Literature DB >> 12020065

Tipifarnib (Janssen Pharmaceutica).

Peter Norman1.   

Abstract

Janssen is developing tipifarnib (formerly known as R-1 15777), an inhibitor of RAS farnesylation, for the potential treatment of neoplasia [287030], [289610]. Janssen commenced clinical trials in the US, in conjunction with the National Cancer Institute, in April 1997 [287030], [289610], and by May 1999, phase II trials in patients with advanced non-small cell lung cancer were being planned [325960]. By February 2001, phase III trials for the potential treatment of pancreatic cancer and leukemia had been initiated [399065], and by June 2001, it was in phase II trials for RAS-dependent solid tumors [412618]. In November 2001, Credit Lyonnais Securities predicted NDAfilings in 2002 and 2003 for pancreatic cancer and other cancers, respectively, and projected US introductions for these indications in 2004 and 2005, respectively [436939].

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Year:  2002        PMID: 12020065

Source DB:  PubMed          Journal:  Curr Opin Investig Drugs        ISSN: 1472-4472


  6 in total

1.  Investigation of the effect of the farnesyl protein transferase inhibitor R115777 on isoprenylation and intracellular signalling by the prostacyclin receptor.

Authors:  Sarah J O'Meara; B Therese Kinsella
Journal:  Br J Pharmacol       Date:  2004-08-31       Impact factor: 8.739

2.  Structures of Cryptococcus neoformans protein farnesyltransferase reveal strategies for developing inhibitors that target fungal pathogens.

Authors:  Michael A Hast; Connie B Nichols; Stephanie M Armstrong; Shannon M Kelly; Homme W Hellinga; J Andrew Alspaugh; Lorena S Beese
Journal:  J Biol Chem       Date:  2011-08-04       Impact factor: 5.157

Review 3.  Suppression of farnesyltransferase activity in acute myeloid leukemia and myelodysplastic syndrome: current understanding and recommended use of tipifarnib.

Authors:  Pearlie K Epling-Burnette; Thomas P Loughran
Journal:  Expert Opin Investig Drugs       Date:  2010-05       Impact factor: 6.206

4.  Crystal structures of the fungal pathogen Aspergillus fumigatus protein farnesyltransferase complexed with substrates and inhibitors reveal features for antifungal drug design.

Authors:  Mark F Mabanglo; Michael A Hast; Nathan B Lubock; Homme W Hellinga; Lorena S Beese
Journal:  Protein Sci       Date:  2014-01-31       Impact factor: 6.725

5.  MicroRNAs as possible indicators of drug sensitivity in breast cancer cell lines.

Authors:  Katharina Uhr; Wendy J C Prager-van der Smissen; Anouk A J Heine; Bahar Ozturk; Marijn T M van Jaarsveld; Antonius W M Boersma; Agnes Jager; Erik A C Wiemer; Marcel Smid; John A Foekens; John W M Martens
Journal:  PLoS One       Date:  2019-05-07       Impact factor: 3.240

6.  Bacteria Are New Targets for Inhibitors of Human Farnesyltransferase.

Authors:  Lea Weber; Anna Hagemann; Jila Kaltenhäuser; Manuela Besser; Patrick Rockenfeller; Anja Ehrhardt; Ewa Stuermer; Hagen Sjard Bachmann
Journal:  Front Microbiol       Date:  2021-11-30       Impact factor: 5.640

  6 in total

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