Breast Cancer Drugs Flashcards
MOA of pertuzumab
Monoclonal antibody that specifically targets the extracellular dimerisation domain (subdomain 2) of the HER2 protein and therefore blocks ligand dependent heterodimerisation of HER2 therefore inhibiting intracellular signaling. Also undergoes antibody dependent cell mediated cytotoxicity
Side effects of pertuzumab
Chills Anaemia Rash Arthralgia Febrile neutropenia
Place in therapy of pertuzumab
In combo with trastuzumab and docetaxel in metastatic breast cancer HER2+ve who have not received anti-HER2 therapy. Also as neo-adjuvant in combination with trastuzumab and chemo in patients with locally licensed advanced or early stage HER2 breast cancer
MOA of everolimus
Selective inhibitor of mTOR (mammalian target of rapamycin) mTOR is a key serine-threonine kinase which is known to be upregulated in breast cancers
Side effects of everolimus
Stomatitis Rash Fatigue Infections Diarrhoea Nausea decreased appetite
Place in therapy of everolimus
Treatment of ER/PR+, HER2 neu/-ve advanced breast cancer in combination with exemestane in postmenopausal women after progression following hormonal treatment
MOA of trastuzumab
Binds to sub domain IV, a juxta-membrane region of HER2s extracellular domain this prevents activation of HER2 and also undergoes antibody dependent cell mediated cytotoxicity
Side effects of trastuzumab
Cardiotoxicity Nausea and vomiting Diarrhoea Myalgia/ arthralgia Rash
Place in therapy for trastuzumab
Metastatic or early breast cancer with HER2+ve (neo-adjuvant or adjuvant therapy)
MOA of exemestane, anastrozole and letrozole
Aromatase inhibitors, prevent the conversion of androgens into oestrogen sun postmenopausal women and prevents it from peripheral tissues
Side effects of anastrozole, exemestane and letrozole
Decreased bone density
Sweats
Weight gain
Hot flushes
MOA of tamoxifen
Enters cell by passive diffusion and binds to oestrogen receptor thereby inhibiting ER dependent gene transcription
Side effects of tamoxifen
Hot flushes
Weight gain
Sweats
Increased risk of endometrial cancer
