Table 1.
Agents that target the BCR pathway in CLL
Compound | Target | Status |
---|---|---|
Dasatinib | LYN, BTK | Phase 2 in CLL completed Approved for CML |
Fostamatinib (R788) | SYK | Phase 2 in CLL completed Phase 3 in rheumatoid arthritis ongoing |
PRT060318 | SYK | preclinical |
P505-15 | SYK | preclinical |
GS-1101 (CAL-101) | PI3Kδ | Phase 1 in CLL completed Phase 2/3 in CLL ongoing |
Everolimus | mTOR | Phase 2 in CLL completed Approved for relapsed renal cell carcinoma |
Ibrutinib (PCI-32765) | BTK | Phase 1 in CLL completed Phase 2/3 in CLL ongoing |
AVL-292 | BTK | Phase 1b in CLL ongoing |
Ruboxistaurin | PKC | Phase 3 in Diabetic Retinopathy completed Phase 3 in Diabetic Neuropathy completed |
Sotrastaurin | PKC | Phase 2 in renal transplant rejection completed Phase 2 in DLBCL ongoing |
Enzastaurin | PKC, AKT | Phase 2 in Waldenström macroglobulinemia completed Phase 2 in DLBCL and FL ongoing |