Farnesyltransferase inhibitors: Where are we now?

  • A.M. T
  • C. C
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Abstract

Importance of the field: Farnesyltransferase inhibitors (FTIs) target multiple pathways implicated in the pathogenesis of solid and hematologic malignancies. Areas covered in this review: Novel preclinical and clinical data on FTIs. What the reader will gain: Results of clinical trials of FTIs are critically summarized: Phase I II studies demonstrated that tipifarnib (the most extensively investigated FTI) had antileukemic activity. The rates of complete response (CR), partial response (PR) and/or CR with incomplete platelet recovery (CRp) in patients with MDS and refractory/poor-risk AML were 5 25% and 11 14%, respectively (hematological improvement, 17 35% and 8 9.5%, respectively). A Phase III study comparing tipifarnib with best supportive care, including hydroxyurea in patients with untreated AML >= 70 years old showed no survival benefit in the tipifarnib arm. A two-gene classifier (RASGRP1:APTX gene expression ratio) predicted response and survival, indicating that a two-gene expression assay may help select patients with AML who would benefit from tipifarnib. Take home message: Patient selection should become a priority for targeted agent drug development. Clinical trials selecting patients who would benefit from FTIs should be designed to define the role of FTIs in the treatment of hematological malignancies and solid tumors. © 2010 Informa UK, Ltd.

Author-supplied keywords

  • *3 benzyl 7 cyano 2,3,4,5 tetrahydro 1 (1h imidazo
  • *lonafarnib/ae [Adverse Drug Reaction]
  • *lonafarnib/cb [Drug Combination]
  • *lonafarnib/cm [Drug Comparison]
  • *lonafarnib/ct [Clinical Trial]
  • *lonafarnib/dt [Drug Therapy]
  • *lonafarnib/pd [Pharmacology]
  • *tipifarnib/ae [Adverse Drug Reaction]
  • *tipifarnib/cb [Drug Combination]
  • *tipifarnib/cm [Drug Comparison]
  • *tipifarnib/ct [Clinical Trial]
  • *tipifarnib/dt [Drug Therapy]
  • *tipifarnib/pd [Pharmacology]
  • *tipifarnib/po [Oral Drug Administration]
  • K ras protein/ec [Endogenous Compound]
  • Ras protein/ec [Endogenous Compound]
  • abdominal cramp/si [Side Effect]
  • acute lymphoblastic leukemia/dt [Drug Therapy]
  • acute myeloblastic leukemia/dt [Drug Therapy]
  • anorexia/si [Side Effect]
  • ataxia/si [Side Effect]
  • bortezomib/cb [Drug Combination]
  • breast cancer/dt [Drug Therapy]
  • carboplatin/cb [Drug Combination]
  • cisplatin/dt [Drug Therapy]
  • clinical trial
  • colorectal cancer/dt [Drug Therapy]
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  • cyclophosphamide/cb [Drug Combination]
  • dehydration/si [Side Effect]
  • diarrhea/si [Side Effect]
  • docetaxel/cm [Drug Comparison]
  • doxorubicin/cb [Drug Combination]
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  • erlotinib/cb [Drug Combination]
  • fatigue/si [Side Effect]
  • fever/si [Side Effect]
  • fluorouracil/cb [Drug Combination]
  • gastrointestinal symptom/si [Side Effect]
  • gemcitabine/ae [Adverse Drug Reaction]
  • gemcitabine/cb [Drug Combination]
  • gemcitabine/ct [Clinical Trial]
  • gemcitabine/dt [Drug Therapy]
  • gene expression
  • head and neck cancer/dt [Drug Therapy]
  • hematologic malignancy
  • hematological parameters
  • human
  • hydroxyurea/cm [Drug Comparison]
  • hyperbilirubinemia/si [Side Effect]
  • imatinib/cb [Drug Combination]
  • imatinib/cm [Drug Comparison]
  • kidney failure/si [Side Effect]
  • lung non small cell cancer/dt [Drug Therapy]
  • mesothelioma/dt [Drug Therapy]
  • mesylic acid/cm [Drug Comparison]
  • multiple myeloma/dt [Drug Therapy]
  • myelodysplastic syndrome/dt [Drug Therapy]
  • myelofibrosis/dt [Drug Therapy]
  • nausea/si [Side Effect]
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  • oncogene K ras
  • paclitaxel/ae [Adverse Drug Reaction]
  • paclitaxel/cb [Drug Combination]
  • paclitaxel/ct [Clinical Trial]
  • paclitaxel/dt [Drug Therapy]
  • pancreas tumor/dt [Drug Therapy]
  • patient selection
  • polydipsia/si [Side Effect]
  • prostate cancer/dt [Drug Therapy]
  • review
  • solid tumor
  • sorafenib/cb [Drug Combination]
  • squamous cell carcinoma/dt [Drug Therapy]
  • taxane derivative/cb [Drug Combination]
  • temozolomide/cm [Drug Comparison]
  • thrombocytopenia/si [Side Effect]
  • trastuzumab/cb [Drug Combination]
  • trastuzumab/ct [Clinical Trial]
  • trastuzumab/dt [Drug Therapy]
  • treatment response
  • urinary tract tumor/dt [Drug Therapy]
  • vincristine XT - abdominal cramp / side effect /
  • vomiting/si [Side Effect]

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Authors

  • Tsimberidou A.M.

  • Chandhasin C.

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