C H A P T E R 1 4
Antineoplastic agents
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TABLE 14.6
DRUGS IN FOCUS Cancer cell–specific agents
Drug name
Dosage/route
Usual indications
Protein tyrosine kinase inhibitors
everolimus (Afinitor,
Certican)
10 mg/day PO with food
Treatment of people with advanced renal cell
carcinoma after failure of treatment with
sunitinib or sorafenib
Special considerations:
pneumonitis, serious-to-
fatal infections, oral ulcerations, and elevations
in blood glucose, lipid and creatinine levels may
occur, monitor person very closely; do not use in
pregnancy
gefitinib (Iressa)
250 mg/day PO
Monotherapy for treatment of people with locally
advanced or metastatic non–small cell lung
cancer after failure with platinum-based or
docetaxel chemotherapies; use limited to people
doing well on therapy—not for new use
Special considerations:
interstitial lung disease
may occur; monitor pulmonary function closely;
eye changes may require stopping the drug for
a while; do not use during pregnancy; numerous
drug–drug interactions are possible
imatinib (Glivec)
Chronic-phase chronic myelocytic
leukaemia (CML): 400 mg/day PO,
may be increased to 600 mg/d if
needed
Blast-crisis CML: 600 mg/day PO, may
be increased to 400 mg PO b.d.
First-line CML treatment: 400 mg/day
PO
GI stromal tumours: 400–600 mg/day
PO
Treatment of CML people in blast crisis or in
chronic phase after interferon-alpha therapy;
treatment of people with Kit-positive malignant
GIST; first-line treatment of CML
Special considerations:
administer with a meal
and a full glass of water; arrange for small,
frequent meals if GI upset is a problem; provide
analgesics for headache and muscle pain; monitor
full blood count and for oedema to arrange for
dose reduction if needed; person should receive
consultation to deal with high cost of drug
lapatinib (Tykerb)
1250 mg (5 tablets) orally once daily
on days 1–21 in combination with
capecitabine 2000 mg/m2 per day
PO in 2 doses approximately 12 hours
apart on days 1–14; give in a repeating
21-day cycle; reduce dose to
750 mg/day PO with severe hepatic
dysfunction
In combination with capecitabine for the treatment
of people with advanced or metastatic breast
cancer whose tumours overexpress HER2 and
who have received prior treatment including an
anthracycline, taxane and trastuzumab
Special considerations:
monitor heart function
closely and decrease dose as needed; monitor
for rash, GI toxicity; avoid grapefruit juice; many
drug–drug interactions are possible
nilotinib (Tasigna)
400 mg PO b.d., approximately
12 hours apart without food
Treatment of chronic-phase and accelerated-phase
Philadelphia chromosome–positive chronic
myelogenous leukaemia in adult people resistant
or intolerant to prior therapy that included
imatinib
Special considerations:
monitor for prolonged
QT interval, bone marrow suppression and
possible liver toxicity
sorafenib (Nexavar)
400 mg PO b.d. on an empty stomach
Treatment of people with advanced renal cell
carcinoma and unresectable hepatocellular
carcinoma
Special considerations:
monitor for skin
reactions, hand-foot syndrome, hypertension
sunitinib (Sutent)
50 mg/day PO for 4 weeks, followed by
2 weeks of rest; repeat cycle
Treatment of GI stromal tumour if person is
intolerant to or tumour progresses after imatinib
therapy
Special considerations:
monitor for GI
disturbances, bone marrow suppression; adjust
dose as needed
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