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Table 4 Small molecule inhibitors

From: Novel and emerging therapies for B cell lymphoma

Drug

Class

Patient population

N

ORR

CR

Grade 3 AE

Reference

M7583

BTK inhibitor

R/R DLBCL, WM, MCL, MZL, SLL

18

50%

11%

Diarrhea

[80]

ME-401

PI3Kδ

R/R FL, CLL

31

83%

NA

Diarrhea, rash

[81]

LAM-002A

Endosomal protein inhibitor

R/R DLBCL, MCL, FL, MZL, CLL

24

NA

NA

Tumor lysis syndrome

[82]

INCB057643

BET protein inhibitor

R/R FL, DLBCL

5

33% (DE)

None

Hyperglycemia, thrombocytopenia, anemia, hyperbilirubinemia, Increased INR

[83]

MRG-106

miR-155 inhibitor

Mycosis fungoides

38

NA

NA

Pruritus, tumor flare

[84]

DS-3201b

EZH1/2 dual inhibitor

PTL, AITL, DLBCL, FL, MZL

15

53%

6.6%

Pneumonia

[85]

Apatinib

VEGFR-2 tyrosine kinase inhibitor

R/R NHL

21

47.6%

9.5%

None

[86]

  1. Abbreviations: N number of patients, ORR overall response rate, CR complete response rate, AE adverse events, R/R relapsed and refractory, DLBCL diffuse large B cell lymphoma, CLL chronic leukemic leukemia, tFL transformed follicular lymphoma, FL follicular lymphoma, WM Waldenström’s macroglobulinemia, MZL marginal zone lymphoma, MCL mantle cell lymphoma, PTL peripheral T cell lymphoma, AITL angio-immunoblastic T cell lymphoma, NHL non-Hodgkin lymphoma, VEGFR-2 vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor, PI3Kδ phosphatidylinositol 3 kinase delta, BET bromodomain and extraterminal protein inhibitor, EZH enhancer of zeste homolog, miR micro RN, DE dose escalation phase, NA data unavailable