Tyrosine Kinase Inhibitors Flashcards
Sunitinib
- Target
- Cancer Type
- Toxicity
- MOA
- MO Delivery
- Resistance
- Other
Target:
VEGF receptor Tyrosine Kinase
Cancer Type:
GIST
Toxicity:
Stocking glove syndrome, THYROID
MOA:
Binding to ATP binding site inhibiting action
MO Delivery:
Oral
Resistance:
- Inhibits drug binding (TK activity stays the same, dose response curve is shifted to the RIGHT out of Therapeutic window)
- Kinase OverExpression
Other:
- Metabolized by Cyt p-450 (drug-drug ints. anticipated)
Nilotinib
- Target
- Cancer Type
- Toxicity
- MOA
- MO Delivery
- Resistance
- Other
Target:
BCR-ABL Tyrosine Kinase Inhibitor
Cancer Type:
- Chronic Myelogenic Leukemia (CML)
- Acute Lymphoblastic Leukemia
Toxicity:
-Thyroid (moderate - less than Sora-, Suni-, and Imatinib)
MOA:
- Bind ATP binding site, inhibiting action
MO Delivery:
- Oral
Resistance:
- Inhibits drug binding (TK activity stays the same, dose response curve is shifted to the RIGHT out of Therapeutic window)
- Kinase OverExpression
Other:
- Metabolized by Cyt p-450 (drug-drug ints. anticipated)
Bortezomib
- Target
- Cancer Type
- Toxicity
- MOA
- MO Delivery
- Resistance
- Other
Target:
26-S Proteosome Tyrosine Kinase Inhibitor
Cancer Type:
Multiple Myeloma
Toxicity:
CARDIAC
MOA:
Blocks Degradation of IkB-alpha by 26-S proteosome, Keeping NFkB from translocating to the nucleus and creating increased pro-apoptotic and decreased anti-apoptotic forces in the cells
MO Delivery:
IV or INJECTION
MO Delivery:
- Oral
Resistance:
- Inhibits drug binding (TK activity stays the same, dose response curve is shifted to the RIGHT out of Therapeutic window)
- Kinase OverExpression
Other:
- Metabolized by Cyt p-450 (drug-drug ints. anticipated)
Erlotinib
- Target
- Cancer Type
- Toxicity
- MOA
- MO Delivery
- Resistance
- Other
Target:
- EGFR Tyrosine Kinase Inhibitor
Cancer Type:
- Lung, Breast, Pancreatic**
Toxicity:
- Thyroid (less than Sora- Suni-, or Imatinib)
- Dermal Toxicity (used sometimes to monitor)
MOA:
Bind ATP binding site, Inhibiting Action
MO Delivery:
Oral
Resistance:
- Inhibits drug binding (TK activity stays the same, dose response curve is shifted to the RIGHT out of Therapeutic window)
- Kinase OverExpression
Other:
- Metabolized by Cyt p-450 (drug-drug ints. anticipated)
Imatinib
- Target
- Cancer Type
- Toxicity
- MOA
- MO Delivery
- Resistance
- Other
Target:
BCR-ABL Tyrosine Kinase Inhibitor
Cancer Type:
- Chronic Myelogenic Leukemia (CML)
- Acute Lymphoblastic Leukemia
Toxicity:
-THYROID
MOA:
- Bind ATP binding site, inhibiting action
MO Delivery:
- Oral
Resistance:
- Inhibits drug binding (TK activity stays the same, dose response curve is shifted to the RIGHT out of Therapeutic window)
- Kinase OverExpression
Other:
- Metabolized by Cyt p-450 (drug-drug ints. anticipated)
Gefitinib
- Target
- Cancer Type
- Toxicity
- MOA
- MO Delivery
- Resistance
- Other
Target:
- EGFR Tyrosine Kinase Inhibitor
Cancer Type:
- Lung and Breast
- *Pancreatic Erlotinib only
Toxicity:
- Dermal Toxicity
MOA:
Bind ATP binding site, Inhibiting Action
MO Delivery:
Oral
Resistance:
- Inhibits drug binding (TK activity stays the same, dose response curve is shifted to the RIGHT out of Therapeutic window)
- Kinase OverExpression
Other:
- Metabolized by Cyt p-450 (drug-drug ints. anticipated)
Sorafenib
- Target
- Cancer Type
- Toxicity
- MOA
- MO Delivery
- Resistance
- Other
Target:
VEGF receptor Tyrosine Kinase
