Skip to main content

Table 1 Landmark clinical trials in the development of small-molecule EGFR TKIs

From: Clinical development of targeted and immune based anti-cancer therapies

Drug Name Clinical Trial ID Trial Name Population Comparator Year Sponsor Phase N Median OS (months) Median PFS (months)
Small-molecule EGFR TKIs
 1st Generation EGFR TKI
  Gefitinib (Iressa®/ZD1839)
   Gefitinib (250 mg/d) NCT00322452 IPASS NSCLC Chemotherapy 2006–2010 AstraZeneca III 1329 18.6 vs 17.3 5.7 vs 5.8/24.9 vs 6.7%
   Gefitinib (250 mg/d) NCT01203917 IFUM NSCLC (EGFR+) None 2010–2013 AstraZeneca IV 1060 19.2 7.0
  Erlotinib (Tarceva®)
   Erlotinib (150 mg/d) NCT00036647 BR.21 NSCLC Placebo 2001–2004 OSI Pharmaceuticals III 731 6.7 vs 4.7 2.2 vs 1.8
   Erlotinib (150 mg/d) NCT00556712 SATURN NSCLC Placebo 2010–2013 Hoffmann-La Roche Obs 289 12.4 vs 11.0 12.3 vs 11.1
   Erlotinib (150 mg/d) NCT01328951 IUNO NSCLC Placebo 2011–2016 Hoffmann-La Roche III 643 9.7 vs 9.5 3.0 vs 2.8
   Erlotinib (100 mg/d) + Gemcitabine (1000 mg/m2/w) NCT02694536   Pancreatic cancer None 2006–2009 Hoffmann-La Roche III 80 7.5 4.9
  Lapatinib (Tykerb®)
   Lapatinib (1250 mg/d) + capecitabine (2000 mg/m2) NCT00078572   Breast (HER2+) Capecitabine 2004–2006 GSK III 408 17.3 vs 14.9 7.2 vs 4.3
   Lapatinib (1500 mg/d) + letrozole (2.5 mg/d) NCT00073528   Breast (ER/PR +) Letrozole 2003–2018 Norvatis III 1285 33.3 vs 32.3 8.1 vs 3.0
   Lapatinib (1500 mg/d) NCT00374322 TEACH Breast (HER2+) Placebo 2006–2013 GSK III 3166 7.3 vs 8.0% 13.3 vs 15.8%
 2nd Generation EGFR TKI
  Afatinib (BIBW 2992/Gilotrif®)
   Afatinib (50 mg/d) NCT00525148 LUX-Lung 2 NSCLC None 2007–2015 Boehringer Ingelheim II 129 26.8 10.2
   Afatinib (40 mg/d) NCT00949650 LUX-Lung 3 NSCLC, Adenocarcinoma Pemetrexed + cisplatin 2009–2017 Boehringer Ingelheim III 345 28.2 vs 28.2 11.2 vs 6.9
   Afatinib (40 mg/d) NCT01121393 LUX-Lung 6 NSCLC, Adenocarcinoma Gemcitabine + cisplatin 2010–2017 Boehringer Ingelheim III 364 23.1 vs 23.5 11.0 vs 5.6
   Afatinib (40-50 mg/d) NCT01523587 LUX-Lung 8 NSCLC Erlotinib 2012–2017 Boehringer Ingelheim III 795 NR 2.4 vs 1.9
   Afatinib (40 mg/d) + vinorelbine (25 mg/m2) NCT01125566 LUX-Breast 1 Breast (HER2+) Trastuzumab + vinorelbine 2010–2018 Boehringer Ingelheim III 508 19.6 vs 28.6 5.5 vs 5.6
   Afatinib (40 mg/d) NCT01271725 LUX-Breast 2 Breast (HER2+) Afatinib + vinorelbine + paclitaxel 2011–2017 Boehringer Ingelheim II 74 NR NR
   Afatinib (40 mg/d) NCT01441596 LUX-Breast 3 Breast (HER2+) Investigator’s choice 2011–2015 Boehringer Ingelheim II 121 13.3 vs 12.0 2.7 vs 4.2
  Dacomitinib (Vizimpro®)
   Dacomitinib (45 mg/d) NCT01774721 ARCHER 1050 NSCLC (EGFR mutant) Gefitinib 2013–2016 SFJ Pharmaceuticals III 440 16.9 vs 11.9 14.7 vs 9.2
Vandetanib (Caprelsa®)
   Vandetanib (300 mg/d) NCT00410761 ZETA Thyroid Placebo 2006–2019 Sanofi III 437 13.9 vs 16.0% 30.5 vs 19.2
   Vandetanib (300 mg/d) NCT00409968 NCT00411671 NCT00411632 NCT00410059 NCT00410189 BATTLE Program NSCLC Erlotinib, erlotinib + bexarotene, sorafenib 2006–2018 United States Department of Defense II 255 33.0% 1.8
  Neratinib (Nerlynx®)
   Neratinib (240 mg/d) NCT00878709 ExteNET Breast Cancer Placebo 2009–2020 (active) Puma Biotechnology, Inc. III 2840 4.7 vs 8.0 (DFS) NR
 3rd Generation EGFR TKI
  Osimertinib (Tagrisso®)
   Osimertinib (80 mg/d) NCT01802632 AURA extension NSCLC (EGFR-T790 M) None 2013–2018 AstraZeneca I/II 201 [603] NR 9.7
   Osimertinib (80 mg/d) NCT02094261 AURA 2 NSCLC (EGFR-T790 M) None 2014–2019 AstraZeneca II 210 NR 8.6
   Osimertinib (80 mg/d) NCT02151981 AURA 3 NSCLC Chemotherapy 2014–2018 (active) AstraZeneca III 419 NR 10.1 vs 4.4
  Rociletinib
   Rociletinib (500–750 mg BD) NCT01526928   NSCLC None 2012–2019 Clovis Oncology, Inc. I/II 605   13.1
  Naquotinib
   Naquotinib (dose NR) NCT02588261 SOLAR NSCLC Erlotinib or gefitinib 2016–2017 (terminated) Astellas Pharma Inc III 530 NR NR