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SBL > 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
Q

Which tyrosine kinase inhibitor is used in adults w/ chronic, accelerated, or blast phase CML that is resistant or intolerant to prior TKI therapy?

A

Ponatinib

26
Q

What is the MOA of the GF receptor inhibitor, Cetuximab?

A

Antibody directed against extracellular domain of EGFR

27
Q

The activity of the GF receptor inhibitor, Cetuximab, is restricted to patients with tumors expressing what?

A

Wild-type RAS, including KRAS and NRAS

28
Q

What are 3 unique AE’s of the GF receptor inhibitor, Cetuximab?

A
  • Acneiform skin rash
  • Hypersensitivity infusion rxn
  • Hypomagnesemia
29
Q

Treatment of which cancer with Cetuximab comes with a black box warning?

A

↑ risk of sudden death when combined w/ radiation for head and neck cancer

30
Q

What is the MOA of the GF receptor inhibitor, Panitumumab; only efficacious in tumors with what??

A
  • Inhibition of EGFR signaling path
  • Only efficaious in tumors expressing wild-type RAS
31
Q

What are the 2 unique AE’s associated w/ the GF receptor inhibitor, Panitumumab?

A

Acneiform skin rash and hypomagnesemia

32
Q

What is the MOA of the GF receptor inhibitor, Necitumumab?

A

Inhibitor of EGFR signaling path

33
Q

The GF receptor inhibitor, Necitumumab, has the same AE’s as cetuximab and panitumab with the addition of what?

A

Venothrombolic and arterioembolic events

34
Q

What is the MOA of the GF receptor inhibitor, Erlotinib; who responds best to this drug?

A
  • Inhibitor of the tyrosine kinase domaine assoc. w/ EGFR
  • Pt’s who are non-smokers are more responsive
35
Q

Unique AE’s associated w/ the GF receptor inhibitor, Erlotinib?

A

Acneiform rash and anorexia

36
Q

What is the MOA of the GF receptor inhibitor, Afatinib?

A

Inhibitor of tyrosine kinase domains assoc. w/ EGFR, HER2, and HER4

37
Q

What are the unique AE’s assoc. w/ Oseimertinib?

A

Cardiac toxicities –> QTc prolongation and cardiomyopathy

38
Q

What is the MOA of the GF receptor inhibitor, Bevacizumab?

A

Binds all forms VEGF-A and prevents interaction w/ target VEGF receptors

39
Q

What are the 5 unique AE’s of the GF receptor inhibitor, Bevacizumab, Ziv-afibercept, and Ramucirumab?

A
  • HTN
  • ↑ incidence of arterial thromboembolic events (TIA, stroke, angina, MI)
  • Wound healing complications
  • GI perforations
  • Proteinuria
40
Q

What is the unique MOA of the GF receptor inhibitor, Ziv-aflibercept?

A

Soluble receptor to VEGF-A, VEGF-B, and PIGF; binds ligands of VEGF and prevents their interactions with VEGFR

41
Q

What is the MOA of the GF receptor inhibitor, Ramucirumab?

A

Targets VEGF-R2 receptor, inhibits binding of VEGF-A, -C, -D and downstream signaling

42
Q

What are the 3 cancers that the VEGF-R2 receptor inhibitor, Ramucirumab can be used for?

A
  • Advanced gastric or GE junction adenocarcinoma
  • Metastatic NSCLC
  • Metastatic CRC
43
Q

What is the MOA of the GF receptor inhibitor, Sorafenib?

A

Inhibits multiple RTK’s, including VEGF-R2 and R3, PDGFR-β, and raf kinase

44
Q

What are 4 unique AE’s associated with the GF receptor inhibitor, Sorafenib?

A
  • HTN
  • Bleeding complications
  • Fatigue
  • Skin rash and hand-foot syndrome
45
Q

Which 2 cancers is the GF receptor inhibitor, Sorafenib, used for?

A
  • Advanced renal cell cancer
  • Also approved for advanced hepatocellular cancer
46
Q

What is the MOA of the GF receptor inhibitor, Sunitinib?

A

Similar to sorafenib, inhibits multiple RTKs: PDGFR-α and β, VEGF-R1, R2, and R3, c-kit

47
Q

What are the AE’s of the GF receptor inhibitor, Sunitinib?

A
  • HTN
  • Bleeding complications
  • Fatigue
  • ↑ risk of cardiac dysfunction: can lead to CHF
48
Q

Which 2 cancers can be treated with the GF receptor inhibitor, Sunitinib?

A
  • Advanced renal cell cancer
  • GI stromal tumors after disease progression on or w/ intolerance to imatinib
49
Q

What is the MOA of the GF receptor inhibitor, Pazopanib?

A

Inhibits multiple RTKs: VEGF-R2 and R3, PDGFR-β, and raf kinase

50
Q

What are 3 AE’s associated with the GF receptor inhibitor, Pazopanib?

A
  • HTN
  • Bleeding complications
  • Fatigue
51
Q

Which cancer is the GF receptor inhibitor, Pazopanib, used for?

A

Advanced renal cell cancer

52
Q

What are main AE’s associated with Bleomycin?

A
  • Allergic rxn
  • HYPOtension
  • Skin toxicity
  • Pulmonary fibrosis
  • Mucositis

SBL (44 decks)

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