Table 2

EGFR-targeted agents in clinical developmenta

AgentMechanism of action in vitro IC50 HER1 (KBb,c; CGd) HER2 (KBc; CGd)Clinical status
ZD1839EGFR-TK inhibitorPhase III
gefitinib)HER1 (23–79 nm; ≤80 nm)(Approved)
HER2 (3.7–10 μm; N/A)
OSI-774EGFR-TK inhibitorPhase III
(erlotinib)HER1 (2–20 nm; ≤100 nm)
HER2 (0.2 μm; <3 μm)
CI-1033 (none)EGFR-TK/HER2 inhibitorPhase I
HER1 (1.7 nm; 7.4 nm)
HER2 (5 nm; N/A)
C225 (cetuximab)Anti-EGFR antibodyPhase II/III
ABX-EGF (none)Anti-EGFR antibodyPhase I/II
EGF-P64K (none)VaccinePhase II/III
DAB389-EGF (none)ImmunotoxinPhase II
  • a See Refs. 45 46 47 48 .

  • b KB, kinase/binding inhibition; CG, cell growth inhibition; N/A, not available.

  • c KB varies based on the source of purified HER1/2.

  • d CG varies based on cell line tested.