2023-10-21T02:03:50+03:00[Europe/Moscow] en true <p>erlotinib, gefitinib, afatinib, osimertinib</p>, <p>forms an irreversible/covalent bond with a groove near K-RAS mutation locking it into off state</p>, <p>GTP; GDP</p>, <p>Tyr-K domain; competitive inhibition; ATP</p>, <p>c</p>, <p>immature; VEGF</p>, <p>prevent new vessels + destroys recent ones</p>, <p>bevacizumab</p>, <p>recognize/destroy neoplastic cells before they become clinically meaningful </p>, <p>CTLA-4; PD-1</p>, <p>T-cell death; inactivation</p>, <p>act on T-cells &amp; prevent their inactivation</p>, <p>act on the ligand expressed by tumor cells that inactivates T-cells</p>, <p>nivolumab, pembrolizumab</p>, <p>atezolizumab, durvalumab </p>, <p>ipilimumab </p>, <p>blocks CTLA-4 suppressive signal; maintains T-cell activation </p>, <p>resistance eventually develops </p> flashcards
Pharmacology of Targeted Therapy/Immune therapy

Pharmacology of Targeted Therapy/Immune therapy

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  • erlotinib, gefitinib, afatinib, osimertinib

    What are EGFR inhibitors? (4)

  • forms an irreversible/covalent bond with a groove near K-RAS mutation locking it into off state

    Sotorasib MOA?

  • GTP; GDP

    K-RAS turns on when _____ binds to it & off when ______ binds to it.

  • Tyr-K domain; competitive inhibition; ATP

    EGFR inhibits the ________ by ________ of __________ binding.

  • c

    Which is a humanized mAB?

    a) Erlotinib

    b) Sotorasib

    c) Bevacizumab

    d) Ipilimumab

  • immature; VEGF

    Tumor vessels are ________ and depend on _______ to mature and

    stabilize.

  • prevent new vessels + destroys recent ones

    What is Anti-VEGF function? (2)

  • bevacizumab

    What is our VEGF inhibitor?

  • recognize/destroy neoplastic cells before they become clinically meaningful

    What is the role of the immune system?

  • CTLA-4; PD-1

    What are the Immune checkpoints? (2)

  • T-cell death; inactivation

    Activation of immune checkpoints leads to ________ or _________.

  • act on T-cells & prevent their inactivation

    Anti-PD-1 MOA?

  • act on the ligand expressed by tumor cells that inactivates T-cells

    Anti-PD-L1 MOA?

  • nivolumab, pembrolizumab

    What are the Anti- PD1 inhibitors? (2)

  • atezolizumab, durvalumab

    What are the Anti- PD- L1 inhibitors? (2)

  • ipilimumab

    What is the CTLA-4 inhibitor?

  • blocks CTLA-4 suppressive signal; maintains T-cell activation

    CTLA-4 inhibitor MOA?

  • resistance eventually develops

    What is the problem with BRAF-mutation therapeutics?