Chemotherapy Flashcards
Alkylating Agents
- Nitrogen Mustards - cyclophosphamide ifosphamide, melphalan
- Nitrosoureas - Lomustine (CCNU), carmustine.
- Platinums - carbo, cis, oxaliplatin
- Busulfan
- Methylating agents - free radical formation - dacarbazine, procarbazine temozolomide.
Antimetabolites
- Folate analogues - interfere with folate metabolism - MTX
- Pyridamide analogues - inhibid DNA polymerase - ARA-C, Fluorouracil, HU
- Purine analogues - block purine synthesis and interconversion - 6-MP, 6-TG fludarabine, clofarabine, cladribine, nelarabine
Antibiotics
Includes dactinomycin, doxorubicin, daunorubicin, idarubicin, mitoxantrone, and bleomycin.
Mechanism: intercalation, DNA strand brakes via topoisomerase II, free radical formation
Plant Products
- Vinca alkaloids - Vincristine, vinblastine, venoralbine - block microtubule polymerization thus inhibiting mitosis
- Texans - paclitaxxel, docetaxel - microtubule inhibitor
Topoisomerase inhibitors
also plant based
- Camptothecins - Topoisomerase I Inhibitors - topotecan, irinotecan
* irinotecan is a prodrug, converted the liver and GI tract to be more potent, conjugated in the liver bu UGT1A1. Deficiency in this (Gilbert, Criigler Najjar), or inhibitors (valproate) increase toxicity. - Epipodophllotoxines - Topoisomerase II inhibitor - VP16
Asparaginase
Depletes asparagine. Tumour cells are sensitive to this and cannot up regulate asparagine synthase.
Decreases protein synthesis so antithrombin, protein c and s depletion all lead to potential thrombosis.
Corticosteroids
Receptor mediated lympholysis, apoptosis by binding to intracellular receptors.
Retinoids
APL and NBL have a role for this. These are differentiating agents. T
Arsenic
Leads to apoptosis, degradation of PML-RARa. Side effects include QT prolongation, convulsions, dermatitis, and hepatotoxicity.
Interferon a
This is antiangiogenic. It leads to activation of immune cells. Frequently with fevers, riggers. Poorly tolerated from a side effect standpoint.
Monoclonal antibodies
- Rituximab - anti CD20
- Gemtuzumab - anti CD33
- Alemtuzumab - anti CD52
- bevacizumab - anti VEGF
- Ipilumab - CTLA4 inhibition
- Brentuzimab - anti CD30
- Blinatumumab - BiTe CD19-CD3
- Nivolumab - PD-1
- Pembrolizumab - PDL1 inhibitor
Kinase inhibitors
- Imatinib/dasatinib - TKIs,
- Pazopanib - VEGFR
- Sunitinib - C-KIT
- Trametinib - MEK inhibitor
- Vorinostat - HDAC
- Bortezomib - Proteasome
- Crizotinib - ALK inhibitor
- Sirolimus/everolimus - mTOR inhibitors