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Therapeutics IV > Exam 1 Table > Flashcards

Exam 1 Table Flashcards

1
Q

5-fluorouracil (5-FU) target

A

Thymidylate synthase - blocks uracil to thymine conversion

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2
Q

5-fluorouracil (5-FU) drug class

A

Anti-metabolite; uridine analog

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3
Q

5-fluorouracil (5-FU) cell cycle phase

A

S

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4
Q

5-fluorouracil (5-FU) dose limiting side effect

A

Myelosuppression

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5
Q

5-fluorouracil (5-FU) rescue drug

A

Thymidine

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6
Q

5-fluorouracil (5-FU) synergy drug

A

Leucovorate

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7
Q

5-fluorouracil (5-FU) unique resistance mechanisms

A

-Downregulation of activating enzymes that convert 5-FU to fd-UMP
-Upregulation of thymidylate synthase

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8
Q

5-fluorouracil (5-FU) genetic testing

A

~5% of the population has gene polymorphisms that result in a deficiency of the enzyme dihydropyrimidine dehydrogenase (DPD) which breaks down 5-FU

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9
Q

Cytarabine target

A

Converted to Ara-CTP intracellularly -> competitive inhibitor of DNA polymerase alpha

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10
Q

Cytarabine drug class

A

Anti-metabolite; cytosine analog

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11
Q

Cytarabine cell cycle phase

A

S

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12
Q

Cytarabine indication

A

-Leukemia
-Lymphoma

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13
Q

Cytarabine dose limiting side effect

A

Myelosuppression

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14
Q

Cytarabine synergy drug

A

Tetrahydrouridine because of inhibition of cytidine deaminase

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15
Q

Cytarabine unique resistance mechanisms

A

-Downregulation of activating enzymes
-Upregulation of cytidine deaminases
-Downregulation of influx transporters

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16
Q

6-mercaptopurine (6-MP) target

A

Blocks multiple enzymes in de novo purine biosynthesis

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17
Q

6-mercaptopurine (6-MP) drug class

A

Antimetabolite; purine analog, thio-analog of adenine

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18
Q

6-mercaptopurine (6-MP) cell cycle phase

A

S

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19
Q

6-mercaptopurine (6-MP) dose limiting side effects

A

Hematologic toxicity, myelosuppression

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20
Q

6-mercaptopurine (6-MP) drug interactions

A

Allopurinol increases 6-MP toxicity

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21
Q

6-mercaptopurine (6-MP) unique resistance mechanisms

A

Loss of HGPRT (activating enzyme)

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22
Q

6-mercaptopurine (6-MP) genetic testing

A

TPMT polymorphism loss of function - (TPMT inactivates 6-MP) - dose adjustment needed

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23
Q

Methotrexate target

A

DHFR inhibitor

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24
Q

Methotrexate drug class

A

Antimetabolite, antifolate

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25
Q

Methotrexate cell cycle phase

A

S

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26
Q

Methotrexate dose limiting side effect

A

myelosuppression

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27
Q

Methotrexate rescue drug

A

Leucovorin

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28
Q

Methotrexate unique resistance mechanisms

A

-Amplification of DHFR or resistant mutation of DHFR
-Decreased polyglutamation

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29
Q

Chlorambucil target

A

Cross-links DNA

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30
Q

Chlorambucil drug class

A

Alkylating agent; mechlorethamine derivative

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31
Q

Chlorambucil cell cycle phase

A

Non-specific

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32
Q

Chlorambucil dose limiting side effect

A

-Myelosuppression
-N/V
-Carcinogenic (secondary malignancies) and teratogenic (ALL alkylators)

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33
Q

Alkylating agent/platinum agent unique resistance mechanisms

A

-Increased expression of DNA repair enzymes
-Increased glutathione concentrations to reduce reactive intermediates
-Increased expression of cellular glutathione S-transferase (GST)

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34
Q

Cyclophosphamide target

A

Cross-links DNA

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35
Q

Cyclophosphamide drug class

A

Alkylating agent; requires hydroxylation by CYP450 (prodrug)

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36
Q

Cyclophosphamide cell cycle phase

A

Non-specific

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37
Q

Cyclophosphamide dose limiting side effects

A

-Hemorrhagic cystitis - acrolein buildup in bladder
-Mild bone marrow toxicity due to high ADH in these cells that break down metabolite

