Saxagliptin

Detailed information

General information about assessment reports

Since 2006, an Environmental Risk Assessment (ERA) for the active pharmaceutical substance shall accompany an application for a marketing authorisation in EU for a medicinal product for human use. Parts of environmental data are available in the public assessment report (PAR/EPAR for centrally approved medicines). Environmental considerations are not included in the benefit-risk assessment for human medicines. If new data emerge after approval that necessitate an update of the environmental risk assessment, a variation application (“type IB C.I.z variation”) must be submitted to the regulatory authority.

All approved medicinal products, i.e. Qtern (dapagliflozin, saxagliptin), Komboglyze (metformin, saxagliptin) and Onglyza (saxagliptin), originate from AstraZeneca. The most recent assessment report containing environmental information for Qtern is presented below.

Assessment report Qtern

Assessment report for saxagliptin from Qtern, AstraZeneca, 26 May 2016, EMA/428168/2016.

Hazard

Persistence: In aerobic OECD 308 studies, DT₅₀ values of 20–23 days in water and 20–30 days in the whole system were measured. Under anaerobic conditions, DT₅₀ values were 18–23 days in water and 22–32 days in the whole system. A significant shift of the substance to sediment was observed from day 14 onwards. All values were determined at 20°C.

Bioaccumulation: OECD 107.
log D_ow = -1.74 at pH 4
log D_ow = 0.114 at pH 8.2
log D_ow = 0.169 at pH 9

Toxicity: There are data for 3 trophic levels, most sensitive fish (Pimephales promelas) NOEC ≥ 9500 microg/L. Comment: Values reported as greater than are not according to the guidelines. The actual value may be lower.

Risk

The risk, PEC/PNEC, calculated from data in the assessment report from a European perspective:

PEC refined = 0.07 microg/L.

PNEC = Lowest NOEC, 9500 microg/L/10 (Assessment Factor (AF) for 3 chronic studies) = 950 microg/L.

PEC/PNEC = 0.000074 which gives the risk insignificant.

Fass environmental information

Fass environmental information for Onglyza (saxagliptin) from AstraZeneca (retrieved on 2026-06-25).

Metabolism and excretion

"Following a single 50 mg dose of ¹⁴C‑saxagliptin, 24%, 36%, and 75% of the dose was excreted in the urine as saxagliptin, its major metabolite, and total radioactivity respectively. A total of 22% of the administered radioactivity was recovered in faeces representing the fraction of the saxagliptin dose excreted in bile and/or unabsorbed medicinal product from the gastrointestinal tract."

Hazard

Persistence: Saxagliptin is not considered readily biodegradable and is not expected to partition to any significant extent into sludge during wastewater treatment. In water–sediment systems, the substance was shown to degrade under aerobic conditions, with half-lives in the water phase of 20–23 days and in the total system of 20 days (low organic carbon content, LOC) and 30 days (high organic carbon content, HOC). A substantial fraction of the applied radioactivity was recovered in the sediment, part of which was extractable. Two main degradation products were identified, while mineralization was limited (< 2% as ¹⁴CO₂). At the end of the study, 3% and 7.3% of the parent compound remained in the LOC and HOC systems, respectively. As the half-life in the total system was ≤ 32 days and less than 15% of the parent compound remained at the end of the study, it is concluded that saxagliptin degrades in the environment.

Bioaccumulation: OECD 107.
log D_ow = -1.74 at pH 4
log D_ow = 0.114 at pH 8.2
log D_ow = 0.169 at pH 9

Toxicity: There are data for 3 trophic levels, most sensitive fish (Pimephales promelas) NOEC 9500 microg/L.

Risk

PEC/PNEC is based on total sold amount API (active pharmaceutical ingredient) in Sweden year 2024.

PEC = 0.00017429 microg/L.

PNEC = Lowest NOEC, 9500 microg/L/10 (Assessment Factor (AF) for 3 chronic studies) = 950 microg/L.

PEC/PNEC = 0.00000018 which gives the risk insignificant.