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AZD7762 + gemcitabine
- Development stage
- Discontinued
- Lead developer
- AstraZeneca
- Modality
- Small Molecules
- Administration
- Intravenous
01
Overview
AZD7762 + gemcitabine is a combination therapy comprising AZD7762, a selective inhibitor of checkpoint kinase 1 (Chk1), and gemcitabine, a nucleoside antimetabolite chemotherapeutic. AZD7762 acts by inhibiting Chk1 and Chk2, disrupting DNA damage checkpoints and enhancing the cytotoxic effects of DNA-damaging agents like gemcitabine, which incorporates into DNA and inhibits DNA synthesis. The combination has been investigated primarily for advanced solid tumors due to preclinical evidence of synergistic antitumor activity. In clinical studies, the maximum tolerated dose of AZD7762 in combination with gemcitabine (1,000 mg/m²) was found to be 30 mg, but further development was halted due to unpredictable cardiac toxicities associated with AZD7762.
- Other names
- AZD7762 + gemcitabine
02
Targets
CHEK2 (Checkpoint kinase 2)CHEK1 (Checkpoint kinase 1)
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