On February 26, 2024 Bayer reported that the U.S. Food and Drug Administration (FDA) has granted Breakthrough Therapy designation for BAY 2927088 for the treatment of adult patients with unresectable or metastatic non-small cell lung cancer (NSCLC) whose tumors have activating HER2 (ERBB2) mutations, and who have received a prior systemic therapy (Press release, Bayer, FEB 26, 2024, View Source [SID1234640480]). BAY 2927088 is an oral, reversible tyrosine kinase inhibitor (TKI) that potently inhibits mutant human epidermal growth factor receptors 2 (HER2), including HER2 exon 20 insertions and HER2 point mutations, as well as epidermal growth factor receptors (EGFR), with high selectivity for mutant vs wild-type EGFR.1,2

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Lung cancer is the leading cause of cancer-related deaths worldwide.3 NSCLC is the most common type of lung cancer, accounting for more than 85% of cases.4 Activating HER2 mutations are found in 2% to 4% of advanced NSCLC.5 Currently there are no available therapies that have received full approval in the U.S. for patients with NSCLC in the metastatic or advanced setting harboring HER2 activating mutations.

The Breakthrough Therapy designation is supported by preliminary clinical evidence from the Phase I, open-label, multicenter first-in-human study (NCT05099172) evaluating the safety, pharmacokinetics and preliminary efficacy of BAY 2927088 in adult patients with advanced NSCLC harboring HER2 or EGFR.

"Early clinical evidence suggests that BAY 2927088, our investigational novel oral tyrosine kinase inhibitor, has the potential to benefit patients with NSCLC harboring a HER2 mutation that have progressed on a prior systemic therapy and currently have no other approved treatment available," said Dominik Ruettinger, M.D., Ph.D., Head of Research and Early Development for Oncology at Bayer’s Pharmaceuticals Division. "This Breakthrough Therapy designation is a significant milestone in our relentless efforts to develop innovative therapies for the treatment of lung cancer characterized by specific genomic markers. We will continue working closely with the FDA to advance BAY 2927088 through the clinic and look forward to providing these patients with lung cancer and their physicians with a targeted, effective treatment option."

The FDA’s Breakthrough Therapy designation is intended to expedite the development and review of drug candidates that treat serious or life-threatening diseases or conditions, and preliminary clinical evidence indicates that the drug may demonstrate substantial improvement on one or more clinically significant endpoints over available therapies.6

BAY 2927088 was derived from Bayer’s long-standing strategic research alliance with the Broad Institute of MIT and Harvard in Cambridge, MA, USA.