Vadadustat
Vadadustat is an oral inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase. In phase 3 trials of patients with chronic kidney disease (CKD) (not undergoing dialysis and undergoing dialysis) and anaemia, vadadustat was non-inferior to darbepoetin alfa for change in the haemoglobin level from baseline and haemoglobin maintenance, and major cardiovascular adverse events.[174]Eckardt KU, Agarwal R, Aswad A, et al. Safety and efficacy of vadadustat for anemia in patients undergoing dialysis. N Engl J Med. 2021 Apr 29;384(17):1601-12.
https://www.nejm.org/doi/10.1056/NEJMoa2025956
http://www.ncbi.nlm.nih.gov/pubmed/33913638?tool=bestpractice.com
The most common adverse reactions were hypertension and diarrhoea. Pooled results from two phase 3 trials in patients with non-dialysis-dependent CKD showed that vadadustat was non-inferior to darbepoetin alfa for haematological efficacy, but did not meet non-inferiority criterion for cardiovascular safety (a composite of death from any cause, non-fatal myocardial infarction, or non-fatal stroke).[175]Chertow GM, Pergola PE, Farag YMK, et al; PRO2TECT Study Group. Vadadustat in patients with anemia and non-dialysis-dependent CKD. N Engl J Med. 2021 Apr 29;384(17):1589-600.
https://www.nejm.org/doi/10.1056/NEJMoa2035938
http://www.ncbi.nlm.nih.gov/pubmed/33913637?tool=bestpractice.com
Increased risk of thrombotic vascular events, including major adverse cardiovascular events, has been reported. Vadadustat is approved by the US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) for the treatment of anaemia caused by CKD in adults who have been receiving dialysis for at least 3 months. It is only approved for patients who are on dialysis. UK guidelines recommend vadadustat as an alternative option to erythropoiesis-stimulating agents for symptomatic anaemia in CKD in patients who are on dialysis.[150]UK Kidney Association. Clinical practice guideline: anaemia of chronic kidney disease. Sep 2024 [internet publication].
https://www.ukkidney.org/sites/default/files/documents/FINAL%20VERSION%20-%20%20UKKA%20ANAEMIA%20OF%20CKD%20GUIDELINE%20-%20Feb2025_1.pdf
[176]National Institute for Health and Care Excellence. Vadadustat for treating symptomatic anaemia in adults having dialysis for chronic kidney disease. Jan 2025 [internet publication].
https://www.nice.org.uk/guidance/ta1035
[177]Ha JT, Hiremath S, Jun M, et al. Hypoxia-inducible factor prolyl hydroxylase inhibitors in kidney disease. NEJM Evid. 2024 Sep;3(9):EVIDoa2300189.
http://www.ncbi.nlm.nih.gov/pubmed/39186635?tool=bestpractice.com
Roxadustat
Roxadustat is an oral inhibitor of HIF prolyl hydroxylase that stimulates erythropoiesis and regulates iron metabolism. Roxadustat may potentially serve as an alternative to erythropoiesis-stimulating agents for the management of anaemia in patients with CKD.[178]Chen N, Hao C, Peng X, et al. Roxadustat for anemia in patients with kidney disease not receiving dialysis. N Engl J Med. 2019 Sep 12;381(11):1001-10.
https://www.nejm.org/doi/full/10.1056/NEJMoa1813599
http://www.ncbi.nlm.nih.gov/pubmed/31340089?tool=bestpractice.com
[179]Chen N, Hao C, Liu BC, et al. Roxadustat treatment for anemia in patients undergoing long-term dialysis. N Engl J Med. 2019 Sep 12;381(11):1011-22.
https://www.nejm.org/doi/full/10.1056/NEJMoa1901713
http://www.ncbi.nlm.nih.gov/pubmed/31340116?tool=bestpractice.com
[180]Akizawa T, Iwasaki M, Otsuka T, et al. Phase 3 study of roxadustat to treat anemia in non-dialysis-dependent CKD. Kidney Int Rep. 2021 Jul;6(7):1810-28.
https://www.kireports.org/article/S2468-0249(21)01085-8/fulltext
http://www.ncbi.nlm.nih.gov/pubmed/34307976?tool=bestpractice.com
[181]Barratt J, Andric B, Tataradze A, et al. Roxadustat for the treatment of anaemia in chronic kidney disease patients not on dialysis: a Phase 3, randomized, open-label, active-controlled study (DOLOMITES). Nephrol Dial Transplant. 2021 Aug 27;36(9):1616-28.
https://academic.oup.com/ndt/article/36/9/1616/6291250
http://www.ncbi.nlm.nih.gov/pubmed/34077510?tool=bestpractice.com
[182]Zheng Q, Yang H, Fu X, et al. The efficacy and safety of roxadustat for anemia in patients with chronic kidney disease: a meta-analysis. Nephrol Dial Transplant. 2021 Aug 27;36(9):1603-15.
http://www.ncbi.nlm.nih.gov/pubmed/33051677?tool=bestpractice.com
[183]Zhou Q, Mao M, Li J, et al. The efficacy and safety of roxadustat for anemia in patients with dialysis-dependent chronic kidney disease: a systematic review and meta-analysis. Ren Fail. 2023 Dec;45(1):2195011.
https://www.tandfonline.com/doi/full/10.1080/0886022X.2023.2195011
http://www.ncbi.nlm.nih.gov/pubmed/37489561?tool=bestpractice.com
The EMA has approved the use of roxadustat for the treatment of adults with symptomatic anaemia associated with CKD. The FDA has requested further trials on the safety of roxadustat in both non-dialysis-dependent and dialysis-dependent patient populations. UK guidelines recommend roxadustat as an alternative option to erythropoiesis-stimulating agents for symptomatic anaemia in CKD in patients who are not on dialysis at the start of treatment.[150]UK Kidney Association. Clinical practice guideline: anaemia of chronic kidney disease. Sep 2024 [internet publication].
