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Table 1. Different complement-modulating drugs listed by activity level along with references of experimental/clinical application.

From: New Insights of an Old Defense System: Structure, Function, and Clinical Relevance of the Complement System

 

Substance

Activity

Experimental

Clinical (phase I-III)

C1

C1 inhibitor

Inhibition of C1r and C1s, Kallikrein

(137139)

(140,141)

 

scFv (QuVHVL)

Antibody against glomerular heads

(175)

 
  

of C1q

  

C3

Compstatin

Peptidic C3 inhibitor

(170)

(169)

C5

Eculizumab

Humanized mAb against C5

(159)

(145,160)

 

Pexelizumab

Humanized mAb against C5

 

(112,113)

 

TNX-558

Humanized Ab against C5a

(145)

 
 

TNX-234

Humanized Ab against factor D

(145)

 
 

Anti-C5a

Ab against C5a

(55,61-63)

 
 

ARC1905

Aptamer based C5 inhibitor

 

(174)

C5aR

C5aR inhibitor

C5aR antagonist

(41,60)

 
 

Neutrazumab

Ab against C5aR

(145)

 
 

PMX-53 (C5aR inhibitor)

Peptidic C5aR antagonist

(166,167,176)

(168)

 

JPE-1375, JSM-7717

Small molecule C5aR antagonists

(145)

 

CR1

sCR1/TP10

Extracellular part of CR1

(145,147)

 
 

sCR1-sLex/TP20

Soluble CR1

(148)

 
 

Microcept/APT070

Soluble CR1

(149,150)

 

CRegs

CD55

Recombinant DAF

(152,153)

 
 

CD59 inhibitors

Peptides that modulate CD59 expression

(154)

 
 

C4BP

Complement regulator

(157,158)

 
 

CAB-2/MLN-2222

Chimera of DAF and MCP

(151)

 

Serine protease

Nafamostat (FUT-175)

Serine protease inhibitor

(177)

(143,144)

 

Factor D inhibitors

Small molecule serine protease inhibitors

(146)

 

Others

Hu-Max-CD38; Hu-Max ZP3

Humanized mAb against CD38 (triggers

(145)

 
  

complement)

  
 

rhMBL

Recombinant MBL

(171)

 
 

Anti-properdin

Ab against properdin

(163)

 
 

TA106

Ab against factor B

(162)

 
 

Ofatumumab

Humanized anti-CD20 mAb

(164)

(165)