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Table 1 Pharmacokinetics of Agents Recommended by NCCN Guideline for PCNSL

From: Current and emerging therapies for primary central nervous system lymphoma

  Preferred regimens Agent a MW (Da) Route Protein binding (%) CSF (brain)/blood (%) Reference
Induction R+MTX(8)
R+MTX(8)+ TMZ
R+M(3.5)VP(+WBRT in con.)
R+MTX(3.5)+TMZ(+WBRT in con.)
MTX(M) 454 iv 46.5-54 2-20 [25, 26]
rituximab(R) 143857 iv NA 0.1 [27, 28]
temozolomide (TMZ) 194 oral 15 20-30 [29,30,31]
procarbazine(P) 221 oral NA NA [32]
vincristine(V) 824 iv 75 undetected [33]
Consolidation ASCT with condition regimen
BCNU+T
TBC
HD-AraC(±VP16)
thiotepa(T) 189 iv NA 95-100 [34]
carmustine (BCNU) 214 iv 80 20-30 [35]
Busulfan(B) 246 iv 32 95 [36]
cyclophosphamide(C) 261 iv 20 50 [37]
etoposide (VP16) 589 iv 97 0.5-5 [38]
cytarabine (AraC) 243 iv 13 6-22 [39, 40]
Refractory/Relapse Retreat with HD-MTX
±R
+R+ibrutinib
Ibrutinib
TMZ
Lenalidomide or others
ibrutinib 440 oral irreversible 1-20(28.7c) [14, 41]
lenalidomide 259 oral 30 11p-20 [42, 43]
topotecan 421 iv/oral 35 13-68 [44]
cisplatin 300 iv 90 50 [45]
pemetrexed 427 iv 81 <5 [46]
pomalidomide 273 oral 12-44 17-19 [15]
  1. Abbreviations: a associated conditions collected from the public data sources of drugbank (https://www.drugbank.ca/drugs); c corrected for protein binding; con consolidation; CSF cerebrospinal fluid; iv intravenous; MTX methotrexate (g/m2); MV molecular weight; NA not available; NCCN national comprehensive cancer network; p nonhuman primates