Saxagliptin is a DPP-4 inhibitor with shorter half-life than sitagliptin. Possible increased risk of heart failure.
Also known as: Onglyza
DPP-4 + azole antifungal: increased saxagliptin levels.
Saxagliptin is metabolised by CYP3A4 to the active metabolite 5-hydroxy saxagliptin (~50% of activity). Ketoconazole potently inhibits CYP3A4, increasing saxagliptin levels ~2.5-fold and reducing active metabolite formation. Total activity AUC increases moderately. The FDA recommends reducing dose to 2.5 mg/day when coadministered with strong CYP3A4 inhibitors (ketoconazole, itraconazole, clarithromycin).
DPP-4 + azole antifungal: CYP3A4 inhibited, saxagliptin levels increased ~2.5-fold. Reduce dose to 2.5 mg/day.
Ketoconazole inhibits CYP3A4, increasing saxagliptin levels ~2.5-fold. Reduce dose to 2.5 mg/day.
Blood glucose
Hypoglycaemia
Reduce saxagliptin dose to 2.5 mg/day when coadministered with strong CYP3A4 inhibitors.
DailyMed/FDA (NIH/NLM) — approved Saxagliptin (Onglyza) label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c5116390-e0fe-4969-94cb-e9de5165fbab
No documented food or drink interactions.
No documented disease interactions.
No documented pregnancy or breastfeeding information.
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
Inhibits DPP-4, increasing incretins. Active metabolite (5-hydroxy saxagliptin) has longer half-life.
Blocks DPP-4, increasing GLP-1 and GIP. Active metabolite 5-hydroxy saxagliptin contributes ~50% of activity.
Oral bioavailability: 75%. Food does not significantly affect absorption. Tmax: 2 hours.
Metabolised by CYP3A4 (and to a lesser extent CYP2D6) to active metabolite 5-hydroxy saxagliptin. Inhibited by ketoconazole (max dose 2.5 mg).
2.5 hours (saxagliptin); 3.1 hours (5-hydroxy). Elimination: ~60% urine, ~28% faeces.
Medicines from the same therapeutic group (ATC classification) or the same pharmacological class.
