Drug intelligence / Profile preview

cisplatin + gemcitabine + seliciclib

Development stage
Unknown
Lead developer
Cyclacel Pharmaceuticals
Modality
Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen consisting of three agents: - **Cisplatin** is a platinum-based chemotherapy drug that forms DNA crosslinks, leading to apoptosis in rapidly dividing cells. - **Gemcitabine** is a nucleoside analog that inhibits DNA synthesis by incorporation into DNA and inhibition of ribonucleotide reductase, also resulting in cell death. - **Seliciclib** (also known as roscovitine or CYC202) is an orally active small molecule inhibitor of cyclin-dependent kinases (CDK2, CDK7, CDK9), disrupting cell cycle progression and transcriptional regulation. Seliciclib has been investigated primarily for its antitumor activity and potential synergy with cytotoxic agents. The combination aims to enhance antitumor efficacy by targeting cancer cells through multiple mechanisms—DNA damage/cell cycle arrest (cisplatin/gemcitabine) and direct inhibition of key cell cycle regulators (seliciclib). While cisplatin plus gemcitabine is an established regimen for several cancers including non-small cell lung cancer, bladder cancer, biliary tract cancers, ovarian cancer, cervical cancer, mesothelioma and pancreatic cancer[1][4][5][7], seliciclib remains investigational with ongoing research into its use in solid tumors such as non-small cell lung cancer[6][8][9][10].

02

Targets

DNARNR (Ribonucleotide reductase)DNA polymerase familyCDK7CDK1 (Cyclin-dependent kinase 1)CDK2 (Cyclin-dependent kinase 2)CDK9 (Cyclin-dependent kinase 9)CDK5 (Cyclin-dependent kinase 5)

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