Drug intelligence / Profile preview

zotiraciclib

Development stage
Phase 2
Lead developer
Cothera Bioscience
Modality
Small Molecules
Administration
Oral
01

Overview

Zotiraciclib is an orally bioavailable, potent, spectrum-selective multi-kinase inhibitor developed for the treatment of cancer, particularly brain tumors such as glioblastoma and anaplastic astrocytoma. It was discovered by S*BIO in Singapore and is being developed by Adastra Pharmaceuticals. Zotiraciclib acts primarily by inhibiting cyclin-dependent kinases (CDKs), especially CDK9, leading to depletion of short-lived survival proteins like c-MYC and MCL-1 that are overexpressed in many cancers including glioblastoma. The drug also inhibits other kinases such as CDK1, CDK2, CDK7, Janus kinase 2 (JAK2), and FMS-like tyrosine kinase 3 (FLT3). Preclinical studies show it crosses the blood-brain barrier and can synergize with temozolomide to induce cell death in glioblastoma cells through suppression of transcriptional processes and cellular energy production. Zotiraciclib has received orphan drug designation from both the FDA and EMA for gliomas[1][3][5][6][8].

Other names
zotiraciclib citrateTG02 citrateTG-02 citrateTG 02 citrate
02

Targets

CDK1 (Cyclin-dependent kinase 1)CDK2 (Cyclin-dependent kinase 2)CDK3 (Cyclin-dependent kinase 3)CDK5 (Cyclin-dependent kinase 5)CDK7CDK9 (Cyclin-dependent kinase 9)FLT3 (Fms related receptor tyrosine kinase 3)FYN (Proto-oncogene tyrosine-protein kinase Fyn)JAK2 (Janus kinase 2)LCK (Proto-oncogene tyrosine-protein kinase Lck)TYK2 (Tyrosine kinase 2)

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