Table 2.

Summary of selected drugs in clinical trials targeting MAPK and/or PI3K pathways

ClassDrugsTrialsComments
EGFR MoAbNimotuzumab (h-HR3), zalutumumab (HuMax-EGFR), necitmumab (IMC-11F8), matuzumab (EMD7200)Phase I, IINimotuzumab and zalutumumab in trials in irinotecan resistant mCRC. Necitumumab in trials as first line with mFOLFOX6
RAF inhibitorsSorafenib, PLX-4032, RAF265, XL281Phase I-IIISorafenib in several phase II-III trials in mCRC to look for benefit in relation to KRAS and BRAF mutations
MEK inhibitorsCI-1040, PD0325901, AZD6244, AS703026, GSK1120212, PD-325901, RO5126766, GDC-0973, TAK-733Phase I, IIAZD6244 in phase II trial in patients with refractory mCRC
PI3K inhibitorsPI3K and mTOR inhibitors: BEZ235, BGT226, XL765, SF1126, PF-04691502Phase I, IISeveral agents in phase II trials in patients with metastatic breast cancer
PI3K inhibitors: BKM120, XL147, GDC0941, PX-866, CAL-101, GSK1059615
AKT inhibitorsperifosine (KRX-0401), MK2206, VQD-002 (API-2), XL418, GSK2141795, SR13668, GSK690693, nelfinavirPhase I, IINelfinavir is an antiretroviral protease inhibitor shown to inhibit AKT
mTOR inhibitorsRapamycin-sirolimus, temsirolimus, everolimus, AP23573, AZD8055, OSI-027, palomid 529Phase I, IIEverolimus with bevacizumab in patients with refractory mCRC. Sirolimus in phase II trial with patients having germline mutations in PTEN

NOTE: Data are from http://clinicaltrials.gov.