Chemo Drugs Flashcards
Alkylating Agents Classes
Nitrogen mustards
Nitrosureas
Platinum Drugs
Miscellanous
Nitrogen Mustards
Melphalan, Cyclophosphamide, Ifosfamide, Chlorambucil and Estramustine
Men Can Inject Cocaine Everday
Nitrosureas
Carmustine, Lomustine, Nimustine and Streptozocin (Streptozotocin
“Ustines” and streptozocin
Platinum Drugs
Carboplatin, Cisplatin, and Oxaliplatin
“Platins”
Miscellanous Alkylating Drugs
Busulfan, Procarbazine
Nitrogen Mustards MOA
- Link two Guanine molecules together causing DNA damage
(Azridium intm. –> Chloro)
N-7 Alkylation
Nitrosurea Alkylating Agents MOA
- Have a chloroethyl group that attaches to oxygen on Guanine
- 06 alkylation
Streptozcin MOA
- Has a methyl group
- Get an O6 methylation to Guanine
Platinum Alkylating Agents MOA
- Alkylate and cross link (inter or intra) two Guanine molecules
- DNA damage –> N7 alkylation
Bulsulfan MOA
Remove mesylate (CH3SO3-) to form R–CH2+
Cause intra- and inter-crosslink of DNA molecules
N7 alkylation
Procarbazine MOA
Form methyldiazonium ion (CH3-N+≡N) and methyl cation (CH3+)
Nonspecific alkylating agent which methylates guanine at O6
Antimetabolite Examples And…..
5-Fluorouracil (5-FU), capecitabine, gemcitabine, cytarabine and azacitidine
“ines”
Antimetabolite MOA
Incoporate into the double strand of the DNA molecule Cause breaks Destroy the DNA molecules
Miscoding due to incorporation into DNA/RNA (incorporation into DNA molecule)
Antimitotics Examples
Taxanes
Paclitaxel
Docetaxel
“axes”
Antimitotic MOA
Bind to free tubulin (mitotic spindle) –> Stable bonding
Produce stable microtubules
Inhibit microtubule disassembly (spindles stick)
Vinca Alkyloids Examples
Vinblastine, vincristine, vindesine and vinorelbine
“Vin”
MOA Vinca Alkyloids
Prevent microtube polymerization
- Do not allow microtubule to form spindle
Inhibit formation of mitotic spindle
Antitumour Antibiotics Examples
- Antracyclines
- DNA intercelating agents
Daunorubicin, doxorubicin, epirubicin, idarubicin and mitoxantrone
“ubicins”
Anthracyclines MOA
Intercalate with DNA perpendicular to its longitudinal axis
Cause single and double stranded DNA cleavage
PARP Inhibitors MOA
What does PARP Stand for?
Involved in DNA repair (inhibit DNA repair)
PARP: Poly (ADP-ribose) polymerase
PARP Inhibitor Examples
Olaparib, rucaparib, niraparib, iniparib and talazoparib
“paribs” suffix
PARP Inhibitors MOA
Block DNA repair in cancer cells and cause cancer cell death
Targeted Tx Agents
- Tyrosine Kinase Inhibitors
Monoclonal Antibodies
Apoptosis Inducing Agents
Angiogenesis Inhibitors
Tyrosine Kinase Inhibitor Examples
Imatinib, Gefitinib, Ibrutinib
“inibs”
Monoclonal ANtibodies Examples
Prastuzumab, Pertuzumab, T-DM1, Bevacizumab, Rituximab
“umabs”
Apoptosis Inducing Examples
Bortezomib, Oblimersen (nucleotide drug),
THINK O’s
Angiogenesis Inhibitors
Bevacizumab, Sunitinib
Tyrosine Kinase Inhibitor MOA
Tyrosine kinase (TK) domain is present in growth factor receptors, such as epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor (VEGFR), and signaling protein kinases such as Ras and Raf
- Inhibit angiogensis
Immatinib MOA
Tyrosine-Kinase Inhibitor
Inhibit BCR-ABL tyrosine kinase
Inhibit proliferation and induce apoptosis in BCR-ABL positive cells
Gefitnib MOA
Inhibitor of epidermal growth factor receptor (EGFR)
Signaling via EGF-EGFR promotes DNA synthesis, proliferation, migration and survival
Monoclonal Antibodies MOA
Bind to subdomain IV of Her2 protein
Pertuzumab MOA
Monoclonal antibody binds to subdomain II of Her2 protein
Block homodimerization of Her2 and heterodimerization of Her2-Her3
-
Inhibit Her2-signaling pathway and decrease cell growth
THINK ER
Bortezomib MOA
Proteasome inhibitor and apoptosis-inducing agent
Bind to 26S proteasome, prevent proteosome-mediated degradation of pro-apoptotic factors and induce apoptosis
Bevacizumab MOA
- Starve Cancer cells
- Anti-angiogenesis monoclonal antibody blocking vascular endothelial growth factor (VEGF)
- VEGF and its receptors (VEGFR) can induce and promote angiogenesis (take out either one)
Sunlitib MOA
Multiple-targeted tyrosine kinase inhibitor
Inhibit VEGFR, platelet-derived growth factor receptor (PDGFR), colony stimulating factor receptor (CSFR) and tyrosine-protein kinase KIT (CD117)
Angiogenesis inhibitor
Sun –> Star –> Millions
PD-1 Mechanism
programmed cell death protein 1 (CD279)
Surface protein on T-cells
Prevent T-cells from killing other cells upon binding PD-L1
Check immune responses
PD- L1 Mechanism
programmed cell death ligand 1 (CD274 or B7-H1)
Transmembrane protein
Prevent T-cells from killing PD-L1-containging cells
PD-1 and PD-L1 Cancer Mechanism. Prevent cancer?
PD-L1 binds to PD-1 and inhibits T-cell killing of tumour cell
Blocking PD-L1 allows T cell killing of tumour cell
Pd-1 Inhibitors
Pembrolizumab
Nivolumab
Cemiplimab
PD-L1 Inhibitors
Atezolizumab
Avelumab
Durvalumab
Tamoxifen MOA and What is it?
- Block ER and inhibit breast cancer cell growth
May slightly increase the chance of getting uterine cancer (ER in breast to block function, if goes to uterus activates ER) - Hormonal Tx
Think TAMMY
How do hormones promote cancer?
Hormones can bind estrogen receptor (ER) and progesterone receptor (PR) to promote cancer cell growth
