Clinical trial NCT01751919: A Clinical Trial to Compare the Pharmacokinetics of Imatinib Mesylate Tablet 400mg (1 Tablet) and Glivec Film-coated Tablet 100mg (4 Tablets)(Phase I)
Official title: A Randomized, Open-label, Single-dose, Crossover Clinical Trial to Compare the Pharmacokinetics of Imatinib Mesylate Tablet 400 mg (1 Tablet) and Glivec Film-coated Tablet 100 mg (4 Tablets) After Oral Administration in Healthy Male Subjects (Phase I)
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Chronic Myeloid Leukemia
Gastrointestinal Stromal Tumor
Keywords: CML
GIST
Lead sponsor: Dong-A ST Co., Ltd.
Sponsor class: INDUSTRY
First posted: 2012-12-18
Enrollment: 37
Sex: MALE
Minimum age (years): 20
Maximum age (years): 50
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: RANDOMIZED
Intervention model: CROSSOVER
Primary purpose: TREATMENT

Brief summary: 1. Investigational Product

   1. Imatinib mesylate tablet 400 mg
   2. Glivec film-coated tablet 100 mg (Comparator)
2. Expected target disease

   1. chronic myeloid leukemia
   2. Gastrointestinal stromal tumors
3. Study design : Randomized, open-label, single dose, two-period, two-way, crossover study

   1. 36 healthy subjects, 2 groups (18 subjects/group)
   2. 2 Period (either 1-a(1 tablet) or 1-b(4 tablet))
   3. wash-out period : 14 days
4. Evaluation on pharmacokinetics(PKs) and safety

   1. PKs : Cmax, AUClast, Tmax, AUCinf, t1/2
   2. safety : adverse events, physical examination, vital sign, ECG, Laboratory test
5. Statistical method

   1. Demography Characteristics
   2. Pharmacokinetic parameters
   3. Safety data


Eligibility criteria: Inclusion Criteria:

* healthy male volunteers between the ages of 20 to 50 years old
* weight more than 55kg and within the range of ±20% of ideal body weight (IBW)
* having neither congenital/chronic diseases nor pathological symptoms/findings as results of medical examination
* doctor determines to be suitable as subjects within 3 weeks ago before administration

Exclusion Criteria:

* Hypersensitivity(or history of hypersensitivity) to medicines including imatinib mesylate
* Active Liver Diseases or exceed 1.5 times the normal range of AST, ALT, total bilirubin
* Creatinine clearance \< 80 mL/min
* Gastrointestinal diseases or surgeries that affect absorption of drug
* Excessive drinking(exceed 21units/week)
* Smoking over 10 cigarettes per day

Primary outcomes:
measure: Maximum concentration in plasma (Cmax) of Imatinib mesylate
timeFrame: Pre-dose(0h) AND 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 24, 48, 72 h post-dose
measure: Area under the plasma concentration-time curve from zero time until the last measurable concentration (AUClast) of Imatinib mesylate
timeFrame: Pre-dose(0h) AND 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 24, 48, 72 h post-dose
Secondary outcomes:
measure: Time to Cmax (Tmax) of Imatinib mesylate
timeFrame: Pre-dose(0h) AND 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 24, 48, 72 h post-dose
measure: Area under the plasma concentration-time curve from time zero to infinity (AUCinf) of Imatinib mesylate
timeFrame: Pre-dose(0h) AND 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 24, 48, 72 h post-dose
measure: Terminal Elimination Half-life (t1/2) of Imatinib mesylate
timeFrame: Pre-dose(0h) AND 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 24, 48, 72 h post-dose
Other outcomes:
Locations:
city: Daegu
country: Korea, Republic of
facility: Kyungpook National University
Study officials:
References:
citation: Parrillo-Campiglia S, Ercoli MC, Umpierrez O, Rodriguez P, Marquez S, Guarneri C, Estevez-Parrillo FT, Laurenz M, Estevez-Carrizo FE. Bioequivalence of two film-coated tablets of imatinib mesylate 400 mg: a randomized, open-label, single-dose, fasting, two-period, two-sequence crossover comparison in healthy male South American volunteers. Clin Ther. 2009 Oct;31(10):2224-32. doi: 10.1016/j.clinthera.2009.10.009.
citation: Nikolova Z, Peng B, Hubert M, Sieberling M, Keller U, Ho YY, Schran H, Capdeville R. Bioequivalence, safety, and tolerability of imatinib tablets compared with capsules. Cancer Chemother Pharmacol. 2004 May;53(5):433-8. doi: 10.1007/s00280-003-0756-z.