Cell Cycle Targets
This cycle specific drug class inhibits disassembly of microtubules to prevent cell replication in the M phase.
What are Taxanes?
Ex. paclitaxel, docetaxel
Pembrolizumab (Keytruda) is an immune checkpoint inhibitor because it blocks this pathway.
What is the PD-1/PD-L1 pathway?
Keytruda is also approved to treat cancers of any type with the following genetic mutations: MSI-H, dMMR, or TMB-H
This is a monoclonal antibody that inhibits angiogenesis by binding and neutralizing VEGF-A
What is Bevicizumab (Avastin)?
Avastin works by disrupting blood flow to the tumor and starving it of nutrients and oxygen by binding to VEGF. Some tumor cells can induce angiogenesis by secreting VEGF to enable and support their growth, while redirecting blood flow to evade drug delivery. Avastin helps normalize blood flow and inhibit this process leading to enhanced efficacy
Bi-specifics modify this immune protein to exert their mechanism
What is an antibody?
Bi-specifics are humanized antibodies with modified Fab regions that are specific for two different sites.
DAILY DOUBLE:
This is Lauren and Lakin's preferred snacks to binge while studying for finals
Salt n Vinegar chips (Lauren) and A tub of almond butter (Lakin)
Irinotecan inhibits topoisomerase I to halt this phase of the cell cycle.
What is the S-phase?
Topoisomerase I cuts and repairs DNA strands during replication to prevent torsional friction from damaging DNA coils during this process.
This immunotherapy monoclonal antibody was the first in its class, approved in 1997 for Non-Hodgkin's Lymphoma.
What is rituximab (Rituxan)?
Rituxan targets CD20 on B-lymphocytes, activating complement-dependent B-cell cytotoxicity. It can also bind to human Fc receptors to activate natural killer cells.
This targeted therapy class is commonly used in blood cancers and blocks the 26S proteasome to induce apoptosis, especially in plasma cells and rapidly dividing tumor cells
What are proteasome inhibitors?
Bortezomib, Carfilzomib, Ixazomib
BiTE is the acronym describing this subset of bi-specifics that target receptors on T-cells.
What is a Bi-specific T-cell engager?
Tri-specifics modify variation sites on antibodies to increase specificity to this type of cell.
What is a tumor cell?
Tri-specifics target one immune cell receptor (typically CD3 or CD16) and two tumor antigens, increasing the tumor specificity and decreasing off-target side effects.
These two classes cross-link with DNA, binding to amino acid (s) to interfere with DNA synthesis and replication, resulting in cell death
What are Platinum Compounds and Alkylating agents?
Nivolumab (Opdivo) is commonly used with this anti-CTLA-4 therapy due to their synergistic anti-tumor effect.
What is ipilimumab?
When used together, nivolumab and ipilimumab enhance T-cell function greater than either antibody alone for improved responses in metastatci melanoma and advanced renal cell carcinoma.
These medications block the mTOR pathway involved in cell growth
Everolimus, Tacrolimus, Sirolimus
This receptor is the target of Zanidatamab (Ziihera), which is the only bi-specific therapy that targets two distinct binding sites on the same receptor.
HER2
DAILY DOUBLE
This is a crime that both Lauren and Lakin have been involved in while attending pharmacy school.
What is a victim of car theft?
This class of agent inhibits topoisomerase II, leading to double-strand DNA breaks and creation of oxygen-free radicals that damage cells
What are Anthracyclines?
durvalumab (Imfinzi) is a monoclonal antibody that increases cytotoxic T-cell activity, proliferation and cytokine production by blocking the interaction between PD-L1/PD-1 with this cluster of differentiation (CD).
What is CD80?
also known as B7.1
This is one example of a PARP inhibitor
What is olaparib/rucaparib?
These are commonly used for BRCA gene mutations, blocking ADP ribose polymerase, preventing them from repairing their own DNA, inducing apoptosis
This protein is overexpressed on the surface of multiple myeloma cells as well as some plasma cells. It is also one of the targets of the bispecifc, Linozyfic (linvoseltamab), along with CD3.
What is BCMA (B-cell maturation antigen)?
The FDA has approved this tri-specific antibody for certain uses in oncology.
What is a trick question?
The FDA has yet to approve any tri-specific therapies
This anthracycline has a lifetime cumulative dose due to cardiotoxicity
(extra 10 points if you can state the lifetime cumulative dosing WITH units!)
What is Doxorubicin?
450-550 mg/m^2
Lenalidomide (Revlimid), an immunomodulatory agent, exhibits a 3-fold increase in it's half-life when the CrCl drops below 60. Lenalidomide should be avoided once the CrCl drops below this CrCl.
What is a trick question?
Revlimid has suggestions for renal dose adjustments to be safely used at any CrCl
This class of targeted therapy turns off oncogenic signaling in cancers driven by kinase activation signaling pathways (RAS/RAF, JAK/STAT, PI3K/AKT/mTOR) via mutations, amplifications, or fusion proteins
What are Tyrosine Kinase Inhibitors?
These inhibit tumor cell proliferation, inducing apoptosis, reducing angiogenesis and limiting metastasis
This mammalian cell line is well-suited for producing complex functional proteins and is commonly used to produce bi-specific monoclonal antibodies.
What are Chinese Hamster Ovary (CHO) cells?
This class of therapy is still in developmental phases, but has achieved more specificity than the tri-specifics
What are tetra-specifics?