13 - Cancer Chemotherapy Flashcards
Drugs acting on S phase
CHEM 665
- cytarabine
- hydroxyurea
- etoposide
- methotrexate
- 6 - thioguanine
- 6 - mercaptopurine
- 5-FU
Drug acting on G2 phase
Bleomycin
Drugs acting on M phase
- Vincristine
- Vinblastine
- Paclitaxel (Taxane)
Drugs that for DNA cross-links
CCCB
- Cyclophosphamide
- Cisplatin
- Carmustin
- Busulfan
Drugs that form hydrogen peroxide which generate free radicals
- Procarbazine
- Dacarbazine
Rescue agent for Cyclophosphamide
MESNA
Cystitis can be prevented by adequate hydration
Rescue agent for Cisplatin
Amifostine
Decrease nephrotoxicity by administering mannitol with forced hydration
Has a wider spectrum of coverage in solid tumors and has less renal and GI side effects
Carboplatin
- widely used in transplant regimen
Part of FOLFOX and FOLFIRI regimen (solid tumors) that are resistant to Cisplatin and Carboplatin
Oxaliplatin
Ototoxic medications
- aspirin
- ibuprofen
- cisplatin
- kanamycin (most ototoxic aminoglycoside)
- Gentamycin
- Lasix
Highest carcinogenic potential among alkylating agents
Procarbazine
Alkylating agent used for CML
Busulfan
Drugs causing pulmonary fibrosis
BBBAN Me
- Busulfan
- Bleomycin
- Bromocriptine
- Amiodarone
- Nitrofurantoin
- Methotrexate
Special alkylating agent that is for brain tumors
Carmustine
- highly lipophilic
SE: CNS toxicity
Alkylating agents
- cyclophosphamide
- cisplatin
- procarbazine
- dacarbazine
- carmustine
- busulfan
Antimetabolites
- methotrexate
- 6 - mercaptopurine
- 5 - fluorouracil
- cytarabine
- gemcitabine
inhibits dihydrofolate reductase
Methotrexate
rescue therapy for Methotrexate
Leucovorin (Folinic acid)
Inhibits de novo purine nucleotide synthesis
6 - mercaptopurine
6-MP metabolism is inhibited by
- Allopurinol
- Febuxostat
MOA of Pemetrexed
inhibits:
- thymidylate synthase
- dihydrofolate reductase
- purine nucleotide synthesis
Inhibits thymidylate synthase causing thymineless death of cells
5-Fluorouracil
Prodrug of 5-FU
Tegafur
Inhibits:
- DNA repair and synthesis
- ribonucleotide reductase with reduced formation of dNTPs
Cytarabine
- most specific for the S phase in cell cycle
Gemcitabine
- used for pancreatic CA
- can be used for solid tumors
*-BINE - inhibits ribonucleotide reductase
Drugs that inhibit ribonucleotide reductase
- Fludarabine
- Cladribine
- Cytarabine
- Gemcitabine
Drugs that have SE of hand-foot syndrome
- “Palmar-plantar erythrodysesthesia”
- redness, swelling and pain sometimes with blistering
- Capecitabine
- Pemetrexed
Natural Product Anti-cancer drugs
- Vincristine
- Vinblastine
- Etoposide
- Topotecan
- Paclitaxel
Prevents microtubule assembly
- Vincristine (crispy nerves: peripheral neuropathy)
- Vinblastine (BM suppression)
Prevents microtubule disassembly
Taxane
- Paclitaxel
- Docetaxel
- Cabazitaxel
- Inhibits Topoisomerase II (DNA Gyrase)
- inhibits mitochondrial electron transport
Etoposide
E2poside
Inhibits Topoisomerase I
Topotecan
Camptothecin that is used for advanced ovarian CA (2nd line) and small cell lung CA
Topotecan
Camptothecin that is used for metastatic colon CA
Irinotecan
- Intercalates between base pairs
- inhibits topoisomerase II
- generates free radicals
Doxorubicin
SE:
- ruby red: red urine
- Cardiomyopathy
Rescue therapy for Doxorubicin
Dexrazoxane
Anthracycline
- Doxorubicin
- Daunorubicin
- Idarubicin
- Epirubicine
- Mitoxantrone
Anthracycline used for ALL
Daunorubicin
Anthracycline used for AML
Idarubicine
Antitumor drug that generates free radicals causing DNA strand breaks
- also intercalates with DNA
Bleomycin
- Binds to double-stranded DNA
- inhibits DNA-dependent RNA synthesis
Actinomycin
other name: dactinomycin
- oldest antitumor antibiotic
Inhibits tyrosine kinase activity of:
- BCR-ABL oncogene in CML
- cKit tyrosine kinase in GIST
Imatinib
Gleevec
- imatinib mesylate
- GIST
Tyrosine kinase inhibitor that is also used for idiopathic pulmonary fibrosis
Nintedanib
Acts on breast CA cells that overexpress Her-2/neu
Trastuzumab / Pertuzumab / Lapatinib
- monoclonal antibody
Use: metastatic breast CA
SE of Trastuzumab
Cardiomyopathy
like doxorubicin
Monoclonal antibody that inhibits binding of VEGF to VEGFR.
- inhibits tumor vascular permeability
- enhances tumor blood flow and drug delivery
Bevacizumab
- inhibits angiogenesis
Drug that acts a multiple kinase inhibitor against VEGFR1 to 3 kinases and is used for thyroid cancer
Levatinib
Binds to surface protein in NHL cells inducing complement-mediated lysis, direct toxicity and induction of apoptosis
Rituximab
Binds to EGFR inhibiting downstream EGFR signaling, enhances response to chemo and radiotherapy
Cetuximab
Bevacizumab
- inhibits binding of VEGF
Inhibits EGFR tyrosine kinase
Erlotinib
Cetuximab
- binds to EGFR
MOA is endogenous glycoproteins with antineoplastic, immunosuppressive and antiviral actions
Interferon-alpha
hydrolyzes circulating L-asparaginase leading to rapid inhibition of protein synthesis
Asparaginase
- used for ALL
Vitamin derivative that allows DNA transcription and differentiation of immature leukemic promyelocytes into mature granulocytes
All-trans retinoic acid
Antifolate analog
Pralatrexate
Inhibits polymerase alpha and beta (DNA)
- Fludarabine
- Cladribine
DNA hypomethylating agent used for myelodysplastic syndrome
Decitabine
Alkylating agent used for brain tumors (astrocytoma and glioblastoma multiforme)
Temozolomide
Mitotic inhibitor (microtubule) used for metastatic breast CA
Eribulin
CD30 used for Hodgkin Lymphoma
Brentuximab
mTOR inhibitor used as an immunosuppressant in organ transplantation
Everolimus
Sirolimus
anti-CD20 used for CLL and Follicular lymphoma
Obinutuzumab
IgG4 isotype antibody that blocks protective mechanism of CA
targets PD-1
Pembrolizumab
EGFR-TK inhibitor for advanced non-small cell lung CA
Osimertinib
First therapeutic proteasome inhibitor used for multiple myeloma and mantle cell lymphoma
Bortezomib
