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Cancer Agents Flashcards

1
Q

MOA of olaparib

A

PARP inhibitor
Inhibition of poly (ADP-ribose) polymerase → ↓ repair of single-strand DNA breaks

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2
Q

Complications associated with olaparib

A
  • Myelosuppression
  • Fluid retention and edema
  • GI toxicity (e.g., diarrhea)
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3
Q

Tamoxifen MOA and indications

A

ER/PR positive, pre-menopausal

Competitive estrogen antagonist of breast tissue
Agonist of estrogen receptors for bone tissue, endometrium and myometrium

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4
Q

Complications associated with tamoxifen

A
  • Hot flushes
  • Increased risk of endometrial Ca
  • Increased VTE
  • Increased risk of uterine sarcoma
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5
Q

Aromatase inhibitors MOA and indications

A

Letrozole, anastrozole
ER/PR positive, postmenopausal

Inhibits aromatase –> decreases conversion of androstendione to estrone, decrease conversion of testosterone to estrodiol –> decrease tumour growth

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6
Q

Aromatase inhibitors side effects

A

Hot flashes
Night sweats
Vaginal dryness
Increase risk of OP
Myalgias/arthralgias

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7
Q

MOA of raloxifene

A

Competitive estrogen antagonist for breast, endometrium and myometrium
Agonist of estrogen receptor in bone tissue  inhibition of osteoclasts

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8
Q

Side effects of raloxifene

A

Increased risk of VTE and cataracts
Hot flushes
Decrease risk of endometrial Ca and uterine sarcoma

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9
Q

Trastuzumab MOA

A

For all HER2 positive tumours

Humanised monoclonal antibody against HER2 tyrosine kinase receptor –> decrease HER2 initiated cellular signalling and increase antibody-dependent cytotoxicity –> decrease tumour growth

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10
Q

Trastuzumab side effects

A
  • Cardiotoxicity, dilated cardiomyopathy
  • GI symptoms
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11
Q

Bevacizumab MOA

A

Monoclonal antibody directed against vascular endothelial growth factor. In lung cancer, can be added to platinum-based chemotherapy in patients not treated with immunotherapy

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12
Q

Bevacizumab side effects

A

Increased risk of thrombosis, stroke, myocardial infarction, and hemoptysis

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13
Q

MTX MOA

A

Antifolate agent

Inhibition of dihydrofolate reductase –> decreases formation of pyrimidine nucleotides and purine nucleotides –> decrease DNA synthesis

Inhibits AICAR transformylase

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14
Q

MTX adverse effects

A

Myelosuppression, anaemia
Hepatotoxicity
Pulmonary fibrosis, pneumonitis
Mucositis
Megaloblastic anemia
Teratogenic
Neurotoxicity

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15
Q

Pemetrexid MOA

A

Antifolate agent

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16
Q

Pemetrexid adverse effects

A

Alopecia
Erythematous pruritic rash
Desquamation
Anaemia
Pharyngitis
GI symptoms

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17
Q

Cytarabine MOA

A

Pyrimidine antagonists

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18
Q

Cytarabine adverse effects

A

Myelosuppression
Megaloblastic anaemia
Hepatotoxicity
Pancreatitis
Respiratory distress
Neurotoxicity

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19
Q

5-FU and Capecitabine MOA

A

Pyrimidine antagonists
Capecitabine - prodrug for 5-FU

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20
Q

5-FU and Capecitabine adverse effects

A

Myelosuppression
Hand foot syndrome
Cardiotoxicity
GI symptoms
Hepatotoxicity
Hyperammonemic encephalopathy

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21
Q

Gemcitabine MOA

A

Pyrimidine antagonist

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22
Q

Gemcitabine adverse effects

A

Myelosuppression
Capillary leak syndrome
HUS
Hepatotoxicity

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23
Q

6-MP/Azathioprine MOA

A

Purine antagonists
Azathioprine is prodrug for 6-MP

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24
Q

6-MP/azathioprine adverse effects

A

Myelosuppression
GI symptoms
Hepatotoxicity
Secondary malignancy

Increased SE with allopurinol and/or febuxostat

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25
Q

Fludarabine and cladribine MOA

A

Purine antagonist

Cladribine –> Hairy cell leukaemia
Fludarabien –> CLL, low grade lymphomas

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26
Q

Fludarabine adverse effects

A

Autoimmune effects
Myelosuppression
Neurotoxicity

27
Q

Cladribine adverse effects

A

Myelosuppression
Headache
Nephro/neuro/cardio/hepatotoxicity

28
Q

Hydroxyurea MOA

A

Ribonucleotide reductase inhibitors
Increases production of HbF

29
Q

Hydroxyurea adverse effects

A

Myelosuppression
Macrocytosis
Megaloblastic anaemia
Secondary malignancy
Birth defects
Pulmonary toxicity

30
Q

MOA of
Cyclophosphamide
Ifosfamide
Chlorambucil
Melphalan
Temozolomide

A

Ankylation of DNA/RNA –> reduced DNA replication

31
Q

Cyclophosphamide and Ifosfamide adverse effects

A

Bladder toxicity - haemorrhagic cystitis, bladder carcinoma
Myelosuppression
SIADH
Pulmonary toxicity
Cardiac toxicity
Infertility
Ifosfamide –> Fanconi, neurotoxicity

