Imatinib mesylate in the treatment of gastrointestinal stromal tumour

Dejka M. Steinert, John C. McAuliffe, Jonathan C. Trent

Research output: Contribution to journalReview article

17 Citations (Scopus)

Abstract

Imatinib mesylate is a selective and potent small-molecule inhibitor of tyrosine kinases, including Kit, platelet-derived growth factor receptor, and the BCR-Abl fusion protein. Kit plays an important role in gastrointestinal stromal tumours (GISTs) and is one of the most exciting therapeutic targets discovered so far. Clinical trials have consistently shown the dramatic efficacy of imatinib mesylate in patients with GIST. This article will review the development and pharmacology of this small-molecule inhibitor and summarise the clinical trials of imatinib mesylate for the treatment of GIST. Although imatinib mesylate has significantly improved the outcomes of most patients with advanced GIST, unanswered questions remain: what is the role of imatinib mesylate in the pre- and postoperative settings? What is the mechanism of the antitumour activity of imatinib? How do you manage patients whose tumours are refractory to imatinib mesylate?

Original languageEnglish (US)
Pages (from-to)105-113
Number of pages9
JournalExpert Opinion on Pharmacotherapy
Volume6
Issue number1
DOIs
StatePublished - Jan 2005
Externally publishedYes

Fingerprint

Gastrointestinal Stromal Tumors
Therapeutics
Clinical Trials
Platelet-Derived Growth Factor Receptors
Imatinib Mesylate
Protein-Tyrosine Kinases
Pharmacology

Keywords

  • Clinical trial
  • Gastrointestinal stromal tumour
  • Imatinib mesylate
  • Kit
  • Sarcoma
  • Targeted therapy

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

Cite this

Imatinib mesylate in the treatment of gastrointestinal stromal tumour. / Steinert, Dejka M.; McAuliffe, John C.; Trent, Jonathan C.

In: Expert Opinion on Pharmacotherapy, Vol. 6, No. 1, 01.2005, p. 105-113.

Research output: Contribution to journalReview article

Steinert, Dejka M. ; McAuliffe, John C. ; Trent, Jonathan C. / Imatinib mesylate in the treatment of gastrointestinal stromal tumour. In: Expert Opinion on Pharmacotherapy. 2005 ; Vol. 6, No. 1. pp. 105-113.
@article{84653f3b1bee432e845a15970d99789c,
title = "Imatinib mesylate in the treatment of gastrointestinal stromal tumour",
abstract = "Imatinib mesylate is a selective and potent small-molecule inhibitor of tyrosine kinases, including Kit, platelet-derived growth factor receptor, and the BCR-Abl fusion protein. Kit plays an important role in gastrointestinal stromal tumours (GISTs) and is one of the most exciting therapeutic targets discovered so far. Clinical trials have consistently shown the dramatic efficacy of imatinib mesylate in patients with GIST. This article will review the development and pharmacology of this small-molecule inhibitor and summarise the clinical trials of imatinib mesylate for the treatment of GIST. Although imatinib mesylate has significantly improved the outcomes of most patients with advanced GIST, unanswered questions remain: what is the role of imatinib mesylate in the pre- and postoperative settings? What is the mechanism of the antitumour activity of imatinib? How do you manage patients whose tumours are refractory to imatinib mesylate?",
keywords = "Clinical trial, Gastrointestinal stromal tumour, Imatinib mesylate, Kit, Sarcoma, Targeted therapy",
author = "Steinert, {Dejka M.} and McAuliffe, {John C.} and Trent, {Jonathan C.}",
year = "2005",
month = "1",
doi = "10.1517/14656566.6.1.105",
language = "English (US)",
volume = "6",
pages = "105--113",
journal = "Expert Opinion on Pharmacotherapy",
issn = "1465-6566",
publisher = "Informa Healthcare",
number = "1",

}

TY - JOUR

T1 - Imatinib mesylate in the treatment of gastrointestinal stromal tumour

AU - Steinert, Dejka M.

AU - McAuliffe, John C.

AU - Trent, Jonathan C.

PY - 2005/1

Y1 - 2005/1

N2 - Imatinib mesylate is a selective and potent small-molecule inhibitor of tyrosine kinases, including Kit, platelet-derived growth factor receptor, and the BCR-Abl fusion protein. Kit plays an important role in gastrointestinal stromal tumours (GISTs) and is one of the most exciting therapeutic targets discovered so far. Clinical trials have consistently shown the dramatic efficacy of imatinib mesylate in patients with GIST. This article will review the development and pharmacology of this small-molecule inhibitor and summarise the clinical trials of imatinib mesylate for the treatment of GIST. Although imatinib mesylate has significantly improved the outcomes of most patients with advanced GIST, unanswered questions remain: what is the role of imatinib mesylate in the pre- and postoperative settings? What is the mechanism of the antitumour activity of imatinib? How do you manage patients whose tumours are refractory to imatinib mesylate?

AB - Imatinib mesylate is a selective and potent small-molecule inhibitor of tyrosine kinases, including Kit, platelet-derived growth factor receptor, and the BCR-Abl fusion protein. Kit plays an important role in gastrointestinal stromal tumours (GISTs) and is one of the most exciting therapeutic targets discovered so far. Clinical trials have consistently shown the dramatic efficacy of imatinib mesylate in patients with GIST. This article will review the development and pharmacology of this small-molecule inhibitor and summarise the clinical trials of imatinib mesylate for the treatment of GIST. Although imatinib mesylate has significantly improved the outcomes of most patients with advanced GIST, unanswered questions remain: what is the role of imatinib mesylate in the pre- and postoperative settings? What is the mechanism of the antitumour activity of imatinib? How do you manage patients whose tumours are refractory to imatinib mesylate?

KW - Clinical trial

KW - Gastrointestinal stromal tumour

KW - Imatinib mesylate

KW - Kit

KW - Sarcoma

KW - Targeted therapy

UR - http://www.scopus.com/inward/record.url?scp=12744272175&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=12744272175&partnerID=8YFLogxK

U2 - 10.1517/14656566.6.1.105

DO - 10.1517/14656566.6.1.105

M3 - Review article

C2 - 15709888

AN - SCOPUS:12744272175

VL - 6

SP - 105

EP - 113

JO - Expert Opinion on Pharmacotherapy

JF - Expert Opinion on Pharmacotherapy

SN - 1465-6566

IS - 1

ER -