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PHARM Heme-Onc II > Anti-neoplastic Drugs II > Flashcards

Anti-neoplastic Drugs II Flashcards

1
Q

plant alkaloid anti-cancer drugs include what classes?

A
  • mitotic inhibitors
  • topoisomerase inhibitors
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2
Q

mitotic inhibitors

  • are what kind of anti-cancer drugs?
  • include what classes?
A
  • are plant alkaloids.
    • includes:
      • vinca alkaloids: “vin”
      • taxanes: “taxel”
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3
Q

which drugs are vinca alkaloids?

A
  • vin -
    • vincristine
    • vinblastine
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4
Q

vinca alkaloids

  • are what kind of drug?
  • have what MOA?
  • have what indications?
  • AE/CI?
A

_vin_cristine, _vin_blastine

  • are mitotic inhibitors
  • MOA: prevent microtubule polymerization → no spindle formation in M-phase
    • thus, are non-DNA binding.
    • also, are vesicants: v for vesicants
  • indications: HL, NHL, others
  • AE/CI
    • both
      • GI effects (constipation)
      • alopecia
    • vincristine - peripheral neuropathy
    • vinblastine - bone marrow suppression
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5
Q

vincristine

  • what kind of drugs?
  • MOA?
  • indications?
  • AE/CI?
A
  • mitotic spindle inhibitors (vinca alkaloids)
  • MOA: prevent microtubule polymerization → no spindle formation in M-phase
    • thus, are non-DNA binding.
    • also, are vesicants: v for vesicants
  • indications: HL, NHL, others
  • AE/CI
    • peripheral neuropathies: dose-limiting toxicity
    • GI effects (constipation)
    • alopecia
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6
Q

vinblastine

  • what kind of drugs?
  • MOA?
  • indications?
  • AE/CI
A
  • mitotic spindle inhibitors (vinca alkaloids)
  • MOA: prevent microtubule polymerization → no spindle formation in M-phase
    • thus, are non-DNA binding.
    • also, are vesicants: v for vesicants
  • indications: HL, NHL, others
  • AE/CI
    • bone marrow suppression: dose limiting toxicity
    • GI effects (constipation)
    • alopecia
    • C/I: leukopenia
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7
Q

what is significant benefit of vincristine & why is this important?

A

is bone marrow sparing. thus, is desirable to combination therapy. cristine = “christ save us all”

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8
Q

compare and contrast the AEs of vinca alkaloids

A

(mitotic inhibitors)

  • both
    • GI effects
    • alopecia
  • vincristine - peripheral neuropathy
  • vinblastine - bone marrow suppression

*vincristine is bone sparing

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9
Q

which drugs are taxanes?

A
  • - taxel
    • paclitaxel
    • docetaxel
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10
Q

taxanes

  • what type of drugs?
  • MOA?
  • clinical indications
  • AEs
A

paclitaxel, docetaxel

  • are mitotic spindle inhibitors
  • MOA: inhibit microtubule dissociation
    • also, are irritants
  • clinical indications - tx of advanced cancers after anthracycline failures
  • AEs:
    • both
      • peripheral neuropathy
      • myelosuppression
    • paclitaxel - infusion rx hypersensitivity
    • docetaxel - alopecia
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11
Q

paclitaxel

  • what type of drugs?
  • MOA?
  • clinical indications
  • AEs
A
  • are mitotic spindle inhibitors (taxanes)
  • MOA: inhibit microtubule dissociation
    • also, are irritants
  • clinical indications - tx of advanced cancers after anthracycline failures
  • AEs:
    • peripheral neuropathy
    • myelosuppression - neutropenia, thrombocytopenia
    • infusion rxn hypersensitivity
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12
Q

docetaxel

  • what type of drugs?
  • MOA?
  • clinical indications
  • AEs
A
  • are mitotic spindle inhibitors (taxanes)
  • MOA: inhibit microtubule dissociation
    • also, are irritants
  • clinical indications - tx of advanced cancers after anthracycline failures
  • AEs:
    • peripheral neuropathy
    • myelosuppression - neutropenia, anemia
    • alopecia
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13
Q

compare / contrast the AEs of the taxanes

A

(mitotic inhibitors)

