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Tyler's Cards > Class and MOA > Flashcards

Class and MOA Flashcards

1
Q

What drugs are in the Alkylating Agents class?

A

Drugs in this class are:
- Cyclophosphamide
- lfosfamide
- Busulfan
- Melphalan
- Bendamustine

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2
Q

What is the class and MOA of Cyclophosphamide?

A

This drug in the following class:
- Alkylating Agents

This drug’s MOA is as follows:
- Alkylates and cross-links DNA preventing DNA synthesis and cell division

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3
Q

What is the class and MOA of lfosfamide?

A

This drug in the following class:
- Alkylating Agents

This drug’s MOA is as follows:
- Alkylates and cross-links DNA preventing DNA synthesis and cell division

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4
Q

What is the class and MOA of Busulfan?

A

This drug in the following class:
- Alkylating Agents

This drug’s MOA is as follows:
- Alkylates and cross-links DNA preventing DNA synthesis and cell division

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5
Q

What is the class and MOA of Melphalan?

A

This drug in the following class:
- Alkylating Agents

This drug’s MOA is as follows:
- Alkylates and cross-links DNA preventing DNA synthesis and cell division

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6
Q

What is the class and MOA of Bendamustine?

A

This drug in the following class:
- Alkylating Agents

This drug’s MOA is as follows:
- Alkylates and cross-links DNA preventing DNA synthesis and cell division

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7
Q

What drugs are in the Anti-Androgens class?

A

Drugs in this class are:
- Flutamide
- Abiraterone acetate
- Apalutamide
- Bicalutamide
- Enzalutamide
- Nilutamide
- Darolutamide

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8
Q

What is the class and MOA of Flutamide?

A

This drug in the following class:
- Anti-Androgens

This drug’s MOA is as follows:
- Non-steroidal anti-androgen that inhibits androgen uptake and inhibits binding of androgen in target tissues

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9
Q

What is the class and MOA of Abiraterone acetate?

A

This drug in the following class:
- Anti-Androgens

This drug’s MOA is as follows:
- Selectively and irreversibly inhibits CYP17 an enzyme required for biosynthesis and inhibits the formation of testosterone

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10
Q

What is the class and MOA of Apalutamide?

A

This drug in the following class:
- Anti-Androgens

This drug’s MOA is as follows:
- Nonsteroidal androgen receptor antagonist

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11
Q

What is the class and MOA of Bicalutamide?

A

This drug in the following class:
- Anti-Androgens

This drug’s MOA is as follows:
- Non-steroidal anti-androgen that inhibits androgen uptake and inhibits binding of androgen in target tissues

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12
Q

What is the class and MOA of Enzalutamide?

A

This drug in the following class:
- Anti-Androgens

This drug’s MOA is as follows:
- Pure androgen receptor signaling inhibitor

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13
Q

What is the class and MOA of Nilutamide?

A

This drug in the following class:
- Anti-Androgens

This drug’s MOA is as follows:
- Non-steroidal anti-androgen that inhibits androgen uptake and inhibits binding of androgen in target tissues

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14
Q

What is the class and MOA of Darolutamide?

A

This drug in the following class:
- Anti-Androgens

This drug’s MOA is as follows:
- Competitive androgen receptor inhibitor, also inhibits androgen receptor translocation and androgen receptor-mediated transcription

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15
Q

What drugs are in the VEGF Inhibitors class?

A

Drugs in this class are:
- Axitinib
- Cabozantinib
- Lenvatinib
- Vandetanib
- Pazopanib
- Regorafenib
- Sorafenib
- Sunitinib

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16
Q

What is the class and MOA of Axitinib?

A

This drug in the following class:
- VEGF Inhibitors

This drug’s MOA is as follows:
- Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

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17
Q

What is the class and MOA of Cabozantinib?

A

This drug in the following class:
- VEGF Inhibitors

This drug’s MOA is as follows:
- Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

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18
Q

What is the class and MOA of Lenvatinib?

A

This drug in the following class:
- VEGF Inhibitors

This drug’s MOA is as follows:
- Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

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19
Q

What is the class and MOA of Vandetanib?

A

This drug in the following class:
- VEGF Inhibitors

This drug’s MOA is as follows:
- Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

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20
Q

What is the class and MOA of Pazopanib?

A

This drug in the following class:
- VEGF Inhibitors

This drug’s MOA is as follows:
- Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

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21
Q

What is the class and MOA of Regorafenib?

A

This drug in the following class:
- VEGF Inhibitors

This drug’s MOA is as follows:
- Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

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22
Q

What is the class and MOA of Sorafenib?