32
Q

Chlorambucil adverse effects

A

Myelosuppression
Oral ulcerations
GI symptoms
Pulmonary fibrosis
Infertility

33
Q

Melphalan adverse effects

A

Myelosuppression
Pulmonary toxicity
Hypokalaemia
Peripheral oedema
Secondary leukaemia

34
Q

Temozolomide adverse effects

A

Myelosuppression
Neurotoxicity
PJP

35
Q

Busulfan MOA

A

Cross-links between DNA strands –> reduced DNA replication

36
Q

Busulfan adverse effects

A

Severe myelosuppression
Pulmonary fibrosis
Hyperpigmentation
Electrolyte imbalance
Cardio/hepato/neurotoxicity

37
Q

MOA of
Cisplatin
Carboplatin
Oxaliplatin

A

Platinum based agents
Cross-links between DNA strands –> reduced DNA replication

38
Q

Platinum based agents adverse effects

A

Myelosuppression
Nephrotoxicity - Fanconi syndrome
Neurotoxicity
Ototoxicity
Chemo induced N+V

39
Q

Irinotecan/topotecan MOA

A

Topoisomerase I inhibitors

40
Q

Topoisomerase I inhibitor (irinotecan/topotecan) adverse effects

A

Myelosuppression
GI symptoms
Cholinergic syndrome
Alopecia

Irinotecan - pulmonary toxicity

41
Q

Etoposide MOA

A

Topoisomerase II inhibitors

42
Q

Etoposide adverse effects

A

Myelosuppression
Alopecia
Hypotension
Mucositis

43
Q

Vincristine and vinblastine MOA

A

Vinca alkaloids - binds and inhibition of B-tubulin –> mitotic arrest in M phase

44
Q

Vincristine adverse effects

A

Neurotoxicity
Paralytic ileus, constipation
Extravasation
Acute bronchospasm
Uric acid nephropathy

45
Q

Vinblastine adverse effects

A

Myelosuppression
Extravasation
Pulmonary toxicity

46
Q

MOA of
Docetaxel
Paclitaxel

A

Hyperstabilisation of polymerised microtubules –> mitotic arrest

47
Q

Docetaxel and paclitaxel adverse effects

A

Myelosuppression
Neuropathy
Hepatotoxicity
Hypersensitivity reactions
Nail changes
Fluid retention

48
Q

Bleomycin MOA

A

Induces formation of free radicals –> breakage of DNA strand –> cell cycle arrest of G2 and M phase

49
Q

Bleomycin adverse effects

A

Bleomycin induced lung injury
- Pulmonary fibrosis
- Bronchiolitis obliterans
- Aucte pnuemonitis
Hyperpigmentation of skin
Minimal myelosuppression
Mucositis
Alopecia

50
Q

MOA of
Doxorubicin
Daunorubicin
Idarubicin

A

Anthracyclines
Inhibitors topoisomerase II

51
Q

Anthracycle adverse effects

A

Anthracycline induced cardiotoxicity
- Dilated cardiomyopathy with systolic CHF
- Dose dependent
Myelosuppression
Alopecia
Urine discolouration
Extravasation
Infertility

52
Q

MOA of
Erlotinib
Afatinib
Osimertinib

A

EGFR TKI
Inhibits HER1/EGFR tyrosine kinase

53
Q

EGFR TKI adverse effects

A

Dermatologic toxicity
Fatigue
GI toxicity
Hepatotoxicity
Ocular toxicity
Nephrotoxicity

54
Q

MOA of
Sunitinib
Sorafenib
Pazopanib

A

VEGFR TKI
Inhibition of VEGF tyrosine kinase

55
Q

VEGFR TKI adverse effects

A

GI toxicity
Dermatologic toxicity - rash, hand foot syndrome
Cardiac toxicity
Fatigue
Thyroid toxicity

56
Q

MOA of
Alectinib
Crizotinib

A

ALK TKI
Inhibition of anaplastic lymphoma kinase

57
Q

Alectinib and crizotinib adverse effects

A

GI toxicity
Fluid retention and oedema
Dermatologic toxicity
Ocular/neuro/hepatotoxicity

58
Q

Dabrafenib and encorafenib MOA

A

V600E mutated-BRAF oncogene inhibitors

59
Q

BRAF V600E inhibitors adverse effects

A

General
- Dermatologic toxicity
- GI toxicity
- Fatigue
- QT prolongation
Cardiomyopathy
Febrile reactions
Hyperglycaemia
VTE

60
Q

Trametinib MOA

A

MEK inhibitor
Inhibits MAPK signalling pathway

61
Q

Trametinib adverse effects

A

Hepatotoxicity
Dermatologic toxicity
GI toxicity

62
Q

Palbociclib MOA

A

CDK inhibitor
Inhibits CDK 4 and 6

63
Q

Palbociclib adverse effects

A

Myelosuppression
Pulmonary toxicity

BPT Flashcards (32 decks)

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