Drug intelligence / Profile preview

MK-1496

Development stage
Phase 1
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

MK-1496 is an orally available, highly potent and selective small molecule inhibitor of polo-like kinase 1 (PLK1), a serine/threonine kinase involved in cell cycle control, particularly mitosis. Overexpression of PLK1 is frequently observed in various human tumors, making it a promising target for cancer therapy. By selectively inhibiting PLK1, MK-1496 induces G2/M cell cycle arrest and subsequent apoptosis in tumor cells. The drug has demonstrated anti-proliferative activity both in vitro and in vivo. It has been evaluated primarily for the treatment of neoplasms and malignant solid tumors, with clinical trials reaching phase I. The most common adverse effects are hematologic toxicities such as neutropenia and leukopenia, which are considered mechanism-based effects due to PLK1 inhibition[3][4][5][6].

Other names
1037254-47-9CS17H9370CCS-17H9370CCS 17H9370CUNII-CS17H9370CUNII-CS-17H9370CUNII-CS 17H9370C(1S)-1-(4-((1S)-1-Aminoethyl)phenyl)-2-(tert-butylamino)ethanol
02

Targets

PLK1 (Polo like kinase 1)

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