ANTI-CANCER

Anastrozole
- Inhibitor of steroid synthesis ->inhibits conversion of androstenedione to estrone by blocking
aromatase
- Used to treat estrogen dependent breast cancer

Aminoglutethimide
- similar to Anastrozole but it inhibits conversion of cholesterol pregnenolone
- Used for estrogen dependent breast cancer

Bleomycin
- G2 phase inhibitor is part of ABVD regimen (Adriamycin, Bleomycin, Vinblstine & decarbazine)
for Hodgkin disease
- Mixture of glycoproteins that results in production of free radicals after binding to DNA
o Creates single and double stranded breaks in DNA
- Uses: testicular carcinoma and squamous cell carcinoma
- Side effect: pulmonary fibrosis

Carmustine(BCNU), Lomustine (CCNU)
- Alkylating agents cause DNA cross linking and strand breaks
- Highly lipophilic nitrosoureas that easily cross BBB; used to treat brain tumors

Cisplatin
- Alkylating agent; contains platinum
- Causes nephrotoxicity and acoustic nerve damage
- Used to treat testicular and lung carcinomas

Carboplatin
- Similar to Cisplatin; less nephrotoxicity & neurotoxicity but greater myelosuppression

Cyclophosphamide
- Alkylating agent used to treat non-Hodgkin lymphoma and breast/ovarian carcinomas
- Side effect: hemorrhagic cystitis ->decreased by vigorous hydration and use of MENSA

Doxorubicin (Adriamycin)
- Intercalates in DNA to dec. replication and transcription
- Part of AVBD regimen; used to treat myelomas, sarcomas & lymphomas
- Side effects: cardiotoxicity & dilated cardiomyopathy(presents as biventricular CHF->dyspnea,
orthopnea & peripheral edema)

Daunorubicin
- Similar to Doxrubicin but used primarily to treat AML

Etoposide
- G2 phase inhibition->causes double stranded DNA breaks and degradation
- Inhibits topoisomerase II
- Uses: small cell carcinoma of lung/prostate and testicular cancers


Fluorouracil (5-FU)
- S-phase antimetabolite causes myelosuppression
- Inhibits thymidylate synthase causing thymineless death
- Uses: colon cancer and superficial tumors (eg. Basal cell carcinoma)

Flutamide
- Androgen receptor antagonist
- Uses: carcinoma of prostate, antagonize residual androgens after orchiectomy
- Side effects: gynecomastia & libido changes

Interferon Alpha
- Cytokine used to treat hairy cell leukemia, CML, malignant melanoma & Kaposi sarcoma
- Normally produced by virally infected cells to prevent infection of adjacent cells

Leuprolide, Goserelin, Nafarelin
- GnRH agonists used to treat metastatic carcinoma of prostate
- Also used to treate: endometriosis, BPH, & precocious puberty
- If administered in a pulsatile manner, they stimulate release of FSH & LH
o Can be used to manage infertility

Mercaptopurine(6-MP), Thioguanine (6-TG)
- Purine metabolites used to treat leukemias and lymphomas
- Needs activation by hypoxanthine-guanine phosphoribosyltransferase 9HGPRT) and inhibits
many enzymes involved in purine metabolism

Methotrexate
- S phase inhibitor of dihydrofolate reductase->dec DNA and protein synthesis; folic acid analog
- Uses: leukemias, non-hOdgkin lylmphoma, RA & therapeutic abortions
- Side effects: myelosuppression -> treat it with Leucovorin

Paclitaxel
- M phase agent(derived from yew tree) which prevents mitotic spindle from breaking down(ie.
Keeps the microtubule stable)-> inhibits completion of anaphase
- Uses: ovarian/breast carcinomas

Prednisone
- Glucocorticoid; triggers apoptosis & can lead to hypercortisolism w/ Cushing-like symptoms
- Drug must be tapered gradually to prevent life threatening adrenal insufficiency
- Uses: leukemias, lymphomas, RA & asthma

Rituximab
- Monoclonal antibody which binds CD20 antigen on B cells
- Adverse rxns: fever, chills, headache, nausea
- Uses: low grade non-Hodgkin lymphoma

Tamoxifen
- Estrogen receptor partial agonist -> may inc. risk of endometrial carcinoma
- Primary agent used to treat estrogen receptor positive breast cancer
Trastuzumab
- Monoclonal antibody; binds to receptor tyrosine kinase Erb-B2H(HER-2)->overexpressed on
some breast cancers
- Used to treat metastatic breast cancer

Vincristine (Oncovin)
- M phase inhibitor which blocks microtubule polymerization and spindle formation
- Vinca alkaloid used as part of MOPP for lymphomas, Wilms tumor and choriocarcinomas
o MOPP Mechlorethamine, Oncovine, Procarbazine & Prednisone

Vinblastine
- Similar MOA as Vincristine; part of AVBD regimen