Abivertinib – EGFR & BTK Inhibitor

Abivertinib 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 a first-line therapy for NSCLC patients with confirmed EGFR mutational status.

Several Phase I and II clinical trials have been completed, with over 600 NSCLC patients receiving treatment with Abivertinib in China, the U.S., and Europe with positive results published in Clinical Cancer Research.

FDA granted IND clearance for Phase II study to treat  patients resistant to Tagrisso (Osimertinib), a third-generation EGFR inhibitor.

Abivertinib also has 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. In addition, BTK  plays a critical role in immune regulation and host inflammatory responses. Sorrento Therapeutics is conducting global trials of Abivertinib for patients hospitalized with Covid-19.

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.