TABLE 1

Kinase inhibitors in clinical development

KinaseInhibitorsDevelopment StageDisease IndicationComments
IKK (NF-κB)IMD-0354Phase 2?COPDDiscontinued
Bay 65-1942PreclinicalCOPDOral
p38 MAPKDilmapimodPhase 2COPDOral
LosmapimodPhase 2COPDOral
PH-797804Phase 2COPDOral
PF-03715455Phase 2Asthma, COPDInhaled
AZD7624Phase 2COPDInhaled
RV-568Phase 2COPDInhaled
JNKSP600125PreclinicalAsthma, COPD?Oral
MEK1/ERKTrametinibPhase 3CancerOral
ASK-1GS-4997Phase 2DiabetesOral
PI3KIdelisibApprovedB cell malignancyOral PI3Kδ-selective
TG100-115PreclinicalAsthma, COPDInhaledPI3Kγ/δ-selective
GSK2269557Phase 2COPDInhaled PI3Kδ-selective
RV-1729Phase 2Asthma, COPDInhaled PI3Kγ/δ-selective
JAKLAS194046PreclinicalAsthma, COPDInhaled
R256PreclinicalAsthma, COPDInhaled
VR560PreclinicalAsthma, COPDInhaled
SYKFostamatinibPhase 3Arthritis, lymphomaOral
R112Phase 2RhinitisNasal, discontinued
R343Phase 2AsthmaInhaled, discontinued
LAS189386PreclinicalAsthmaInhaled
RTKBIBW 2948Phase 2COPDInhaled EGFR
MasitinibPhase 2Severe asthmaOral, PDGFR, c-Kit
ROCKFasudilApprovedCerebral vasospasmOral
  • ASK, apoptosis signal-regulatory kinase; EGFR, epidermal growth factor receptor; ERK, extracellular regulating kinase; IKK, inhibitor of kB kinase; JAK, Janus-activated kinase; JNK, Jun NH2-terminal kinase; MAPK, mitogen-activated protein kinase; NF-κB, nuclear factor-kappa B; PDGFR, platelet-derived growth factor receptor; PI3K, phosphoinositide-3-kinase; ROCK, Rho-associated protein kinase; RTK, receptor tyrosine kinase; Syk, spleen tyrosine kinase.