Comparison of Pharmacokinetics and Safety of Two Formulations of Letrozole (2.5 mg) in Healthy Male Volunteers
Journal of Korean Society for Clinical Pharmacology and Therapeutics
; : 135-144, 2012.
Article
in En
| WPRIM
| ID: wpr-190983
Responsible library:
WPRO
ABSTRACT
BACKGROUND: Letrozole is an oral non-steroidal inhibitor of the aromatase enzyme, which has proven to be a useful drug against breast cancer. METHODS: This single-dose, randomized 2 x 2 crossover study was conducted in healthy male volunteers. Participants of each sequence group (each 13 volunteers for sequence group) received, in randomized sequence, a single oral 2.5-mg dose of generic letrozole (test) or branded letrozole (reference). Each treatment period was separated by a 5-week washout period. Blood samples were collected for up to 312 hours after drug administration, and drug concentrations were determined using validated LC/MS-MS. Pharmacokinetic properties were obtained using noncompartmental analysis. Drug tolerability was assessed throughout the study, using measurements of vital signs, physical examination, clinical chemistry testing, EKG, and interviews. RESULTS: A total of 26 subjects completed the study. The geometric mean ratios (90% CI) of Cmax and AUClast were 0.92 (0.85 - 0.99) and 1.01 (0.97 - 1.04), respectively. No serious AEs were reported, and there were no clinically significant differences between test and reference groups. CONCLUSION: The findings from this study suggest bioequivalence between two formulations of letrozole in healthy male volunteers. The safety profile of two formulations had similar characteristics.
Key words
Full text:
1
Index:
WPRIM
Main subject:
Physical Examination
/
Triazoles
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Breast
/
Aromatase
/
Therapeutic Equivalency
/
Cross-Over Studies
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Clinical Chemistry Tests
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Electrocardiography
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Vital Signs
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Nitriles
Type of study:
Clinical_trials
Limits:
Humans
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Male
Language:
En
Journal:
Journal of Korean Society for Clinical Pharmacology and Therapeutics
Year:
2012
Type:
Article