https://www.ukkidney.org/sites/default/files/documents/FINAL%20VERSION%20-%20%20UKKA%20ANAEMIA%20OF%20CKD%20GUIDELINE%20-%20Feb2025_1.pdf
[184]National Institute for Health and Care Excellence. Roxadustat for treating symptomatic anaemia in chronic kidney disease. Jul 2022 [internet publication].
https://www.nice.org.uk/guidance/ta807
Tenapanor
Tenapanor is a first-in-class sodium/hydrogen exchanger-3 (NHE3) inhibitor that acts locally in the gut to block the NHE3 transporter protein, which is crucial to the paracellular phosphate absorption pathway. Tenapanor has been shown to significantly reduce serum phosphate concentrations compared with placebo, with minimal adverse effects.[185]Block GA, Bleyer AJ, Silva AL, et al. Safety and efficacy of tenapanor for long-term serum phosphate control in maintenance dialysis: a 52-week randomized phase 3 Trial (PHREEDOM). Kidney360. 2021 Oct 28;2(10):1600-10.
https://journals.lww.com/kidney360/fulltext/2021/10000/safety_and_efficacy_of_tenapanor_for_long_term.9.aspx
http://www.ncbi.nlm.nih.gov/pubmed/35372979?tool=bestpractice.com
[186]Pergola PE, Rosenbaum DP, Yang Y, et al. A randomized trial of tenapanor and phosphate binders as a dual-mechanism treatment for hyperphosphatemia in patients on maintenance dialysis (AMPLIFY). J Am Soc Nephrol. 2021 Jun 1;32(6):1465-73.
https://journals.lww.com/jasn/fulltext/2021/06000/a_randomized_trial_of_tenapanor_and_phosphate.20.aspx
http://www.ncbi.nlm.nih.gov/pubmed/33766811?tool=bestpractice.com
[187]Block GA, Rosenbaum DP, Yan A, et al. Efficacy and safety of tenapanor in patients with hyperphosphatemia receiving maintenance hemodialysis: a randomized phase 3 trial. J Am Soc Nephrol. 2019 Apr;30(4):641-52.
https://journals.lww.com/jasn/fulltext/2019/04000/efficacy_and_safety_of_tenapanor_in_patients_with.14.aspx
http://www.ncbi.nlm.nih.gov/pubmed/30846557?tool=bestpractice.com
Diarrhoea was the most common adverse effect, occurring in 43% to 53% of patients, with approximately 5% of patients developing severe diarrhoea. Most patients had mild or moderate episodes that resolved spontaneously or with a dose reduction.[185]Block GA, Bleyer AJ, Silva AL, et al. Safety and efficacy of tenapanor for long-term serum phosphate control in maintenance dialysis: a 52-week randomized phase 3 Trial (PHREEDOM). Kidney360. 2021 Oct 28;2(10):1600-10.
https://journals.lww.com/kidney360/fulltext/2021/10000/safety_and_efficacy_of_tenapanor_for_long_term.9.aspx
http://www.ncbi.nlm.nih.gov/pubmed/35372979?tool=bestpractice.com
[186]Pergola PE, Rosenbaum DP, Yang Y, et al. A randomized trial of tenapanor and phosphate binders as a dual-mechanism treatment for hyperphosphatemia in patients on maintenance dialysis (AMPLIFY). J Am Soc Nephrol. 2021 Jun 1;32(6):1465-73.
https://journals.lww.com/jasn/fulltext/2021/06000/a_randomized_trial_of_tenapanor_and_phosphate.20.aspx
http://www.ncbi.nlm.nih.gov/pubmed/33766811?tool=bestpractice.com
[187]Block GA, Rosenbaum DP, Yan A, et al. Efficacy and safety of tenapanor in patients with hyperphosphatemia receiving maintenance hemodialysis: a randomized phase 3 trial. J Am Soc Nephrol. 2019 Apr;30(4):641-52.
https://journals.lww.com/jasn/fulltext/2019/04000/efficacy_and_safety_of_tenapanor_in_patients_with.14.aspx
http://www.ncbi.nlm.nih.gov/pubmed/30846557?tool=bestpractice.com
Tenapanor is approved by the FDA as add-on therapy to reduce serum phosphorus levels in CKD patients on dialysis who have had an inadequate response or are intolerant to previously tried phosphate binders. Tenapanor is not approved by the EMA.
Veverimer
Veverimer, a non-absorbed polymer that selectively binds and removes hydrochloric acid from the gastrointestinal lumen, is being investigated for the treatment of metabolic acidosis in patients with CKD. It has been shown to significantly increase serum bicarbonate concentration, with minimal adverse effects. The FDA is currently reviewing an application for approval.[188]Wesson DE, Mathur V, Tangri N, et al. Veverimer versus placebo in patients with metabolic acidosis associated with chronic kidney disease: a multicentre, randomised, double-blind, controlled, phase 3 trial. Lancet. 2019 Apr 6;393(10179):1417-27.
http://www.ncbi.nlm.nih.gov/pubmed/30857647?tool=bestpractice.com
[189]Wesson DE, Mathur V, Tangri N, et al. Long-term safety and efficacy of veverimer in patients with metabolic acidosis in chronic kidney disease: a multicentre, randomised, blinded, placebo-controlled, 40-week extension. Lancet. 2019 Aug 3;394(10196):396-406.
http://www.ncbi.nlm.nih.gov/pubmed/31248662?tool=bestpractice.com