Drug Doses/PK Flashcards
Tamoxifen
Antiestrogen SERM
20mg po daily Half-life 7-14 d Metabolism Hepatic Excretion Fecal Substrate of CYP3A4, 2C9, 2D6 P-gp inhibitor
Enzalutamide
Antiandrogen
160mg po daily Half-life 6-8 days Wafarin Substrate 2C8, A4 Inducer 3A4, 2C9, 2C19
Abiraterone
Antiandrogen
1000 mg po daily + Prednisone 5 mg BID Half life 12H Metabolism Hepatic Excretion Fecal 3A4 inhibitors and inducers Inhibitor 2D6, 2C8
Leuprolide
LHRH agonist
3.75 mg IM Qmonth to 22.5 mg IM Q3 months
Half life 3-5H
Metabolism Hydrolysis of C terminal amino acids
Excretion renal
No DDI
Bevacizumab
VEGF inhibitor
IV administered over 90 min on an every 2-3 week schedule
Half life 20 days
No DDI
Cetuximab
EGFR inhibitor
LD: 400 mg/m2 IV ovre 90 min
MD: 250 mg/m2 IV QW
Premedicate with benadryl
Half life 5 days
Erlotinib
EGFR inhibitor
150 mg po daily (with food) Half life 24-36H Metabolism hepatic Excretion fecal CYP inducer/inhibitors Warfarin Gastric pH altering med
Lapatinib
EGFR inhibitor
1250 mg po daily
Half life 24H
Metabolism Hepatic
CYP inducers/inhibitors
Trastuzumab
HER 2 antibody
LD: 8 mg/kg IV over 90 min
MD: 6 mg/kg IV Q3W
Half life 6-16 days
Crizotinib
ALK TKI
250mg po BID Half life 42H (reduced with high fat meal) Metabolism hepatic Excretion fecal/urine CYP inducers/inhibitors
Vemurafenib
BRAF TKI
960 mg po BID Half life 57H Metabolism hepatic Excretion fecal CYP inducers/inhibitors Inhibitor of 1A2, 2D6, P-gp Induces 3A4
Dabarafenib
BRAF TKI
150 mg po BID Half life 8H/10-21H (high fat meal) Metabolism hepatic Excretion fecal/urine CYP inducers/inhibitors Induces 2B6, 2C19, 2C9, 3A4
Trametinib
MEK TKI
2 mg po daily Half life 4-5 days Metabolsim deacetylation/glucuronidation Excretion fecal/urine Inhibits 2C8 Induces 3A4
Cobimetinib
MEK TKI
60 mg po daily for 21 days of 28 day cycle Half life 44H Metabolism Hepatic Excretion fecal Inducer/inhibitors 3A4
Palbociclib
CDK inhibitor
125 mg po daily for 21 days with 7 days off Half life 29H (take with food) Metabolism hepatic Excretion fecal/urine CYP inducers/inhibitors CYP substrate