Drug intelligence / Profile preview

MK-8776

Development stage
Phase 2
Lead developer
Merck
Modality
Small Molecules
Administration
Intravenous
01

Overview

MK-8776 is a potent, selective, and orally bioavailable small molecule inhibitor of checkpoint kinase 1 (Chk1), an essential regulator of the DNA damage response and cell cycle progression. By inhibiting Chk1, MK-8776 disrupts cell cycle arrest in response to DNA damage, thereby enhancing the cytotoxic effects of DNA-damaging agents such as gemcitabine and cytarabine. This mechanism provides potential radiosensitization and chemosensitization activities. The drug was originally developed by Schering-Plough (later acquired by Merck) for use in oncology indications including acute myeloid leukemia (AML), solid tumors, lymphoma, Hodgkin disease, adult erythroleukemia, and non-Hodgkin lymphoma. Clinical trials have demonstrated that MK-8776 is generally well tolerated both as monotherapy and in combination with chemotherapeutic agents[2][3][4][5][8].

Other names
SCH 900776SCH900776SCH-900776MK-8776MK8776MK 8776
02

Targets

CHEK1 (Checkpoint kinase 1)

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