Targeted Therapies

mAbs require what premeds

apap 650mg PO + diphenhydramine IV/PO

anti-cluster of differentiation (CD) agents

Rituximab, blinatumomomab, brentuximab vedotin, daratumumab

what is the moa of anti CD agents

bind to specific antigens expressed on the cell sruface causing cell death

rituximab target

CD20

rituximab generic

rituxan

biosimilars of rituximab

riabni, ruxience, truxima

rituximab safety concerns

hepatitis B reactivation; needs hep b panel prior to treatment. consider antiviral (entacavir) prophylaxis

epidermal growth factor receptor (EGFR) inhibitors

cetuximab

EGFR inhibitor moa

inhibit pathways involved in cellular proliferation, differenctiation and survival

cetuximab generic

erbitux

KRAS mutation (not wild type) means what

lack of response to anti-EGFR drugs

can only use anti EGFR drugs wtih WHAT KRAS type?

wild type

BRAF600E mutation; requirements if you want to use an antiEGFR drug?

must also use in combo with a BRAF inhibitor

cetuximab/EGFR inhibitor safety concerns

acneiform rash within first two weeks of therapy; means treatment is working. Advise with general skin care and topical steroids for acne rash.

Human epidermal grwoth factor receptor 2 (HER2) inhibitor drugs

trastuzumab, ado-trastuzumab emtansine, fam-trastuzumab deruxtecan, pertuzumab

trastuzumab generic

herceptin

trastuzumab biosimilars

kanjiniti, herzuma, ogivri, ontruxant, trazimera

ado-trastuzumab emtansine generic

kadcyla

fam-trastuzumab deruxtecan generic

enhertu

pertuzumab generic

perjeta

HER2 inhibitors safety concerns

cardio tox; cardiomyopathy. Monitor LVEF (ECHO or MUGA scan) at baseline and during treatment

vascular endothelial growth factor (VEGF) inhibitors

bevacizumab

VEGF inhibitor moa

inhibit growth of blood vessels needed for tumor proliferation

bevacizumab generic

avastin

bevacizumab biosimilars

alymsys, mvasi, vegzelma, zirabev

bevacizumab/VEGF inhibitor safety concerns

impaired wound healing (do not admi for 28 day before/after surgery), thrombotic evens, hemorrhage/fatal bleeding and GI perforation

program death receptor 1 (PD1) inhibitors

pembrolizumab, nivolumab

PD1 inhibitor moa

bind to the PD1 receptor on the T cells to block PD1 ligands from binding; increases T cell activation and antitumor response. Immunotherapy

pembrolizumab generic

keytruda

nivolumab generic

opdivo

PD1 inhibitor safety concerns

immune mediated toxicities (endocrine, colitis, hepatotox, pneumonitis, thyroid disorders)

may require systemic steroid and management of whatever tox pops up

cytotoxic t-lymphocyte antigen 4 (CTLA-4) inhibitor

ipilimumab

CTLA-4 inhibitor moa

binds to CTLA4 receptor, removes the brake from T cell activation; increases T cell responsivness and antitumor response; immunotherapy

ipilimumab generic

yervoy

what is the role of tyrosine kinase proteins

intracellular singaling pathways that control growth and differentiation of cells

how are TKIs givien

orally

what must be true to use a TKI

must test positive for a certain genetic target/mutation

BCR-ABL inhibitors

imatinib, dasatinib, nilotinib

BCR-ABL inhibitors moa

block tyrosine kinase singalling protein produced by the BCR-ABL fusion gener that causes uncontrolled cell division

BCR-ABL fusion gene is also known as

philadelphia chromosome

imatinib generic

gleevec

dasatinib generic

sprycel

nilotinib generic

tasigna

BCR-ABL inhibitors safety concerns

fluid retention, qt prolongation, GI upset (abdominal pain)

BCR-ABL inhibitor with greatest QT prolongation risk

nilotinib

how to take imatinib

with food or within 1 hr after a meal

BRAF inhibitors

dabrafenib, vemurafenib

BRAF inhibitors moa

inhibit certain mutated forms of protein kinase BRAF, blocking tumor cell growth

Targets for BRAF inhibitors

BRAF V600E or V600K mutation

dabrafenib generic

tafinlar

vemurafenib generic

zelboraf

Braf inhibitor safety concerns

new malignancies (basal cell carinoma), QT prolongation, febrile reactions, hyperglycemia, skin rash

Mitogen-activated extracellular kinase (MEK) 1 and 2 inhibitors

cobimetinib, trametinib

MEK ½ inhibitors moa

inhibit MEK, signalling protien downstream from RAF

Cobimetinib generic

cotellic

trametinib generic

mekinist

MEK ½ mutation target

BRAF V600E or V600K with BRAF inhibitor use

MEK ½ inhibitors safety concerns

retinopathy, rhadomyolisis

EGFR inhibitors (TKIs)

afatinib, erlotinib

EGFR inhibitors (TKIs) target

EGFR gene mutation (exon 19 deletion or exon 21 substitution)

afatinib generic

gilotrif