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Pharma 2- Semmelweis > B-37. Cancer chemotherapy V. (Small molecule signal transduction inhibitors) > Flashcards

B-37. Cancer chemotherapy V. (Small molecule signal transduction inhibitors) Flashcards

1
Q

Small molecule signal transduction inhibitor classes

A
  • Small molecule signal transduction inhibitor classes
    1. Bcr-Abl inhibitors
    2. EGFR inhibitors
    3. Multi-tyrosine kinase inhibitors
    4. BRAF kinase inhibitors
    5. Others
    6. mTOR inhibitors
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2
Q

Bcr-Abl inhibitor drugs

A
  • Bcr-Abl inhibitors:
    1. Ima-, Dasa-, Bosu-, and Nilotinib**
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3
Q
  • Imatinib
    • MOA
    • Kinetics
    • Indications
    • Side effects
A
  • Imatinib
    • MOA: inhibits multiple Tyr kinases (Bcr-Abl fusion protein, c-Kit, PDGFR, stem cell factor, c-kit)
    • Kinetics: oral admin (all -tinibs + -fenibs are oral!)
    • Indications: CML and ALL; GIST (c-Kit); myelodysplastic syndrome
    • Side effects:
      • Fluid retention - ankle / periorbital edema
      • GI effect - nausea, vomiting
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4
Q
  • Dasatinib
    • Indication
  • Bosutinib, Nilotinib
    • Indication
A

Dasatinib - for CML and AML only; given in imatinib-resistant cases

Bosutinib, Nilotinib - newer; for resistant CML only (in trials for GIST + neurodegenerative diseases)

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5
Q

EGFR inhibitor drugs

A
  • EGFR inhibitors:
    1. Gefi-,Erlo-, andLapatinib**
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6
Q
  • GefitinibandErlotinib
    • Indication
    • Side effects
    • Kinetics
A

GefitinibandErlotinib

  • Indication: NSCLC refractory to other treatment (both); pancreatic cc. (only erlotinib)
  • Side Effects:
    • Skin rash - papulopustular acneiform; via EGFR effects in skin
    • Diarrhea (common, mild) and ↑ LFTs
  • Kinetics: oral admin; CYP3A4 metab
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7
Q
  • Lapatinib
    • MOA
    • Indication
    • Kinetics
    • Side effects
A

Lapatinib

  • MOA: inhibits both EGFR1 and EGFR2 (Her-2)
  • Indication: Her-2+ breast cc. (if trastuzumab ineffective)
  • Kinetics: crosses BBB well → good for metastases
  • Side effects: cardiotoxicity + GI sfx
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8
Q
  • BRAF Kinase Inhibitors
    • Drug
    • MOA
A

Vemurafenib

  • MOA: inhibition of mutated BRAF (V600E) → ↓ melanoma growth / survival / metastases
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9
Q

Multi-tyrosine kinase inhibitors drugs

A
  • Multi-tyrosine kinase inhibitors:
    1. Sorafenib
    2. Sunitinib
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10
Q
  • Sorafenib
    • MOA
    • Indications
    • Side effects
A

Sorafenib

  • MOA: inhibit VEGFR-2/3, PDGFR-β
  • Indications: renal cell cc. and hepatocellular cc.
  • Side effects:
    • Skin effects - including hyperkeratosis and rashes
    • Hypertension- with ↑ risk of hemorrhage (all VEGF inhibitors); via endothelial VEGFR effects
    • Hepatoxicity
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11
Q
  • Sunitinib
    • MOA
    • Side effects
    • Indications
A

Sunitinib

  • Similar to sorafenib in sfx and MOA
  • Indications: renal cc. and GIST
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12
Q

Other small molecule signal transduction inhibitors drugs

A
  • Others:
    1. All-trans Retinoic Acid (ATRA)
    2. Bortezomib, (carfilzomib)
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13
Q
  • All-trans-retinoic acid
    • MOA
    • Kinetics
    • Indications
A

ATRA (all-trans-retinoic acid; aka tretinoin)

  • MOA: binds RAR → inhibits binding of promyelocytic leukemic factor → ↑ differentiation of leukemic cells with maturation blockage due to PML/RARA fusion protein
  • Kinetics: oral admin
  • Indications: acute promyelocytic leukemia (high remission rate); also given for severe acne
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14
Q
  • Bortezomib, (Carfilzomib)
    • MOA
    • Kinetics
    • Indications
    • Side Effects
A

Bortezomib, (Carfilzomib)

  • MOA: inhibits chymotrypsin activity of proteasome → arrest at G2-M phase → apoptosis
  • Kinetics: i.v. admin
  • Indications: multiple myeloma and mantle cell lymphoma
  • Side Effects:
    • Peripheral neuropathy - common; in 30%
    • Myelosuppression- can cause herpes zoster reactivation (prevent with acyclovir)
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15
Q

mTOR inhibitor drugs

A
  • mTOR inhibitors:
    1. Everolimus and Temsirolimus**
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16
Q
  • Everolimus, Temsirolimus
    • MOA
    • Kinetics
    • Indications
    • Side effects
A

Everolimus, Temsirolimus

  • MOA: inhibition of mRNAs coding for various glycolysis, cell cycle, etc. proteins → ↓ proliferation
  • Kinetics: oral admin
  • Indications: renal cc. (both drugs) and breast cancer (everolimus only)
  • Side Effects:
    • HS reactions - including anaphylaxis
    • Myelosuppression
    • Stomatitis

Pharma 2- Semmelweis (43 decks)

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