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seliciclib
- Development stage
- Phase 2
- Lead developer
- Cyclacel Pharmaceuticals
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Seliciclib is an orally available small molecule inhibitor of cyclin-dependent kinases (CDKs), specifically targeting CDK2, CDK7, and CDK9 by competing for their ATP binding sites. This inhibition disrupts cell cycle progression and can induce apoptosis in cancer cells. Seliciclib is a 2,6,9-substituted purine analog developed primarily by Cyclacel Pharmaceuticals. It has been investigated for several indications including non-small cell lung cancer (NSCLC), leukemia, Cushing disease (pituitary ACTH hypersecretion), cystic fibrosis, rheumatoid arthritis, nasopharyngeal cancer, HIV infection, herpes simplex infection and chronic inflammation disorders. The drug has reached phase II clinical trials in several indications but has not received regulatory approval due to dose-limiting toxicities such as hypokalemia and liver enzyme elevations[1][2][3][4][6].
- Brand names
- Seliciclib
- Other names
- roscovitineR-roscovitine
02
Targets
PDXK (Pyridoxal kinase)CDK7CDK2 (Cyclin-dependent kinase 2)P-TEFb (Positive transcription elongation factor b)CDK6 (Cyclin-dependent kinase 6)CDK8 (Cyclin-dependent kinase 8)CDK4 (Cyclin-dependent kinase 4)CDK1 (Cyclin-dependent kinase 1)
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