FDA Awards Breakthrough Therapy Designation to Novel HER2-Activating NSCLC Therapy


The FDA has granted a breakthrough therapy designation to BAY 2927088 for the treatment of non-small cell lung cancer harboring HER2-activating mutations.

Lung with cancer cells: © catalin - stock.adobe.com

Lung with cancer cells: © catalin - stock.adobe.com

  • The FDA has granted a breakthrough therapy designation to BAY 2927088, an oral, small molecule tyrosine kinase inhibitor (TKI) for patients with non-small cell lung cancer (NSCLC) harboring HER2-activating mutations.
  • Breakthrough therapy designation is intended to expedite the development and review of drugs that treat serious conditions and show improvement over currently available therapies.
  • This designation marks a new potential treatment for the most common type of lung cancer.

The FDA has granted a breakthrough therapy designation to BAY 2927088 in NSCLC with HER2-activating mutations.1

“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, MD, PhD, head of research and early development for oncology at Bayer’s pharmaceuticals division, in a press release.

BAY 2927088 is an oral, small molecule TKI with the potential to inhibit mutant HER2 receptors, including HER2 exon 20 insertions, HER2 point mutations, and EGFR mutations.

The designation is supported by findings from a phase 1 study (NCT05099172). The study’s primary end points are incidence of treatment-emergent adverse events (AEs), treatment-emergent serious AEs, severity of AEs, number of patients who discontinue treatment due to an AE, maximum tolerated dose, dose-limiting toxicities, overall response rate (ORR), and pharmacokinetics.2 Secondary end points include recommended phase 2 dose, disease control rate, duration of response, progression-free survival, and overall survival.

Patients in the dose-escalation portion of the study are receiving doses of BAY 2927088 that are increased in a stepwise fashion until the maximum tolerated dose is reached. The dose-expansion portion is initiated after the dose-escalation portion, and the dose-extension portion begins once all ongoing participants in the expansion cohort have received at least 12 weeks of treatment.

Patients are eligible to participate in the study if they have documented histologically or cytologically confirmed NSCLC, disease progression following at least 1 prior systemic therapy, an ECOG performance status of 0 or 1, a minimum life expectancy of at least 12 weeks, adequate marrow function, and adequate kidney function. Patients are not eligible for trial enrollment if they have any unresolved toxicity greater than grade 2 from previous anticancer treatment, a history of central nervous system metastases, history of spinal cord compression, history of congestive heart failure, or known hepatitis or HIV infections.

“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,” said Ruettinger in a press release.1

1. Bayer receives U.S. FDA breakthrough therapy designation for BAY 2927088 for non-small cell lung cancer harboring HER2 activating mutations. News release. Bayer. February 26, 2024. Accessed February 27, 2024. http://tinyurl.com/bddnrb6e
2. First in human study of BAY2927088 in participants who have advanced non-small cell lung cancer (NSCLC) with mutations in the genes of epidermal growth factor receptor (EGFR) and/​or human epidermal growth factor receptor 2 (HER2). ClinicalTrials.gov. Updated January 29, 2024. Accessed February 27, 2024. https://clinicaltrials.gov/study/NCT05099172
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