Antineoplastics - Hormonal Agents, Signal Transduction Inhibitors, and Miscellaneous Flashcards
glucocorticoid that induces lymphocyte apoptosis
Prednisone
MOA: bind to Estrogen receptors and act as agonists/antagonists depending on target tissue
Selective Estrogen Receptor Modulators (SERMS)
Pure Estrogen Receptor Antagonist with no agonist activity
Fulvestrant
Selective Estrogen Receptor Downregulator (SERD)
Fulvestrant
Agonist in non-breast tissues
Tamoxifen
Antiestrogen in the uterus and breast
Raloxifene
Antagonist in breast
Tamoxifen
Chemopreventive agent for women at risk of breast cancer
Tamoxifen
Prophylactic for breast cancer in high risk postmenopausal women
Raloxifene
agonist at bone to prevent postmenopausal Osteoporosis
Raloxifene
SERM that does not cause endometrial hyperplasia
Raloxifene
SERM that causes endometrial hyperplasia
Tamoxifen
increases ER degradation, reducing number in cells
Fulvestrant
used in Tamoxifen-resistant breast cancer
Fulvestrant
inhibit Aromatase to prevent Estrone synthesis from Androstenedione
Aromatase inhibitors
Non-steroidal Aromatase inhibitors
Anastrozole and Letrozole
Steroidal Aromatase Inhibitor
Exemestane
Irreversible inhibitor of Aromatase
Exemestane
Competitive reversible inhibitors of Aromatase
Anastrozole and Letrozole
Androgen Receptor Blocker
Flutamide
GnRH analogs
Goserelin and Leuprolide
MOA of Flutamide
non-steroidal, competitive antagonist of androgen receptor
indications for Flutamide
Prostatic Carcinoma
Indications for GnRH analogs
Prostatic Carcinoma
stimulate release of FSH and LH from ant. pit
GnRH analogs
AE: mild gynecomastia and reversible hepatotoxicity
Flutamide
Biphasic response (initial phase/flare and delayed phase)
GnRH analogs
Concurrent administration with Flutamide counteracts effects
GnRH analogs
inhibits EGFR Tyrosine Kinase; for NSCLC
Gefitinib
inhibits EGFR Tyrosine Kinase for colorectal cancer expressing KRAS wild type
Cetuximab
EGFR Tyrosine Kinase inhibitor for pancreatic cancer and NSCLC
Erlotinib
inhibits EGFR and ErbB2
Lapatinib
Humanized monoclonal ab against ErbB2 (HER2)
Trastuzumab
Used in breast cancer with HER2 over expression but causes cardiotoxicity
Trastuzumab
used for NSCLC and Pancreatic Cancer; inhibits EGFR and ErbB2
Lapatinib
inhibits Bcr-Abl in CML
Imatinib
inhibits c-kit –> used for GIST
Imatinib
Idiopathic Hypereosinophilic Syndrome
Imatinib
Inhibits RAF Serine/Threonine Kinase
Sorafenib
Used against Renal Cell Carcinoma
Sorafenib
Inhibits VEGF-R2, VEGF-R3, and PDGFR-beta
Sorafenib
Proteasome inhibitor that inhibits growth and induces apoptosis
Bortezomib
Used for Mantle Cell Lymphoma
Bortezomib
Inhibits Angiogenesis and VEGFR-1, 2, and PDGFR
Sunitinib
Used for Renal Cell Carcinoma and GIST
Sunitinib
Used against ALL due to tumor cells lacking exogenous source of L-Asparagine (normal cells have Asparagine Synthase)
Asparaginase
AE of Asparaginase
pancreatitis, decreased clotting factors, seizures and coma, hypersensitivity
Kills cells in S phase and inhibits Ribonucleotide Reductase, inhibiting DNA Synthesis
Hydroxurea
used for Sickle Cell Anemia and Malignant Melanoma
Hydroxyurea
AE of Hydroxyurea
Skin hyperpigmentation, macrocytosis, myelosuppression
MOA: stimulates NK cells to kill transformed cells by increasing HLA expression on tumor cells
Interferon alpha
AE of Interferon alpha
flu-like symptoms
Indications of Interferon alpha
Kaposi Sarcoma, Hairy Cell Leukemia, Renal Cell Carcinoma, HPV, HBV, and HCV