Drug intelligence / Profile preview

SRA737 + gemcitabine

Development stage
Unknown
Lead developer
GSK
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

SRA737 + gemcitabine is a combination therapy under investigation for the treatment of advanced solid tumors and certain genetically defined cancers. SRA737 is an orally bioavailable small molecule inhibitor of checkpoint kinase 1 (CHK1), a key regulator in the DNA damage response pathway. By inhibiting CHK1, SRA737 abrogates DNA repair in tumor cells exposed to genotoxic stress or chemotherapy, thereby enhancing cancer cell death. Gemcitabine is a nucleoside analog antimetabolite that interferes with DNA synthesis and induces apoptosis in rapidly dividing cells. The combination leverages the chemosensitizing effect of CHK1 inhibition to potentiate the cytotoxicity of gemcitabine. Clinical trials have shown this regimen to be generally well tolerated at recommended doses and have demonstrated objective responses in several tumor types including anogenital cancer, cervical cancer, high-grade serous ovarian cancer, rectal cancer, and small cell lung cancer[5][7][6].

Other names
checkpoint kinase 1 inhibitor SRA737CHK1 inhibitor SRA737CHK-1 inhibitor SRA737CHK 1 inhibitor SRA737gemcitabine hydrochloride
02

Targets

DNACHEK1 (Checkpoint kinase 1)RRM1

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