Drug intelligence / Profile preview

MK-8776 + cytarabine

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Intravenous
01

Overview

MK-8776 + cytarabine is an investigational combination therapy for acute myeloid leukemia (AML) and other acute leukemias. MK-8776 is a selective small molecule inhibitor of checkpoint kinase 1 (Chk1), developed to abrogate cell cycle arrest and enhance DNA damage in cancer cells. Cytarabine (also known as AraC or cytosine arabinoside) is a nucleoside analog antimetabolite that inhibits DNA synthesis and is a standard component of AML therapy. Preclinical and clinical studies suggest that inhibiting Chk1 with MK-8776 disrupts DNA repair and cell-cycle checkpoints following cytarabine-induced DNA damage, increasing cancer cell death. The combination has been evaluated in relapsed/refractory AML in phase I/II trials. MK-8776 was developed by Merck Sharp & Dohme and tested with cytarabine to overcome resistance and increase efficacy in leukemias[1][3][5].

Other names
MK-8776 + AraCSCH900776 + cytarabineMK-8776 + cytosine arabinoside
02

Targets

CHEK2 (Checkpoint kinase 2)CHEK1 (Checkpoint kinase 1)CDK2 (Cyclin-dependent kinase 2)

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