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Targeted
Therapy
Dr. Mohammed Fathy, MD
Lecturer of Clinical Oncology
Zagazig University
Introduction
Target
Imatinib
Specific Tyrosine Kinase
Inhibitors (TKI)
B-RAF Inhibitors
MEK Inhibitors
Monoclonal
Antibodies (Mab)
Small molecule
Trastuzumab
Tyrosine Kinase Inhibitors
(TKIs)
Indications
Gefitinib
Toxicity
Diarrhea
Supplied as
Trade name
Tablet
NSCLC non-
squamous
advanced
Interstitial lung
disease
Skin rash &
reactions
Iressa
(AstraZeneca)
250 mg
Dose
limiting
Indications
Erlotinib
Toxicity
Supplied as
Trade name
Tablet
NSCLC non-
squamous
advanced
Diarrhea
Skin rash
Tarceva
(Roche)
150 mg25 mg
Interstitial lung disease
Pancreatic cancer
100 mg
Dose
limiting
Indications
Sorafenib
Toxicity
Supplied as
Trade name
Tablet
HCC Unresectable
Hand-foot skin reaction
Skin reactions
Nexavar
(Bayer)
200 mg
Met. RCC
Dose
limiting
Hypertension
Diarrhea
Indications
Sunitinib
Toxicity
Supplied as
Trade name
Tablet
Met. RCC
Bleeding events
Hematosuppression
Sutent
(Pfizer)
12.5 mg
GIST (2L)
Dose
limiting
Hypertension
Diarrhea
Bleeding
Mucositis
N&V Fatigue
25 mg 50 mg
Dose 50 mg once daily 4 weeks
out of 6weeks
Indications
Imatinib
Toxicity
Supplied as
Trade name
TabletCML
Myelosuppression
Glivec
(Novartis)
GIST +ve c-kit
(1L)
Dose
limiting
Taken with food +
large glass of water
100 mg
Administration
Monoclonal Antibodies
(MAbs)
Introduction
Specific to protein on cell
membrane
Naked
Drug
conjugate
Radio
conjugate
Immunotoxin
Oncotoxin
Selective
Minimal
toxicity
Infusion-related
cytokine release
syndrome (IRCRS)
Indications
Trastuzumab
Toxicity
Supplied as
Trade name
VialBreast Cancer
HER2+ve
Cardiomyopathy
Herceptin(Roche)
Dose limiting
Monitor ECG, ECHO
(EF%)
440 mg
Administration
IRCRS
Storage Refrigeration at 2–8oC,
Do not freeze
Dilute 250ml NS
Reconstituted
solution
Stable for 28
days upon
refrigeration
Hematosuppression
Powder
Reconstitute Sterile water +
Benzyl alcohol
Do not shake
Indications
Rituximab
Toxicity
Supplied as
Trade name
VialB-cell NHL
+ve CD20
Hypersensitivity
reactions
Mabthera (Roche)
Dose limiting
Premedication
100 mg
Administration
IRCRS
Storage Refrigeration at 2–8oC,
protect from light
Dilute NS, D5% (1-4 mg/mL)
Reconstituted
solution
Stable for 24 hours
upon refrigeration
Arrhythmias
500 mg
Initial rate 50mg/hr
  rate by 50mg/hr
upto 400mg/hr
Watch for TLS
Indications
Cetuximab
Toxicity
Supplied as
Trade name
VialMet. CRC wild
k-ras
Severe IRCRS
Erbitux (BMS/Merk)
Dose limiting
Premedication
100 mg
Administration
Storage Refrigeration at 2–8oC,
Do not freeze, shake
Dilute Do not dilute
Reconstituted
solution
Stable upto 12
hours at 2–8oC &
for 8hrs at room
temp.
Acneform rash
Monitor for
hypoMg
SCC H&N
Indications
Bevacizumab
Toxicity
Supplied as
Trade name
VialMet. CRC
Thromboembolism
Avastin (Roche)
Dose limiting
Hypertension
100 mg
Administration
Storage Refrigeration at 2–8oC, Do not
freeze, shake, protect from light
Dilute NS
Reconstituted
solution
Stable upto 8
hours upon
refrigerationGI perforation
NSCLC
Met. RCC
Wound dehiscence
Bleeding
Nephrotic S
IRCRS
Impair
wound
healing
400 mg
28 days after
surgery

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Targeted therapy