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38
Q

Drug that must be given with Cyclophosphamide

A

Mesna is administered with cyclophosphamide to block hemorrhagic cystitis - free thiol on mesna reacts with and inactivates acrolein metabolites in urine

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39
Q

Mitomycin C target

A

Bifunctional adducts on DNA (cross-links)

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40
Q

Mitomycin C drug class

A

alkylating agent (aziridine containing natural product)

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41
Q

Mitomycin C cell cycle phase

A

Non-specific

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42
Q

Mitomycin C dose limiting side effect

A

Myelosuppression

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43
Q

Cisplatin target

A

Forms intrastrand crosslinks - covalent crosslink between G and A

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44
Q

Cisplatin drug class

A

-Platinum drugs - covalent cross linkers
-Prodrug - requires non-enzymatic conversion to the active aqua form

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45
Q

Cisplatin cell cycle phase

A

Non-specific

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46
Q

Cisplatin dose limiting side effect

A

-Nephrotoxicity in proximal tube
-Minimal bone marrow toxicity (good in combination with other drugs)
-Severe N/V
-Peripheral neuropathy
-Ototoxicity
-Carboplatin: cutaneous rash, vomiting, hypotension

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47
Q

Irinotecan target

A

Topo I inhibitor (water soluble) - binds and forms a ternary drug-enzyme-DNA complex -> blocks DNA religation

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48
Q

Irinotecan drug class

A

-Topo I inhibitor: camptothecins
-Prodrug into SN-38 via carboxylesterases

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49
Q

Irinotecan cell cycle phase

A

S

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50
Q

Irinotecan unique resistance mechanisms

A

-P-glycoprotein (PGP) overexpression
-Multidrug resistant protein (MRP) overexpression
-Glutathione S-transferase overexpression
-Topoisomerase downregulation
-Mutation to prevent inhibitor binding

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51
Q

Irinotecan genetic testing

A

~10% of the population has polymorphisms predicting low expression of UGT1A1, leading to increased toxicity of irinotecan

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52
Q

Doxorubicin target

A

Topo II inhibitor - intercalates and inhibits double strand religation

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53
Q

Doxorubicin drug class

A

Topo 2 inhibitor; anthracyclines

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54
Q

Doxorubicin cell cycle

A

-Non-specific
-A little G2/M

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55
Q

Doxorubicin dose limiting side effects

A

Cardiotoxicity due to free radical damage, severe local tissue damage if extravasated

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56
Q

Doxorubicin synergetic drugs

A

Dexrazoxane protects against anthracycline-induced cardiotoxicity by binding to iron

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57
Q

Doxorubicin unique resistance mechanisms

A

Glutathione S-transferase (GST) overexpression - the only topo 2 to have this resistance

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58
Q

Etoposide target

A

Topo II inhibitor - inhibits double strand religation

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59
Q

Etoposide drug class

A

Topo 2 inhibitor; epipodophyllotoxin glucose analog (does not intercalate)

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60
Q

Etoposide cell cycle

A

G2

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61
Q

Resistance mechanisms for all topo 2 inhibitors

A

-PGP overexpression
-Topoisomerase II downregulation or mutation
-Increased DNA damage repair enzyme

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62
Q

Bleomycin target

A

Intercalates into DNA - forms DNA free radical - leads to DNA single and double strand breaks

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63
Q

Bleomycin drug class

A

Glycopeptide antibiotic - imidazole free radical, thiazole intercalator

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64
Q

Bleomycin cell cycle

A

-G2
-M

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65
Q

Bleomycin dose limiting side effects

A

Pulmonary toxicity and rash because of lack of bleomycin aminohydrolase

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66
Q

Bleomycin resistance mechanisms

A

Increased levels of bleomycin aminohydrolase

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67
Q

Vincristine target

A

Tubulin -> inhibition of microtubule assembly (tubulin polymerization) and microtubule shortening

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68
Q

Vincristine drug class

A

Vinca alkaloids - microtubule destabilizer

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69
Q

Vincristine cell cycle

A

M

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70
Q

Vincristine dose limiting side effects

A

-Neurotoxicity
-Peripheral neuropathy
-Myelosuppression is mild and rarely clinically significant

