Drug intelligence / Profile preview

sch2047069

Development stage
Preclinical
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

**SCH2047069** is a novel, orally bioavailable small molecule inhibitor of **Kinesin spindle protein (KSP; also known as Eg5)**, a mitotic kinesin required for the formation of bipolar mitotic spindles during cell division. By inhibiting KSP, SCH2047069 causes mitotic arrest, leading to cell death via irreversible antiproliferative effects. The compound demonstrates antitumor activity in multiple preclinical cancer models as a single agent and enhances efficacy in combination with other chemotherapeutics such as paclitaxel, gemcitabine, or vincristine. It is distinguished from other KSP inhibitors by its oral bioavailability and ability to cross the blood-brain barrier. Developers sought oral dosing for improved convenience and potential for dose-dense regimens. The mechanism of action is marked by intracellular accumulation of cells in mitosis and increased phosphorylation of histone H3. SCH2047069 has shown activity against solid tumors (e.g., colon cancer, glioblastoma) and hematologic malignancies (e.g., AML, lymphoma) in preclinical studies[1][2][5][8].

Other names
sch2047069sch-2047069sch 2047069
02

Targets

KIF11 (Kinesin Spindle Protein)

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