CML Drugs--Fitz

Question 1

Imatinib

Answer 1

MOA: BCR-ABL1 ATP antagonist, c-kit antagonist

Resistance: change in target protein

PK: CYP3A4 metabolism, PO

TU: CML, GI w/ c-kit

Tox: CHF, MI, edema, BM suppression

Question 2

Bosutinib

Answer 2

MOA: BCR-ABL1 ATP antagonist, c-kit antagonist

Resistance: change in target protein

PK: CYP3A4 metabolism, PO

TU: CML, GI w/ c-kit

Tox: CHF, MI

Question 3

Dasatinib

Answer 3

MOA: BCR-ABL1 ATP antagonist, c-kit antagonist

Resistance: change in target protein

PK: CYP3A4 metabolism, PO

TU: CML, GI w/ c-kit

Tox: CHF, MI

Question 4

Nilotinib

Answer 4

MOA: BCR-ABL1 ATP antagonist, c-kit antagonist

Resistance: change in target protein

PK: CYP3A4 metabolism, PO

TU: CML, GI w/ c-kit

Tox: CHF, MI, edema

Question 5

Erlotinib

Answer 5

MOA: EGFR antagonist

Resistance: change in target protein

PK: CYP3A4 metabolism, PO

TU: metastatic non-small cell lung cancer

Tox: rare interstitial lung disease, CHF, MI

Question 6

Gefitinib

Answer 6

MOA: EGFR antagonist

Resistance: change in target protein

PK: CYP3A4 metabolism, PO

TU: metastatic non-small cell lung cancer

Tox: rare interstitial lung disease, CHF, MI