Biologics Flashcards
Imatinib
Tyrosine Kinase Inhibitor Targeting Catalytic Cleft on ABL
Inhibits PDGF-R and c-KIT
Used to treat CML
T(9:22) that creates BRC-ABL Philly Chromosome
Susceptible to resistance when cleft mutations limit imatinib binding
ATRA/Arsenic
Targets the Retinoic Acid Receptor and displaces PML-RAR protein.
Used to treat Acute Promyelotic Leukemia (APML)
Toxicity= ATRA Syndrome- Leukocytosis (high neutrophil count) Capillary leak (pulmonary edema) Renal Failure
Rituximab
Monoclonal antibody (chimeric) targeting CD20 on B cells.
USed to treat B Cell malignancies (and autoimmune disorders)
Crizotinib
Tyrosine Kinase Inhibitor targeting ALK
Used in Non Small Cell Lung Cancer.
Also works for large T Cell Lymphoma since it targets ALK
Thalidomide
Unclear MOA but used to treat skin diseases associated with leprosy as well as multiple myeloma
It is a teratogen that causes focomelia (short limbs)
Trastuzumab (Herceptin)
Targets HER2 and prevents dimerization
Used for breast, stomach, and esophageal cancer.
Can cause cardiotoxicity.
Cetuximab
Chimeric monoclonal antibody that targets EGFR
Can cause resistances with BRAF mutations.
Erlotinib
Tyrosine Kinase Inhibitor that targets EGFR
Bevacizumab
VEGFR inhibitor.
Toxicities include pulmonary hemorrhage, HTN, Proteinurea
VERY EXPENSIVE
Vemurafinib
Small molecule RAF inhibitor that targets V600EBRAF mutation
Used to treat melanoma
Can lead to other skin cancers, There is resistance in those that have V600E mutations (in colon cancer)
Bortezomib
Antibody that inhibits proteasomes.
Toxicity can lead to neuropathy and myelosuppression.
Used to treat Multiple Myeloma.
Nivolumab
PD-1 Inhibitor
Can lead to immune mediated pneumonitis, colitis,
Fatigue, Rash, muscolokeletal pain, pruritis.