A

This drug in the following class:
- VEGF Inhibitors

This drug’s MOA is as follows:
- Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

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23
Q

What is the class and MOA of Sunitinib?

A

This drug in the following class:
- VEGF Inhibitors

This drug’s MOA is as follows:
- Binds to VEGF and other endothelial growth factors receptors on endothelial cells blocking signals that promote the growth and survival of new blood vessels

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24
Q

What drugs are in the EGFR Inhibitors class?

A

Drugs in this class are (not all inclusive):
- Gefitinib
- Erlotinib
- Osimertinib
- Afatinib

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25
Q

What is the class and MOA of Gefitinib?

A

This drug in the following class:
- EGFR Inhibitors

This drug’s MOA is as follows:
- EGFR inhibitors are highly selective tyrosine kinase inhibitors that covalently bind to epidermal growth factor receptors and irreversibly inhibit tyrosine kinase phosphorylation and downregulate EGFR signaling preventing cell growth.

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26
Q

What is the class and MOA of Erlotinib?

A

This drug in the following class:
- EGFR Inhibitors

This drug’s MOA is as follows:
- EGFR inhibitors are highly selective tyrosine kinase inhibitors that covalently bind to epidermal growth factor receptors and irreversibly inhibit tyrosine kinase phosphorylation and downregulate EGFR signaling preventing cell growth.

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27
Q

What is the class and MOA of Osimertinib?

A

This drug in the following class:
- EGFR Inhibitors

This drug’s MOA is as follows:
- EGFR inhibitors are highly selective tyrosine kinase inhibitors that covalently bind to epidermal growth factor receptors and irreversibly inhibit tyrosine kinase phosphorylation and downregulate EGFR signaling preventing cell growth.

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28
Q

What is the class and MOA of Afatinib?

A

This drug in the following class:
- EGFR Inhibitors

This drug’s MOA is as follows:
- EGFR inhibitors are highly selective tyrosine kinase inhibitors that covalently bind to epidermal growth factor receptors and irreversibly inhibit tyrosine kinase phosphorylation and downregulate EGFR signaling preventing cell growth.

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29
Q

What drugs are in the BRAF Inhibitors class?

A

Drugs in this class are:
- Dabrafenib
- Vemurafenib
- Encorafenib

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30
Q

What is the class and MOA of Dabrafenib?

A

This drug in the following class:
- BRAF Inhibitors

This drug’s MOA is as follows:
- Selectively targets mutated forms BRAF kinase (V600-) and interferes with the mitogen-activated protein kinase (MAPK) signaling pathway that regulates the proliferation and survival of melanoma cells.

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31
Q

What is the class and MOA of Vemurafenib?

A

This drug in the following class:
- BRAF Inhibitors

This drug’s MOA is as follows:
- Selectively targets mutated forms BRAF kinase (V600-) and interferes with the mitogen-activated protein kinase (MAPK) signaling pathway that regulates the proliferation and survival of melanoma cells.

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32
Q

What is the class and MOA of Encorafenib?

A

This drug in the following class:
- BRAF Inhibitors

This drug’s MOA is as follows:
- Selectively targets mutated forms BRAF kinase (V600-) and interferes with the mitogen-activated protein kinase (MAPK) signaling pathway that regulates the proliferation and survival of melanoma cells.

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33
Q

What drugs are in the BCR-ABL TKIs class?

A

Drugs in this class are:
- Bosutinib
- Dasatinib
- lmatinib
- Nilotinib
- Ponatinib
- Asciminib

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34
Q

What is the class and MOA of Bosutinib?

A

This drug in the following class:
- BCR-ABL TKIs

This drug’s MOA is as follows:
- Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia

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35
Q

What is the class and MOA of Dasatinib?

A

This drug in the following class:
- BCR-ABL TKIs

This drug’s MOA is as follows:
- Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia

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36
Q

What is the class and MOA of lmatinib?

A

This drug in the following class:
- BCR-ABL TKIs

This drug’s MOA is as follows:
- Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia

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37
Q

What is the class and MOA of Nilotinib?

A

This drug in the following class:
- BCR-ABL TKIs

This drug’s MOA is as follows:
- Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia

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38
Q

What is the class and MOA of Ponatinib?

A

This drug in the following class:
- BCR-ABL TKIs

This drug’s MOA is as follows:
- Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia

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39
Q

What is the class and MOA of Asciminib?

