QTERN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for QTERN (QTERN).
QTERN is a fixed-dose combination of dapagliflozin, a sodium-glucose cotransporter 2 (SGLT2) inhibitor, and saxagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor. Dapagliflozin reduces renal glucose reabsorption, increasing urinary glucose excretion. Saxagliptin increases incretin hormones, enhancing insulin secretion and decreasing glucagon levels.
| Metabolism | Dapagliflozin is primarily metabolized via UGT1A9; saxagliptin is metabolized via CYP3A4/5. |
| Excretion | Fecal (59% unchanged) and renal (42% unchanged, primarily via tubular secretion). |
| Half-life | Terminal half-life approximately 5 hours; supports twice-daily dosing. |
| Protein binding | 93% bound to serum albumin. |
| Volume of Distribution | 55 L (approximately 0.79 L/kg for a 70 kg adult), indicating extensive tissue distribution. |
| Bioavailability | Oral: 75% on empty stomach; food reduces AUC by 30%. |
| Onset of Action | Oral: Onset within 1 hour; peak effect at 2-4 hours. |
| Duration of Action | Duration up to 12 hours; clinical effect lasts over the dosing interval. |
One tablet orally twice daily; each tablet contains dapagliflozin 10 mg and saxagliptin 5 mg.
| Dosage form | TABLET |
| Renal impairment | eGFR >=45 mL/min/1.73 m2: no dose adjustment. eGFR 30-44: not recommended. eGFR <30 or ESRD: contraindicated. |
| Liver impairment | Child-Pugh Class A (mild): no adjustment. Child-Pugh Class B (moderate): not recommended. Child-Pugh Class C (severe): contraindicated. |
| Pediatric use | Safety and efficacy not established; use not recommended in pediatric patients. |
| Geriatric use | No dose adjustment based on age alone; assess renal function (eGFR) prior to initiation and monitor regularly. Elderly patients may have higher risk of volume depletion and renal impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for QTERN (QTERN).
| Breastfeeding | Unknown if excreted in human milk. Dapagliflozin: present in rat milk. Saxagliptin: present in rat milk. M/P ratio not available. Avoid breastfeeding during therapy. |
| Teratogenic Risk | QTERN (dapagliflozin/saxagliptin) is contraindicated in the second and third trimesters due to risk of fetal renal toxicity from SGLT2 inhibitor. First trimester risk cannot be excluded; animal studies show renal effects. No human data. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
["History of serious hypersensitivity reaction to dapagliflozin or saxagliptin","History of angioedema","Type 1 diabetes mellitus","Diabetic ketoacidosis","Severe renal impairment (eGFR <30 mL/min/1.73 m²), end-stage renal disease, or dialysis"]
| Precautions | ["Pancreatitis","Heart failure","Hypoglycemia with concomitant sulfonylurea or insulin","Genitourinary infections","Volume depletion/hypotension","Acute kidney injury","Diabetic ketoacidosis","Lower limb amputation","Hypersensitivity reactions","Severe and disabling arthralgia"] |
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| Monitor renal function (serum creatinine, eGFR) and blood glucose. In pregnancy, monitor fetal growth via ultrasound. Assess for volume depletion. |
| Fertility Effects | No human data on fertility. Animal studies show no impairment with dapagliflozin or saxagliptin at clinically relevant doses. |