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Generic or research name | Type | Mechanism | Clinical trial-ovarian cancer, other | Clinical dose range (route) | Company |
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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 |
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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 |
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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 |
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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 |
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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 |
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CUDC-101 | Small molecule TKI | Multi-targeted HDAC/EGFR 1, 2 | None, Phase I solid tumors | Dose escalation, unknown starting dose | Curis, Inc. |
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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 |
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Matuzumab, EMD 72000 | Humanized MAb | Extracellular domain binding and ligand blockade | Phase II , other head+neck, lung, gastric | 800 mg weekly (IV) | EMD Serono/Merk KGaA |
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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 |
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RO5083945 | Glycoengineered MAb | Binds to EGFR extracellular domain, inhibits dimers | None, Phase I solid tumors | Dose escalation start at 50 mg (IV) | Roche Pharmaceuticals |
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