Table 2: Non-FDA approved EGFR inhibitors. Data derived from the NCI Drug Dictionary and Clinical Trials Search http://www.nci.nih.gov/Templates/drugdictionary and [4, 47].

Generic or research nameTypeMechanismClinical trial-ovarian cancer, otherClinical dose range (route)Company

CI-1033PD 183805CanertinibSmall molecule TKIIrreversible binding to ATP-binding site EGFR 1, 2, 3, 4Phase II50 mg–200 mg daily day 1–21 (oral)Pfizer

EKB-569PelitinibSmall molecule TKIIrreversible binding to TK domain of EGFR 1, 2, 4None, Phase I in solid tumors25 mg daily (oral)Wyeth-Ayerst

PKI-166Small molecule TKIReversible binding to TKI domain EGFR 1, 2None, Phase I in solid tumors600 mg–700 mg 2 weeks on/offNovartis

AV-412Second generation dual TKIReversible binding to TKI domain EGFR 1,2None, active Phase I trial in solid tumorsDose escalation daily, dose escalation three times/wkAVEO Pharmaceuticals

BIBW-2992TovokSecond generation dual TKIIrreversible binding to TKI domain EGFR 1, 2None, Phase I in solid tumors and Phase II in lung, breast, cancer50 mg daily (oral), 70 mg daily 2weeks on/offBoehringer Ingelheim's

CUDC-101Small molecule TKIMulti-targeted HDAC/EGFR 1, 2None, Phase I solid tumorsDose escalation, unknown starting doseCuris, Inc.

BMS-690154Small molecule TKIBinds tyrosine kinase domains of EFGR1, 2 and VEGFR-2None, Phase I in combo with paclitaxel and carboplatinDose escalation, unknown starting doseBristol-Myers Squibb

Matuzumab, EMD 72000Humanized MAbExtracellular domain binding and ligand blockadePhase II E G F R + , other head+neck, lung, gastric800 mg weekly (IV)EMD Serono/Merk KGaA

PertuzumabHumanized MAbExtracellular her2 ligand blockade, prevents dimers with EGFR-1Phase II, lung, breast, prostate840 mg load followed by 420 mg every 3 weeks (IV)Merck Serono

RO5083945Glycoengineered MAbBinds to EGFR extracellular domain, inhibits dimersNone, Phase I E G F R + solid tumorsDose escalation start at 50 mg (IV)Roche Pharmaceuticals