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Randomized, placebo‐controlled single‐ascending‐dose study to evaluate the safety, tolerability and pharmacokinetics of the HIV nucleoside reverse transcriptase inhibitor, BMS‐986001, in healthy subjects
Author(s) -
Urata Y.,
Paintsil E.,
Cheng Y.C.,
Matsuda T.,
Sevinsky H.,
Hawthorne D.,
Bertz R.,
Hanna G.J.,
Grasela D.,
Hwang C.
Publication year - 2014
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/jcph.252
Subject(s) - pharmacokinetics , tolerability , reverse transcriptase inhibitor , nucleoside reverse transcriptase inhibitor , pharmacology , placebo , medicine , reverse transcriptase , human immunodeficiency virus (hiv) , adverse effect , anesthesia , virology , chemistry , antiretroviral therapy , viral load , rna , alternative medicine , pathology , biochemistry , gene
The objectives of this study were to evaluate the safety, tolerability and pharmacokinetics (PK) of BMS‐986001 as a single oral dose in healthy male subjects. Sixty‐four healthy male subjects were randomized to receive a single dose of BMS‐986001 or placebo in this single‐blind, placebo‐controlled, sequential ascending‐dose study. There were eight treatment groups (10, 30, 100, 300, 600, and 900 mg fed; and 100 and 300 mg fasted) of eight subjects each (BMS‐986001 n = 6/placebo n = 2). BMS‐986001 was well tolerated, with no serious adverse events (AEs), deaths, or discontinuations due to AEs reported. AEs were experienced by 14.6% of subjects receiving BMS‐986001; however, these did not appear to be dose related and were not considered to be related to study drug. BMS‐986001 was rapidly absorbed and exhibited a linear dose–exposure relationship across the dose range studied. PK appeared similar whether administered with or without food. Administration of BMS‐986001 as a single dose was generally safe and well tolerated. A linear dose–exposure relationship was seen across all doses studied, with no apparent food effect. Further clinical development is warranted.

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