Drug intelligence / Profile preview

TB008

Development stage
Preclinical
Lead developer
Therabene
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Oral
01

Overview

**TB008** is a proprietary proteolysis-targeting chimera (PROTAC) developed by Therabene as a first-in-class CDK9 degrader for oncology applications. It consists of a CDK9-binding moiety linked via an alkyl chain or polyethylene glycol linker to a cereblon E3 ligase recruiter, enabling targeted ubiquitination and proteasomal degradation of CDK9. TB008 demonstrates potent CDK9 kinase inhibition (IC50 3.5 nM), effective degradation in cancer cell lines (e.g., MIA-PaCa-2, NCI-H358), moderate lipophilicity (LogP 2.75), high absorption, and good solubility (LogS -3.83), positioning it as a promising targeted therapy for CDK9-dependent cancers like non-small cell lung carcinoma and pancreatic cancer.[1][7]

02

Targets

CDK9 (Cyclin-dependent kinase 9)

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