ZL-2201 / ZAI Lab - LARVOL DELTA

Discovery and Characterization of ZL-2201, a Potent, Highly Selective, and Orally Bioavailable Small-molecule DNA-PK Inhibitor. (PubMed, Cancer Res Commun) - "More importantly, we identified phospho-MCM2 (Ser108) as a potential proximal biomarker of DNA-PK inhibition that warrants further preclinical and clinical evaluation. ZL-2201, a potent and selective DNA-PK inhibitor, can target tumor models in combination with DNA DSB-inducing agents such as radiation or doxorubicin, with potential to improve recurrent therapies in the clinic."

Journal • Ataxia • Immunology • Movement Disorders • Oncology • Primary Immunodeficiency • MCM2 • PRKDC

Discovery and characterization of ZL-2201, a potent, highly-selective, and orally bioavailable small-molecule DNA-PK inhibitor (AACR 2022) - "In conclusion, ZL-2201 demonstrates potent and selective inhibition of DNA-PK enzymatic activity, strong synergy with DNA damaging agents in vitro and in vivo, antitumor activity against multiple human xenograft models, and a favorable projected human PK profile. ZL-2201 is expected to enter clinical development in 2022."

Oncology • ATM

Zai Lab to Present New Oncology Research at 2022 AACR Annual Meeting (GlobeNewswire) - "Three poster presentations will highlight additional key programs in Zai Lab’s internal oncology pipeline....Preclinical data will measure the enhanced antitumor effect by combining ZL-1201 with the current standard of care antibody treatments in hematologic and solid tumor models. Data from ZL-1211, a CLDN18.2-specific monoclonal antibody will be presented with preclinical results supporting effective targeting of CLDN18.2+ gastric cancer, including CLDN18.2-low expressing malignancies....Another presentation will feature the discovery and development of ZL-2201, a novel, orally bioavailable, selective DNA-PK inhibitor."

Preclinical • Gastric Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor

Zai Lab Announces Financial Results and Corporate Updates for Twelve Months Ended December 31, 2021 (GlobeNewswire) - "Anticipated 2022 Zai Milestone: Simurosertib: Initiate a Phase 2 biomarker-driven proof-of-concept study in the second quarter of 2022; ZL-1201: Determine a recommended Phase 2 dose in the ongoing Phase 1 trial in mid-2022; Present preclinical data of ZL-1201 in combination with standard of care therapeutic antibodies in hematologic and solid tumor models at the 2022 AACR annual meeting; ZL-1211: Present preclinical data of ZL-1211 (Claudin18.2), ZL-2201 (DNA-PK), and ZL-1218 (CCR8) at the 2022 AACR annual meeting."

Clinical • New P2 trial • Preclinical • Hematological Malignancies • Oncology • Solid Tumor