Pharm- Target Therapies & Biologicals Flashcards
Bcr-Abl tyrosine kinase inhibitors
imatinib, dastinib
Membrane Associated Receptor Tyrosine Kinases
Gefitinib, Erlotinib, Lapatinib, Sunitinib, Sorafenib
-tx of solid tumors that were driven by receptor tyrosine kinases
Growth Factor Receptor Tyrosine Kinase Signaling
EGRF, PDGFR, VEGFR
mutataed B-RAF kinase
Vemurafenib
BCR-ABL drugs
dasatinib, imatinib
no antibodies
EGRF-receptor drugs & Abs
Erolotinib, Gefitinib
Abs- Cetuximab, Panitumumab
HER2-receptor drugs & Abs
Lapatinib
Ab- Trastuzumab
PDGFR- receptor, VEGFR- receptor
Sunitinib, Sorafenib
-no antibodies
VEGF-ligand Ab
Bevacizumab
Angiogenesis inhibitors
Ab- Bevacizumab
RTK inhibitors- Sunitinib & sorafenib
Antibodies to other epitopes
Rituximab- for CD20+ B cell lymphoma
Bortezomib (IV)
26S proteasome target
- multiple myeloma, mantle cell lymphoma
- reactivation of varicella zoster
Vorinostat (PO)
Histone deacetylase (HDAC) inhibitor
- Cutaneous T cell lymphoma
- pulmonary embolism, venous thrombosis
Anastrazole
Aromatase inhibitor
-estrogen dependent breast cancer
Exemestane
Aromatase inactivator
-advanced breast cancer
Worst chemo drug offenders: CINV > 90%
carmustine, cisplatin, cyclophosphamide, dacarbazine, mechlorethamine
-all of these are mainly alkylating agents
5-HT3 receptor antagonists
Ondansetron, Granisetron
- Cytotoxic durg
- emesis- acute
Central acting Dopamine D2 receptor antagonists
Metoclopramide
Cytotoxic drug
-emesis- acute
Neurokinin NK1 receptor antagonists
Aprepitant
- Cytotoxic drug
- emesis- delayed & acute
Cannabinoid CB1 receptor agonist
Dronabinol
-cytotoxic drug
emesis- refractory to other agents
antiemetic 5HT3 Receptor Antagonist
Ondansetron, Granisetron, Dolasetron, Palonosetron
Ondansetron
IV, oral, oral dissolving tablet
t 1/2 = 4 hrs, hepatic metabolism
Granisetron
IV, oral, transdermal patch
t 1/2= 10 hrs, hepatic metabolism
used for delayed emesis
Dolasetron
oral only
t 1/2= 8 hrs, active metabolite
used for delayed emesis
Palonosetron
IV, oral
t 1/2 =40 hrs, hepatic & renal elimination
dexamethasone
potent glucocorticoid useful for acute & delayed emesis