Document Detail

Lonafarnib in cancer therapy.
MedLine Citation:
PMID:  16732721     Owner:  NLM     Status:  MEDLINE    
Farnesyl transferase inhibitors (FTIs) are anticancer agents that were designed to block the post-translational attachment of the prenyl moiety to C-terminal cysteine residue of Ras and thus inactivate it. Because Ras plays an important role in tumour progression and the ras mutation is one of the most frequent aberrations in cancer, FTIs have been expected to exert excellent therapeutic activities. Phase I and II clinical trials confirmed relevant antitumour activity and low toxicity; however, no improvement in overall survival has been reported in Phase III trials. The exact mechanism of action of this class of agents is currently unknown. Increasing lines of evidence indicate that the cytotoxic actions of FTIs are not due to the inhibition of Ras proteins exclusively, but to the modulation of other targets, including RhoB, the centromere-binding proteins and other proteins that have not yet been identified. This review describes the pharmacological and clinical data as well as mechanisms of action of FTIs, especially lonafarnib (SCH-66336), a non-peptidomimetic inhibitor that has shown anticancer activity.
Floriana Morgillo; Ho-Young Lee
Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.; Review    
Journal Detail:
Title:  Expert opinion on investigational drugs     Volume:  15     ISSN:  1744-7658     ISO Abbreviation:  Expert Opin Investig Drugs     Publication Date:  2006 Jun 
Date Detail:
Created Date:  2006-05-30     Completed Date:  2007-10-26     Revised Date:  2007-11-15    
Medline Journal Info:
Nlm Unique ID:  9434197     Medline TA:  Expert Opin Investig Drugs     Country:  England    
Other Details:
Languages:  eng     Pagination:  709-19     Citation Subset:  IM    
M. D. Anderson Cancer Center, Department of Thoracic/Head & Neck Medical Oncology, Houston, TX, USA.
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MeSH Terms
Antineoplastic Agents / administration & dosage,  pharmacokinetics,  therapeutic use*
Carcinoma, Non-Small-Cell Lung / drug therapy*,  enzymology
Colorectal Neoplasms / drug therapy*,  enzymology
Drug Administration Schedule
Drug Evaluation, Preclinical
Drug Therapy, Combination
Enzyme Inhibitors / administration & dosage,  pharmacokinetics,  therapeutic use*
Farnesyltranstransferase / antagonists & inhibitors
Leukemia / drug therapy*,  enzymology
Lung Neoplasms / drug therapy*,  enzymology
Piperidines / administration & dosage,  pharmacokinetics,  therapeutic use*
Pyridines / administration & dosage,  pharmacokinetics,  therapeutic use*
Randomized Controlled Trials as Topic
Grant Support
R01 CA100816/CA/NCI NIH HHS; R01 CA109520/CA/NCI NIH HHS
Reg. No./Substance:
0/Antineoplastic Agents; 0/Enzyme Inhibitors; 0/Piperidines; 0/Pyridines; 193275-84-2/lonafarnib; EC

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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