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What do these attributes mean for patients with T2DM?
It is anticipated that the primarily non-renal route of elimination of lina-
gliptin will allow this compound to be used in people with renal insuf-
ficiency without dose adjustments. This has potentially important impli-
cations for T2DM management in light of the fact that at least a third of
people with diabetes have some degree of renal impairment and that
many current T2DM treatments are contraindicated in patients with
renal impairment. 84 122
The high potency of linagliptin means that a low dose of linagliptin can
be administered to T2DM patients in small tablets; features that are cru-
cial to the good tolerability of a drug and the willingness of people with
T2DM to take their medication as prescribed. Additionally, these attri-
butes lend linagliptin to inclusion in fixed-dose combinations. The high
selectivity of linagliptin for the DPP-4 enzyme rather than DPP-8 or DPP-9
is reassuring, in that no untoward off-target interactions are expected,
helping to confer a placebo-like tolerability profile. As linagliptin binds
tightly to the DPP-4 enzyme, a single dose taken at any time of the day
is sufficient to provide a full 24 hours of glycaemic control.
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