A

This drug in the following class:
- BCR-ABL TKIs

This drug’s MOA is as follows:
- Inhibits BCR-ABL tyrosine kinase - the abnormal gene product of the Philadelphia chromosome in chronic myeloid leukemia
- This drug is a novel first in class STAMP (Specifically Targeting the ASL Myristoyl Pocket) inhibitor. This drug potently inhibits ABL1 kinase activity of the BCR-ABL1 fusion protein via allosteric binding to the ASL myristoyl pocket.

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40
Q

What drugs are in the Somatostatin Analogs class?

A

Drugs in this class are:
- Octreotide
- Lanreotide

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41
Q

What is the class and MOA of Octreotide?

A

This drug in the following class:
- Somatostatin Analogs

This drug’s MOA is as follows:
- Mimics natural somatostatin by inhibiting serotonin release and the secretion of gastrin, VIP, insulin, glucagon, secretin, motilin, and pancreatic polypeptide
- Control symptoms that result from release of peptides and neuroamines from neuroendocrine tumors and help control the disease itself

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42
Q

What is the class and MOA of Lanreotide?

A

This drug in the following class:
- Somatostatin Analogs

This drug’s MOA is as follows:
- Mimics natural somatostatin by inhibiting serotonin release and the secretion of gastrin, VIP, insulin, glucagon, secretin, motilin, and pancreatic polypeptide
- Control symptoms that result from release of peptides and neuroamines from neuroendocrine tumors and help control the disease itself

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43
Q

What is the MOA of Tretinoin?

A

This drug’s MOA is as follows:
- Binds one or more nuclear receptors and decreases proliferation and induces differentiation of APL cells

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44
Q

What is the MOA of Arsenic Trioxide?

A

This drug’s MOA is as follows:
- Induces apoptosis in APL cells via DNA fragmentation and damages the fusion protein: promyelocytic leukemia (PML)-retinoic acid receptor (RAR) alpha

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45
Q

What is the MOA of Hydroxyurea?

A

This drug’s MOA is as follows:
- Antimetabolite that selectively inhibits ribonucleoside diphosphate reductase and interferes with DNA repair.
- In sickle cell anemia, this drug increases hemoglobin F levels.

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46
Q

What is the general MOA of the Monoclonal Antibodies class?

A

The MOA of this drug class is as follows:
- Bind to specific targets (immune cells. cell receptors. tumor molecules. etc.) to exert anti-tumor effects, the specific target varies per antibody.
- This leads to very specific anti-tumor effects using biologic agents.

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47
Q

What drugs are in the Anti-PD-1 class?

A

Drugs in this class are:
- Nivolumab
- Pembrolizumab
- Cemiplimab
- Dostarlimab
- Retifanlimab
- Nivolumab+Relatlimab

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48
Q

What drugs are in the Anti-PD-L1 class?

A

Drugs in this class are:
- Atezolizumab
- Avelumab
- Durvalumab

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49
Q

What drugs are in the Anti-CTLA4?

A

Drugs in this class are:
- lpilimumab
- Tremelimumab

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50
Q

What is the class and MOA of Nivolumab?

A

This drug in the following class:
- Immunotherapy - Anti-PD-1

This drug’s MOA is as follows:
- Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.

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51
Q

What is the class and MOA of Pembrolizumab?

A

This drug in the following class:
- Immunotherapy - Anti-PD-1

This drug’s MOA is as follows:
- Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.

52
Q

What is the class and MOA of Cemiplimab?

A

This drug in the following class:
- Immunotherapy - Anti-PD-1

This drug’s MOA is as follows:
- Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.

53
Q

What is the class and MOA of Dostarlimab?

A

This drug in the following class:
- Immunotherapy - Anti-PD-1

This drug’s MOA is as follows:
- Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.

54
Q

What is the class and MOA of Retifanlimab?

A

This drug in the following class:
- Immunotherapy - Anti-PD-1

This drug’s MOA is as follows:
- Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.

55
Q

What is the class and MOA of Nivolumab+Relatlimab?

A

This drug in the following class:
- Immunotherapy - Anti-PD-1 + Anti-LAG-3

This drug’s MOA is as follows:
- Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.

56
Q

What is the class and MOA of Atezolizumab?

A

This drug in the following class:
- Immunotherapy - Anti-PD-L1

This drug’s MOA is as follows:
- Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.

57
Q

What is the class and MOA of Avelumab?

A

This drug in the following class:
- Immunotherapy - Anti-PD-L1

This drug’s MOA is as follows:
- Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.

58
Q

What is the class and MOA of Durvalumab?

A

This drug in the following class:
- Immunotherapy - Anti-PD-L1

This drug’s MOA is as follows:
- Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.

59
Q

What is the class and MOA of lpilimumab?

