Tyrosine Kinase Inhibitors

Imatinib Mesylate
(Gleevec®, Novartis
Oncology)


BCR-ABL

Dasatinib
(Spryicel ®, Bristol Myers
Squibb)

Hematological malignancies
o Philadelphia chromosome positive chronic myeloid leukemia (Ph+ CML) and
lymphoblastic leukemia (Ph+ ALL)
o Adult patients with myelodysplastic/ myeloproliferative diseases (MDS/MPD)
associated with PDGFR (platelet-derived growth factorreceptor) gene rearrangements
adjuvant treatment of adult patients following complete gross resection of Kit (CD117)
positive Gastrointestinal Stromal Tumors (GIST).
Patient info: http://www.nlm.nih.gov/medlineplus/druginfo/meds/a606018.html
Indications
o Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) in
chronic phase; or with resistance or intolerance to prior therapy including
imatinib
o Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL)
with resistance or intolerance to prior therapy.
On-line resources
o Patient Info: http://www.nlm.nih.gov/medlineplus/druginfo/meds/a607063.html

Nilotinib
(Tasigna (R), Novartis)



bosutinib tablets (Bosulif,
Pfizer, Inc.)
Newly diagnosed Philadelphia chromosome positive chronic myeloid leukemia (Ph+
CML) in chronic phase
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.
On-line resources:
 Manufacturer’s website: http://www.us.tasigna.com/index.jsp
 FDA Approval: http://www.cancer.gov/cancertopics/druginfo/fda-nilotinib
 Prescribing information insert:
http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/022068s004s005l
bl.pdf
 Patient information:
http://www.nlm.nih.gov/medlineplus/druginfo/meds/a608002.html
chronic, accelerated, or blast phase Philadelphia chromosome positive (Ph+) chronic
myelogenous leukemia (CML) in adult patients with resistance or intolerance to prior
therapy



EGFR (ErbB1)
Lapatinib

and
(Tykerb®, Glaxo Smith Skline)
HER-2 [ErbB2]

Gefitinib (Iressa ®)

EGFR

Erlotinib
(Tarceva ®, Genentech)


With capecitabine, for the treatment of patients with HER2 + advanced or metastatic
breast cancer in patients who have received prior therapy including an anthracycline,
a taxane, and trastuzumab.
With letrozole for the treatment of postmenopausal ER+/HER2+ women in whom
hormonal therapy is indicated.
On-Line resources:
o FDA Approval: http://www.cancer.gov/cancertopics/druginfo/fda-lapatinib
o Prescribing information insert:
http://www.tykerb.com/pdf/TKB962R0_Product_Brochure.pdf
o Manufacturer’s Info: http://www.tykerb.com/
o Patient Information:
http://www.nlm.nih.gov/medlineplus/druginfo/meds/a607055.html
As of June 17, 2005 IRESSA is only to be used in patients who are benefiting or
have benefited from IRESSA. After September 2005, no new patients will be
allowed access to IRESSA unless they are being enrolled into a clinical trial that was
been approved by an IRB prior to June 17, 2005.
Prior to this announcement, IRESSA’s indication was for advanced recurrent NSCLC
NSCLC
o Maintenance therapy
o Progressive disease
Pancreatic cancer: Locally advanced, unresectable or metastatic
Tarceva website for patients
Temsirolimus
(Torisel ®, Pfizer)


Advanced Renal Cell Carcinoma
Pfizer healthcare professional website for Torisel



Advanced renal cell carcinoma after failure of treatment with sunitinib or sorafenib
pediatric and adult patients with tuberous sclerosis complex (TSC) who have
subependymal giant cell astrocytoma (SEGA) that requires therapeutic intervention
but cannot be curatively resected
postmenopausal women with advanced hormone receptor-positive, HER2-negative
breast cancer in combination with exemestane, after failure of treatment with letrozole
or anastrozole
adults with renal angiomyolipoma, associated with tuberous sclerosis complex (TSC),
who do not require immediate surgery.
Novartis patient education website for Afinitor

Medullary thyroid cancer



Multiple Myeloma
Mantle Cell Lymphoma
Millenium website for patients



Unresectable hepatocellular carcinoma
Advanced renal cell carcinoma
Bayer Health Care website for providers
mTOR
Everolimus

(Afinitor ®, Novartis)

EGFR,
MET/VEGF,
RET
Vandetanib
Proteasome
inhibitor
Bortezomib
Multiple
tyrosine kinase
inhibitors
(Caprelsa (R), Astra
Zeneca)
(Velcade®, Millenium)
Sorafenib
(Nexavar ®, )


including
VGFR, PDGFR
Sunitinib

(Sutent ®, Pfizer) )

Pfizer website for providers
(Votrient ®, GSK)



Advanced renal cell carcinoma as single agent
advanced soft tissue sarcoma (STS) who have received prior chemotherapy
GSK website for providers
vismodegib

metastatic basal cell carcinoma or with locally advanced basal cell carcinoma that
has recurred following surgery or who are not candidates for surgery, and who are
not candidates for radiation.
Pazopanib
VEGFR;
Hedgehog
pathway
Advanced renal cell carcinoma (RCC)
Gastrointestinal stromal tumor (GIST) after disease progression on or intolerance to
imatinib mesylate
Progressive, well-differentiated pancreatic neuroendocrine tumors (pNET) in patients
with unresectable locally advanced or metastatic disease
(Erivedge ® Capsule,
Genentech, Inc)