cancer chemotherapy drugs

how does cancer form

mutation in the cell, proliferation of those cells, dissemination/metastasis

metastasis

The spread of cancer cells to locations distant from their original site.

s phase fraction

Laboratory test performed to determine the number of cells that are dividing at any one time.

what happens during s phase

DNA replication and repair

the severity of a tumor is determined by

a high S phase fraction

cyclophosphamide drug class

alkylating agent

What is the MOA of cyclophosphamide?

transfers alkyl groups to DNA (causing damage and crosslinking)

in what phase of the cell cycle does cyclophosphamide work?

All phases of the cell cycle

doxorubicin drug class

non-specific antitumor antibiotic

doxorubicin MOA

Inhibit topoisomerase II, intercalates DNA, generate free radicals

in what phase of the cell cycle does doxorubicin work?

all phases of the cell cycle

antimetabolites work in what phase of the cell cycle

beginning of S phase

methotrexate drug class

antifolate agent

methotrexate MOA

inhibits dihydrofolate reductase

in what phase of the cell cycle does methotrexate work?

s phase

5-fluorouracil drug class

pyrimidine analogue

5-fluorouracil MOA

inhibits pyrimidine synthesis (DNA and RNA)

in what phase of the cell cycle does 5-fluorouracil work?

S phase

hydroxyurea drug class

ribonucleotide reductase inhibitor

hydroxyurea MOA

inhibits DNA (not RNA) synthesis by blocking ribonucleotide reductase (DNA->RNA process)

in what phase of the cell cycle does hydroxyurea work?

s phase

etoposide drug class

Topoisomerase II inhibitor

etoposide MOA

inhibits topoisomerase II

in what phase of the cell cycle does etoposide work?

s phase

bleomycin drug class

G2/M-Specific antitumor antibiotic

bleomycin MOA

causes oxidative damage to DNA

in what phase of the cell cycle does bleomycin work?

G2 mostly, but also M

vincristine drug class

vinca alkaloids

vincristine MOA

inhibits tubulin polymerization (growth) which prevents mitosis

in what phase of the cell cycle does vincristine work in?

M phase

paclitaxel drug class

Taxanes

paclitaxel MOA

inhibits microtubule disassembly, preventing mitosis

in what phase of the cell cycle does paclitaxel work?

M phase

what receptor status for breast cancer has the best prognosis

Estrogen receptor +, progesterone receptor +, and growth factor receptor -

tamoxifen drug class

Selective Estrogen Receptor Modulator (SERM)

tamoxifen MOA

binds estrogen-binding site on hormone binding receptor which prevents estrogen stimulation DNA synthesis

Tamoxifen binding

antagonist in breast tissue, agonist in bone and endometrium

what must be true for tamoxifen to treat breast cancer

the cancer must be ER positive

leuprolide MOA

GnRH analogue that overstimulates and desensitizes the anterior pituitary

what is the pituitary response to GnRH

stimulates LH and FSH; increases folicular development

flutamide drug class

Antiandrogen

flutamide MOA

blocks androgen receptor; prevents effects of testosterone

receptor tyrosine kinases

molecules activated by ligands and phosphates to activate a response (cell proliferation)

erlotinib drug class

EGFR RTK inhibitors (TKIs)

erlotinib MOA

inhibits the tyrosine kinase domain of the EGFR RTK and prevents phosphorylation by ATP (activation)

immune checkpoints

checkpoint proteins on cells and T cells that prevent immune response from being so strong it destroys healthy cells

pembrolizumab drug class

PD-1 inhibitor (checkpoint inhibitor) monoclonal antibody

pembrolizumab MOA

binds PD-1 (Programmed Death-1) receptors on T-cells and inhibits the negative immune regulation caused by PD-1 receptor activation by PD-L1.

CAR stands for ___ and does what?

chimeric antigen receptor; allows T cells to attach to cancer cell proteins

Axicabtagene Ciloleucel drug class

CAR T-cell Therapy

Axicabtagene ciloleucel MOA

block surface proteins on blood cancer cells

Axicabtagene Ciloleucel is used to treat what type of cancer

B-cell non-Hodgkin lymphoma (blood cancer)

blinatumomab drug class

"bring closerers" monoclonal antibody

blinatumomab MOA

binds to CD19 on leukemia cells and CD3 on T cells to bring the cancer cell and T cell close together

what do cancer treatment vaccines do?

help the immune system recognize tumor associated antigens

Talimogene laherparepvec drug class

oncolytic virus

Talimogene laherparepvec MOA

HSV-1 based virus that infects cancer and normal cells

-normal cells kill virus

Talimogene laherparepvec is used to treat

melanoma that returns after surgery

BCG MOA

causes an immune response against cancer cells in the bladder

BCG is used to treat

bladder cancer