Gene (locus) | Alteration | Possible drug/therapeutic targeting abnormalities |
FHIT (3p14.2) | Loss (80% of SCLC) | |
RASSF1 (3p21.3) | Loss (>90% of SCLC) | |
RARB (3p24) | Loss (72% of SCLC) | |
TP53 (17p13.1) | Mutation and deletion (>75% of SCLC) | p53 adenoviral vector (Advexin) |
c-Kit | Overexpressed | Tyrosine kinase inhibitor (imatinib) |
Src | Constitutively activated | Src inhibitor (dasatinib) |
c-Met | Amplified, overexpressed or mutated | siRNA, c-Met inhibitor SU11274 |
RB1 | Altered (>90% of SCLC) | |
PI3K/Akt/mTOR | Constitutively activated | PI3K inhibitor (LY294002) mTOR inhibitor (rapamycin) and its derivatives (CCI-779, RAD001, AP23576) |
Bcl-2 | Overexpressed | Antisense oligonucleotide (oblimersen sodium) Inhibitor of Bcl-2 (ABT-737) |
VEGF | Overexpressed | Humanised monoclonal antibody (bevacizumab) VEGFR-2 and EGFR inhibitor (ZD6474) |
FHIT: fragile histidine triad; RASSF: Ras-association domain family; RARB: retinoic acid receptor-β; TP53: tumour protein p53; RB: retinoblastoma; PI3K: phosphoinositide 3-kinase; mTOR: mammalian target of rapamycin; Bcl: B-cell lymphoma; VEGF: vascular endothelial growth factor; siRNA: small interfering RNA; EGFR: epidermal growth factor.