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Pharma 2nd semester > B.36. Cancer Chemotherapy V (small molecule signal transduction inhibitors) > Flashcards

B.36. Cancer Chemotherapy V (small molecule signal transduction inhibitors) Flashcards

1
Q

common characteristics of small-molecule TKI

A
  1. orally active
  2. once-daily dosing
  3. hepatic P450 metabolism
  4. act intracellularly
  5. act on mutated, constitutively active receptors that no longer rely on ligand binding
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2
Q

list the small molecules signal-transducing inhibitors

A 
"-nib"--> TK inhibitor 
Imatinib
Gefitinib
Erlotinib
Lapatinib
Sunitinib
Ibrutinib
Crizotinib
Trametinib (+Dabrafenib)

Bortezomib
Everolimus
Tretinoin-ATRA

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3
Q

what is Imatinib and what is its function?

A

Tyrosine Kinase inhibitor

binds to the BCR-ABL1 fusion gene and inhibits protein activity

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4
Q

what is Imatinib used for?

A

CML (positive Philadelphia chromosome translocation)
Gastrointestinal stromal tumors (+ for C-kit tyrosine kinase)
ALL

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5
Q

what are the side effects of Imatinib?

A 
Diarrhea, nausea, vomiting 
Myalgia
Fluid retention, peripheral edema
CHF
hepatotoxicity
bone marrow suppression
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6
Q

what mutation causes resistance to Imatinib?

A

T315I mutation

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7
Q

what are Gefitinib and Erlotinib?

A 
EGFR antagonists (1st generation) 
inhibits the TK domain of the receptor
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8
Q

indications for Gefitinib and Erlotinib?

A

non-small cell lung carcinoma

Erlo–> pancreatic cancer

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9
Q

side effects of Gefitinib, Erlotinib and Lapatinib

A

rash (acne-like)
Diarrhea

lapatinib–> cardiotoxicity

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10
Q

what is Lapatinib?

A

tyrosine kinase inhibitor

HER2/neu and EGFR pathways

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11
Q

when do we use Lapatinib?

A

Breast cancer (HER2 positive)

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12
Q

what is Sunitinib?

A

Receptor tyrosine kinase inhibitor

Antiangiogenic (PDGF-R, VEGF-R) –> limits vascularization to the tumor

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13
Q

when do we use Sunitinib?

A

Renal cell carcinoma

Imatinib resistant GIST (mutant c-kit)

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14
Q

side effects of Sunitinib

A

HYPERTENSION!

bleeding, nausea, diarrhea, vomiting

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15
Q

Side effects of Ibrutinib

A

most important:
hypertension
secondary malignancies–> non-melanoma skin cancers

also: URTI, sinusitis, myelosuppression

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16
Q

what is Ibrutinib?

A

TK inhibitor

binds to Bruton’s tyrosine kinase in B-cells and inhibit their activation

17
Q

indications for Ibrutinib

A

CLL
Waldenström macroglobulinemia
mantle cell lymphoma
marginal zone lymphoma

18
Q

what is Crizotinib?

A

ALK kinase inhibitor

ROS1 oncogene inhibitor

19
Q

when do we give Crizotinib?

A

non-small cell lung carcinoma

20
Q

when do we give Bortezombin?

A

multiple myeloma

21
Q

when do we give the combination Dabrafenib +Trametinib?

A

malignant melanoma

22
Q

side effects of Crizotinib

A

Nausea, vomiting, diarrhea
GI perforations
hepatotoxicity

23
Q

side effects of Bortezomib?

A

peripheral neuropathy
thrombocytopenia
heart failure, hypotension

24
Q

what is Bortezomib?

A

proteasome inhibitor

results in down-regulation of the NFᴋB signalling pathway

25
Q

what is Dabrafenib?

A

BRAF inhibitor

26
Q

what is Trametinib?

A

MEK inhibitor

27
Q

what are the side effects of dabrafenib and trametinib?

A

skin problems
dabrafenib–> hyperkeratosis, hand-foot syndrome
trametinib–> acneiform dermatitis, rash

28
Q

what is Everolimus?

A

mTOR inhibitor

Derivative of sirolimus

29
Q

when is Everolimus used?

A

HER2 negative breast cancer
renal cell carcinoma
neuroendocrine tumors
liver, renal transplantation

30
Q

side effects of Everolimus

A

stomatitis
infections
diarrhea
intestinal pulmonary disease

31
Q

what is Tretinoin-ATRA( all-trans retinoic acid)?

A

Vitamin A derivative

32
Q

what does Tretinoin-ATRA do

A

binds to retinoid X receptor (RXR) and retinoic acid receptor (RAR)
is a differentiating agent–> promotes differentiation of promyelocytes

33
Q

when is Tretinoin used?

A

AML-M₃ type (acute promyelocytic leukemia)
*used as adjunct to chemotherapy
acne (topical agent)

34
Q

side effects of Tretinoin

A

‘Differentiation syndrome’ (leukocyte maturation sy.)–> fever, ARDS, pleural and pericardial effusion, AKI
CNS symptoms
dry skin
osteomalacia

Pharma 2nd semester (49 decks)

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