Antineoplastic Agents Flashcards
Cyclophosphomide
alkylating agent, bischloroethylamine
directly damages DNA
prodrug of Mechloroethylamine
Mechlorethamine
alkylating agent, bischloroethylamine
directly damages DNA
Super toxic old school chemo agent
Nitrosoureas (Class)
alkylating agent
little cross-resistance w/ other chemo agents
directly damages DNA
can cross the BBB
Procarbazine
alkylating agent
prodrug
little cross-resistance
leukemogenic
Cisplatin
Platinum Coordination Complex
forms x-linked w/DNA
nephrotoxicity/acoustic nerve dysfunction
Methotrexate
anti-tumor antimetabolite Inhibits DNA precursor synthesis folic acid analogue inhibits DHFR can be rescued w/ folinic acid multiple resistance mechanisms S-phase specific
6-Mercaptopurine
anti-tumor antimetabolite, purine antagonist
inhibits DNA synthesis
Converted to active form by HGPRT
downregulation of HGPRT is common resistance mechanisms
metabolized by xanthine oxidase
allopurinol inactivates xanthine oxidase, increases activity
S-phase specific
6-thioguanine
anti-tumor antimetabolite, purine antagonist
inhibits DNA synthesis
Converted to active form by HGPRT
downregulation of HGPRT is common resistance mechanisms
5-fluorouracil
antitumor antimetabolite, pyrimidine antagonist
metabolites (f-dUMP) inhibt thymidylate synthetase
F-U, F-DUMP
Capecitabine
antitumor antimetabolite, pyrimidine antagonist
oral prodrug of 5-FU
good for CC and refractory BC
Cytarabine
antitumor antimetabolite, pyrimidine antagonist
cytosine arabinoside (araC)
converted to araCMP and araCTP by deoxycytidine kinase
DCK loss tumor cell resistance
Daunorubicin
Antitumor antibiotic, anthracycline
DNA intercalation
Topo II inhibition
irreversible toxicity at high doses
Doxorubicin
Antitumor antibiotic, anthracycline
DNA intercalation
Topo II inhibition
irreversible toxicity at high doses
Bleomycin
antitumor antibiotic
DNA strand scission
active against broad spectrum
PULMONARY FIBROSIS/ANAPHYLACTIC REACTIONS
Vinblastine
Mitotic Spindle Poison, vinca alkyloid inhibits tubule poly acute nausea, vomiting and DD bone marrow suppression (blastin' bone marrow?) super effective against lymphomas resistance by tubulin gene mutations
Vincristine
Mitotic Spindle Poison, vinca alkyloid
inhibits tubule poly
milder side-effects than ‘blastine, significant neurotoxicity
resistance by tubulin gene mutations
Paclitaxel
mitotic spindle poison, plant alkyloid
ENHANCES TUBULINE POLY, BLOCKS DISAssembly (compare w/ ‘blastine & ‘cristine)
good for the ovarian cancers
Topotecan
topo inhibitor, camptothecans
binds to topo I, blocks relegation of single strand break
works during S-phase
Irinotecan
topo inhibitor, camptothecans
binds to topo I, blocks relegation of single strand break
works during S-phase
Etoposide
topo inhibitor
binds topo II, blocks relegation of single strand break
S-phase specific
Tamoxifen
selective estrogen response modulator (SERM)
competitive inhibition of estrogen binding
partial agonist of Es Rec
efficacy varies according to tissue-specific expression of ER
low toxicity
good for breast and endomet cancer
risk of thrombosis/uterine cancer
Raloxifen
selective estrogen response modulator (SERM)
competitive inhibition of estrogen binding
good for breast and endomet cancer in presence of osteoporosis
risk of thrombosis/uterine cancer?
Letrozole
aromatase inhibitor
blocks androgen conversion to estrogen
good for post-menopausal women cause compensatory ovarian production of estrogen
more effective than tamoxifen
no inc. risk of thrombosis/uterine cancer
Anastrozole
aromatase inhibitor
blocks androgen conversion to estrogen
good for post-menopausal women cause compensatory ovarian production of estrogen
more effective than tamoxifen
no inc. risk of thrombosis/uterine cancer
Exemestane
aromatase inhibitor
blocks androgen conversion to estrogen
good for post-menopausal women cause compensatory ovarian production of estrogen
more effective than tamoxifen
no inc. risk of thrombosis/uterine cancer
Leuprolide
Synthetic analogue of GnRH
pulsatile dose elevates levels of androgens
continuous high dose lowers androgen level
as effective as estrogen therapy or orchiectomy in treatment of prostate cancer
Flutamide
Androgen receptor antagonist
Used in conjunction with Leuprolide to block the pulse of androgens at start of therapy
Erlotinib
Small molecule inhibitor of EGFR kinase
lung cancer
head and neck cancer
Cetuximab
chimeric EGFR antibody
colon cancer
head and neck cancer
Trastuzumab
chimeric HER2 ab
breast cancer
Imatinib
Small molecule inhibitor of BCR/Abl
approved for CML
Brentuximab Vedotin
Chimeric Anti-CD30 ab conjugated to Vedotin
super toxic mit spin poison
