Targeted Therapy Flashcards
What are the 4 parts of pharmacokinetics?
Absorption, Distribution, Metabolism and Excretion
What is the first pass effect?
- When orally administered drugs dose is significantly reduced due to absorption by GI endothelium.
5 Cytotoxic Therapies
- Antimetabolites
- Alkylating Agents
- Topoisomerase Inhibitors
- Anti-Tumour Antibiotics
- Mitotic Inhibitors
Two Specific Types of Targeted Therapy
- Monoclonal Antibodies (-mabs)
- Tyrosine Kinase Inhibitor (-nibs)
Example Of Monoclonal Antibody
Cetuximab, blocks external domain of EGFR. Preventing downstream signaling cascades.
Example Of Tyrosine Kinase Inhibitor
Erlotinib, blocks internal domain, preventing downstream signaling cascades.
Trastuzumab
Monoclonal Antibody that binds to external domain of HER2. No natural ligand to bind to.
Vemurafenib
Tyrosine Kinase Inhibitor, inhibits mutant brafv600e, thus blocking downstream signaling cascades.
Hormone Therapy
The process of providing drugs that either reduce the amount of hormones or binding to receptors.
GnRH Agonist (goserelin)
Used to stop signaling pathway between hypothalamus and pituitary gland- this stopping production of estrogen- meaning cancer cells can’t bind. not ideal for younger women as it stops production of estrogen and presents early onset menopause.
Aromatase Inhibitor (anastrazole)
Limits estrogen production through aromatase in adrenal glands. Usually used in conjunction with goserelin.
Selective Estrogen Receptor Modulator (Tamoxifen)
Binds to estrogen receptor in cell to stop estrogen from binding.
Anti-Androgen (bicalutamide)
In prostate cancer, preferentially binds to androgen receptors to stop binding of testosterone.
Androgen Biosynthesis Inhibitor (abiraterone)
Chemical Castration, stops all production of testosterone everywhere. Usually not used, lowered sex drives, decrease in penis size etc.
