PMID- 21353117
OWN - NLM
STAT- MEDLINE
DCOM- 20110624
LR  - 20141120
IS  - 1879-114X (Electronic)
IS  - 0149-2918 (Linking)
VI  - 32
IP  - 14
DP  - 2010 Dec
TI  - Relative bioavailability and tolerability of two formulations of bicalutamide 
      50-mg tablets: a randomized-sequence, open-label, two-period crossover study in 
      healthy Korean male subjects.
PG  - 2496-501
LID - 10.1016/j.clinthera.2011.01.017 [doi]
AB  - BACKGROUND: Bicalutamide is an oral nonsteroidal antiandrogenic drug used in the 
      treatment of prostate cancer. A new generic 50-mg tablet formulation of 
      bicalutamide has recently been developed. OBJECTIVE: This study evaluated the 
      relative bioavailability and tolerability of the new generic formulation of 
      bicalutamide 50-mg tablets (test) and the currently marketed formulation 
      (reference) in healthy Korean male subjects. The study was conducted to meet 
      Korean regulatory requirements for authorization to market the generic 
      formulation. METHODS: This was a randomized-sequence, open-label study in which 
      healthy Korean male subjects (aged 20-55 years) received single doses of the test 
      and reference formulations in a 2-period crossover fashion, with a 6-week washout 
      period between doses. Blood samples for the determination of plasma bicalutamide 
      concentrations were obtained at regular intervals over 672 hours after dose 
      administration. Pharmacokinetic parameters were determined using noncompartmental 
      methods. Relative bioavailability was evaluated by comparing the log-transformed 
      C(max) and AUC(0-672) of the 2 formulations; Korean regulatory requirements for 
      the assumption of bioequivalence were met if the 90% CIs fell within the range of 
      0.80 to 1.25. Tolerability was assessed based on physical examinations, vital 
      signs, clinical laboratory tests, electrocardiograms (ECGs), and adverse events 
      (AEs) (spontaneously reported or observed by investigators). RESULTS: Of 47 
      volunteers screened for inclusion, 38 were enrolled and 32 completed the study 
      (mean [SD] age, 24.9 [3.7] years; mean height, 173.8 [6.2] cm; mean weight, 66.1 
      [7.1] kg). Median T(max) was 24 hours for both formulations. The C(max) of the 
      test and reference formulations was 1176.2 (191.6) and 1118.9 (209.5) mug/L, 
      respectively. The corresponding values for AUC(0-672) were 277,503 (66,865) and 
      271,961 (75,597) mug . h/L. The 90% CIs for the geometric mean ratios of 
      log-transformed C(max) and AUC(0-672) were 1.00 to 1.11 and 0.99 to 1.07, 
      respectively. Thirty-three AEs were reported, including 17 events in 9 subjects 
      who received the test formulation and 16 events in 12 subjects who received the 
      reference formulation. All AEs were mild, and no subjects discontinued the study 
      because of AEs. CONCLUSIONS: In this single-dose study in healthy Korean male 
      subjects, the pharmacokinetic parameters of the new generic formulation of 
      bicalutamide 50-mg tablets did not differ significantly from those of the 
      reference formulation. The new generic formulation met Korean regulatory criteria 
      for the assumption of bioequivalence to the currently marketed formulation. Both 
      formulations were well tolerated. Korea Food and Drug Administration registration 
      number: PSPD 3057.
CI  - Copyright (c) 2010 Elsevier HS Journals, Inc. All rights reserved.
FAU - Lee, Seunghwan
AU  - Lee S
AD  - Department of Pharmacology and Clinical Pharmacology, Seoul National University 
      College of Medicine and Hospital, Seoul, Korea.
FAU - Yoon, Seo Hyun
AU  - Yoon SH
FAU - Cho, Joo-Youn
AU  - Cho JY
FAU - Shin, Sang-Goo
AU  - Shin SG
FAU - Jang, In-Jin
AU  - Jang IJ
FAU - Yu, Kyung-Sang
AU  - Yu KS
LA  - eng
PT  - Journal Article
PT  - Randomized Controlled Trial
PT  - Research Support, Non-U.S. Gov't
PL  - United States
TA  - Clin Ther
JT  - Clinical therapeutics
JID - 7706726
RN  - 0 (Androgen Antagonists)
RN  - 0 (Anilides)
RN  - 0 (Drugs, Generic)
RN  - 0 (Nitriles)
RN  - 0 (Tablets)
RN  - 0 (Tosyl Compounds)
RN  - A0Z3NAU9DP (bicalutamide)
SB  - IM
MH  - Administration, Oral
MH  - Adult
MH  - Androgen Antagonists/adverse effects/blood/*pharmacokinetics
MH  - Anilides/adverse effects/blood/*pharmacokinetics
MH  - Area Under Curve
MH  - Biological Availability
MH  - Cross-Over Studies
MH  - Drugs, Generic/adverse effects/*pharmacokinetics
MH  - Humans
MH  - Male
MH  - Middle Aged
MH  - Nitriles/adverse effects/blood/*pharmacokinetics
MH  - Republic of Korea
MH  - Tablets
MH  - Tosyl Compounds/adverse effects/blood/*pharmacokinetics
MH  - Young Adult
EDAT- 2011/03/01 06:00
MHDA- 2011/06/28 06:00
CRDT- 2011/03/01 06:00
PHST- 2010/12/14 00:00 [accepted]
PHST- 2011/03/01 06:00 [entrez]
PHST- 2011/03/01 06:00 [pubmed]
PHST- 2011/06/28 06:00 [medline]
AID - S0149-2918(11)00018-X [pii]
AID - 10.1016/j.clinthera.2011.01.017 [doi]
PST - ppublish
SO  - Clin Ther. 2010 Dec;32(14):2496-501. doi: 10.1016/j.clinthera.2011.01.017.