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71
Q

Vincristine resistance mechanisms

A

PGP substrate

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72
Q

Eribulin target

A

Microtubule end - inhibition of microtubule assembly/elongation (polymerization)

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73
Q

Eribulin drug class

A

Microtubule destabilizer - halichondrin B analog

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74
Q

Eribulin cell cycle phase

A

M

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75
Q

Eribulin dose limiting side effects

A

Lower rate of neurotoxicity than vinca

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76
Q

Paclitaxel target

A

Tubulin inhibition of microtubule disassembly (depolymerization)

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77
Q

Paclitaxel drug class

A

Taxanes - microtubule stabilizer

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78
Q

Paclitaxel cell cycle phase

A

M

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79
Q

Paclitaxel dose limiting side effects

A

-Myelosuppression
-Neurotoxicity - sensory neuropathy common but reversible

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80
Q

Paclitaxel drug interactions

A

Cross-resistant with other large molecule antitumor agents

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81
Q

Paclitaxel resistance mechanisms

A

-PGP substrate (except for cabazitaxel)
-Tubulin mutations

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82
Q

Ixabepilone target

A

Tubulin inhibition of microtubule disassembly (depolymerization)

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83
Q

Ixabepilone drug class

A

Microtubule stabilizer - epothilone B analog

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84
Q

Ixabepilone cell cycle phase

A

M

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85
Q

Ixabepilone dose limiting side effects

A

-Myelosuppression
-Neurotoxicity - sensory neuropathy common but reversible

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86
Q

Ixabepilone drug interactions

A

NOT cross-resistant to taxanes

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87
Q

Ixabepilone resistance mechanisms

A

Poor PGP substrate

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88
Q

Enzalutamide target

A

Androgen receptor

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89
Q

Enzalutamide drug class

A

Full AR antagonist

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90
Q

Enzalutamide cell cycle phase

A

G1

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91
Q

Enzalutamide indication

A

Metastatic and non-metastatic prostate cancer

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92
Q

Enzalutamide resistance mechanisms

A

AR mutation that results in androgen independent activation and prevent binding of AR antagonists = castration resistant prostate cancer (CRPC)

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93
Q

Abiraterone target

A

-17 alpha-hydrolase and C17,20 lyase
-CYP17 catalyzes conversion of pregnenolone and progesterone to DHEA and androstenedione

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94
Q

Abiraterone drug class

A

Steroid analog

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95
Q

Abiraterone cell cycle phase

A

G1

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96
Q

Abiraterone dose limiting side effect

A

Increased cholesterol

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97
Q

Tamoxifen target

A

Estrogen receptor

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98
Q

Tamoxifen drug class

A

SERM; partial agonist; prodrug (CYP2D6)

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99
Q

Tamoxifen cell cycle phase

A

G1

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100
Q

Tamoxifen indication

A

Pre and postmenopausal women with ER-positive breast cancer

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101
Q

Tamoxifen dose limiting side effects

A

Hot flashes; increased incidence of endometrial cancer

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102
Q

Tamoxifen drug interactions

A

CYP2D6 inhibitors

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103
Q

Tamoxifen resistance mechanisms

A

Variant of CYP2D6 that decreases metabolism of tamoxifen

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104
Q

Fulvestrant target

A

Estrogen receptor

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105
Q

Fulvestrant drug class

A

SERD; pure estrogen antagonist; no agonist effects

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106
Q

Fulvestrant cell cycle phase

A

G1

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107
Q

Fulvestrant indication

A

ER+ metastatic breast cancer - postmenopausal women who have progressed on other antiestrogen therapy

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108
Q

Prednisolone drug class

A

Corticosteroid

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109
Q

Prednisolone cell cycle phase

A

G1

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110
Q

Prednisolone indication

A

Used as palliative care for inflammation, edema and pain management

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111
Q

Letrozole target

A

Aromatase

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112
Q

Letrozole drug class

A

Non-steroidal competitive aromatase (CYP19) inhibitor

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113
Q

Letrozole cell cycle phase

A

G1

114
Q

Letrozole indication

A

Postmenopausal breast cancer

115
Q

Letrozole dose limiting side effects

A

Increased extent of bone density loss - increased risk of fracture

116
Q

Exemestane target

A

Aromatase

117
Q

Exemestane drug class

A

Steroidal aromatase inhibitor; suicide inhibitor (irreversible)

