Cancer Agents Flashcards
MOA of olaparib
PARP inhibitor
Inhibition of poly (ADP-ribose) polymerase → ↓ repair of single-strand DNA breaks
Complications associated with olaparib
- Myelosuppression
- Fluid retention and edema
- GI toxicity (e.g., diarrhea)
Tamoxifen MOA and indications
ER/PR positive, pre-menopausal
Competitive estrogen antagonist of breast tissue
Agonist of estrogen receptors for bone tissue, endometrium and myometrium
Complications associated with tamoxifen
- Hot flushes
- Increased risk of endometrial Ca
- Increased VTE
- Increased risk of uterine sarcoma
Aromatase inhibitors MOA and indications
Letrozole, anastrozole
ER/PR positive, postmenopausal
Inhibits aromatase –> decreases conversion of androstendione to estrone, decrease conversion of testosterone to estrodiol –> decrease tumour growth
Aromatase inhibitors side effects
Hot flashes
Night sweats
Vaginal dryness
Increase risk of OP
Myalgias/arthralgias
MOA of raloxifene
Competitive estrogen antagonist for breast, endometrium and myometrium
Agonist of estrogen receptor in bone tissue inhibition of osteoclasts
Side effects of raloxifene
Increased risk of VTE and cataracts
Hot flushes
Decrease risk of endometrial Ca and uterine sarcoma
Trastuzumab MOA
For all HER2 positive tumours
Humanised monoclonal antibody against HER2 tyrosine kinase receptor –> decrease HER2 initiated cellular signalling and increase antibody-dependent cytotoxicity –> decrease tumour growth
Trastuzumab side effects
- Cardiotoxicity, dilated cardiomyopathy
- GI symptoms
Bevacizumab MOA
Monoclonal antibody directed against vascular endothelial growth factor. In lung cancer, can be added to platinum-based chemotherapy in patients not treated with immunotherapy
Bevacizumab side effects
Increased risk of thrombosis, stroke, myocardial infarction, and hemoptysis
MTX MOA
Antifolate agent
Inhibition of dihydrofolate reductase –> decreases formation of pyrimidine nucleotides and purine nucleotides –> decrease DNA synthesis
Inhibits AICAR transformylase
MTX adverse effects
Myelosuppression, anaemia
Hepatotoxicity
Pulmonary fibrosis, pneumonitis
Mucositis
Megaloblastic anemia
Teratogenic
Neurotoxicity
Pemetrexid MOA
Antifolate agent
Pemetrexid adverse effects
Alopecia
Erythematous pruritic rash
Desquamation
Anaemia
Pharyngitis
GI symptoms
Cytarabine MOA
Pyrimidine antagonists
Cytarabine adverse effects
Myelosuppression
Megaloblastic anaemia
Hepatotoxicity
Pancreatitis
Respiratory distress
Neurotoxicity
5-FU and Capecitabine MOA
Pyrimidine antagonists
Capecitabine - prodrug for 5-FU
5-FU and Capecitabine adverse effects
Myelosuppression
Hand foot syndrome
Cardiotoxicity
GI symptoms
Hepatotoxicity
Hyperammonemic encephalopathy
Gemcitabine MOA
Pyrimidine antagonist
Gemcitabine adverse effects
Myelosuppression
Capillary leak syndrome
HUS
Hepatotoxicity
6-MP/Azathioprine MOA
Purine antagonists
Azathioprine is prodrug for 6-MP
6-MP/azathioprine adverse effects
Myelosuppression
GI symptoms
Hepatotoxicity
Secondary malignancy
Increased SE with allopurinol and/or febuxostat
Fludarabine and cladribine MOA
Purine antagonist
Cladribine –> Hairy cell leukaemia
Fludarabien –> CLL, low grade lymphomas