mardi 30 août 2011

The twelve US (FDA) approved small molecule protein kinase inhibitors.

Other names
Cancer type

Nonreceptor tyrosine kinase inhibitor
Glivec, Gleevec
a multitargeted c-kit, PDGF-R and c-ABL inhibitor
Newly diagnosed adult patients with Philadelphia chromosome positive (Ph+) chronic myeloid leukemia (CML) in chronic phase;

Patients with Philadelphia chromosome positive (Ph+) chronic myeloid leukemia (CML) in blast crisis, accelerated phase, or in chronic phase after failure of interferon-alpha therapy;

Pediatric patients with Ph+ CML in chronic phase who are newly diagnosed or whose disease has recurred after stem cell transplant or who are resistant to interferon-alpha therapy;

Adult patients with relapsed or refractory Philadelphia chromosome positive acute lymphoblastic leukemia (ALL);
Adult patients with myelodysplastic/ myeloproliferative diseases (MDS/MPD) associated with PDGFR (platelet-derived growth factor receptor) gene re-arrangements;

Adult patients with aggressive systemic mastocytosis (ASM) without the D816V c-Kit mutation or with c-Kit mutational status unknown;
Adult patients with hypereosinophilic syndrome (HES) and/or chronic eosinophilic leukemia (CEL);
Adult patients with unresectable, recurrent and/or metastatic dermatofibrosarcoma protuberans (DFSP);

Patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST);

-Adjuvant treatment of adult patients following complete gross resection of Kit (CD117) positive GIST.
Receptor tyrosine kinase inhibitor
Iressa, ZD-1839
EGFR and Akt inhibitor
Locally advanced or metastatic non-small-cell lung cancer (NSCLC) after failure of platinum-based and docetaxel chemotherapy
Receptor tyrosine kinase inhibitor
Tarceva, CP-358774, OSI-774, NSC-718781
EGFR inhibitor
 Locally advanced or metastatic non-small cell lung cancer (NSCLC) after failure of at least one prior chemotherapy regimen;

Maintenance treatment of NSCLC patients whose disease has not progressed after four cycles of platinum-based first-line chemotherapy;

In combination with gemcitabine for treatment of patients with locally advanced, unresectable or metastatic pancreatic carcinoma.
Receptor tyrosine kinase inhibitor
VEGFR, PDGFR and RAF/MEK/ERK cascade inhibitor
Unresectable hepatocellular carcinoma (HCC);

Advanced renal cell carcinoma (RCC)
Nonreceptor tyrosine kinase inhibitor
Sprycel, BMS-354825, BMS354825
ATP-competitive, dual SRC/ABL inhibitor. It inhibits all members of the Src family, including c-Src, Lck, Fyn, and Yes
Chronic phase Philadelphia chromosome-positive chronic myelogenous leukemia (CP-CML);

Chronic phase (CP) chronic myelogenous leukemia (CML) with resistance or intolerance to prior therapy;

Chronic myelogenous leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (ALL) with resistance or intolerance to prior therapy.
Receptor tyrosine kinase inhibitor
multitargeted FLT3, PDGFRs, VEGFRs, and Kit kinase inhibitor
Advanced renal cell carcinoma;

Gastrointestinal stromal tumor (GIST) after disease progression on, or intolerance to, imatinib mesylate
Nonreceptor tyrosine kinase inhibitor
Tasigna, AMN-107
Inhibitor of BCR-ABL
Adult patients with newly diagnosed Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) in chronic phase (CP-CML);

Chronic phase (CP) and accelerated phase (AP) Philadelphia chromosome positive (Ph+) chronic myelogenous leukemia (CML) in adult patients resistant or intolerant to prior therapy that included imatinib.
Receptor tyrosine kinase inhibitor
EGFR and HER2 inhibitor
Hormone-receptor- and HER2-positive advanced breast cancer;

HER2-overexpressing breast cancer
Receptor tyrosine kinase inhibitor
VEGFR-1, -2, and -3 inhibitor
Advanced renal cell carcinoma
Receptor tyrosine kinase inhibitor
VEGFR and EGFR inhibitor
Unresectable, locally advanced, or metastatic medullary thyroid cancer
Serine/threonine kinase inhibitor
Zelboraf, PLX-4032, RG7204, R7204 & RO5185426
BRAf inhibitor
Unresectable or metastatic melanoma carrying the mutant BRAFV600E.
Serine/threonine kinase inhibitor
Xalkori, PF-2341066
ALK and HGFR inhibitor
Locally advanced or metastatic non-small cell lung cancer (NSCLC) that is ALK-positive as detected by an approved FDA-approved test.

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