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Seliciclib, a cell-cycle modulator that acts through the inhibition of cyclin-dependent kinases

Robert C Jackson1, Anna L Barnett, Steven J McClue

  • 1Pharmacometrics Ltd, 51 North Road, Whittlesford, Cambridge CB22 4NZ, UK +44 1382 206062 ; +44 1382 206067 ; rjackson1943@aol.com.

Expert Opinion on Drug Discovery
|March 14, 2013
PubMed

Insights

Seliciclib, a CDK inhibitor, shows anti-tumor activity by blocking transcription and downregulating key cancer-related genes. It is orally available and well-tolerated, with ongoing Phase II trials for lung and nasopharyngeal cancers.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Seliciclib targets cyclin-dependent kinases 2, 7, and 9.
  • It inhibits transcription, downregulating Mcl-1 and cyclin D1 mRNA.
  • Possesses single-agent and synergistic anti-tumor activity.

Purpose of the Study:

  • To summarize the mechanism of action, anti-tumor activity, and clinical development of Seliciclib.
  • To outline its pharmacokinetic properties and determined clinical dosing.
  • To report on its safety profile and ongoing clinical trials.

Main Methods:

  • In vitro and in vivo studies evaluating anti-tumor effects.
  • Pharmacokinetic and pharmacodynamic assessments.
  • Phase I and II clinical trials to determine dosing, safety, and efficacy.

Main Results:

  • Seliciclib inhibits transcription and selectively downregulates Mcl-1 and cyclin D1.
  • Demonstrates anti-tumor activity alone and synergistically with other agents.
  • Achieves high oral bioavailability; Phase I trials established dosing.
  • Major toxicities (nausea, vomiting, hypokalemia, elevated creatinine/LFTs) are reversible.
  • Non-myelosuppressive and non-intestinal toxic.

Conclusions:

  • Seliciclib is an orally bioavailable CDK inhibitor with demonstrated anti-tumor activity.
  • Its toxicity profile is manageable and reversible, supporting further clinical development.
  • Ongoing Phase II trials in non-small cell lung cancer and nasopharyngeal carcinoma are evaluating its efficacy.

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