Cancer Pharmacology (Kruse) Flashcards
How is mercaptopurine activated
Inactive in parent form
Metabolized by HGPRT
What antibodies did we cover in lectures
Bevacizumab & Ziv-aflibercept
What antimetabolite purine analog did we discuss in class
Mercaptopurine (6-MP)
What antitumor antibiotic causes single and double stranded DNA breaks
Bleomycin
What antitumor antibiotic inhibits topoisomerase 2 and intercalates DNA
Doxorubicin
What are the common M Phase cell cycle inhibitors we discuses in class and what are their drug classes
Natural Antineoplastic Agents
Bleomycin - Antitumor antibiotic
Paclitaxel & Docetaxel - Taxane
Vinblastine & Vincristine - Vinca Alkaloids
What are the side effects of Bleomycin
Pulmonary toxicities
What are the side effects of Vinblastine
Alopecia
Bone marrow supression
Myelosuppression to a great extent than vincristine
What are the side effects of Vincristine
Alopecia
Bone marrow supression
Cumulative neurologic toxicities to a greater extent than vinblastine
What drug binds to beta tubulin and inhibits microtubule assembly (depolarization)
Vinblastine & Vincristine
What drug category is carmustine
Nitrosourea - Alkylating agent
What drug class are Vinblastine & Vincristine
Vinca Alkaloids
What drug class in Ziv-aflibercept
Tyrosine Kinase growth factor receptor inhibitor
What drug class is Doxorubicin
Anthracycline
What drug inhibits the BCR-ABL fusion protein & what is it’s MOA
Imatnib
Inhibits the ABL tyrosine kinase
What drug is a calcium channel blocker that inhibits P-glycoprotein transporters
Verapamil
What drug is used as an implantable wafer in the brain to treat malignant glioma as an adjunct to surgery and radiation
Carmustine
What drug reduces the toxic side effects of methotrexate
Leucovorin
What drugs are associated withe the p-glycoprotein resistance mechanism & what are their MOA
Vinca alkaloids
Etoposide & anthracyclines - Inhibit topoisomerase 2
Paclitaxel
Dactinomycin - intercalates DNA
What drugs bind to beta tubulin and stabilize microtubule formation
Paclitaxel, Docetaxel & Cabazitaxel
What enzyme metabolizes mercaptopurine to the inactive metabolite
Xanthine oxidase (first pass)
What is the adverse side effect of Doxorubicin
Cardiovascular toxicity from production of free radicals
What is the drug class of Paclitxael, Docetaxel & Cabazitaxel
Taxanes
What is the MOA of Bevacizumab
Monoclonal antibody that binds to VEGF-A preventing ligands from binding to it
What is the MOA of ziv-aflibercept
Binds VEGF-A, VEGF-B and prevents them from binding to VEGF receptor
Also binds PIGF
What is the side effect of Docetaxel
Hypersensitivity, neutropenia and hair loss
What is the side effect of Paclitaxel
Hypersensitivity reactions in hands and toes
Change in taste
What taxane avoids the mechanism of resistance of P-glycoprotein
Cabazitaxel
Which taxane has a greater cellular uptake and is retained intracellularly longer, leading to smaller dose and less side effects
Docetaxel
