Gleevec (imatinib mesylate)
The following drug information is obtained from various newswires, published
medical journal articles, and medical conference presentations.
Gleevec has been approved for treatment of patients with chronic
myeloid leukemia (CML) in myeloid blast crisis, accelerated phase,
or chronic phase, for whom interferon-alpha therapy has failed. It
is available in oral capsule formulation. Gleevec is the first
anti-cancer drug developed with rational drug design, based on the
understanding of how cancer cells work.
CML is caused by a reciprocal translocation between chromosomes
nine and 22 that results in the "Philadelphia
chromosome", a known marker for the disease. There are an
estimated 4,500 new cases of CML each year in the United States and
2,400 Americans die from the disease annually.
The response to Gleevec was evaluated in three international,
open-label, single-arm, phase II studies in 1,027 patients
diagnosed with Philadelphia chromosome positive CML. Effectiveness
was rated primarily by hematologic response, but cytogenetic
response was also measured.
Patients in chronic phase showed a hematologic response of 88%
and a cytygenetic response of 49%. The response rates for these two
measures were 63% and 21% for those in accelerated phase and 26%
and 13.5% in blast crisis.
Adverse events associated with the use of imatinib mesylate may
include (but are not limited to) the following:
- fluid retention
- muscle cramps
- musculoskeletal pain
- skin rash
Mechanism of Action
Gleevec (imatinib mesylate) is a protein-tyrosine kinase
inhibitor that blocks the constitutive abnormal tyrosine kinase,
Bcr-Abl tyrosine kinase, that is created by the Philadelphia
chromosome abnormality found in CML. The drug inhibits
proliferation and induces apoptosis in Bcr-Abl positive cells and
in fresh leukemic cells. The preciseness with which Gleevec targets
the cancer cells is more advanced than most other oncology
products. (from Gleevec Prescribing Information)
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