China-based Dizal Pharmaceutical Co., Ltd (SHA: 688192), spun out from AstraZeneca’s China drug discovery unit in 2017, announced that the National Medical Products Administration (NMPA) has approved a Phase II clinical study for its pipeline candidate DZD1516. The trial will evaluate DZD1516, a small-molecule HER2-targeted tyrosine kinase inhibitor, in combination with Roche’s trastuzumab emtansine (Kadcyla) for patients with HER2-positive advanced breast cancer.
Drug Profile
DZD1516 is a highly selective small-molecule HER2 inhibitor capable of penetrating the blood-brain barrier. HER2-positive breast cancers frequently metastasize to the central nervous system (CNS), with 40–60% of cases affected. Traditional chemotherapy and macromolecular targeted drugs often fail to cross the blood-brain barrier effectively.
Phase I Results
A global, multi-center Phase I study (Jan 17, 2022) showed DZD1516 was well-tolerated at doses <300 mg twice daily. The drug demonstrated selectivity for wild-type EGFR (>300-fold) and no diarrhea or rash adverse events. The Kpuu, CSF ratio of 2.13 indicates complete blood-brain barrier penetration.
Company Pipeline
Dizal Pharma has two drugs in global pivotal trials and five in global multi-center studies, advancing its oncology-focused pipeline.-Fineline Info & Tech
