NMEs with RI-related labeling impact
| Compound Name | Max AUC Ratio | Cmax Ratiob | Labeling Impact | Reference |
|---|---|---|---|---|
| AUC ≥2 | ||||
| Albiglutidea | 2.82 (severe) | 2.61 (severe) | Monitor renal function | FDA, 2014ag |
| Ceftolozane | 2.55 (moderate) | 1.04 (moderate) | Monitor CrCL and adjust dose if necessary | FDA, 2014al |
| Dapagliflozin | 2.31 (severe); dapagliflozin-3-O-glucorunide: 3.22 (severe) | 1.34 (severe); dapagliflozin-3-O-glucorunide: 1.38 (severe) | Contraindicated (severe, ESRD, dialysis) | FDA, 2014j |
| Naloxegol | 3.19 (severe) | 2.24 (severe) | Reduce dose (CrCL <60 ml/min) | FDA, 2014t |
| Peramivir | 18.08 (ESRD) | 1.21 (ESRD) | Reduce dose (CrCL <50 ml/min), administer after dialysis | FDA, 2014ac |
| Tazobactam | 2.00 (moderate) | 1.28 (moderate) | Monitor CrCL and adjust dose if necessary | FDA, 2014al |
| AUC ratio <2, with dosing information | ||||
| Apremilast | 1.89 (severe); M12: 2.92 (severe) | 1.43 (severe); M12: 1.43 (severe) | Reduce dose (severe) | FDA, 2014aa |
| Dalbavancin | 1.97 (severe) | 0.99 (severe) | Adjust dose (CrCL <30 ml/min, without dialysis) | FDA, 2014g |
| Empagliflozin | 1.67 (severe) | 1.23 (severe) | Contraindicated (severe, ESRD, dialysis) | FDA, 2014n |
| Olaparib | 1.66 (mild) | 1.27 (mild) | Monitor for toxicity | FDA, 2014s |
| Pirfenidone | 1.09 (severe); 5-carboxy: 5.88 (severe) | 1.13 (severe); 5-carboxy: 2.97 (severe) | Not recommended (ESRD on dialysis), monitor for adverse reactions | FDA, 2014i |
| No dedicated RI study, with dosing information | ||||
| Eliglustat | Not evaluated | Not evaluated | Not recommended (moderate, severe) | FDA, 2014e |
| Netupitant | Not evaluated | Not evaluated | Avoid use (severe, ESRD) | FDA, 2014a |
AUC and Cmax values presented have been calculated by the DIDB Editorial Team using mean values available from the NDA review documents and may differ from those presented in the product label. CrCL, creatinine clearance; ESRD, end-stage renal disease.
↵a No exact AUC ratio for severe RI is provided in the product label; however, according to the sponsor, albiglutide exposure was increased by approximately 30%–40% in patients with RI (all stages).
↵b The Cmax ratios presented are for the same impairment state as the maximal AUC ratio; however, they may not be the Cmax ratio observed when considering other impairment states.