A Phase I, Open-Label, Parallel-Group Study to Evaluate the Pharmacokinetics and Safety of GSK1265744 in Subjects With Severe Renal Impairment and Healthy Matched Control Subjects

GSK1265744 (744) is an integrase strand transfer inhibitor (INSTI) currently in development
for both the treatment and prevention of human immunodeficiency virus (HIV) infection. Renal
elimination of unchanged 744 is extremely low, with no parent 744 detected in the urine after
a single 30 mg radiolabeled dose. Despite the minimal contribution of renal clearance on
overall 744 elimination, renal impairment may potentially inhibit some pathways of hepatic
and gut drug metabolism and transport, and as a result may impact 744 pharmacokinetics. The
current Food and Drug Administration (FDA) draft guidance for renal impairment studies
suggests that a pharmacokinetic (PK) study in patients with renal impairment be conducted
even for those drugs primarily metabolized or secreted in bile.

The study will be comprised of two cohorts (severe renal impairment and normal renal
function) of 8 subjects each. Upon enrolment, each subject will be admitted to the study
center and undergo serial PK sampling following a single dose of oral 744 30 milligrams (mg).
Subjects will return to the clinic for follow-up evaluations 10-14 days after the 744 30 mg
dose.