as dispersed tablets

Interventions

• DrugDasatinib as tablets

  2 50-mg tablets plus 240 mL noncarbonated, nonrefrigerated water. Oral, single dose, 1 day

  Also known as: Dasatinib/BMS-354825

• DrugDasatinib as liquid

  100 mg administered as 10 mL of liquid drug (10 mg/mL) plus 230 mL noncarbonated, nonrefrigerated water. Oral, single dose, 1 day

  Also known as: Dasatinib/BMS-354825

• DrugDasatinib as dispersed tablets

  2 50-mg dispersed tablets in 30 mL of 100% orange juice followed by 15 mL of orange juice plus 195 mL noncarbonated, nonrefrigerated water. Liquid (oral solution), single dose, 1 day.

  Also known as: Dasatinib/BMS-354825

Primary outcomes

1. Maximum Observed Concentration (Cmax) of Dasatinib

   Single-dose pharmacokinetic parameters, including Cmax, were derived using noncompartmental methods from plasma dasatinib concentration-time data.

   Time frame: Days 1-2, Days 5-6, and Days 9-10

2. Area Under the Plasma Concentration-time Curve From Zero to the Last Time of the Last Quantifiable Concentration (AUC[0-T])of Dasatinib

   Single-dose pharmacokinetic, such as AUC(0-T),parameters were derived using noncompartmental methods from plasma dasatinib concentration-time data.

   Time frame: Days 1-2, Days 5-6, and Days 9-10

3. Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC[0-INF]) of Dasatinib

   Single-dose pharmacokinetic parameters, such as AUC(0-INF) were derived using noncompartmental methods from plasma dasatinib concentration-time data.

   Time frame: Days 1-2, Days 5-6, and Days 9-10

Secondary outcomes

1. Time of Maximum Observed Plasma Concentration (Tmax) of Dasatinib

   Single-dose pharmacokinetic parameters, such as Tmax, were derived using noncompartmental methods from plasma dasatinib concentration-time data.

   Time frame: Days 1-2, Days 5-6, and Days 9-10

2. Half-life of Dasatinib

   Time frame: Days 1-2, Days 5-6, and Days 9-10

3. Number of Participants With at Least 1 Adverse Event (AE), With at Least 1 Treatment-related AE, Who Discontinued Due to AEs, and With at Least 1 Serious Adverse Event (SAE)

   An AE is any new untoward medical occurrence or worsening of a preexisting medical condition in a patient or clinical investigation participant who has received an investigational (medicinal) product that does not necessarily have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of investigational product, whether or not considered related to the investigational product. An SAE is an untoward medical event that at any dose results in death, persistent or significant disability/incapacity; is life-threatening or a congenital anomaly/birth defect; or requires or prolongs hospitalization; is an important medical event that may not be immediately life-threatening or result in death or hospitalization but may jeopardize the participant or may require medical or surgical intervention.

   Time frame: Continually from enrollment through Day 9 and at study discharge on Day 10

4. Number of Participants With Clinically Significant Changes in Vital Signs or Electrocardiogram (ECG) Findings

   Blood pressure and heart rate were measured after the participant had been seated quietly for at least 5 minutes. ECG findings were recorded after the participant had been supine for at least 5 minutes. Clinically significant as reported by principal investigator.

   Time frame: Day -1, Screening, and Days 1, 5, 9 and 10 (at study discharge)

5. Number of Participants With Marked Abnormalities in Results of Clinical Laboratory Tests

   Criteria for normal: bilirubin (0.2 to 1.3 mg/dL); lactate dehydrogenase (101 to 227 U/L); eosinophils (0.06 to 0.87\*103 c/μL); erythrocytes (4.2 to 5.8\*10\^6 c/μL). Participants were required to fast for a minimum of 4 hours prior to the collection of specimens for clinical laboratory tests at screening and for at least 8 hours prior to collection on Day -1. Marked abnormalities were reported for the treatment regiment that participants received just prior to clinical laboratory testing.

   Time frame: Day -1, Screening, and Day 9 of current treatment regimen

Baseline characteristics

Related links

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