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Heme and Lymph Exam 1 > Cancer Pharm: Anti-tumor antibiotics > Flashcards

Cancer Pharm: Anti-tumor antibiotics Flashcards

1
Q

What are the major MOA of the anthracyclines?

A
  • Inhibition of topoisomerase II
  • Generation of free radicals
  • DNA intercalation –> blocking of DNA and RNA synthesis
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2
Q

What is the dose limited toxicity associated with the anthracyclines?

A
  • Myelosuppression mainly neutropenia
  • Some cases, mucositis
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3
Q

What is a major AE associated with anthracyclines?

A

Cardiotoxicity; both an acute and chronic form

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4
Q

Which class of cancer drugs is associated with radiation recall rxns causing erythema and desquamation of the skin at sites of prior radiation?

A

Anthracyclines

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5
Q

Which anthracycline is more active in producing complete remissions and in improving survical in pt’s with acute myelogenous leukemia?

A

Idarubicin

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6
Q

What is the MOA of the anthracycline, Mitoxantrone?

A
  • Binds and breaks strands of DNA
  • Inhibits both DNA and RNA synthesis
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7
Q

Which AE is unique to the anthracycline, Mitoxantrone?

A

Blue discoloration of the fingernails, sclera, urine

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8
Q

What is Dexrazoxane and why is it used with anthracyclines?

A
  • Iron-chelating agent
  • To prevent or reduce anthracycline-induced cardiotoxicity in women w/ metastatic breast cancer that have received a cumulative dose (>300 mg/m2) of doxorubicin
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9
Q

What is the MOA of mitomycin?

A

Activated to an alkylating agent that cross-links DNA

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10
Q

What is the best available drug for use in combo w/ radiation therapy to attack hypoxic tumor cells?

A

Mitomycin

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11
Q

During which phase of the cell cycle is Mitomycin most active?

A

Active in ALL phases of cell cycle

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12
Q

What are 2 of the unique delayed toxicities associated w/ Mitomycin?

A

Mucositis and hemolytic-uremic syndrome

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13
Q

What are the 2 uses of Mitomycin?

A
  • SCC of the anus in combo w/ 5-FU + radiation
  • Intravesical tx of superficial bladder cancer
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14
Q

What is the MOA of bleomycin; arrests cells in which phase?

A
  • DNA fragmentation and single/double strand breaks due to free radical formation
  • Cells accumulate in G2 phase *Think ‘B’leomycin = bi- = 2*
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15
Q

What is the dose limiting toxicity associated with bleomycin?

A

Pulmonary toxicity –> pneumonitis w/ cough, dyspnea, dry crackles on PE and infiltrates on CXR

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16
Q

Tyrosine kinase inhibitors are metabolized by what CYP?

A

CYP3A4

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17
Q

The tyrosine kinase inhibitor, Imatinib, specifically inhibits what?

A
  • BCR-ABL fusion protein
  • Inhibits RTK’s for PDGFR and c-kit
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18
Q

What are some of the delayed toxicities associated w/ the tyrosine kinase inhibitor, Imatinib?

A
  • Fluid retention w/ ankle and periorbital edema
  • Myalgias
  • CHF
  • Diarrhea
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19
Q

What is the clinical use for the tyrosine kinase inhibitor, Imatinib?

A
  • 1st line for chronic phase CML, in blast crisis, and as 2nd line for chronic phase CML that has progressed on prior IFN-α tx
  • GI stromal tumors expressing c-kit
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20
Q

What is the MOA for the tyrosine kinase inhibitors, Dasatinib and Nilotinib; how do they differ from Imatinib?

A
  • Inhibitor of BCR-ABL, c-kit, and PDGFR-β tyrosine kinases
  • Dasatinib binds active and inactive conformations of ABL kinase; while Nilotinib has higher binding affinity for ABL kinase
  • Overcomes imatinib resistance from mutations in BCR-ABL kinase
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21
Q

What is the clinical use for Dasatinib and Nilotinib?

A

1st line therapy of chronic phase CML

22
Q

What is the MOA of the tyrosine kinase inhibitor, Bosutinib?

A

Inhibitor of BCR-ABL tyrosine kinase

23
Q

What are the unique delayed toxicities of the tyrosine kinase inhibitor, Bosutinib?

A

Fluid retention, skin rash, and hepatotoxicity

24
Q

What is the MOA of the tyrosine kinase inhibitor, Ponatinib; why is it so useful?

