Targeted Cancer Therapy: Small Molecule Drugs Flashcards

1
Q

Erlotinib Mechanism

A

EGFR: TK-Inhibitor
compete with ATP for binding site on EGFR-TK cytosolic domain

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2
Q

Erlotinib Use

A

Non-small Cell Lung cancer

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3
Q

Erlotinib Side Effects

A

Rash
Diarrhea
Fatigue

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4
Q

Gefitinib Mechanism

A

EGFR: TK-Inhibitor
compete with ATP for binding site on EGFR-TK cytosolic domain

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5
Q

Gefitinib use

A

Non-small Cell Lung cancer

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6
Q

Gefinitib Side Effects

A

Rash
Diarrhea
Fatigue

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7
Q

Afatinib Mechanism

A

EGFR: TK-Inhibitor
compete with ATP for binding site on EGFR-TK cytosolic domain

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8
Q

Afatinib use

A

Non-small Cell Lung cancer

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9
Q

Afatinib Side effects

A

Rash
Diarrhea
Fatigue

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10
Q

Alectinib Mechanism

A

Inhibit TK-R targeting ALK

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11
Q

Alectinib Use

A

Metastatic Non-small cell lung cancer

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12
Q

Alectinib Side Effects

A

Edema
Rash
Diarrhea

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13
Q

Crizotinib Mechanism

A

Inhibit TK-R targeting ALK

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14
Q

Crizotinib Use

A

Metastatic Non-small cell lung cancer

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15
Q

Crizotinib Side Effects

A

Edema
Rash
Diarrhea

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16
Q

Imatinib Mechanism

A

TK inhibitor of BCR-ABL fusion protein and C-Kit

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17
Q

Imatinib Use

A

CML
GI Stromal Tumors
ALL

18
Q

Imatinib Side Effects

A

Fluid Retention

19
Q

Dasatinib Mechanism

A

TK inhibitor of BCR-ABL fusion protein and C-Kit

20
Q

Dasatinib use

A

CML
GI Stromal Tumors
ALL

21
Q

Dastinib Side Effects

A

Fluid Retention

22
Q

Nilotinib Mechanism

A

TK inhibitor of BCR-ABL fusion protein and C-Kit

23
Q

Nilotinib Use

A

CML
GI Stromal Tumors
ALL

24
Q

Nilotinib Side Effects

A

Fluid Retention

25
Q

Ruxolitinib mechanism

A

Inhibit Jak1/2 signaling

26
Q

Ruxolitinib use

A

Metastatic Melanoma

27
Q

Ruxolitinib Side effects

A

Bruises
LFT

28
Q

“Rafenib” Drugs

A

Vemurafenib
Dabrafenib
Encorafenib

29
Q

“-Rafenib” drug mechanism

A

Selective Inhibition of mutated BRAF V600E ras/raf kinase

30
Q

“-Rafenib” Drug Use

A

Metastatic Melanoma

31
Q

“-Rafenib” Drug side effects

A

Joint pain
rash
diarrhea
fatigue

32
Q

“-Zomib” Drugs

A

Bortezomib
Carfilzomib
Ixazomib

33
Q

“-Zombib” Drug Mechanism

A

Specific inhibitor of Catalytic portion of 26S of proteosome

Induce G2-M Phase arrest and apoptosis of cells

34
Q

“-Zomib” drug use

A

multiple myeloma
mantel cell lymphoma

35
Q

“-Zomib” drug side effects

A

fatigue
N/D
Peripheral neuropathy
Herpes Reactivation

36
Q

Palbociclib mechanism

A

Inhibit Cyclin-Dependent Kinase 4/6

induce arrest at G1-S phase

37
Q

Palbociclib Use

A

Advanced or metastatic Breast Cancer: HR+ or HER-

used with aromatase inhibitor

38
Q

Palbociclib Side Effects

A

Myelosuppression
Pneumonitis

39
Q

Olaparib Mechanism

A

Poly (ADP-Ribose) Pol Inhibitor to decrease DNA Repair

40
Q

Olaparib Use

A

advanced or metastatic breast, ovarian, pancreatic, prostate cancer

41
Q

Olaparib Side Effects

A

Myelosuppression
Edema
Diarrhea