Table 1.
Novel epidermal growth factor receptor inhibitors under evaluation for non-small cell lung cancer (http://www.clinicaltrials.gov)
| Agent | Description | Trial | Phase | Design |
|---|---|---|---|---|
| Afatinib | Irreversible dual EGFR/HER2 inhibitor | NCT00796549 | II | Advanced EGFR-mutant NSCLC |
| NCT01647711 | I | Intermittent high doses of afatinib in advanced T790M-mutant NSCLC pts | ||
| NCT01553942 | II | Before chemoradiation and after surgery in Stage III EGFR-mutant NSCLC | ||
| NCT01156545 | II | Afatinib versus afatinib + simvastatin in previously treated non-ADC NSCLC | ||
| NCT00730925 | II | Demographically and genotypically selected NSCLC pts | ||
| NCT01480141 | II | As neoadjuvant therapy in NSCLC pts who are deemed to be surgical candidates | ||
| NCT01003899 | II | Third-line therapy for Stage IIIb/IV EGFR-mutant NSCLC pts | ||
| Icotinib | Potent and specific EGFR TKIs | NCT01665417 | IV | Icotinib as first-line and maintenance therapy in EGFR mutated pts with lung ADC |
| NCT01465243 | IV | Dose escalation of icotinib in advanced NSCLC after routine icotinib therapy | ||
| NCT01688713 | II | NSCLC patients with brain metastasis | ||
| NCT01724801 | III | Icotinib versus whole brain RT in pts with EGFR-mutant NSCLC | ||
| NCT01516983 | I/II | In combination with whole brain RT in pts with EGFR-mutant NSCLC | ||
| NCT01514877 | II | In combination with whole brain RT in pts with EGFR-mutant NSCLC | ||
| NOV120101 | Pan-HER inhibitor | NCT01718847 | II | NSCLC patients with acquired resistance to first-generation EGFR TKIs |
| BMS-690514 | VEGFR and EGFR TKIs | NCT00743938 | II | BMS-690514 versus erlotinib in previously treated NSCLC pts |
| NCT01167244 | II | EGFR mutation-positive NSCLC pts treated with prior gefitinib or erlotinib | ||
| CO-1686 | Irreversible mutant-selective inhibitor of EGFR | NCT01526928 | I/II | Mutant EGFR NSCLC pts previously treated with first-line gefitinib or erlotinib |
| HM61713 | Mutant-selective EGFR-inhibitor | NCT01588145 | I | Pts progressed after at least two prior chemotherapy and/or EGFR TKI regimens |
| Dacomitinib | Irreversible pan-HER inhibitor | NCT01000025 | III | Dacomitinib versus placebo in Stage IIIB or IV pretreated NSCLC pts |
| NCT00818441 | II | Selected ADC pts with or without HER2 mutated or amplified NSCLC | ||
| CUDC-101 | Multitarget inhibitor of HDAC, EGFR, and HER2 | NCT01171924 | I | Advanced solid tumors including NCSLC |
| AP26113 | Dual ALK/EGFR inhibitor | NCT01449461 | I/II | Advanced solid tumors including NCSLC |
| XL647 | Multiple TKIs, including EGFR, VEGFR2, HER2, and EphB4 | NCT01487174 | III | XL647 or erlotinib in subjects with Stage IIIB/IV NSCLC, progressed after first- or second-line chemotherapy |
Abbreviations: ADC, adenocarcinoma; ALK, anaplastic lymphoma kinase; EGFR, epidermal growth factor receptor; EphB4, ephrin type-B receptor-4; HDAC, histone deacetylase; HER, human epidermal growth factor receptor; NSCLC, non-small cell lung cancer; pts, patients; RT, radiotherapy; TKI, tyrosine kinase inhibitor; VEGFR, vascular endothelial growth factor receptor.