Abivertinib (AC0010) is a potent, irreversible, third-generation small molecule tyrosine kinase inhibitor (TKI) that selectively targets mutant forms of the epidermal growth factor receptor (EGFR).
Abivertinib inhibits the T790M “gatekeeper” mutation of EGFR and common activating mutations (L858R and del19) but has minimal inhibitory activity towards the normal (wild-type) receptor. The T790M mutation of EGFR is the major cause of acquired resistance and is detected in more than half of patients treated with first-generation EGFR TKIs, such as Tarceva (erlotinib) and Iressa (gefitinib).
Abivertinib is initially being developed as an oral treatment for patients with NSCLC in whom prior EGFR-directed therapy has failed due to the emergence of the EGFR T790M mutation. ACEA is also evaluating abivertinib as first-line therapy for NSCLC patients with confirmed EGFR mutational status.
Several Phase 1 and 2 clinical trials have been completed, with over 500 NSCLC patients receiving treatment with abivertinib in China, the U.S., and Europe. We have recently submitted a new drug application (NDA) to the Chinese FDA and anticipate a positive recommendation for abivertinib as a treatment for NSCLC in China in the near future.
Abivertinib may also have clinical utility as an inhibitor of Bruton’s tyrosine kinase (BTK) which impacts B cell proliferation and survival and is currently being investigated in clinical trials for B cell lymphoma.
For more information about our completed and ongoing clinical trials, please visit www.clinicaltrials.gov.
Abivertinib is an investigational drug candidate and has not yet been approved for use by the U.S. Food and Drug Administration (FDA), China Food and Drug Administration (CFDA) or other regulatory authorities.