118
Q

Exemestane cell cycle phase

A

G1

119
Q

Exemestane indication

A

Postmenopausal ER+ breast cancer patients who have progressed on antiestrogen therapy

120
Q

Exemestane dose limiting side effects

A

-Minimal toxicity
-Hot flashes
-Occasional peripheral edema
-Weight gain
-Increased cholesterol

121
Q

Leuprolide target

A

GnRH receptor

122
Q

Leuprolide drug class

A

GnRH analog

123
Q

Leuprolide cell cycle phase

A

G1

124
Q

Leuprolide indication

A

Premenopausal

125
Q

Leuprolide dose limiting side effects

A

-Transient worsening symptoms to initial (flare) effects
-Long term: hot flashes, sexual dysfunction, gynecomastia

126
Q

Imatinib target

A

BCR-Abl tyrosine kinase

127
Q

Imatinib drug class

A

Type 2 small molecule Bcr-Abl inhibitor

128
Q

Imatinib cell cycle phase

A

G1

129
Q

Imatinib indication

A

Primary indication for chronic myeloid leukemia (CML) and GIST

130
Q

Imatinib dose limiting side effects

A

-N/V
-Fluid retention (edema)
-Neutropenia
-Thrombocytopenia

131
Q

Imatinib resistance mechanisms

A

“Gatekeeper” T315I mutation

132
Q

Imatinib genetic testin

A

Philadelphia chromosome

133
Q

Ponatinib target

A

BCR-Abl tyrosine kinase

134
Q

Ponatinib drug class

A

Bcr-Abl inhibitor

135
Q

Ponatinib cell cycle phase

A

G1

136
Q

Ponatinib indication

A

T315I mutation

137
Q

Ponatinib genetic testing

A

Can inhibit the T315I mutation

138
Q

Midostaurin target

A

fms-like tyrosine kinase 3 (FLT3) in AML

139
Q

Midostaurin drug class

A

First gen FLT3 inhibitor for AML

140
Q

Midostaurin cell cycle phase

A

G1

141
Q

Crenolanib target

A

fms-like tyrosine kinase 3 (FLT3) in AML

142
Q

Crenolanib drug class

A

Second gen (more specific) FLT3 inhibitor for AML

143
Q

Crenolanib cell cycle phase

A

G1

144
Q

Quizartinib target

A

fms-like tyrosine kinase 3 (FLT3) in AML

145
Q

Quizartinib drug class

A

Type II FLT3 inhibitor for AML

146
Q

Quizartinib cell cycle phase

A

G1

147
Q

Quizartinib indication

A

Specific for internal tandem duplication (ITD) mutations

148
Q

Quizartinib genetic testing

A

Internal tandem duplication (ITD) mutations

149
Q

Sirolimus target

A

Inhibit the mammalian target of Rapamycin (mTOR; serine-threonine kinase)

150
Q

Sirolimus drug class

A

Rapamycin analogues

151
Q

Sirolimus cell cycle phase

A

G1

152
Q

Sirolimus drug interactions

A

Inhibits immune response by blocking IL-2 signaling transduction

153
Q

Alectinib target

A

Anaplastic lymphoma kinase (ALK)

154
Q

Alectinib drug class

A

ALK inhibitors

155
Q

Alectinib cell cycle phase

A

G1

156
Q

Alectinib indication

A

ALK-positive NSCLC who have progressed on or intolerant to crizotinib

157
Q

Alectinib genetic testing

A

Fusion gene of ALK to ELM4

158
Q

Dabrafenib target

A

BRAF-V600

159
Q

Dabrafenib drug class

A

Second gen BRAF-V600 inhibitor

160
Q

Dabrafenib cell cycle phase

A

G1

161
Q

Dabrafenib indication

A

Combination with trametinib for BRAF V600E/K-mutant metastatic melanoma

162
Q

Dabrafenib drug interactions

A

Activation of wild type BRAF remains a problem, combination with trametinib seems to stem from induction of squamous cell carcinomas