A
  • Inhibits ALL known mutant forms of BCR-ABL
  • Also inhibits kinases including VEGF-R, PDGF, FGF, Flt3, TIE-2, Src family, Kit, TET and EPH
25
Which tyrosine kinase inhibitor is used in adults w/ chronic, accelerated, or blast phase CML that is resistant or intolerant to prior TKI therapy?
Ponatinib
26
What is the MOA of the GF receptor inhibitor, Cetuximab?
Antibody directed against extracellular domain of **EGFR**
27
The activity of the GF receptor inhibitor, Cetuximab, is restricted to patients with tumors expressing what?
**Wild-type *RAS***, including ***KRAS*** and ***NRAS***
28
What are 3 unique AE's of the GF receptor inhibitor, Cetuximab?
- **Acneiform skin rash** - **Hypersensitivity infusion rxn** - **Hypomagnesemia**
29
Treatment of which cancer with Cetuximab comes with a black box warning?
↑ risk of **sudden death** when combined w/ **radiation** for **head** and **neck cancer**
30
What is the MOA of the GF receptor inhibitor, Panitumumab; only efficacious in tumors with what??
- **Inhibition** of **EGFR signaling** path - Only efficaious in tumors expressing **wild-type *RAS***
31
What are the 2 unique AE's associated w/ the GF receptor inhibitor, Panitumumab?
**Acneiform skin rash** and **hypomagnesemia**
32
What is the MOA of the GF receptor inhibitor, Necitumumab?
**Inhibitor** of **EGFR** signaling path
33
The GF receptor inhibitor, Necitumumab, has the same AE's as cetuximab and panitumab with the addition of what?
**Venothrombolic** and **arterioembolic events**
34
What is the MOA of the GF receptor inhibitor, Erlotinib; who responds best to this drug?
- **Inhibitor** of the **tyrosine kinase** domaine assoc. w/ **EGFR** - Pt's who are **non-smokers** are **more responsive**
35
Unique AE's associated w/ the GF receptor inhibitor, Erlotinib?
**Acneiform rash** and **anorexia**
36
What is the MOA of the GF receptor inhibitor, Afatinib?
**Inhibitor** of tyrosine kinase domains assoc. w/ **EGFR, HER2**, and **HER4**
37
What are the unique AE's assoc. w/ Oseimertinib?
**Cardiac toxicities** --\> **QTc prolongation** and **cardiomyopathy**
38
What is the MOA of the GF receptor inhibitor, Bevacizumab?
Binds **all** forms **VEGF-A** and prevents interaction w/ target **VEGF receptors**
39
What are the 5 unique AE's of the GF receptor inhibitor, **Bevacizumab, Ziv-afibercept, and Ramucirumab**?
- **HTN** - ↑ incidence of **arterial thromboembolic events** (TIA, stroke, angina, MI) - **Wound healing** complications - **GI perforations** - **Proteinuria**
40
What is the unique MOA of the GF receptor inhibitor, Ziv-aflibercept?
**Soluble** receptor to **VEGF-A**, **VEGF-B**, and **PIGF**; binds ligands of VEGF and prevents their interactions with VEGFR
41
What is the MOA of the GF receptor inhibitor, Ramucirumab?
Targets **VEGF-R2 receptor**, inhibits binding of **VEGF-A, -C, -D** and **downstream signaling**
42
What are the 3 cancers that the VEGF-R2 receptor inhibitor, Ramucirumab can be used for?
- **Advanced gastric** or **GE junction** adenocarcinoma - **Metastatic NSCLC** - **Metastatic CRC**
43
What is the MOA of the GF receptor inhibitor, Sorafenib?
**Inhibits** multiple RTK's, including **VEGF-R2** and **R3**, **PDGFR-**β, and **raf kinase**
44
What are 4 unique AE's associated with the GF receptor inhibitor, Sorafenib?
- **HTN** - **Bleeding complications** - **Fatigue** - **Skin rash** and **hand-foot syndrome**
45
Which 2 cancers is the GF receptor inhibitor, Sorafenib, used for?
- **Advanced renal cell cancer** - Also approved for **advanced hepatocellular cancer**
46
What is the MOA of the GF receptor inhibitor, Sunitinib?
Similar to **sorafenib**, inhibits multiple RTKs: **PDGFR-α** and **β**, **VEGF-R1, R2**, and **R3**, **c-kit**
47
What are the AE's of the GF receptor inhibitor, Sunitinib?
- **HTN** - **Bleeding complications** - **Fatigue** - ↑ risk of **cardiac dysfunction**: can lead to **CHF**
48
Which 2 cancers can be treated with the GF receptor inhibitor, Sunitinib?
- **Advanced renal cell cancer** - **GI stromal tumors** after disease progression on or w/ **intolerance** to **imatinib**
49
What is the MOA of the GF receptor inhibitor, Pazopanib?
**Inhibits** multiple **RTKs**: **VEGF-R2** and **R3**, **PDGFR-β**, and **raf kinase**
50
What are 3 AE's associated with the GF receptor inhibitor, Pazopanib?
- **HTN** - **Bleeding complications** - **Fatigue**
51
Which cancer is the GF receptor inhibitor, Pazopanib, used for?
**Advanced renal cell** cancer
52
What are main AE's associated with Bleomycin?
- **Allergic rxn** - **HYPOtension** - **Skin toxicity** - **Pulmonary fibrosis** - **Mucositis**

Heme and Lymph Exam 1 (14 decks)

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