Drug intelligence / Profile preview

DCZ0858

Development stage
Preclinical
Lead developer
Shanghai Institute of Materia Medica
Modality
Small Molecules
Administration
Intravenous
01

Overview

DCZ0858 is a novel small molecule silicone derivative of natural osalmid developed as an antineoplastic agent. It has demonstrated significant antitumor activity in preclinical studies against diffuse large B-cell lymphoma (DLBCL) and multiple myeloma (MM). Mechanistically, DCZ0858 induces apoptosis in tumor cells via both the intrinsic and extrinsic apoptotic pathways and causes cell cycle arrest at the G0/G1 phase. The drug inhibits the JAK2/STAT3 signaling pathway in DLBCL and suppresses mTORC1 and mTORC2 signaling in MM, overcoming resistance from the bone marrow microenvironment. Preclinical animal studies indicate DCZ0858 has robust antitumor effects with minimal toxicity to normal tissues and organs. Its encouraging safety and efficacy profile suggest potential for further clinical development in hematological malignancies[1][3][5][7][9].

02

Targets

Mechanistic target of rapamycin complex 1CDK6 (Cyclin-dependent kinase 6)Mechanistic target of rapamycin kinase complex 2CDK4 (Cyclin-dependent kinase 4)JAK2 (Janus kinase 2)STAT3 (Signal Transducer and Activator of Transcription 3)CCND1 (Cyclin D1)

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