Topoisomerase inhibitors

1. Topoisomerase
Inhibitors
Dr. Mohammed Fathy, MD
Lecturer of Clinical Oncology
Zagazig University

2. Type
Introduction
Cycle specific
Phase specific
Activity
S
phase

3. Mechanism of action
Introduction (Cont.,)
Camptothecin
Inhibit topo I
Epipodophyllotoxin
Inhibit topo II
Inhibit
Topoisomerase
enzymes

4. Include
Introduction (Cont.,)
Irinotecan
Camptothecin
Epipodophyllotoxin
Etoposide
Topotecan
Teniposide

5. Indications
Irinotecan
NSCLC
Toxicity
Myelosuppression
Colorectal
cancer
Dose
Limiting
FOLFIRI
Prof use diarrhea
Flushing during administration
LFT abnormalities
XELIRI
FOLFOXIRI
Administration
If diarrhea, abdominal cramps, or diaphoresis
(mostly cholinergic in nature) develops during
infusion of : atropine, 0.25 to 1.0 mg IV & reduce
dose to 100 mg/m2
For 1st poorly formed stool preceding delayed
diarrhea : loperamide (Imodium), 4 mg PO, then
2 mg every 2 hours (4 mg PO every 4 hours at
night) until patient is free of diarrhea for 12
hours

6. Irinotecan (Cont.,)
Campto (Pfizer)Trade name
Supplied as
Vials 100 mg
Storage
At room temperature
Dilute D5% (or NS) (0.12–1.1 mg/mL)
Reconstituted solution
Stable for 24 hours at room
temperature. When diluted in D5%,
the drug is stable for 48 hours if
refrigerated & protected from light
solution
Protect from light

7. Indications
Etoposide
Lung cancer
Toxicity
Myelosuppression (neutropenia)Testicular
carcinoma
Dose
Limiting
BEP
Hypotension: if rapidly infused
Pain at injection site
Administration
Slow intravenous infusion over at least 30
minutes (to avoid hypotension).
Cisplatin
+Vepsid
Lymphoma
CHOPE

8. Etoposide (Cont.,)
VePesid (Bristol-Myers Squibb)Trade name
Supplied as
Vials 100 mg
Storage
Dilute D5% or NS (0.2-0.4 mg/mL)
Reconstituted solution
Stable for 24 hours at room
temperature & stable for 96
hours if refrigerated &
protected from light
Solution or
powder
below 25oC
Capsule 50 mg
Etopul (EUP)
Lastet (Nippon)