Drug intelligence / Profile preview

PRT3645

Development stage
Phase 1
Lead developer
Prelude Therapeutics
Modality
Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

PRT3645 is a highly potent, selective, and brain-penetrant small molecule inhibitor of cyclin-dependent kinase 4 (CDK4) and cyclin-dependent kinase 6 (CDK6). It is being developed as an antineoplastic agent with the goal of extending the reach of currently approved CDK4/6 inhibitors to address patients with brain metastases and central nervous system (CNS) cancers. The drug is designed to cross the blood-brain barrier effectively, making it suitable for treating tumors within the CNS. Its mechanism involves inhibiting CDK4 and CDK6 activity, which are key regulators of cell cycle progression from G1 to S phase; this inhibition can result in cell cycle arrest and reduced proliferation in cancer cells dependent on these kinases. The primary developer is Prelude Therapeutics. Clinical development has focused on advanced or metastatic solid tumors including breast cancer, glioblastoma, non-small cell lung cancer (NSCLC), sarcoma, head and neck squamous cell carcinoma (HNSCC), malignant mesothelioma, and endometrial cancer[1][3][7][9].

Other names
CDK4/6 inhibitor PRT3645
02

Targets

CDK4 (Cyclin-dependent kinase 4)CDK6 (Cyclin-dependent kinase 6)

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