A

This drug in the following class:
- Immunotherapy - Anti-CTLA4

This drug’s MOA is as follows:
- Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.

60
Q

What is the class and MOA of Tremelimumab?

A

This drug in the following class:
- Immunotherapy - Anti-CTLA4

This drug’s MOA is as follows:
- Immune checkpoint inhibitors remove inhibitory signals of T-cell activation, which enables tumor- reactive T-cells to overcome regulatory mechanisms and mount an effective antitumor response.

61
Q

What drugs are in the Immune Modulators (IMiDs) class?

A

Drugs in this class are:
- Lenalidomide
- Pomalidomide
- Thalidomide

62
Q

What is the class and MOA of Lenalidomide?

A

This drug in the following class:
- Immune Modulators (IMiDs)

This drug’s MOA is as follows:
- The mechanism of action is still under investigation but it is believed to exert direct cytotoxic effects on the tumor cells causing apoptosis

63
Q

What is the class and MOA of Pomalidomide?

A

This drug in the following class:
- Immune Modulators (IMiDs)

This drug’s MOA is as follows:
- The mechanism of action is still under investigation but it is believed to exert direct cytotoxic effects on the tumor cells causing apoptosis

64
Q

What is the class and MOA of Thalidomide?

A

This drug in the following class:
- Immune Modulators (IMiDs)

This drug’s MOA is as follows:
- The mechanism of action is still under investigation but it is believed to exert direct cytotoxic effects on the tumor cells causing apoptosis

65
Q

What drugs are in the GNRH Agonists class?

A

Drugs in this class are:
- Triptorelin
- Goserelin
- Leuprolide
- Histrelin

66
Q

What is the class and MOA of Triptorelin?

A

This drug in the following class:
- GNRH Agonists

This drug’s MOA is as follows:
- Agonist analog of gonadotropin releasing hormone (GnRH) and causes suppression of ovarian and testicular steroidogenesis due to decreased levels of LH and FSH (after initial increase during initiation phase) with subsequent decrease in testosterone (male) and estrogen (female) levels.

67
Q

What is the class and MOA of Goserelin?

A

This drug in the following class:
- GNRH Agonists

This drug’s MOA is as follows:
- Agonist analog of gonadotropin releasing hormone (GnRH) and causes suppression of ovarian and testicular steroidogenesis due to decreased levels of LH and FSH (after initial increase during initiation phase) with subsequent decrease in testosterone (male) and estrogen (female) levels.

68
Q

What is the class and MOA of Leuprolide?

A

This drug in the following class:
- GNRH Agonists

This drug’s MOA is as follows:
- Agonist analog of gonadotropin releasing hormone (GnRH) and causes suppression of ovarian and testicular steroidogenesis due to decreased levels of LH and FSH (after initial increase during initiation phase) with subsequent decrease in testosterone (male) and estrogen (female) levels.

69
Q

What is the class and MOA of Histrelin?

A

This drug in the following class:
- GNRH Agonists

This drug’s MOA is as follows:
- Agonist analog of gonadotropin releasing hormone (GnRH) and causes suppression of ovarian and testicular steroidogenesis due to decreased levels of LH and FSH (after initial increase during initiation phase) with subsequent decrease in testosterone (male) and estrogen (female) levels.

70
Q

What drugs are in the Estrogen Receptor Antagonists class?

A

Drugs in this class are:
- Tamoxifen
- Fulvestrant
- Elacestrant
- Toremifene

71
Q

What is the class and MOA of Tamoxifen?

A

This drug in the following class:
- Estrogen Receptor Antagonists

This drug’s MOA is as follows:
- Binds to estrogen receptors on tumors and other tissue targets inhibiting estrogens effects and thus tumor growth

72
Q

What is the class and MOA of Fulvestrant?

A

This drug in the following class:
- Estrogen Receptor Antagonists

This drug’s MOA is as follows:
- Binds to estrogen receptors on tumors and other tissue targets inhibiting estrogens effects and thus tumor growth

73
Q

What is the class and MOA of Elacestrant?

A

This drug in the following class:
- Estrogen Receptor Antagonists
- Selective estrogen receptor degrader (SERD)

This drug’s MOA is as follows:
- Elacestrant is an estrogen receptor antagonist and nonsteroidal selective estrogen receptor degrader (SERD), which degrades estrogen receptor alpha in a dose-dependent manner, and inhibits estradiol-dependent estrogen-receptor directed gene transcription and tumor growth.

74
Q

What is the class and MOA of Toremifene?

