Hormonal, Non-cytotoxic, and Targeted Chemo Drugs
- Michigan State University College of Osteopathic Medicine
- Hormonal, Non-cytotoxic, and Targeted Chemo Drugs
Last Modified: 2013-11-16
- edema (Imatinib - peripheral, Dasatinib - lung/heart)
- liver fxn abnormalities
- QT interval prolongation
- GI irritation
- CYP3A4 substrate -> drug-drug interactions
- blocks human epidermal growth factor receptor (HER2/neu) - breast cancer
- reversible cardiotoxicity
- Abs bind to B cells for killing by C', phagocytosis, CTLs, NK cells
- kills all B cells - several months to normalize
- vax given post-treatment ineffective
- inhibits DNA methyltransferase -> apoptosis (takes several cycles/doses ~3-4 mos.) and reversal of epigenetic silencing
- at high does MOA becomes anti-pyrimidine
- selective estrogen receptor modulator - agonist in bone/uterus, antagonist in breast
- prodrug metabolized by P450 2D6
- prostate cancer
- over-stimulates pituitary gland to release excess LH/FSH which causes LH/FSH receptors on testes to downregulate -> no testosterone/estrogen release
- initial LH/FSH surge can cause "tumor flare" (bad if spinal/renal metastasis)
- prevent by using gonadotrophin-releasing hormone antagonist instead, or anti-androgens in addition
- breast pain
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