163
Q

Dabrafenib genetic testing

A

BRAF-V600 mutations

164
Q

Trametinib target

A

MEK1 and MEK2

165
Q

Trametinib drug class

A

Type III allosteric MEK inhibitor

166
Q

Trametinib cell cycle phase

A

G1

167
Q

Trametinib indication

A

Combination with dabrafenib

168
Q

Trametinib dose limiting side effects

A

-RASH
-Diarrhea
-Lymphedema

169
Q

Trametinib drug interaction

A

Not indicated for patients that have received prior BRAF inhibitor therapy

170
Q

Acalabrutinib target

A

Bruton’s tyrosine kinase (BTK); also targets Cys481

171
Q

Acalabrutinib drug class

A

Second gen covalent BTK inhibitor

172
Q

Acalabrutinib cell cycle phase

A

G1

173
Q

Acalabrutinib indication

A

B-cell lymphoma: Mantle cell lymphoma and chronic lymphocytic leukemia

174
Q

Gefitinib target

A

EGFR tyrosine kinase

175
Q

Gefitinib drug class

A

First gen reversible EGFR inhibitor

176
Q

Gefitinib cell cycle phase

A

G1

177
Q

Gefitinib indication

A

Approved for NSCLC with exon 19 or 21 mutations

178
Q

Gefitinib dose limiting side effects

A

-Fatigue
-Rash
-Diarrhea

179
Q

Gefitinib resistance mechanisms

A

T790M causes resistance

180
Q

Gefitinib genetic testing

A

EGFR exon 19 or exon 21 (L858R) mutation

181
Q

Afatinib target

A

Covalent inhibitor of all ErbB receptors

182
Q

Afatinib drug class

A

Covalent EGFR inhibitor - second gen

183
Q

Afatinib cell cycle phase

A

G1

184
Q

Afatinib indication

A

Approved for EGFR mutant NSCLC with EGFR mutations

185
Q

Afatinib dose limiting side effects

A

Better rash tolerance

186
Q

Afatinib resistance mechanisms

A

T790M causes resistance

187
Q

Afatinib genetic testing

A

EGFR RGQ PCR Kit (QIAGEN) for detection of EGFR exon 19 deletions or exon 21 (L858R) substitution mutations

188
Q

Osimertinib target

A

EGFR tyrosine kinase

189
Q

Osimertinib drug class

A

Third gen covalent EGFR inhibitor

190
Q

Osimertinib cell cycle phase

A

G1

191
Q

Osimertinib indication

A

Effective for T790M mutant EGFR (replace gefitinib)

192
Q

Osimertinib resistance mechanisms

A

C797 mutation that abrogates covalent binding

193
Q

Lapatinib target

A

EGFR and HER2

194
Q

Lapatinib drug class

A

-EGFR and HER2 reversible inhibitor
-Small molecule TKI

195
Q

Lapatinib cell cycle phase

A

G1

196
Q

Lapatinib indication

A

Approved in combination with capecitabine for the treatment of advanced metastatic breast cancer in patients who have progressed on other therapies

197
Q

Lapatinib dose limiting side effects

A

-Diarrhea
-Nausea
-Vomiting
-Reversible decrease in cardiac function (watch for signs of CHF)

198
Q

Tucatinib target

A

HER2

199
Q

Tucatinib drug class

A

Small molecule TKI HER2 inhibitor

200
Q

Tucatinib cell cycle phase

A

Approved as a second line therapy in combination with trastuzumab and capecitabine for the treatment of advanced metastatic breast cancer who have progressed on other therapies

201
Q

Tucatinib dose limiting side effects

A

Reduced side effects compared to lapatinib or covalent pan-ErbB inhibitors

202
Q

Tucatinib genetic testing

A

HER2+ breast cancer

203
Q

Trastuzumab, pertuzumab target

A

HER2

204
Q

Trastuzumab, pertuzimab drug class

A

Recombinant humanized mAB

205
Q

Trastuzumab, pertuzimab indication

A

Primary indication is the treatment of breast cancers that overexpress HER2

206
Q

Trastuzumab, pertuzimab dose limiting side effects

A

-Flu-like symptoms
-Risk of cardiomyopathy/CHF
-Increases myelosuppression when used in combo with chemo
-Risk of hypersensitivity reactions (immune response)

