Comparison of Pharmacokinetics and Safety of Two Formulations of Letrozole (2.5 mg) in Healthy Male Volunteers.
10.12793/jkscpt.2012.20.2.135
- Author:
Yook Hwan NOH
1
;
Kyun Seop BAE
;
Sang Heon CHO
;
Sangmin CHOE
;
Jong Lyul GHIM
;
Jin Ah JUNG
;
Un Jib KIM
;
Seok Joon JIN
;
Hyun Jung PARK
;
Jung Chul KIM
;
Hyeong Seok LIM
Author Information
1. Department of Clinical Pharmacology and Therapeutics, Asan Medical Center, Seoul, Korea. mdlhs@amc.seoul.kr
- Publication Type:Original Article
- Keywords:
Letrozole;
Pharmacokinetics;
Safety;
Bioequivalence;
Healthy volunteers
- MeSH:
Aromatase;
Breast;
Clinical Chemistry Tests;
Cross-Over Studies;
Electrocardiography;
Humans;
Male;
Nitriles;
Physical Examination;
Therapeutic Equivalency;
Triazoles;
Vital Signs
- From:Journal of Korean Society for Clinical Pharmacology and Therapeutics
2012;20(2):135-144
- CountryRepublic of Korea
- Language:English
-
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.