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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