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HemOnc Week 4 > LM 12.1: Systemic Therapies for Cancer > Flashcards

LM 12.1: Systemic Therapies for Cancer Flashcards

1
Q

what’s the rationale behind targeted cancer therapy?

A

understanding the molecular dependencies and vulnerabilities (weaknesses) and use that to exploit cancer

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2
Q

what three things dictate if a cancer cell proliferates or dies?

A
  1. network of regulatory factors like TF and transcription repressors
  2. tumor microenvironemtn like growth factors and cytokines, M2 macrophages and high collagen content
  3. stress signals like DNA damage

oncogenes and tumor suppressor genes oppose each other

the net effect of these interactions along with the help from the tumor microenvironment (TME) and DNA damage dictate cancer growth.

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3
Q

what is targeted therapy?

A

refers to a new generation of anti-cancer agents designed to interfered with a specific molecular target that plays a critical or vital role in tumor progression and
metastasis

targeted therapy aims to fight the tumor only based on its unique vulnerabilities

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4
Q

what is conventional therapy?

A

more empirical and is based on non-specific cytotoxic chemotherapeutics

conventional therapy targets the entire body of the patient

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5
Q

what are targeted anticancer agents?

A

can be small molecule inhibitors or humanized neutralizing antibodies

typically the names of small molecule inhibitors (SMI) end in “ib” or “in” or “stat”

therapeutic monoclonal antibodies en in “mab”

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6
Q

what is erlotinib?

A

small molecule inhibitors (SMI)

an inhibitor that targets epidermal growth factor receptor (EGFR)

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7
Q

what is midostaurin?

A

small molecule inhibitors (SMI)

targets FLT3 receptor

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8
Q

what is Transtuzumab?

A

therapeutic monoclonal antibodies

monoclonal antibody targeting human epidermal growth factor receptor 2 (HER2)

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9
Q

how do you differentiate between human and mouse genes?

A

human genes are capitalized and mouse genes are lower case

SRC vs src

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10
Q

what are monoclonal antibodies?

A

they target antibodies

mab = monoclonal antibody

ximab = chimeric human-mouse antibody

zumab = humanized mouse antibody

mumab = fully human antibodies

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11
Q

what is personalized medicine?

A

identifies the somatic mutations or application of pathway networks in the cancer lesions of patients and targeting them accordingly

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12
Q

what is precision medicine?

A

this phrase was favored over “personalized medicine” because the tumors are precisely targeted for driver mutations and key amplified pathways

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13
Q

do you usually treat cancer with one drug?

A

targeted mono therapy (one drug against a given target) often doesn’t work because there’s drug resistance and cancer relapse

so you usually do a combination of drugs with or without radiotherapy

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14
Q

what are the different combinations of treatment you can do to treat cancer?

A
  1. surgery followed by mono- or radiotherapy
  2. targeted therapy + conventional chemo
  3. targeted therapy against two molecules simultaneously
  4. targeted therapy combined with immunotherapy
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15
Q

what are A1 targeting agents?

A

they target DNA replication, transcription and DNA damage repair

A1 drugs target:
1. topoisomerase

  1. epigenetic factors (HDACs)
  2. poly ADP ribose polymerase
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16
Q

what drugs target topoisomerase?

A

epirubicin

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17
Q

what drugs target HDACs?

A

romidepsin (istodax)

panobinostat (farydak)

belinostat (beleodaq)

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18
Q

which drugs target poly ADP ribose polymerases?

A

rucaparib (rubraca)

olaparib (lynparza)

niraparib (zejula)

19
Q

what are A2 systemic targeting agents?

A

they target the cell cycle

the issue with these is that when cell cycle inhibitors are employed, all actively dividing cells in the body are targeted

so patients of reproductive age may have side effects and immune surveillance of tumors are further compromised

positive effects may be on pro-tumor immune cells like M2 macrophages and regulatory T cells

A2 drugs target CDK4/6 and HDM2

20
Q

which drugs target CDK4/6?

A

palbociclib (ibrance)

ribociclib (kisqali)

21
Q

what do drugs that target HDM2 do?

A

HDM2 is a homolog of MDM2 and regulates p53 by degrading it

so inhibition of HDM2 would up regulate p53 and give cells control over their cell cycle

however, HDM2 inhibitors will only work if the p53 is a wild type and will NOT work if p53 is mutated or deleted

22
Q

what are A3 systemic targeting agents?

A

they target cell signaling

they target:
1. receptor tyrosin kinases

  1. G-protein coupled receptors (GPCRs)
  2. hormone receptors
  3. other kinases
23
Q

what are the different types of receptor tyrosine kinases that A3 targeting agents target?

A
  1. EGF receptor
  2. human EGF receptor 2 (HER2)
  3. vascular endothelial growth factor receptor 2 (VEGFR2)
  4. Janus Kinase 1/2 (JAK1/2)
  5. insulin-like growth factor 1 receptor (IGF1-R)
24
Q

which drugs target EGF receptors?

A
  1. monoclonal antibodies
    - cetuximab
    - panitimumab
  2. SMI
    - tyrosine kinase inhibitors (TKIs)
  • erlotinib
  • gefitinib
25
Q

what is osimertinib?

A

SMI against EGFR T790M mutation in non-small cell lung cancer

26
Q

what does afatinib do?

A

SMI against EGFR exon 19 deletion or exon 21 substitution

27
Q

which drugs target HER2?

A

monoclonal antibodies = trastuzumab and pertuzumab

SMI = lapatinib

28
Q

which drugs target VEGFR2?

A

lenvatinib

ramucirumab

29
Q

which drug targets JAK1/2?

A

ruxolitinib

30
Q

which drug targets JAK3?

A

tofacitinib

31
Q

which hormone receptors are targeted by systemic targeting agents?

A

estrogen receptors

progesterone receptors

androgen receptors

32
Q

which drug targets IL-6R?

A

tocilizumab

33
Q

what is ALK?

A

anaplastic lymphoma kinase

ALK is an established target in ALK-rearranged non-small lung cancer and pediatric tumors

34
Q

which drugs target ALK?

A

crisotinib

brigatinib

35
Q

which drug targets BRAF?

A

dabrafenib

vemurafenib

BRAF is often mutated in melanoma

36
Q

what disease is N-RAS associated with?

A

melanoma

37
Q

which drug targets SRC?

A

dasatinib

38
Q

what do A4 systemic targeting agents target?

A

cell metabolism

they include antimetabolites (methotrexate), purine analogs (6-mercaptopurine), and pyrimidine analogs (5-FU)

39
Q

what do A5 systemic targeting agents target?

A

protein synthesis

ex. mTOR

40
Q

what do A6 systemic targeting agents target?

A

anti-apoptotic proteins

41
Q

what do A7 systemic targeting agents target?

A

proteasomes

42
Q

what do B1 systemic targeting agents target?

A

angiogenesis

43
Q

what do C1 systemic targeting agents target?

A

immunotherapy

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