azenosertib + gemcitabine

Azenosertib + gemcitabine is an investigational combination therapy comprising **azenosertib** (also known as ZN-c3) and **gemcitabine**, developed primarily for the treatment of advanced cancers with a focus on pancreatic adenocarcinoma and relapsed or refractory osteosarcoma. Azenosertib is an orally available, highly selective, nanomolar inhibitor of the WEE1 tyrosine kinase, which is a critical regulator of the G2/M checkpoint in the cell cycle. Inhibition of WEE1 disrupts cancer cells’ ability to respond to replication stress, especially in tumors with p53 pathway alterations, leading to mitotic catastrophe and cell death. Gemcitabine is a nucleoside metabolic inhibitor that interferes with DNA synthesis. Preclinical and clinical evidence supports **synergistic cytotoxicity** for this combination, particularly in models and patients with pancreatic cancer and osteosarcoma. The combination is being evaluated in multiple phase 1 and 2 studies for safety, maximum tolerated dose, and anti-tumor activity[1][2][3][4][5].

Brand names

Gemzar

Other names

azenosertib + gemcitabine