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PHRM 864: Therapeutics IV > Immune Therapy-Oncology > Flashcards

Immune Therapy-Oncology Flashcards

1
Q

REVIEW: What drug is able to target HER2?

A
  • Tucatinib
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2
Q

REVIEW: What drugs targets a kinases that is produced by the formation of the Philadelphia chromosome?

A
  • Imatinib
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3
Q

REVIEW: What drugs is not a covalent kinase inhibitor?

A
  • Gefitinib
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4
Q

What was the first attempt to use immunotherapy?

A
  • Coley’s Toxin: Basically bacteria that was injected into the tumor to start immune response
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5
Q

Within the cells of the immune system, which one are the most important?

A
  • T & B Cells [Adaptive Immunity]
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6
Q

What are B Cells?

A
  • Antibody producing cells
  • B Cell is triggered by antigen and engulfs it, that makes antigen fragments to help attract the matching T Cell with makes the antibodies
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7
Q

What are some of the common nomenclatures for monoclonal antibodies?

A

Stem:
- mab
Substem:
- Mouse: -o-
- Chirmeric: -xi-
- Humanized: -zu-
- Fully Human: -u-

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8
Q

What does it mean when antibodies are two tiered?

A
  • They are able to affect several cancer events
  • Binding several antibodies to the cancer surface could lead to CDC, ADCC, and elimination of the Tumor cell
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9
Q

What is CDC and ADCC in terms of cancer and oncolgy?

A
  • CDC: Complement-dependent cytotoxicity
  • ADCC: antibody-dependent cellular cytotoxicity
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10
Q

What are the HER2 monoclonal antibodies that are used?

A
  • Trastuzumab & Pertuzumab
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11
Q

What is the mechanism of action for trastuzumab?

A
  • bind to the HER2 receptor and induce cytotoxicity [calling over NK cells]
  • Will also decrease HER2 on the surface with degradation
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12
Q

What is the primary indication for Trastuzumab?

A
  • Treatment of breast cancers with HER2 overexpression
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13
Q

What are some of the toxicites that are for Trastuzumab?

A
  • Flu-like symptoms, Cardiomyopathy [increased with Adriamycin], NO myelosuppression
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14
Q

What is the important thing to know about Trastuzumab?

A
  • Humanized monoclonal antibody for HER2
  • Linked to Human IgG kappa?
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15
Q

What is the mechanism of action for Pertuzumab?

A
  • Binds to HER2 to inhibit dimerization [dimerization is important for HER2 reponses]
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16
Q

What is the important thing to know about Pertuzumab?

A
  • Humanized monoclonal antibody for HER2
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17
Q

What is the CLEOPATRA trial?

A
  • It showed that Pertuzumab+Trastuzuamb was great
  • NO differences in safety and increased survival
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18
Q

What was some ways that Fc engineering improved therapeutic antibodies?

A
  • Margetuximab: increase in CD16A [NK Cells] & decrease in DC32B [B cells]
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19
Q

What are the EGFR monoclonal antibodies that are using cancer?

A
  • Cetuximab & Panitumumab
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20
Q

What is the mechanism of action for Cetuximab?

A
  • Binds to extra cellular EGFR that inhibits EGR & TGF leading to inhibition of Cell Growth and induce apoptosis
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21
Q

What is the primary indication for Cetuximab?

A
  • Treatment for colorectal, head, and neck
22
Q

What is important to know about Cetuximab?

A
  • Chimeric antibody
23
Q

What are some of the toxicities for Cetuximab?

A
  • infusion reactions [1st dose]
  • Rash
  • Muscle weakness
  • Fever
24
Q

What is the mechanism of action for Panitumumab?

A
  • Binds to the EGFR and inhibits the binding of EGF and TGF that leads to inhibition of cell growth and induce apoptosis
25
Q

What are the side effects of Panitumumab?

A
  • Skin rash
  • Diarrhea
26
Q

What is important to know about Panitumumab?