A

This drug in the following class:
- Estrogen Receptor Antagonists

This drug’s MOA is as follows:
- Binds to estrogen receptors on tumors and other tissue targets inhibiting estrogens effects and thus tumor growth

75
Q

What drugs are in the Aromatase Inhibitors class?

A

Drugs in this class are:
- Anastrozole
- Exemestane
- Letrozole

76
Q

What is the class and MOA of Anastrozole?

A

This drug in the following class:
- Aromatase Inhibitors

This drug’s MOA is as follows:
- Inhibits aromatase which is the enzyme responsible for the conversion of androgens to estrogens, this leads to a significant decrease in circulating estrogen.
- This thus reduces estrogen mediated stimulation of breast cancer tissue
- This one is a non-steroidal aromatase inhibitor - it decreases estrogen synthesis without compromising adrenal steroid synthesis

77
Q

What is the class and MOA of Exemestane?

A

This drug in the following class:
- Aromatase Inhibitors

This drug’s MOA is as follows:
- Inhibits aromatase which is the enzyme responsible for the conversion of androgens to estrogens, this leads to a significant decrease in circulating estrogen.
- This thus reduces estrogen mediated stimulation of breast cancer tissue
- This one is a steroidal aromatase inhibitor - it has a similar structure to androgen and irreversibly binds to aromatase

78
Q

What is the class and MOA of Letrozole?

A

This drug in the following class:
- Aromatase Inhibitors

This drug’s MOA is as follows:
- Inhibits aromatase which is the enzyme responsible for the conversion of androgens to estrogens, this leads to a significant decrease in circulating estrogen.
- This thus reduces estrogen mediated stimulation of breast cancer tissue
- This one is a non-steroidal aromatase inhibitor - it decreases estrogen synthesis without compromising adrenal steroid synthesis

79
Q

What drugs are in the Topoisomerase Inhibitors class?

A

Drugs in this class are:
- lrinotecan
- Topotecan
- Etoposide
- Teniposide
- Mitoxantrone

80
Q

What is the class and MOA of lrinotecan?

A

This drug in the following class:
- Topoisomerase I Inhibitors

This drug’s MOA is as follows:
- Topoisomerase is an essential enzyme found in all nucleated cells and is responsible for the regulation of DNA topology.
- DNA is wound around basic proteins called histones and supercoiled however, DNA must be relaxed before it can be copied. Topoisomerase I introduces single stranded nicks into DNA to allow DNA relaxation.
- In the presence of topoisomerase inhibitors, these nicks remain and the DNA is damaged causing cell death.

81
Q

What is the class and MOA of Topotecan?

A

This drug in the following class:
- Topoisomerase I Inhibitors

This drug’s MOA is as follows:
- Topoisomerase is an essential enzyme found in all nucleated cells and is responsible for the regulation of DNA topology.
- DNA is wound around basic proteins called histones and supercoiled however, DNA must be relaxed before it can be copied. Topoisomerase I introduces single stranded nicks into DNA to allow DNA relaxation.
- In the presence of topoisomerase inhibitors, these nicks remain and the DNA is damaged causing cell death.

82
Q

What is the class and MOA of Etoposide?

A

This drug in the following class:
- Topoisomerase II Inhibitors (Podophyllotoxin Derivative)

This drug’s MOA is as follows:
- Topoisomerase is an essential enzyme found in all nucleated cells and is responsible for the regulation of DNA topology.
- DNA is wound around basic proteins called histones and supercoiled however, DNA must be relaxed before it can be copied. Topoisomerase II introduces double stranded nicks into DNA to allow DNA relaxation.
- In the presence of topoisomerase inhibitors, these nicks remain and the DNA is damaged causing cell death.

83
Q

What is the class and MOA of Teniposide?

A

This drug in the following class:
- Topoisomerase II Inhibitors (Podophyllotoxin Derivative)

This drug’s MOA is as follows:
- Topoisomerase is an essential enzyme found in all nucleated cells and is responsible for the regulation of DNA topology.
- DNA is wound around basic proteins called histones and supercoiled however, DNA must be relaxed before it can be copied. Topoisomerase II introduces double stranded nicks into DNA to allow DNA relaxation.
- In the presence of topoisomerase inhibitors, these nicks remain and the DNA is damaged causing cell death.

84
Q

What is the class and MOA of Mitoxantrone?

A

This drug in the following class:
- Topoisomerase II Inhibitors (Anthracenedione)

This drug’s MOA is as follows:
- Topoisomerase is an essential enzyme found in all nucleated cells and is responsible for the regulation of DNA topology.
- DNA is wound around basic proteins called histones and supercoiled however, DNA must be relaxed before it can be copied. Topoisomerase II introduces double stranded nicks into DNA to allow DNA relaxation.
- In the presence of topoisomerase inhibitors, these nicks remain and the DNA is damaged causing cell death.

