-DNA modifier

-Crosslinked DNA

-Alkylating agent

-Hemorrhagic cystitis (bladder toxicity)

-Take in AM

-Can give MESNA

-Alkylating agent

-Hemorrhagic cystitis (bladder toxicity)

-Give MESNA

-DNA crosslinks

-Myelosuppression, pulmonary fibrosis

-DNA crosslinks

-Myelosuppression

-Lipophilic (reaches vomiting center, highly emetogenic)

-IV

-Alkylating agent

-Myelosuppression

-Lipophilic (reaches vomiting center, highly emetogenic)

-Oral

-Methylates guanine

-Very painful (IV)

-Turns pink in UV light

-Inhibits DNA repair

-Oral

-Reacts with A + G, intra and inter crosslinks

-Nephrotoxicity

-Hydrate lots!

-Avoid aminoglycosides

-Reacts with A + G to form intra and inter crosslinks

-Myelosuppression

Anthracycline antibiotics

1. Interfere with TOP II

2. Alter cell membrane transport

3. Quinone free radicals

-Cardiotoxicity

-LVEF before starting treatment

-IV

Antibiotic

-Fe++ chelating glycopeptide

-Superoxide radicals

-Pulmonary fibrosis

-Hyperpigmentation

-TOP I inhibitor

-Myelosuppression

-Severe diarrhea

-Cholinergic syndrome (pretreat with atropine)

-TOP I inhibitor

-Myelosuppression

-TOP II inhibitor (blocks S-G2)

-Myelosuppression

Antimetabolite

-Inhibit DHFR (DNA, RNA, protein synthesis)

-Becomes polyglutamated

-Myelosuppression

-Reversed with leucovorin

Antimetabolite

-Inhibits DHFR and GARFT

-Myelosuppression

-Must give Vit B12 and Folic acid

Antimetabolite

1. Inhibit purine synthesis

2. TIMP converted to TGMP, incorporated into RNA + DNA

-Leukopenia and thrombocytopenia

-Azathioprine is a prodrug of this

-Lower dose if given with allopurinol

Antimetabolite

-Converted to 5-dUMP, inhibits thymidylate synthase

-Ulceration of oral and GI mucosa

-Given with leukovorin to increase efficacy

Antimetabolite

-Converted to 5-FU

-Ulceration of oral and GI mucosa

Antimetabolite

-Pyrimidine antagonist

-Incorporate into DNA

-Myelosuppression

Antimetabolite

-Tri-PO4 competes with cytosine

-Incoporates into DNA

-Myelosuppression

-Fluorides help it stay inside cell

Microtubule inhibitor

-Inhibits polymerization (extension)

-Peripheral neuropathy

-Hyperuricemia (treat with allopurinol)

Microtubule inhibitor

-Inhibits polymerization (extension)

-Myelosuppression

-Hyperuricemia (treat with allopurinol)

Taxane

-Promote polymerization

-Inhibit depolymerization

-Myelosuppression, neuropathy

-Hypersensitivity

Taxane

-Promotes polymerization

-inhibits depolymerization

-Myelosuppression, neuropathy

SERM

-Anti-E breast, E-agonist bone and uterus

-Thromboembolism, endometrial cancer

-Activated by CYP2D6

-Must give with GnRH analog in premenopausal women

SERD

-ER antagonist, promotes R degredation

Aromatase inhibitor

-Prevent androgen -> estrogen conversion

-Osteoporosis

CYP17 inhibitor

-Prevent synthesis of androgens

-Adrenocortical insufficiency (can give prednisone)

GnRH antagonist

1. R desensitization

2. Inhibit FSH and LH

3. Decreased androgen and estrogen

-Synthetic nonapeptides (9 AA's)

Flutamide, Nilutamide, Biclutamide, Enzalutamide

Synthetic antiandrogens

-Increased LH and T

-Give leuprolide or goserelin

Corticosteroid

-Decreased lymphoid mass

-Cushing syndrome

mAb

-Against B-cell CD20

mAb

-Against B-cell CD20

-Give something to protect thyroid

mAb

-Against HER2

-CHF

-Monitor heart function

-Avoid anthracyclines

mAb

-Against EGFR

-Acne rash

-Test for KRAS mutation before

mAb

-Against VEGF (antiangiogenesis)

-Wound healing complication

-Stop 28 days before surgery

-Deamination (Asn to Asp)

-Hepatotoxicity, clotting issues

-Inhibit tumor protein synthesis

-Decrease cell proliferation

-Activate MQs

-Increased cytotoxicity

EGFR kinase domain inhibitor

-Acne rash

-CYP3A4 and 1A2 substrate, caution with smoker

1. Inhibits receptors

2. Inhibits downstream enzyme

-Targets Rs and Raf

Protein synthesis inhibitor

-Binds "A" site of 80s ribosome

1. 26S proteasome inhibitor

2. Sensitizes cancer cells to chemo

-Boron