Phase I evaluation of seliciclib (R-roscovitine), a novel oral cyclin-dependent kinase inhibitor, in patients with advanced malignancies

C Le Tourneau, S Faivre, V Laurence… - European journal of …, 2010 - Elsevier
AIM: Phase I study of seliciclib (CYC202, R-roscovitine), an inhibitor of cyclin-dependent
kinases 2, 7 and 9, causing cell cycle changes and apoptosis in cancer cells. PATIENTS …

[HTML][HTML] A phase I trial of the selective oral cyclin-dependent kinase inhibitor seliciclib (CYC202; R-Roscovitine), administered twice daily for 7 days every 21 days

C Benson, J White, J De Bono, A O'Donnell… - British journal of …, 2007 - nature.com
Abstract Seliciclib (CYC202; R-roscovitine) is the first selective, orally bioavailable inhibitor
of cyclin-dependent kinases 1, 2, 7 and 9 to enter clinical trial. Preclinical studies showed …

Seliciclib in malignancies

IT Aldoss, T Tashi, AK Ganti - Expert opinion on investigational …, 2009 - Taylor & Francis
Cyclins and cyclin-dependent kinases (CDK) form a key part of the regulatory proteins that
govern the cell cycle. Aberrancy in their function can lead to uncontrolled growth and …

Metabolism of the trisubstituted purine cyclin-dependent kinase inhibitor seliciclib (R-roscovitine) in vitro and in vivo

SJ McClue, I Stuart - Drug metabolism and disposition, 2008 - ASPET
Seliciclib (R-roscovitine, CYC202) is a small molecule inhibitor of cyclin-dependent kinases
currently in phase II clinical trials as an anticancer agent. We examined the metabolism of …

The cyclin-dependent kinase inhibitor seliciclib (R-roscovitine; CYC202) decreases the expression of mitotic control genes and prevents entry into mitosis

SR Whittaker, RH Te Poele, F Chan, S Linardopoulos… - Cell Cycle, 2007 - Taylor & Francis
The cyclin-dependent kinase (CDK) inhibitor seliciclib (R-roscovitine, CYC202) shows
promising antitumor activity in preclinical models and is currently undergoing phase II …

Metabolism and pharmacokinetics of the cyclin-dependent kinase inhibitor R-roscovitine in the mouse

BP Nutley, FI Raynaud, SC Wilson, PM Fischer… - Molecular cancer …, 2005 - AACR
Abstract R-roscovitine (seliciclib, CYC202) is a cyclin-dependent kinase inhibitor currently in
phase II clinical trials in patients with cancer. Here, we describe its mouse metabolism and …

In vitro and In vivo Pharmacokinetic-Pharmacodynamic Relationships for the Trisubstituted Aminopurine Cyclin-Dependent Kinase Inhibitors Olomoucine, Bohemine …

FI Raynaud, SR Whittaker, PM Fischer, S McClue… - Clinical cancer …, 2005 - AACR
Purpose: To investigate pharmacokinetic-pharmacodynamic relationships for the
trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine, and …

[HTML][HTML] Roscovitine in cancer and other diseases

J Cicenas, K Kalyan, A Sorokinas… - Annals of …, 2015 - ncbi.nlm.nih.gov
Abstract Roscovitine [CY-202,(R)-Roscovitine, Seliciclib] is a small molecule that inhibits
cyclin-dependent kinases (CDKs) through direct competition at the ATP-binding site. It is a …

CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases

K Bettayeb, N Oumata, A Echalier, Y Ferandin… - Oncogene, 2008 - nature.com
Among the ten pharmacological inhibitors of cyclin-dependent kinases (CDKs) currently in
clinical trials, the purine roscovitine (CYC202, Seliciclib) is undergoing phase 2 trials against …

[HTML][HTML] Discovery and development of Seliciclib. How systems biology approaches can lead to better drug performance

HS Khalil, V Mitev, T Vlaykova, L Cavicchi… - Journal of …, 2015 - Elsevier
Seliciclib (R-Roscovitine) was identified as an inhibitor of CDKs and has undergone drug
development and clinical testing as an anticancer agent. In this review, the authors describe …