85
Q

What drugs are in the Taxanes class?

A

Drugs in this class are:
- Docetaxel
- Cabazitaxel
- Paclitaxel
- NabPaclitaxel

86
Q

What is the class and MOA of Docetaxel?

A

This drug in the following class:
- Taxanes

This drug’s MOA is as follows:
- Taxanes inhibit the mitotic spindle.
- They bind to tubulin and prevent microtubule depolymerization - therefore inhibiting mitosis and inducing apoptosis in cells undergoing the division process.
- These drugs are cell-cycle specific in the M-phase.

87
Q

What is the class and MOA of Cabazitaxel?

A

This drug in the following class:
- Taxanes

This drug’s MOA is as follows:
- Taxanes inhibit the mitotic spindle.
- They bind to tubulin and prevent microtubule depolymerization - therefore inhibiting mitosis and inducing apoptosis in cells undergoing the division process.
- These drugs are cell-cycle specific in the M-phase
- Unlike other taxanes, this drug has a poor affinity for multidrug resistance (MDR) proteins, therefore conferring activity in resistant tumors.

88
Q

What is the class and MOA of Paclitaxel?

A

This drug in the following class:
- Taxanes

This drug’s MOA is as follows:
- Taxanes inhibit the mitotic spindle.
- They bind to tubulin and prevent microtubule depolymerization - therefore inhibiting mitosis and inducing apoptosis in cells undergoing the division process.
- These drugs are cell-cycle specific in the M-phase.

89
Q

What is the class and MOA of NabPaclitaxel?

A

This drug in the following class:
- Taxanes

This drug’s MOA is as follows:
- Taxanes inhibit the mitotic spindle.
- They bind to tubulin and prevent microtubule depolymerization - therefore inhibiting mitosis and inducing apoptosis in cells undergoing the division process.
- These drugs are cell-cycle specific in the M-phase.

90
Q

What drugs are in the Pyrimidine Antagonist class?

A

Drugs in this class are:
- Gemcitabine
- 5Fluorouracil (5FU)
- Capecitabine
- Cytarabine
- Floxuridine

91
Q

What is the class and MOA of Gemcitabine?

A

This drug in the following class:
- Pyrimidine Antagonist

This drug’s MOA is as follows:
- It interferes with DNA and RNA synthesis due to structural similarity to pyrimidine.
- The antimetabolite is substituted for normal building blocks of RNA/DNA and interferes with enzyme activity causing cell death.

92
Q

What is the class and MOA of 5Fluorouracil?

A

This drug in the following class:
- Pyrimidine Antagonist

This drug’s MOA is as follows:
- It interferes with DNA and RNA synthesis due to structural similarity to pyrimidine.
- The antimetabolite is substituted for normal building blocks of RNA/DNA and interferes with enzyme activity causing cell death.
- After activation, F-UMP (an active metabolite) is incorporated into RNA to replace uracil and inhibit cell growth
- The active metabolite F-dUMP inhibits thymidylate synthetase

93
Q

What is the class and MOA of Capecitabine?

A

This drug in the following class:
- Pyrimidine Antagonist

This drug’s MOA is as follows:
- Capecitabine is a prodrug of fluorouracil.
- It interferes with DNA and RNA synthesis due to structural similarity to pyrimidine.
- The antimetabolite is substituted for normal building blocks of RNA/DNA and interferes with enzyme activity causing cell death.
- After activation of Fluorouracil, F-UMP (an active metabolite) is incorporated into RNA to replace uracil and inhibit cell growth
- The active metabolite F-dUMP inhibits thymidylate synthetase

94
Q

What is the class and MOA of Cytarabine?

A

This drug in the following class:
- Pyrimidine Antagonist

This drug’s MOA is as follows:
- Cytarabine is a pyrimidine analog and is incorporated into DNA; however, the primary action is inhibition of DNA polymerase resulting in decreased DNA synthesis and repair.

95
Q

What is the class and MOA of Floxuridine?

A

This drug in the following class:
- Pyrimidine Antagonist

This drug’s MOA is as follows:
- It is catabolized to fluorouracil after intra-arterial administration, resulting in activity similar to fluorouracil
- It inhibits thymidylate synthetase
- It interferes with DNA and RNA synthesis due to structural similarity to pyrimidine.
- The antimetabolite is substituted for normal building blocks of RNA/DNA and interferes with enzyme activity causing cell death.