  • paclitaxel
    • worse peripheral neuropathy
    • neutropenia & thrombocytopenia
    • infusion rxns
  • docetaxel
    • less peripheral neuropathy
    • neutropenia & anemia
    • alopecia
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14
Q

compare and contrast the MOAs of the mitotic inhibitors

A
  • vinca alkaloids: vincristine, vinblastine
    • prevent microtubule polymerization
    • are vesicants (v = vesicant)
  • taxanes: paclitaxel, docetaxl
    • prevent microtubule dissociation
    • are irritants (taxes are irritating)
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15
Q

which mitotic inhibitor drug can caused infusion reaction hypersensitivity?

what is the antidote to this AE?

A
  • paclitaxel (a taxane)
  • tx: dexamethasone - can be given as pre-medication to prevent rxn
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16
Q

topoisomerase inhibitors

  • are what kind of anti-cancer drugs?
  • include what classes?
A
  • plant alkaloids
  • include
    • camptothecans: “tecan”
    • podophyllotoxins: “posides”
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17
Q

which drugs are camptothecins?

A

(topoisomerase inhibitors)

  • - tecans:
    • topotecan
    • irinotecan
18
Q

camptothecins

  • are what kind of drug?
  • MOA?
  • AEs?
A

-tecans: topotecan, irinotecan

  • are topoisomerase inhibitors
  • MOA: binds topo I & prevents resealing of a single strand DNA cut
    • topotecan: does not require activation
    • irinotecan: prodrug that requires activation (SN-38)
  • AEs:
    • topotecan - myelosuppression ; neutropenia, anemia
    • irinotecan - diarrhea (d/t SN38 form)
19
Q

irinotecan

  • is what kind of drug?
  • MOA?
  • AEs/CIs?
A
  • a topoisomerase inhibitor
  • MOA: binds topo I & prevents resealing of a single strand DNA cut
    • A PRODRUG that requires conversion to active form, SN-38, in the liver
  • AEs:
    • diarrhea - d/t SN38 accumulation
20
Q

a UGT-1A1 molecular assay is necessary before treatment with which anti-cancer drug?

why?

A

irinotecan

(a camptothecin topoisomerase inhibitor)

UGT1A1 removes SN-38, irinotecan’s active (but potentially toxic) form. defective UGT-1A1 could lead SN-38 accumulation → excessive cholinergic stimulation → diarrhea

21
Q

which drugs are podophylotoxins?

A
  • posides:
    • etoposide
    • teniposide
22
Q

podophylotoxins

  • what kind of drug?
  • MOA?
  • AEs/CIs?
A

posides: etoposide, teniposide

  • topoisomerase inhibitors
  • MOA: inhibit topoisomerase II → double strand breaks
  • AEs/CIs
    • both: secondary malignancies
    • etoposide - infusion rxns → hypotension
    • teniposide - severe myelosuppresision
23
Q

etoposide

A
  • topoisomerase inhibitor ( podophyllotoxins)
  • MOA: inhibit topoisomerase II → double strand breaks
  • AEs/CIs
    • secondary malignancies
    • infusion rxns → hypotension
24
Q

