Potent IRAK-4 inhibitors have been reported by several groups including some structurally related benzimidazoles as well as alternative fused heterocycles such as the imidazopyridine and imidazopyridazine. Such compounds are reported to have IRAK-1 and IRAK-4 activity with varying degrees of selectivity.
Recently, Nuvation Bio announced positive pooled data from the pivotal Phase 2 TRUST-I and TRUST-II studies at the European Society for Medical Oncology (ESMO). Analysis showed that its small molecule taletrectinib, a new highly selective ROS1/NTRK kinase inhibitor, can cross the patient's blood-brain barrier to treat brain metastases, and nearly 90% of patients with advanced ROS1-positive non-small cell lung cancer (NSCLC) who received treatment had tumor shrinkage. In patients who had never been treated with tyrosine kinase inhibitors (TKIs), disease remission was sustained for nearly 4 years. Nuvation Bio plans to submit a new drug application (NDA) for the drug to the FDA in the fourth quarter of this year. Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.