96
Q

What drugs are in the Purine Antagonist class?

A

Drugs in this class are:
- 6-Mercatopurine (6-MP)
- Fludarabine
- Cladribine
- Clofarabine
- Nelarabine
- Pentostatin
- Thioguanine

97
Q

What is the class and MOA of 6Mercaptopurine?

A

This drug in the following class:
- Purine Antagonist

This drug’s MOA is as follows:
- Purine antagonists inhibit DNA and RNA synthesis by acting as false metabolite.
- The anti-metabolite is incorporated into DNA and RNA eventually inhibiting the ir synthesis.
- They are specific for the S phase of the cell cycle.

98
Q

What is the class and MOA of Fludarabine?

A

This drug in the following class:
- Purine Antagonist

This drug’s MOA is as follows:
- Purine antagonists inhibit DNA and RNA synthesis by acting as false metabolite.
- The anti-metabolite is incorporated into DNA and RNA eventually inhibiting the ir synthesis.
- They are specific for the S phase of the cell cycle.

99
Q

What is the class and MOA of Cladribine?

A

This drug in the following class:
- Purine Antagonist

This drug’s MOA is as follows:
- Purine antagonists inhibit DNA and RNA synthesis by acting as false metabolite.
- The anti-metabolite is incorporated into DNA and RNA eventually inhibiting the ir synthesis.
- They are specific for the S phase of the cell cycle.

100
Q

What is the class and MOA of Clofarabine?

A

This drug in the following class:
- Purine Antagonist

This drug’s MOA is as follows:
- Purine antagonists inhibit DNA and RNA synthesis by acting as false metabolite.
- The anti-metabolite is incorporated into DNA and RNA eventually inhibiting the ir synthesis.
- They are specific for the S phase of the cell cycle.

101
Q

What is the class and MOA of Nelarabine?

A

This drug in the following class:
- Purine Antagonist

This drug’s MOA is as follows:
- Purine antagonists inhibit DNA and RNA synthesis by acting as false metabolite.
- The anti-metabolite is incorporated into DNA and RNA eventually inhibiting the ir synthesis.
- They are specific for the S phase of the cell cycle.

102
Q

What is the class and MOA of Pentostatin?

A

This drug in the following class:
- Purine Antagonist

This drug’s MOA is as follows:
- Purine antagonists inhibit DNA and RNA synthesis by acting as false metabolite.
- The anti-metabolite is incorporated into DNA and RNA eventually inhibiting the ir synthesis.
- They are specific for the S phase of the cell cycle.

103
Q

What is the class and MOA of Thioguanine?

A

This drug in the following class:
- Purine Antagonist

This drug’s MOA is as follows:
- Purine antagonists inhibit DNA and RNA synthesis by acting as false metabolite.
- The anti-metabolite is incorporated into DNA and RNA eventually inhibiting the ir synthesis.
- They are specific for the S phase of the cell cycle.

104
Q

What drugs are in the Platinum Analogue class?

A

Drugs in this class are:
- Carboplatin
- Cisplatin
- Oxaliplatin

105
Q

What is the class and MOA of Carboplatin?

A

This drug in the following class:
- Platinum Analogues

This drug’s MOA is as follows:
- Alkylating agents which covalently binds to DNA and interfere with the function of DNA by producing interstrand DNA cross-links.
- They preferentially bind to the N-7 position of guanine.

106
Q

What is the class and MOA of Cisplatin?

A

This drug in the following class:
- Platinum Analogues

This drug’s MOA is as follows:
- Alkylating agents which covalently binds to DNA and interfere with the function of DNA by producing interstrand DNA cross-links.
- They preferentially bind to the N-7 position of guanine.

107
Q

What is the class and MOA of Oxaliplatin?

A

This drug in the following class:
- Platinum Analogues

This drug’s MOA is as follows:
- Alkylating agents which covalently binds to DNA and interfere with the function of DNA by producing interstrand DNA cross-links.
- They preferentially bind to the N-7 position of guanine.

108
Q

What drugs are in the Hypomethylator class?

A

Drugs in this class are:
- Azacitidine
- Decitabine

109
Q

What is the class and MOA of Azacitidine?

A

This drug in the following class:
- Hypomethylator

This drug’s MOA is as follows:
- Methylation (via methyltransferase) of tumor suppressor genes can contribute to the growth and survival of the cancer. Hypomethylating agents prevent DNA methylation by inhibiting methyltransferase, thus allowing for tumor suppressor gene expression which thus inhibits cancer growth.

110
Q

What is the class and MOA of Decitabine?

