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Highly Selective Compound Gains FDA Acceptance for Next-Gen EGFR Inhibitor in NSCLC
On March 2, 2022, the FDA accepted a novel Investigational New Drug (IND) application for phase 1/2a trials of H002, a broad spectrum, highly selective, fourth-generation compound to treat C797S mutation-driven resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) in patients with non-small-cell lung cancer (NSCLC).
"The IND acceptance and anticipated start of our global clinical studies, represent important milestones in our company's growth and validation of our internally developed small molecule discovery platform," said Mai-Jing Liao, PhD, CEO of RedCloud Bio.
The drug discovery platform combines computational approaches, including computational chemistry and artificial intelligence (AI), with structural pharmacology that differentiates interactions between drug candidates and disease-causing mutations of target proteins at an atomic level.
“TKIs can afford an important therapeutic option for patients with NSCLC. However, emergence of resistant mutations to successive generations of therapeutics can compromise TKIs' efficacy. The C797S mutation, in combination with several other mutations, has emerged as one of the most common mechanisms for on-target resistance to third-generation EGFR TKIs such as osimertinib. These combinations have been found in seven to fifteen percent of third generation TKI-treated NSCLC patients," Dr Liao noted.
H002 has also shown significant inhibitory effects on wide spectrum of single, double, and triple EGFR mutants in laboratory studies.
