Tyrosine Kinase Inhibitors Flashcards

1
Q

Sunitinib

  • Target
  • Cancer Type
  • Toxicity
  • MOA
  • MO Delivery
  • Resistance
  • Other
A

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)

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2
Q

Nilotinib

  • Target
  • Cancer Type
  • Toxicity
  • MOA
  • MO Delivery
  • Resistance
  • Other
A

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)

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3
Q

Bortezomib

  • Target
  • Cancer Type
  • Toxicity
  • MOA
  • MO Delivery
  • Resistance
  • Other
A

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)

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4
Q

Erlotinib

  • Target
  • Cancer Type
  • Toxicity
  • MOA
  • MO Delivery
  • Resistance
  • Other
A

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)

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5
Q

Imatinib

  • Target
  • Cancer Type
  • Toxicity
  • MOA
  • MO Delivery
  • Resistance
  • Other
A

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)

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6
Q

Gefitinib

  • Target
  • Cancer Type
  • Toxicity
  • MOA
  • MO Delivery
  • Resistance
  • Other
A

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)

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7
Q

Sorafenib

  • Target
  • Cancer Type
  • Toxicity
  • MOA
  • MO Delivery
  • Resistance
  • Other
A

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)

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8
Q

Lapatinib

  • Target
  • Cancer Type
  • Toxicity
  • MOA
  • MO Delivery
  • Resistance
  • Other
A

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)

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9
Q

Sirolimus

  • Target
  • Cancer Type
  • Toxicity
  • MOA
  • MO Delivery
  • Resistance
  • Other
A

Target:
-mTOR inhibitor

Cancer Type:
Renal

Toxicity:

MOA:

MO Delivery:

Resistance:

Other:

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10
Q

Temsirolimus

  • Target
  • Cancer Type
  • Toxicity
  • MOA
  • MO Delivery
  • Resistance
  • Other
A

Target:
mTOR Inhibitor

Cancer Type:
Renal

Toxicity:

MOA:

MO Delivery:

Resistance:

Other:

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11
Q

Vemurafenib

  • Target
  • Cancer Type
  • Toxicity
  • MOA
  • MO Delivery
  • Resistance
  • Other
A

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)

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12
Q

Pazopanib

  • Target
  • Cancer Type
  • Toxicity
  • MOA
  • MO Delivery
  • Resistance
  • Other
A

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)

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13
Q

Everolimus

  • Target
  • Cancer Type
  • Toxicity
  • MOA
  • MO Delivery
  • Resistance
  • Other
A

Target:
mTOR inhibitor

Cancer Type:
Renal

Toxicity:

MOA:

MO Delivery:

Resistance:

Other:

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14
Q

Cruzotinib

  • Target
  • Cancer Type
  • Toxicity
  • MOA
  • MO Delivery
  • Resistance
  • Other
A

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)

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15
Q

Dasatinib

  • Target
  • Cancer Type
  • Toxicity
  • MOA
  • MO Delivery
  • Resistance
  • Other
A

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)

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