A
  • Fully humanized monoclonal anitbody
27
Q

What is the mechanism of action for Bevacizumab?

A
  • Binds to VEGF that blocks the intercalation with endothelial receptor stoping cell proliferation
28
Q

What is important to know for Bevacizumab?

A
  • NOT good as single agent [combom with 5-FU]
  • Humanized monoclonal antibody
29
Q

Which one of the following antibodies targets HER2?

A] Neratinib
B] Cetuximab
C] Lapatinib
D] Pertuzumab

A
  • Pertuzumab
30
Q

What was the first immunotherapy?

A
  • Coley Toxin
31
Q

What type of antibody is fakeumab?

A
  • Fully Human
32
Q

What are the important B cell markers?

A
  • CD20: affects the middle
  • CD19: whole thing
  • CD38: Early - Mid - End
33
Q

How does CD20 work within B-Cell Receptors?

A
  • Drives the proliferation [plays a role in lymphoma]
  • Antibodies binding to CD20 can inhibit cell prliferation AND induce antibody-dependent cytotoxcity
34
Q

How does CD38 work in B Cells?

A
  • CD38 are highly expressed in plasma B cells that make antibodies [eliiminate multiple myeloma by ADCC and CDC
35
Q

What is the mechanism of action for Trastuzumab-Emtansine [TDM1]?

A
  • Binds to HER2 and enters the cell inhibiting microtubule assebly
36
Q

What is important to know about Tratuzumab-Emtansine?

A
  • Has BOTH cytoxic agent [Emtansine] & monoclonal antibody [Tratuzumab]
37
Q

What are the toxicities of Trastuzumab-Emtansine?

A
  • Adverse events of trastuzumab
  • Thrombocytopenia
  • Hepatotoxicity
38
Q

What is the way that T-cells are made?

A
  • Start in the bone marrow that moves to the thymus to mature
  • T cell combines with MHC to become active and kill the cell
  • T cells decrease making memory
39
Q

What are some of the Bispecific T-cell Engagers [BiTE]?

A
  • Blinatumomab, Mosunetuzumab,Teclistamab, Taquetamab
40
Q

What is the mechanism of action for Blinatumomab?

A
  • Binds to CD3 to bring an activated T-cell into range of CD19; which is highly expressed on B cell and Leukemia [lyase tumor]
  • NOT chimeric
41
Q

What is the mechanism of action for Mosunetuzumab?

A
  • Targets CD3 and CD20 on non-Hodgkins
42
Q

What is the mechanism of action for Teclistamab?

A
  • Targets T cells and B cells on Myeloma cells
43
Q

What is the mechanism of action for Taquetamab?

A
  • Targets CD3 and Human GPRC5D on Myelona cells
44
Q

What acts as “brakes” or “checkpoints” on the immue system?

A
  • CTLA-4 and PD1
45
Q

What drugs affect CTLA-4 and PD1?

A
  • Ipilimumab, Pembrolizumab, Atezolizumab
46
Q

What is the mechanism of action for Ipilimumab?

A
  • Binds to CTLA-4 and reverse the CTL inhibition [CTL can destroy tumors]
  • Treatment for metastatic melanoma
47
Q

What are the side effects of Ipilimumab?

A
  • GI issues
  • Dermatitis
48
Q

What is the mechanism of Pembrolizumab?

A
  • Binds the PD-1 receptor and blocks its interaction with PD-L1/2 leading to tumor killing
49
Q

What is important to know about pembrolizumab?

treatment?

A
  • PD-1 = T cell
  • PD-L1 = Tumor Cells
  • Treatment for Metastatic melanoma [following Ipilimumab & BRAF] and NSCLC [PD-L1+]
50
Q

What is the mechanism of action for Atezolizumab?

A
  • Binds to PD-L1 and blocks the interaction with PD-1
51
Q
A

PHRM 864: Therapeutics IV (28 decks)

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