contrast the MOAs of the topoisomerase inhibitors

A
  • camptothecins: inhibit topoisomerase I
    • topothecan (active drug)
    • ironothecans (produg, active form = SN-38)
  • podophyllotoxins: inhibit topoisomerase II
    • etoposide
    • teniposide
25
contrast the AEs of the topoisomerase inhibitors
(toposisomerase inhibitors) * camptothecins: * topothecan - myelosuppression * ironothecans - diarrhea * podophyllotoxins: both cause secondary malignancies * etoposide - infusion reaction * teniposide - severe myelosuppression
26
what are the anti-cancer antibodies?
* trastuzumab * T-DMI * pertuzumab * pembrolizumab * bevacizumab * brentuximab vedotin * rituximab / alamtuzumab / natalizumab
27
trastuzumab * what kind of drug? * MOA? * indications? * AEs?
* anti-cancer antibody * binds **HER-2 receptors** → blocking cancer cell replication * indications: HER-2+ cancers * **breast cancer** * **gastric cancer** * pancreatic cancer * AES: * **cardiotoxicity** - “hand over heart, in god we _trust"_ * **fatigue** * anthenia * pain
28
T-DMI * what kind of drug? * MOA? * indications? * AEs?
* anticancer antibody * MOA: T-DMI = complex of _trastuzumab_ & _emtansine_ (toxin carrying vesicle). * T-DMI binds to **HER-2R** expressing cells only → **releases toxin** → cell arrest * indications: **HER-2 + patients who failed trastuzumab therapy** * AE**: well tolerated**
29
pembrolizumab * what kind of drug? * MOA? * indications? * AEs?
* anticancer antibody * MOA: immune checkpoint inhibitor * binds **PD-I** (**programmed cell death inhibitor)** on **T-cells** → apoptosis * indications: many cancers * AEs: **GI side effects**
30
bevacizumab * what kind of drug * MOA * AEs
* anticancer antibody * MOA: inhibits **VEGF → preventing angiogenesis** & thus tumor growth * AEs: * **wound healing complications** * proteinurea * thromboembolism
31
brentuximab vedotin * what kind of drug * MOA * AEs
* anticancer antibody * MOA: is an **Ab-drug conjugate** that targets **CD-30** expressing cells → **releases MMAE** (**anti-tubulin toxin**) → apoptosis * AE - **peripheral neuropathy**
32
natalizumab * what kind of drug * MOA * indications * AEs
* anti-cancer antibodies * MOA: **blocks alpha-4-inegrin** (adhesion molecule) on lymphocytes * indications: **B-cell malignancies resistant to rituximab** * AEs: **inc risk of opportunistic infections**
33
which anti-cancer antibodies are used to treat HER-2 cancers & what are their AEs?
* **trastuzumab:** * **cardiotoxicity** * **fatigue** * asthenia * pain * **TMD-I - n/a** * **pertuzumab - diarrhea**
34
which anticancer antibodies cause an increased risk of infections?
* ritixumab - slightly increased risk of infection * natalizumab - inc risk of _opportunistic infection_
35
which anticancer drug leads to poor wound healing?
bevacizumab
36
list the anticancer antibodies that bind CD molecules and which ones they bind
* brentuximab vedotin: CD-30 * ritixumab: CD-20 (B-lymphocytes) * alamtuzuamb: CD52 (B & T lymphocytes)
37
which anti-cancer antibody binds PD-1?
pembrolizumab
38
imatinib * what kind of drug? * MOA? * indication? * AEs?
* **tyrosine kinase inhibitor** * MOA: inhibitors specific tyrosine kinase receptors → apoptosis * indication: tyrosine kinase dependent tumors * AE: **fluid retention - edema, HF**
39
bortezomib * what kind of drug? * MOA? * indication? * AE?
* proteasome inhibitor * MOA: breaks down proteosome (**protein disposal unit**) * indication: multiple myeloma * AE: **fluid retention** - edema, hypotensio, HF
40
palbociclib * what kind of drug? * MOA? * indication? * AE?
* **a small molecule inhibitor** * **inhibits CDK4 & CDK6** (cell cycle enzymes) * indication: CDK4 & CDK6 dependent tumors * AE: mild myelosuppression
41
which anti-cancer drugs cause _infusion reactions_?
* paclitaxel (mitotic inhibitor) * etoposide (topo II inhibitor) * bevacizumab (Ab) * rituximab (Ab)
42
which anti-cancer drugs can cause edema & HF?
* imatinib (tyrosine kinase inhibitor) * bortezomib (proteasome inhibitor) both cause fluid retention

PHARM Heme-Onc II (3 decks)

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