Table 1 Compounds progressed in clinical development without preclinical data in adjuvant-induced arthritis (AIA) or collagen-induced arthritis (CIA)
CompoundMode of actionClinical phaseIn vivo validationReference
RituximabAnti-CD20ApprovedB cell depletion in non-human primatesLooney10
InfliximabAnti-TNFApprovedEffects on Inflammatory processesMaini and Feldman11
Adulimimab (D2E7)Anti-TNFApprovedNone found on this particular compound
HydrochloroquineAntimalarialApprovedNone found on this particular compound
BelimumabAnti-BlysIIIB cell depletion in non-human primatesHalpern et al12
TRU-015Anti-CD20IIB cell depletion in non-human primatesTrubion Pharmaceuticals13
HuMax-CD20Anti-CD20IIB cell depletion in laboratory tests and animal studiesGenmab14
CimziaF(ab′)PEGylated anti-TNFIIINone found on this particular compound
AVE9897 (MLN 3897)CCR1 antagonistIINone found on this particular compound, however, CCR1 antagonism works therapeutically in mouse CIAAmat et al15
Rhu-DexAnti-CD80IINone found on this particular compound
CRx-102Dipyridimole and prednisoloneIINone found on this particular compound
681323 (GSK)p38 inhibitorIINone found on this particular compoundGlaxoSmithKline16
856553 (GSK)p38 inhibitorIINone found on this particular compoundGlaxoSmithKline16
247150iNOS inhibitionIINone found on this particular compound
Rosiglitazone XR (GSK)PPAR agonistIINone found on this particular compound, however, PPAR agonism works prophylactically in mouse CIATomita et al17
RJW 445380Cathepsin S inhibitorIIDecreased CIA in cathepsin S deficient miceNakagawa et al18
UK 427857CCR5 inhibitorIINone found on this particular compound, however, CCR5 antagonism works prophylactically in mouse CIAYang et al19
  • CCR, Chemokine (C-C motif) receptor; iNOS, inducible nitric oxide synthase; PEG, polyethylene glycol; PPAR, peroxisome proliferator-activated receptor; TNF, tumour necrosis factor.