207
Q

Trastuzumab, pertuzimab drug interactions

A

-Trastuzumab used in combo with pertuzimab-different binding sites for HER2 increases efficacy; drug synergy
-Pertuzimab inhibits dimerization

208
Q

Trastuzumab, pertuzimab genetic testing

A

HER2 expression

209
Q

Cetuximab target

A

EGFR - completely inhibits binding of EGF and TGF-alpha

210
Q

Cetuximab drug class

A

Recombinant chimeric mAB

211
Q

Cetuximab indication

A

Primary indication is in the treatment of colorectal and head and neck cancers

212
Q

Cetuximab dose limiting side effects

A

-Severe infusion reaction (~3%), acneiform rash, asthenias, fever

213
Q

Bevacizumab target

A

VEGF (ligand) - blocks interaction with endothelial receptors

214
Q

Bevacizumab drug class

A

Recombinant humanized MAB

215
Q

Bevacizumab indication

A

-Used in combination with 5-FU based chemotherapy for first-line treatment of metastatic colorectal cancer
-No evidence of efficacy as single agent

216
Q

Ramucirumab target

A

VEGFR (receptor)

217
Q

Ramucirumab drug class

A

VEGFR (receptor) inhibitor mAB

218
Q

Ramucirumab indication

A

-Used in combination with 5-FU based chemotherapy for first-line treatment of metastatic colorectal cancer
-No evidence of efficacy as single agent

219
Q

Rituximab target

A

-Binds CD20 in normal B lymphocytes and immature pre-B cells -> inhibiting B-cell proliferation
-CD20 works with B-cell receptor (BCR) to drive proliferation of B-cells

220
Q

Rituximab indication

A

B-cell lymphomas (non-Hodgkin’s lymphoma), that target different binding sites on CD20

221
Q

Daratumumab target

A

CD38 - a multifunctional transmembrane protein highly expressed on plasma B cells that make antibodies

222
Q

Daratumumab indication

A

Multiple myeloma - cancer of malignant plasma cells

223
Q

Ipilimumab target

A

CTLA-4 receptor - reverses cytotoxic T lymphocyte inhibition caused by CTLA-4 receptor allowing it to destroy tumor cells

224
Q

Ipilimumab drug class

A

Recombinant human mAB

225
Q

Ipilimumab indication

A

Approved for treatment of advanced metastatic melanoma

226
Q

Ipilimumab dose limiting side effect

A

Severe immune-mediated adverse effects (inflammatory response)

227
Q

Ipilimumab synergetic drugs

A

May require high dose corticosteroids to combat inflammatory response

228
Q

Pembrolizumab target

A

Binds PD-1 receptor expressed on T-cells and blocks interaction with PD-L1 and PD-L2 -> blockade of PD-1 prevents inhibitory signaling within T-cells leading to enhanced tumor cell killing

229
Q

Pembrolizumab drug class

A

mAB

230
Q

Pembrolizumab indication

A

-Approved for the treatment of advanced metastatic melanoma following treatment with ipilimumab and a BRAF inhibitor (if BRAF positive)
-Approved for NSCLC if positive for PD-L1

230
Q

Pembrolizumab genetic testing

A

PDL1 test for treatment of NSCLC

230
Q

Atezolizumab target

A

Binds PD-L1 receptor (expressed on macrophages and tumor cells) - blocking interaction with PD-1 on T-cells leading to enhanced tumor killing

