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 name	Type	Mechanism	Clinical trial-ovarian cancer, other	Clinical dose range (route)	Company
CI-1033PD 183805Canertinib	Small molecule TKI	Irreversible binding to ATP-binding site EGFR 1, 2, 3, 4	Phase II	50 mg–200 mg daily day 1–21 (oral)	Pfizer
EKB-569Pelitinib	Small molecule TKI	Irreversible binding to TK domain of EGFR 1, 2, 4	None, Phase I in solid tumors	25 mg daily (oral)	Wyeth-Ayerst
PKI-166	Small molecule TKI	Reversible binding to TKI domain EGFR 1, 2	None, Phase I in solid tumors	600 mg–700 mg 2 weeks on/off	Novartis
AV-412	Second generation dual TKI	Reversible binding to TKI domain EGFR 1,2	None, active Phase I trial in solid tumors	Dose escalation daily, dose escalation three times/wk	AVEO Pharmaceuticals
BIBW-2992Tovok	Second generation dual TKI	Irreversible binding to TKI domain EGFR 1, 2	None, Phase I in solid tumors and Phase II in lung, breast, cancer	50 mg daily (oral), 70 mg daily 2weeks on/off	Boehringer Ingelheim's
CUDC-101	Small molecule TKI	Multi-targeted HDAC/EGFR 1, 2	None, Phase I solid tumors	Dose escalation, unknown starting dose	Curis, Inc.
BMS-690154	Small molecule TKI	Binds tyrosine kinase domains of EFGR1, 2 and VEGFR-2	None, Phase I in combo with paclitaxel and carboplatin	Dose escalation, unknown starting dose	Bristol-Myers Squibb
Matuzumab, EMD 72000	Humanized MAb	Extracellular domain binding and ligand blockade	Phase II EGFR+, other head+neck, lung, gastric	800 mg weekly (IV)	EMD Serono/Merk KGaA
Pertuzumab	Humanized MAb	Extracellular her2 ligand blockade, prevents dimers with EGFR-1	Phase II, lung, breast, prostate	840 mg load followed by 420 mg every 3 weeks (IV)	Merck Serono
RO5083945	Glycoengineered MAb	Binds to EGFR extracellular domain, inhibits dimers	None, Phase I EGFR+ solid tumors	Dose escalation start at 50 mg (IV)	Roche Pharmaceuticals