Antineoplastic

Anastrozole
Bleomycin
Busulfan
Carmustine
Cisplatin
Cyclophosphamide
Doxorubicin
Etoposide
Fluorouracil
Gemtuzumab ozogamicin

Imatinib
Leuprolide
Meraptopurine
Methotrexate
Paclitaxel
Tamoxifen
Trastuzumab
Vincristine

Anastrozole

Estrogen antagonist
Nonsteroidal aromatase
inhibitor






Inhibits aromatase &

conversion to estrone
precursor to estradiol
Lowers estrogen levels
Halts progression of
estrogen-sensitive breast
cancers


Breast cancer in
postmenopausal women

N
HA
Hot flashes
Back pain

Bleomycin

Antitumor
DNA intercalating

Complexes iron-forming
oxygen free radicals that
cause single strand breaks
G2 phase specific





Lymphomas
SCC
Testicular carcinoma
Choriocarcinoma




Pneumonitis & pulmonary

fibrosis
Hyperpigmentation
Mucocutaneous toxicity
Hematology toxicity

Busulfan

Antineoplastic
Alkyl sulfonate bifunctional
alkylating agent
Cross-links DNA strands by
covalently bonding guanine
residues
Prevents DNA replication &
transcription


CML

Use w/ cyclophosphamide prior

allogenic hematopoietic
progenitor cell transplant for
CML





N, V
Myelosuppression
Pulmonary fibrosis

Carmustine

Antineoplastic
Nitrosurea bifunctional
akylating agent






Cross-links DNA strands by

covalently bonding guanine
residues
Prevents DNA replication &
transcription




Brain tumors
Myeloma
Lymphoma
Causes prolonged
myelosuppression




N, V
Hepatotoxicity
Anemia
Leucopenia
Thrombocytopenia
Pulmonary fibrosis

Cisplatin

Antineoplastic
Platinum compound





Forms reactive metabolites

that covalently bond DNA
bases & cross-link DNA
strands


Testicular, ovarian, cervical,

bladder, lung, head/neck
cancers

Less bone marrow suppression





Severe N, V
Ototoxicity & tinnitus
Hypocalcemia
Hypokalemia
Hypomagnesemia
Anemia

Cyclophosphamide

Antineoplastic
Nitrogen mustard bifunctional
akylating agent

Anorexia
N, V
Hemorrhagic cystitis & hematuria
Alopecia
Thrombocytopenia
Leukopenia
Anemia

Rifampin induces CYP & toxicity






Cross-links DNA strands by

covalently bonding guanine residues
Prevents DNA replication &
transcription






Hodgkins ds
Lymphomas, myeloma
Leukemia
Ovarian & breast tumors
RA
Converted to active metabolites by CYP
enzymes




Doxorubicin

Antitumor
DNA intercalating agent
Inserts b/w DNA bases

Cardiomyopathy dose-limiting
Anemia
Leukopenia
Thrombocytopenia
Diarrhea
V
Stomatitis
Alopecia




Complexes iron forming hydroxyl

free radicals that cause strand
breaks
Inhibits topoisomerase II

Colors urine red

Causes deformation & uncoupling

Causes strand breaks

S phase specific




Breast, ovarian, bladder tumors

Bronchogenic carcinoma
Lymphoma & leukemia






Etoposide

Antineoplastic
Podophyllotoxin,
topoisomerase inhibitor






Inhibits mammalian
topoisomerase II & prevents
resealing of nicked DNA
strands
G2 phase specific





Testicular, small cell lung

carcinoma
Lymphoma
Leukemia

N, V
Leukopenia
Thrombocytopenia
Alopecia

Fluorouracil

Antineoplastic
Pyrimidine antimetabolite





Converted to active
nucleotide form


Inhibits thymidylate
synthetase

S phase specific


Colon, breast, rectal, gastric,

pancreatic cancer
Topical for basal cell
carcinoma & actinic keratosis







Diarrhea
V
Stomatitis
Alopecia
Maculopapular rash
Anemia
Leukopenia
Thrombocytopenia

