A review of sitagliptin with special emphasis on its use in moderate to severe renal impairment

Figures & data

Table 1 Risk categories for kidney and mortality outcomes, by estimated glomerular filtration rate (eGFR) and albuminuria or proteinuria stage

Notes: Green indicates low risk (if no other markers of kidney disease, no CKD); yellow indicates moderately increased risk; orange indicates high risk; red indicates very high risk. Reprinted with permission from Macmillan Publishers Ltd: Kidney Int Suppl. 2013;3:1–150. Kidney Disease Improving Global Outcomes (KDIGO). 2012 clinical practice guidelines for the evaluation and management of chronic kidney disease. Copyright © 2013.¹⁵

Abbreviation: CKD, chronic kidney disease.

Table 2 Summary of sitagliptin trials (all doses are in milligrams [mg])

Trial	Number	Duration in weeks	Intervention	Reduction glycated hemoglobin (%)	Comments
Aschner et al^Citation38	741	24	S100 S200	−0.79 −0.94	β-cell function improved
Raz et al^Citation39	521	18	S100 S200	−0.60 −0.48	β-cell function improved
Scott et al^Citation40	743	12	S2.5 od S12.5 od S25 od S50 bid	Reductions in all groups	Maximum reduction with 50 mg bid
Goldstein et al^Citation41	1,091	24	S100 S100 + M1000 S100 + M2000 M1000	−0.83 −1.57 −2.07 −0.99	Additive hypoglycemic effect with combination therapy
Nonaka et al^Citation43	151	12	S100	−0.65	Significantly reduced 2-hour postprandial glucose
Mohan et al^Citation44	530	18	S100	−1.0	Significantly reduced 2-hour postprandial glucose
Charbonnel et al^Citation47	701	24	M ≥ 1,500 Add on S100	−0.65	β-cell function improved
Scott el al^Citation48	273	18	M ≥ 1,500 Add on S100 M ≥ 1,500 Add on R8	−0.73 −0.79	>3 kg weight gain in 21% glitazone-treated group vs 2% sitagliptin group
Nauck et al^Citation49	1,172	52	M ≥ 1500 Add on S100 M ≥ 1500 Add on GL5–20	−0.67 −0.67	Hypoglycemia rate was 5% with sitagliptin vs 32% in glipizide group
Pérez-Monteverde et al^Citation52	492	18 phase A 28 phase B	S100 P15–30 S + M (50/1000 bid) P45	−1.0 −0.9 −1.7 −1.4	Weight reduction with S + M
Hermansen et al^Citation36	441	24	Gm + M Add on S100 Gm Add on S100	−0.89 −0.57	Higher incidence of hypoglycemia when sitagliptin is added to sulfonylurea
Rosenstock et al^Citation54	175	24	P30–45 Add on S100	−0.70	Well tolerated Low risk of hypoglycemia
Fonseca et al^Citation56	313	26	M ≥ 1500 + P ≥ 30 Add on S100	0.70	Well tolerated Low risk of hypoglycemia
Sitagliptin use in chronic kidney disease
Chan et al^Citation59	91	54	S25–50	−0.70	Well tolerated in chronic renal impairment
Arjona Ferreira et al^Citation60	426	54	S25–50 GL2.5–20	Sitagliptin noninferior to glipizide	Higher hypoglycemia risk with glipizide
Arjona Ferreira et al^Citation61	129	54	S25 GL2.5–20	−0.72 −0.89	Well tolerated Low risk of hypoglycemia compared with glipizide

Abbreviations: bid, twice daily; GL, glipizide; Gm, glimepiride; M, metformin; od, once daily; P, pioglitazone; R, rosiglitazone; S, sitagliptin.

Kidney Disease Improving Global Outcomes (KDIGO) 2012 clinical practice guidelines for the evaluation and management of chronic kidney disease Kidney Int Suppl 2013 3 1 150

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