A

This drug in the following class:
- Hypomethylator

This drug’s MOA is as follows:
- Methylation (via methyltransferase) of tumor suppressor genes can contribute to the growth and survival of the cancer. Hypomethylating agents prevent DNA methylation by inhibiting methyltransferase, thus allowing for tumor suppressor gene expression which thus inhibits cancer growth.

111
Q

What drugs are in the Folate Antagonist class?

A

Drugs in this class are:
- Methotrexate
- Pemetrexed

112
Q

What is the class and MOA of Methotrexate?

A

This drug in the following class:
- Folate antagonist

This drug’s MOA is as follows:
- Inhibits dihydrofolate reductase thus inhibiting the formation of reduced folates.
- Inhibits thymidylate synthetase thus inhibiting synthesis of purines and thymidylic acid.
- All this leads to inhibition of DNA synthesis, repair, and cellular replication

113
Q

What is the class and MOA of Pemetrexed?

A

This drug in the following class:
- Folate antagonist

This drug’s MOA is as follows:
- Inhibits dihydrofolate reductase thus inhibiting the formation of reduced folates.
- Inhibits thymidylate synthetase thus inhibiting synthesis of purines and thymidylic acid.
- All this leads to inhibition of DNA synthesis, repair, and cellular replication

114
Q

What drugs are in the anti-tumor antibody class?

A

Drugs in this class are:
- Bleomycin

115
Q

What is the class and MOA of Bleomycin?

A

This drug in the following class:
- Anti-tumor antibody

This drug’s MOA is as follows:
- Inhibits synthesis of DNA by binding to DNA leading to single- and double-strand breaks.

116
Q

What drugs are in the anthracycline class?

A

Drugs in this class are:
- Daunorubicin
- Daunorubicin Liposomal
- Daunorubicin and Cytarabine Liposomal
- Doxorubicin
- Doxorubicin Liposomal
- Idarubicin
- Epirubicin
- Valrubicin

117
Q

What is the class and MOA of Daunorubicin?

A

This drug in the following class:
- Anthracycline

This drug’s MOA is as follows:
- Inhibits DNA and RNA synthesis via:
- Intercalation (direct binding to DNA)
- Inhibition of topoisomerase II (a repair enzyme)
- Steric obstruction

118
Q

What is the class and MOA of Doxorubicin?

A

This drug in the following class:
- Anthracycline

This drug’s MOA is as follows:
- Inhibits DNA and RNA synthesis via:
- Intercalation (direct binding to DNA)
- Inhibition of topoisomerase II (a repair enzyme)
- Steric obstruction

119
Q

What is the class and MOA of Idarubicin?

A

This drug in the following class:
- Anthracycline

This drug’s MOA is as follows:
- Inhibits DNA and RNA synthesis via:
- Intercalation (direct binding to DNA)
- Inhibition of topoisomerase II (a repair enzyme)
- Steric obstruction

120
Q

What is the class and MOA of Epirubicin?

A

This drug in the following class:
- Anthracycline

This drug’s MOA is as follows:
- Inhibits DNA and RNA synthesis via:
- Intercalation (direct binding to DNA)
- Inhibition of topoisomerase II (a repair enzyme)
- Steric obstruction

121
Q

What is the class and MOA of Valrubicin?

A

This drug in the following class:
- Anthracycline

This drug’s MOA is as follows:
- Inhibits DNA and RNA synthesis via:
- Intercalation (direct binding to DNA)
- Inhibition of topoisomerase II (a repair enzyme)
- Steric obstruction

122
Q

What drugs are in the Vinca Alkaloids class?

A

Drugs in this class are:
- Vincristine
- Vinorelbine
- Vinblastine

123
Q

What is the class and MOA of Vincristine?

A

This drug in the following class:
- Vinca Alkaloids

This drug’s MOA is as follows:
- Binds to tubulin and inhibits microtubule formation stopping cell growth by disrupting the formation of the mitotic spindle. These drugs specifically target the M and S phases of the cell cycle.

124
Q

What is the class and MOA of Vinorelbine?

A

This drug in the following class:
- Vinca Alkaloids

This drug’s MOA is as follows:
- Binds to tubulin and inhibits microtubule formation stopping cell growth by disrupting the formation of the mitotic spindle. These drugs specifically target the M and S phases of the cell cycle.

125
Q

What is the class and MOA of Vinblastine?

A

This drug in the following class:
- Vinca Alkaloids

This drug’s MOA is as follows:
- Binds to tubulin and inhibits microtubule formation stopping cell growth by disrupting the formation of the mitotic spindle. These drugs specifically target the M and S phases of the cell cycle.

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