Venetoclax
Venetoclax is an oral B-cell lymphoma-2 (BCL-2) inhibitor. In a phase 2 trial of 30 patients with previously treated WM, venetoclax had an overall response rate of 87%.[108]Castillo JJ, Gustine J, Meid K, et al. Multicenter prospective phase II study of venetoclax in patients with previously treated Waldenstrom macroglobulinemia. Blood. 2018 Nov 29;132(suppl 1):2888.
https://ashpublications.org/blood/article/132/Supplement%201/2888/263549/Multicenter-Prospective-Phase-II-Study-of
Severe neutropenia occurred in 13.3% of patients.[108]Castillo JJ, Gustine J, Meid K, et al. Multicenter prospective phase II study of venetoclax in patients with previously treated Waldenstrom macroglobulinemia. Blood. 2018 Nov 29;132(suppl 1):2888.
https://ashpublications.org/blood/article/132/Supplement%201/2888/263549/Multicenter-Prospective-Phase-II-Study-of
Daratumumab
Daratumumab is an anti-CD38 monoclonal antibody. It has been used extensively in multiple myeloma, and is undergoing clinical trials in WM given its likely efficacy and tolerability.[109]Paulus A, Manna A, Akhtar S, et al. Targeting CD38 with daratumumab is lethal to Waldenström macroglobulinaemia cells. Br J Haematol. 2018 Oct;183(2):196-211.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7294509
http://www.ncbi.nlm.nih.gov/pubmed/30080238?tool=bestpractice.com
[110]Vidal-Crespo A, Matas-Céspedes A, Rodriguez V, et al. Daratumumab displays in vitro and in vivo anti-tumor activity in models of B-cell non-Hodgkin lymphoma and improves responses to standard chemo-immunotherapy regimens. Haematologica. 2020 Apr;105(4):1032-41.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7109732
http://www.ncbi.nlm.nih.gov/pubmed/31296574?tool=bestpractice.com
Everolimus
Everolimus is a mammalian target of rapamycin (mTOR) inhibitor. In a phase 2 trial of 60 patients with relapsed/refractory WM, everolimus had an overall response rate of 50% (all were partial response), and median progression-free survival was 21 months.[111]Ghobrial IM, Witzig TE, Gertz M, et al. Long-term results of the phase II trial of the oral mTOR inhibitor everolimus (RAD001) in relapsed or refractory Waldenstrom macroglobulinemia. Am J Hematol. 2014;89:237-242.
http://www.ncbi.nlm.nih.gov/pubmed/24716234?tool=bestpractice.com
In a phase 2 trial of 33 patients with symptomatic untreated WM, everolimus had an overall response rate of 72.7%.[112]Treon SP, Meid K, Tripsas C, et al. Prospective, multicenter clinical trial of everolimus as primary therapy in Waldenstrom macroglobulinemia (WMCTG 09-214). Clin Cancer Res. 2017 May 15;23(10):2400-4.
https://clincancerres.aacrjournals.org/content/23/10/2400.long
http://www.ncbi.nlm.nih.gov/pubmed/27836860?tool=bestpractice.com
Pneumonitis occurred in 6 patients, with 3 patients requiring hospitalisation.[112]Treon SP, Meid K, Tripsas C, et al. Prospective, multicenter clinical trial of everolimus as primary therapy in Waldenstrom macroglobulinemia (WMCTG 09-214). Clin Cancer Res. 2017 May 15;23(10):2400-4.
https://clincancerres.aacrjournals.org/content/23/10/2400.long
http://www.ncbi.nlm.nih.gov/pubmed/27836860?tool=bestpractice.com
Perifosine
Perifosine is a novel alkylphospholipid Akt inhibitor. In a phase 2 trial of 37 patients with relapsed/refractory WM, perifosine had a partial response rate of 11%.[113]Ghobrial IM, Roccaro A, Hong F, et al. Clinical and translational studies of a phase II trial of the novel oral Akt inhibitor perifosine in relapsed or relapsed/refractory Waldenström's macroglobulinemia. Clin Cancer Res. 2010;16:1033-1041.
http://clincancerres.aacrjournals.org/content/16/3/1033.long
http://www.ncbi.nlm.nih.gov/pubmed/20103671?tool=bestpractice.com
Other studies have reported an overall response rate of 36%.[114]Ghobrial IM, Leleu X, Azab AK, et al. Novel therapeutic agents in Waldenstrom's macroglobulinaemia. Clin Lymphoma Myeloma. 2009;9:84-86.
http://www.ncbi.nlm.nih.gov/pubmed/19362982?tool=bestpractice.com
Panobinostat
Panobinostat is a histone deacetylase (HDAC) inhibitor. In a phase 2 trial of 39 patients with relapsed/refractory WM, panobinostat had an overall response rate of 47%.[115]Ghobrial IM, Campigotto F, Murphy TJ, et al. Results of a phase 2 trial of the single-agent histone deacetylase inhibitor panobinostat in patients with relapsed/refractory Waldenström macroglobulinemia. Blood. 2013 Feb 21;121(8):1296-303.
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3578951
http://www.ncbi.nlm.nih.gov/pubmed/23287861?tool=bestpractice.com
Ofatumumab
Ofatumumab is a fully human anti-CD20 monoclonal antibody. In a phase 2 trial of 37 patients with WM (28 patients with relapsed/refractory WM), ofatumumab had an overall response rate of 32%.[116]Furman RR, Eradat H, DiRienzo CG, et al. A phase II trial of ofatumumab in subjects with Waldenstrom's macroglobulinemia. Blood. 2011;118:3701.
https://ashpublications.org/blood/article/118/21/3701/68991/A-Phase-II-Trial-of-Ofatumumab-in-Subjects-with
Pentostatin plus cyclophosphamide and rituximab
Pentostatin is an antimetabolite chemotherapy agent. In a phase 2 trial of 25 patients with WM, pentostatin plus cyclophosphamide and rituximab had a 2-year progression-free survival rate of 83.6% and a 2-year overall survival rate of 100% in those with untreated WM (n=21).[117]Herth I, Hensel M, Rieger M, et al. Pentostatin, cyclophosphamide and rituximab is a safe and effective treatment in patients with Waldenström's macroglobulinemia. Leuk Lymphoma. Leuk Lymphoma. 2015;56:97-102.
http://www.ncbi.nlm.nih.gov/pubmed/24724778?tool=bestpractice.com
Pirtobrutinib
Pirtoburinib, a non-covalent third-generation Bruton’s tyrosine kinase (BTK) inhibitor, has demonstrated promising activity and good tolerability in the phase 1/2 BRUIN trial of patients with relapsed low-grade B-cell non-Hodgkin’s lymphoma, that also included patients with relapsed WM previously treated with BTK inhibitors.[118]Mato AR, Shah NN, Jurczak W, et al. Pirtobrutinib in relapsed or refractory B-cell malignancies (BRUIN): a phase 1/2 study. Lancet. 2021 Mar 6;397(10277):892-901.
http://www.ncbi.nlm.nih.gov/pubmed/33676628?tool=bestpractice.com