A Randomized, Open-Label, Crossover Phase 1 Study to Evaluate the Effects of Food on the Pharmacokinetics of a Single Oral Dose of a 15-mg Tylerdipine Tablet in Healthy Chinese Male Volunteers

2018 ◽  
Vol 8 (1) ◽  
pp. 126-132
Author(s):  
Lu Wang ◽  
Lijun Xie ◽  
Sufeng Zhou ◽  
Yuanyuan Wang ◽  
Juan Chen ◽  
...  
Keyword(s):  
Oral Dose ◽  
Single Oral Dose ◽  
Phase 1 ◽  
Open Label ◽  
Phase 1 Study ◽  
Male Volunteers ◽  
Crossover Phase ◽  
Healthy Chinese ◽  
Chinese Male

Abstract 2762: An open-label phase 1 study to evaluate the pharmacokinetics of axitinib (AG-013736) in healthy Chinese volunteers

2010 ◽  
Author(s):  
Ying Chen ◽  
Ji Jiang ◽  
Jianyan Zhang ◽  
Michael Tortorici ◽  
Yazdi K. Pithavala ◽  
...  
Keyword(s):  
Phase 1 ◽  
Open Label ◽  
Phase 1 Study ◽  
Open Label Phase ◽  
Healthy Chinese

Pharmacokinetics (PK) and safety of enzalutamide in healthy Chinese males.

2017 ◽  
Vol 35 (15_suppl) ◽  
pp. e14073-e14073
Author(s):  
Qian Chen ◽  
Yan-Mei Liu ◽  
Xiaopeng Zhang ◽  
Risa Fukushi ◽  
Seitaro Asahina
Keyword(s):  
Plasma Concentrations ◽  
Safety Data ◽  
Study Drug ◽  
Upper Respiratory Tract ◽  
Castration Resistant Prostate Cancer ◽  
Open Label ◽  
Single Dose Study ◽  
Male Volunteers ◽  
Healthy Chinese ◽  
Chinese Male

e14073 Background: Enzalutamide (ENZ), an androgen receptor inhibitor, is approved in over 60 countries except China for use in metastatic castration-resistant prostate cancer. The PK of ENZ have been assessed in healthy Caucasian males (Gibbons 2015). This open-label, single-dose study evaluated the PK of ENZ and its major metabolites, and safety of ENZ, in healthy Chinese male volunteers. Methods: Non-elderly healthy Chinese male volunteers received a single oral dose of ENZ (160 mg) under fasting conditions on day 1 and were followed for 50 days. Full PK profiles were obtained for ENZ and its major metabolites, carboxylic acid metabolite (M1; inactive metabolite) and N-desmethyl enzalutamide (M2; active metabolite), on day 1 up to 1176 hours (49 days). Safety data were collected from screening until the end of study visit. Results: 14 healthy Chinese male volunteers were enrolled and received a single ENZ dose (mean age, 29.0 years; mean BMI, 21.7 kg/m2). All volunteers receiving study drug were included in the PK and safety analyses; two subjects withdrew from the study during the study period. ENZ plasma concentration rapidly increased (median tmax of 1.5 hours) followed by a slow decrease (mean t1/2 of 90.7 hours). Plasma concentrations of M1 and M2 increased gradually with a median tmax of 72.0 and 121 hours, respectively. M1 and M2 mean metabolite to parent ratio was 0.206 and 1.32, respectively. Mean AUC0-inf of the sum of ENZ and M2 was 828 μg·h/mL compared to 368 μg·h/mL for ENZ. Cmax and tmax of the sum of ENZ and M2 were comparable to ENZ. Mean t1/2 of the sum of ENZ and M2 was 155 hours, which was similar to that of M2 (162 hours). Treatment-emergent adverse events (TEAEs) were reported in seven out of 14 males (50.0%). Possible/probable drug-related TEAEs were reported in four males (28.6%); one each of upper respiratory tract infection, chest discomfort, increased bilirubin, and decreased white blood cell count. No deaths, serious TEAEs, or TEAEs of grade ≥3 were observed. Conclusions: The PK profiles of ENZ, M1, M2, and the sum of ENZ and M2 in healthy Chinese males were generally consistent with Caucasian males. No clinically relevant safety concerns were reported. Safety and PK profiles indicate that ENZ 160 mg/day is appropriate in a Chinese population.

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