Leuprolide, Goserelin. Inhibits synthesis of sex steroids in both men and women. Suppression of androgen synthesis. Reduction of PSA. Used mostly for prostate cancer; sometimes in combination with an antiandrogen (flutamide)
Nonsteroidal antiandrogen which blocks androgen at receptor site. Used in combination at the beginning of therapy with LHRH analogue for prostate cancer to prevent tumor flare
Nonsteroidal synthetic estrogen to suppress androgen synthesis
Most widely used agent for Colorectal cancer; alsobreast, bladder, esophagus. Can lead to mucositis and myelosuppression
Complex, poor oral bioavailability, thus only given I.V. Undergoes reduction by a dehydrogenase enzyme. Metabolism follows zero-order kinetics at high doses
Vinca alkaloid MOA
Binds to the microtubular protein tubulin in a dimeric form
The drug-tubulin complex adds to the forming end of the microtubules to terminate assembly
Depolymerization of the microtubules occurs
Peripheral neuropathy, constipation, ileus, Alopecia
Fatal if given intrathecally (Never!)
Liver Metabolism. Reduce dose if Total Bili > 3mg/dl
Paclitaxel- ovarian (with cisplatin) and advanced breast cancer, lung cancer, and Kaposi’s sarcoma
Docetaxel- advanced breast cancer, head and neck cancer, gastric cancer, bladder cancer, platinum refractory ovarian cancer.
High-affinity binding to DNA through intercalation, resulting in blockade of DNA and RNA synthesis
DNA strand scission via effects on Topoisomerase II
Binding to membranes altering fluidity
Generation of oxygen radicals
Binds to DNA through an antibiotic-Mg2+ complex
This interaction interrupts DNA-directed RNA synthesis
Binds to double stranded DNA through intercalation between adjacent guanine-cytosine base pairs
Inhibits all forms of DNA-dependent RNA synthesis
Inhibits DNA transcription
Adverse effects: oral ulcers, sun sensitivity, immunosuppression
Use: Wilm’s tumor
Acts through binding to DNA, which results in single and double strand breaks following free radical formation and inhibition of DNA synthesis
accumulation of cells in G2
Lethal anaphylactoid reactions
Pulmonary fibrosis (those over 70 years old or have undergone chest irradiation, or underlying pulmonary disease).
Raynaud’s syndrome, Alopecia, Mucositis
Bleomycin adverse effects
Testicular cancer, Squamous cell carcinomas of the head and neck, cervix, skin, penis, and rectum
Intracavitary therapy in ovarian and breast cancers
Antibodies for CD20
Antibodies for CD33
Antibodies for CD52 (found on all mature lymphocytes)
Antibody for VEGF
Antibody for EGFR
Non-Hodgkin's lymphoma treatment
FATAL INFUSION REACTIONS, TUMOR LYSIS SYNDROME (TLS), SEVERE MUCOCUTANEOUS REACTIONS, and PROGRESSIVE MULTIFOCAL LEUKOENCEPHALOPATHY (PML)
derivative of Rituximab which is radiolabeled with Ytrium
Inihibts VEGF and c-kit
Labeled indications: GI stromal tumor w/ failure or intolerance to imatinib
Advanced renal cell carcinoma
Myelosuppression, GI effects, hand foot syndrome, hypertension, bleeding, hair color changes
Myelosuppression, GI effects, hand foot syndrome, bleeding, incr QT, hypothyroidism, skin discoloration, and venous thromboembolic events
Drugs that lead to hand foot syndrome
5-FU, capecitabine, cytarabine, doxorubicin
TKIs: sorafenib and sunitinib.
Inhibits EGFR (Her2/neu)
Lapatinib, Gefitinib, Erlotinib
Approved world-wide for non-small cell lung carcinoma (NSCLC).
EGF tyrosine kinase receptor (EGFR) inhibitor
Side effects: Acne, GI, asthenia.
INHIBITS HER-1 (EGFR)
Non-small cell lung cancer (NSCLC) – locally advanced or metastatic in patients who have failed at least one prior chemotherapy regimen
Pancreatic cancer – locally advanced, unresectable or metastatic in combination with gemcitabine
Reversible inhibitor of 26S Proteosome
Increases cellular protein, including tumor suppressors. May prevent degradation of pro-apoptotic molecules, allowing continued programmed cell death in neoplastic cells
GI upset and asthenia, a state of general weakness.
Peripheral neuropathy with pain
Shingles, Neutropenia, Thrombocytopenia
analog of cytidine, and is incorporated into DNA during replication and RNA during transcription.
Azacytidine inhibits methyltransferase and causes demethylation of its segment of DNA and RNA.
Indicated for myelodysplastic syndrome of neutropenia, thrombocytopenia, anemia
GI symptoms, Neutropenia, Thrombocytopenia, Liver dysfunction