231
Q

Atezolizumab drug class

A

PD-L1 mAB

232
Q

Trastuzumab emtansine target

A

-Trastuzumab: HER2/Neu receptor
-Emtansine: inhibits microtubule assembly

233
Q

Trastuzumab emtansine drug class

A

-ADC
-Emtansine = cytotoxic agent; microtubule destabilizer

233
Q

Trastuzumab emtansine indication

A

Approved for second line treatment for HER2-positive metastatic breast cancer

234
Q

Trastuzumab emtansine dose limiting side effect

A

-Trastuzumab adverse effects
-Thrombocytopenia
-Hepatotoxicity

235
Q

Trastuzumab emtansine drug interactions

A

Emtansine toxicity significantly reduced because of selective HER2 targeting

236
Q

Trastuzumab emtansine genetic testing

A

HER2

237
Q

Bilnatumomab target

A

Binds to CD3 and brings activated T-cell into proximity of CD19

238
Q

Bilnatumomab drug class

A

Bispecific T-cell engager

239
Q

Bilnatumomab indication

A

Non-Hodgkin lymphomas

240
Q

Mosunetuzumab target

A

CD3 and CD20

241
Q

Mosunetuzumab drug class

A

Bispecific T-cell engager

242
Q

Mosunetuzumab dose limiting side effect

A

Cytokine release syndrome - when immune system responds too aggressively

243
Q

Teclistamab target

A

CD3 on T-cells and B-cell maturation antigen (BCMA) of multiple myeloma cells

244
Q

Teclistamab drug class

A

Bispecific T-cell engager

245
Q

Taquetamab target

A

CD3 on T-cells and GPRC5D on multiple myeloma cells

246
Q

Teclistamab drug class

A

Bispecific T-cell engager

247
Q

Sipuleucel-T target

A

Antigen presenting cells (APCs) activated by ex vivo treatment with PAP-GM-CSF - stimulates patients own immune system to attack cancer

248
Q

Sipuleucel-T drug class

A

PAP-GM-CSF

249
Q

Sipuleucel-T indication

A

Minimally symptomatic metastatic hormone refractory prostate cancer

250
Q

Sipuleucel-T dose limiting factor

A

-Mostly limited to flu-like symptoms
-Possible increased risk of stroke

251
Q

CAR-T target

A

T-cell activation using CD19 as the target

252
Q

CAR-T drug class

A

Chimeric antigen receptor (CAR) T cells

253
Q

CAR-T indication

A

B-cell leukemia

254
Q

Olaparib target

A

PARP trapping to DNA

255
Q

Olaparib drug class

A

Poly ADP ribose polymerase (PARP) inhibitor

256
Q

Olaparib indication

A

Cancers with BRCA1/2 mutations

257
Q

Olaparib genetic testing

A

BRCA1/2 + PARP inhibitor = synthetic lethality

258
Q

Palbociclib target

A

Cdk4/6

259
Q

Palbociclib drug class

A

-Kinase inhibitor - targets kinases directly involved with cell cycle control
-Targets ALL replicating cells

260
Q

Palbociclib cell cycle phase

A

G1

261
Q

Palbociclib indication

A

Cancers arising due to BRCA mutations

262
Q

Palbociclib dose limiting side effect

A

-Neutropenia
-Nausea
-Fatigue
-Diarrhea
-Vomiting

263
Q

Palbociclib genetic testing

A

BRCA1/2

264
Q

Bortemzomib target

A

26S proteasome = ubiquitin-proteasome pathway important for regulation of intracellular proteins

265
Q

Bortemzomib drug class

A

Proteasome inhibitor - blocks ubiquitination-disrupts homeostasis causing cell death

266
Q

Bortemzomib indication

A

Multiple myeloma (B-cell malignancy)

267
Q

5-azacytidine target

A

DNA and DNMT enzymes - part of DNA methylation

268
Q

5-azacytidine drug class

A

DNMT inhibitor - blocks DNA methylation - causes reactivation of tumor suppressor genes

269
Q

5-azacytidine indication

A

Myelodysplastic syndrome

270
Q

Venetoclax target

A

BCL-2; anti-apoptotic protein

271
Q

Venetoclax drug class

A

-BCL-2 inhibitor
-First FDA approved small molecule that inhibits a protein-protein interaction

272
Q

Venetoclax indication

A

Chronic lymphocytic leukemia

273
Q

Venetoclax drug interactions

A

-Combination with 5-azacitidine for AML
-PGP substrate
-CYP3A4

274
Q

Pomalidomide target

A

Binds Cereblon to induce it to ubiquitinate and degrade IKZF TFs that are important in lymphocyte development and regulate cell survival

275
Q

Pomalidomide drug class

A

Thalidomide analog - anti-angiogenic activity

276
Q

Pomalidomide indication

A

Multiple myeloma and Kaposi sarcoma

277
Q

What does every patient need when on Pomalidomide?

A

Patients must be signed up for the REMS program

Therapeutics IV (4 decks)

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