Gemtuzumab ozogamicin

Antineoplastic
Monoclonal Ab & cytotoxic
ABX calicheamicin

Gemtuzumab


Binds CD33 Ag on
hematopoietic cells & sequesters
lysosomes where calicheamicin
is released

Calicheamicin


Causes DNA dbl strand breaks

CD33 (+) AML

Severe myelosuppression &

hypersensitivity rxn






anaphylaxis

Severe pulmonary rxns

Chills
Fever
N
Dyspnea

Imatinib

Antineoplastic
Tyrosine kinase inhibitor





Inhibits oncoprotein bcr-abl

tyrosine kinase expressed by
Philadelphia chromosome
Inhibits leukemic cell
proliferation & induced
apoptosis









CML

Cause hematologic &

cytogenetic remission






Cough
Dyspnea
Pharyngitis
Pneumonia
Abdominal pain
V
Petechiae
Pruritis
Rash
Night sweats
Myalgia
Arthralgia
Thrombocytopenia
Neutropenia

Leuprolide

Antineoplastic, agent for precocious

puberty
GnRH analogue
Pulsatile admin FSH & LH release
Continuous admin down-regulates
GnRH receptors & FSH & LH

Central precocious puberty

Advanced prostate cancer
Endometriosis
Uterine fibroids

IM depot & implants for prostate cancer





Transient in testosterone w/ 1st dose

Use flutamide or other androgen

antagonist

Hot flashes

Mercaptopurine

Antineoplastic
Purine antimetabolite
Converted to nucleotide triphosphate
by phosphoribosyl transferase
Inhibits purine biosynthesis &
salvage pathways
S phase specific




Acute leukemia
CML
Lymphomas
Tumors that delete phosphoribosyltransferase acquire resistance

Cross-react w/ thioguanine

Myelosuppression
Hyperuricemia
Hepatotoxicity

Allopurinol inhibits degradation

Methotrexate

Antineoplastic
Folate reductase inhibitor





Inhibits dihydrofolate reductase

Prevents formation of active folate &
addition of single carbon units to
DNA base precursors
S phase specific







Choriocarcinoma, trophoblastic tumors

Leukemia
Breast, head, neck, lung cancers
Severe psoriasis
RA
Mycosis fungoides
Leucovorin used to minimized
hematologic toxicity & Tx OD






N, V
Stomatitis
Hepatotoxicity
Anemia
Leukopenia
Thrombocytopenia
Nephropathy

Paclitaxel

Antineoplastic
Mitotic inhibitor





Binds tubulin & prevents

depolymerization of
microtubules of mitotic
spindle
M phase specific











Advanced ovarian cancer w/

cisplatin
Non-small-cell lung cancer
Metastatic ovarian or breast
cancer

D
N, V
Alopecia
Anemia
Leukopenia
Thrombocytopenia
Peripheral neuropathy
Arthralgia
Myalgia

Tamoxifen

Antineoplastic
Estrogen receptor antagonist
& partial agonist
Competes w/ estrogen for
receptors in breast & other
tissues
Suppresses breast tumor
growth


Breast cancer & ductal

carcinoma following surgery
& radiation
Advanced breast cancer

CI during pregnancy &

lactation

N
Hot flashes
Menstrual irregularities




Trastuzumab

Antineoplastic
Monoclonal Ab





Binds human epidermal growth

factor-2 (HER2) receptor on
breast cancer cells
Prevents receptor stim. & cell
proliferation
Regression of breast cancer
metastases


Metastatic breast cancer w/

overexpression HER2

Combined w/ paclitaxel

blood levels







Abdominal pain
Anorexia
Diarrhea
V
Back pain
Chills
Fever
Allergic rxns
Doxorubicin risk of
cardiotoxicity

Vincristine

Antineoplastic
Vinca alkaloid, mitotic inhibitor





Binds tubulin & prevents

polymerization of tubulin
dimers forming microtubules of
mitotic spindle
M phase specific







Hodgkins ds
Lymphoma
Leukemia
Neuroblastoma
Rhabdomyosarcoma
Wilms tumor

N, V
Alopecia
Peripheral neuropathy