Anti cancer Flashcards
agents that donate an alkyl group - DNA crosslinks @ position N-7 guanine
alkylating agents
is activated by hepatic cytochrome P450
Cyclophosphamide
treats hematologic and solid malignancies (leukemia’s, lymphomas, breast cancer, ovarian cancer)
Cyclophosphamide
ADR: BM depression, hemorrhagic cystitis, increases risk of bladder cancer, hyponatremia due to SIADH, infertility and premature menopause
Cyclophosphamide
MOA: increase DNA repair, decrease drug permeability, production of trapping agents (thiols)
Alkylating agents
causes cystitis
acrolein
binds and inactivates acrolein and hydration
MESNA
active form of Cyclophosphamide
phosphoramide mustard
nitrosoureas
temozolomide - most used
carmustine
lomustine
streptozotocin
cross BBB and treat brain tumors and cause ADR of neurotoxicity
nitrosoureas
treats insulinoma and induces type 1 diabetes
streptozotocin
MOA: same as Cyclophosphamide, but also forms hydrogen peroxide, which generates free radicals that cause DNA damage
procarbazine
Treats Hodgkins lymphoma
ADR: disulfiram like reaction after drinking alcohol & secondary cancers (acute leukemia - years after)
procarbazine
analogs that bind DNA and form intra strand and inter strand cross links
Platinum analogs
treats solid malignancies - specifically testicular cancer;
Is marrow sparing;
same MOA as Cyclophosphamide
cisplatin
ADR: ototoxicity, neurotoxicity and nephrotoxicity
cisplatin
what drug can prevent nephrotoxicity
amifostine
similar to cisplatin but ADR less renal toxicity, but increase BM depression
carboplatin
inhibit microtubule production and mitotic spindle assembly; acts on M phase
vincristine
vinblastine
resistance: increase efflux of drug from tumor cells (p glycoprotein)
plant alkaloids
Treats: Hodgkins, breast cancer, testicular cancer
vinblastine
toxicity: BM suppression, anorexia, nausea, vomiting, diarrhea, alopecia
vinblastine
treats: childhood leukemias, childhood wilms tumor, neuroblastoma, Hodgkins
vincristine
toxicity: peripheral neuritis with paresthesia, SIADH, muscle weakness
muscle sparing effect!
vincristine
enhance microtubule production and prevent their degradation - improper mitotic spindle function
paclitaxel
docetaxel
ADR: neutropenia, peripheral neuropathy, hypersensitivity reactions, alopecia
paclitaxel
docetaxel
topoisomerase 2 inhibitors
active in late S and early G2 phase
etoposide
teniposide
treats testicular and prostate cancer and small cell lung cancer
etoposide
teniposide
topoisomerase 1 inhibitors
topotecan
irinotecan
treats ovarian cancer and small cell lung cancer
topotecan
irinotecan
pyrimidine analog and is only active against hematologic malignancies (AML, Non-Hodgkins)
cytarabine
acts in S phase
converted to 5’ (ara-CMP) then converted to dCMP kinase converted to ara CTP (active)
cytarabine