Cancer Type:
Hepatocellular Carcinoma
Toxicity:
Stocking glove syndrome, THYROID
MOA:
Binding to ATP binding site inhibiting action
MO Delivery:
Oral
Resistance:
- Inhibits drug binding (TK activity stays the same, dose response curve is shifted to the RIGHT out of Therapeutic window)
- Kinase OverExpression
Other:
- Metabolized by Cyt p-450 (drug-drug ints. anticipated)
Lapatinib
- Target
- Cancer Type
- Toxicity
- MOA
- MO Delivery
- Resistance
- Other
Target:
- EGFR Tyrosine Kinase Inhibitor
Cancer Type:
- Lung, Breast, Pancreatic**
Toxicity:
- Dermal Toxicity (can be used to monitor drug dose)
MOA:
Bind ATP binding site, Inhibiting Action
MO Delivery:
Oral
Resistance:
- Inhibits drug binding (TK activity stays the same, dose response curve is shifted to the RIGHT out of Therapeutic window)
- Kinase OverExpression
Other:
- Metabolized by Cyt p-450 (drug-drug ints. anticipated)
Sirolimus
- Target
- Cancer Type
- Toxicity
- MOA
- MO Delivery
- Resistance
- Other
Target:
-mTOR inhibitor
Cancer Type:
Renal
Toxicity:
MOA:
MO Delivery:
Resistance:
Other:
Temsirolimus
- Target
- Cancer Type
- Toxicity
- MOA
- MO Delivery
- Resistance
- Other
Target:
mTOR Inhibitor
Cancer Type:
Renal
Toxicity:
MOA:
MO Delivery:
Resistance:
Other:
Vemurafenib
- Target
- Cancer Type
- Toxicity
- MOA
- MO Delivery
- Resistance
- Other
Target:
BRAF Tyrosine Kinase Inhibitor
Cancer Type:
Melanoma
Toxicity:
Stocking and Glove
MOA:
Bind ATP binding Site, inhibiting action
MO Delivery:
Oral
MO Delivery:
- Oral
Resistance:
- Inhibits drug binding (TK activity stays the same, dose response curve is shifted to the RIGHT out of Therapeutic window)
- Kinase OverExpression
Other:
- Metabolized by Cyt p-450 (drug-drug ints. anticipated)
Pazopanib
- Target
- Cancer Type
- Toxicity
- MOA
- MO Delivery
- Resistance
- Other
Target:
VEGF receptor Tyrosine Kinase
Cancer Type:
Soft Tissue Sarcoma
Toxicity:
Stocking-Glove Renal
-Thyroid (less than Sora- Suni-, or Imatinib)
MOA:
Binding to ATP binding site inhibiting action
MO Delivery:
Oral
Resistance:
- Inhibits drug binding (TK activity stays the same, dose response curve is shifted to the RIGHT out of Therapeutic window)
- Kinase OverExpression
Other:
- Metabolized by Cyt p-450 (drug-drug ints. anticipated)
Everolimus
- Target
- Cancer Type
- Toxicity
- MOA
- MO Delivery
- Resistance
- Other
Target:
mTOR inhibitor
Cancer Type:
Renal
Toxicity:
MOA:
MO Delivery:
Resistance:
Other:
Cruzotinib
- Target
- Cancer Type
- Toxicity
- MOA
- MO Delivery
- Resistance
- Other
Target:
- EML-4-ALK
Cancer Type:
- Lung Primary Carcinoma
MOA:
- Bind ATP binding site, Inhibiting Action
MO Delivery:
- Oral
Resistance:
- Inhibits drug binding (TK activity stays the same, dose response curve is shifted to the RIGHT out of Therapeutic window)
- Kinase OverExpression
Other:
- Metabolized by Cyt p-450 (drug-drug ints. anticipated)
Dasatinib
- Target
- Cancer Type
- Toxicity
- MOA
- MO Delivery
- Resistance
- Other
Target:
BCR-ABL Tyrosine Kinase Inhibitor
Cancer Type:
- Chronic Myelogenic Leukemia (CML)
- Acute Lymphoblastic Leukemia
Toxicity:
-Thyroid (less than Sora- Suni-, or Imatinib)
MOA:
- Bind ATP binding site, inhibiting action
MO Delivery:
- Oral
Resistance:
- Inhibits drug binding (TK activity stays the same, dose response curve is shifted to the RIGHT out of Therapeutic window)
- Kinase OverExpression
Other:
- Metabolized by Cyt p-450 (drug-drug ints. anticipated)