Introduction to FDO and How It works Applications _ Richard at FIDO Alliance.pdf
09 antineoplastic drugs-ii
1. PSALM OF THE DAY
Psalm 150 verse 6
Let everything that hath breath praise
the LORD. Praise ye the LORD.
2. And JESUS answered him, The first of all the
commandments is, HEAR O ISRAEL; THE
LORD OUR GOD IS ONE LORD:
AND THOU SHALT LOVE THE LORD THY
GOD WITH ALL THY HEART, AND WITH ALL
THY SOUL, AND WITH ALL THY MIND, AND
WITH ALL THY STRENGTH: this is the first
commandment.
And the second is like namely, THOU SHALT
LOVE THY NEIGHBOUR AS THYSELF. There
is none other commandment greater than these.
Mark 12:29-31 c.f. Matthew 22:37-40
6. Vinca Alkaloids
Mechanism of Action
Cell cycle specific
Binds to the microtubular protein tubulin in a
dimeric form
The drug-tubulin complex adds to the forming
end of the microtubules to terminate assembly
Depolymerization of the microtubules occurs
Resulting in mitotic arrest at metaphase,
dissolution of the mitotic spindle, and
interference with chromosome segregation
9. NATURAL PRODUCTS
Topotecan, Irinotecan)
Are Camptothecins
Active metabolites formed in vivo
Inhibit topoisomerase I
Taxol (Paclitaxel) and Docetaxel
Are Taxanes
Inhibit disassembly of microtubules
Given i.v. for ovarian and breast cancer
10. ENDOCRINE THERAPY
Many endocrine cancers retain hormone
receptors e.g. ER in breast
Androgens oppose the effects of
estrogens, and vice versa
Have different toxicities from the other
antineoplastic drugs
11. HORMONES
(a) Glucocorticoids e.g. Prednisone
Use: Lymphoma
(b) Androgens e.g. Testosterone
S/E: Masculinisation
Use: Breast cancer
(c) Estrogens e.g. Oestradiol
S/E: Gynaecomastia
Use: Testicular cancer, Prostate cancer
12. HORMONES
Progestins e.g. Megestrol
S/E : Fluid retention
Main use: Endometrial cancer
GnRH analogs: Goserelin, Leuprolide
Stimulate ,then inhibit release of FSH and
LH
Use: Prostate cancer
14. ENDOCRINE THERAPY
Antiandrogens e.g. Flutamide, Nilutamide
Competitive antagonist at androgen receptor
Use: Prostate cancer
S/E: Fluid retention, gynaecomastia
Finasteride (Proscar®)
5- -Reductase enzyme inhibitor
Use: Prostate cancer
15. MISCELLANEOUS
Immunotherapy: lL-2, InterferonMonoclonal antibodies: Trastuzumab
(Herceptin®) for breast cancer
L-Asparaginase : for acute lymphoblastic
leukemia, S/E hepatotxicity
Hydroxyurea : inhibits
deoxyribonucleotides, S/E:
myelosuppression
16. Avastin (Bevacizumab)
A recombinant humanized antibody to Vascular
Endothelial Growth Factor (VEGF)
Avastin binds to and inhibit VEGF, a protein that
plays a critical role in tumor angiogenesis
At present, Genentech is pursuing broad latestage clinical trials examining its potential use in
multiple tumor types.
17. MISCELLANEOUS
Mitoxanthrone: topoisomerase II inhibitor
Procarbazine: forms active metabolites
which cause DNA strand breaks, D/I with
alcohol
Radioactive isotopes e.g. 131-Iodine, 60Cobalt
18. Cancer Vaccines in Development:
Cervarix
In Phase III studies, Cervarix, one of the new
vaccines highlighted by GSK, demonstrated 100%
effectiveness in preventing persistent infection by the
two human papillomaviruses (HPV) with the highest
risk for causing cervical cancer: HPV16 and HPV18.
Cervarix has the potential to prevent more than 70%
of cervical cancers. Phase III trials enrolling 25,000
women has began. Filing is expected in 2008.
19. JOHN 14: 6
JESUS saith unto him,
I am the way, the truth, and the life:
no man cometh unto the Father,
but by me.
