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PHRM 864 > Oncology (Dykhuizen & Mabe) > Flashcards

Oncology (Dykhuizen & Mabe) Flashcards

1
Q

What are the antimetabolites/Antifolates?

A

5-Fu, cytarabine, 6-MP, methotrexate

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2
Q

5-Fu info

A

antimetabolite; inhibits thymidine synthesis from uracil; S-Phase; thymidine = “antidote”
leucovorin = synergy

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3
Q

Cytarabine (Ara-C)

A

antimetabolite; cytosine analog; competitive inhibitor of DNA polymerase-a, S-Phase, tetrahydrouridine = synergy

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4
Q

6-MP

A

purine analog: blocks the synthesis of purine nucleotides S-Phase “allopurinol: blocks xanthine oxidase from
breaking down 6-MP & can lead to 6-MP toxicity” loss of HGPRT, the activating enzyme deficiency of TPMT increase risk of 6-MP toxicity

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5
Q

methotrexate

A

antifolate
DHFR inhibition reduces FH4 & inhibits TMP synthesis (inhibits RNA and protein synthesis) (also inhibits purine and pyrimidine base synthesis) S-Phase leucovorin = “antidote” “Amplification of DHFR gene or mutation to resistant form
Decreased polyglutamation results in decreased intracellular MTX”

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6
Q

Chlorambucil

A

non-phase specific alykator

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7
Q

cyclophosphamide

A

prodrug alkylator

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8
Q

mitomycin-c

A

alkylator

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9
Q

cisplatin

A

platinum compound; intrastrand cross-links

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10
Q

topo I inhibitor

A

ironotecan, topotecan

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11
Q

topotecan

A

topo-I inhibitor

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12
Q

doxorubicin

A

topo-II inhibitor and intercalator

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13
Q

etoposide

A

topo-II inhibitor

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14
Q

vincristine

A

microtubule inhibitor

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15
Q

Bleomycin

A

topo-II inhibitor and intercalator

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16
Q

erubulin

A

microtubule inhibitor

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17
Q

paclitaxel

A

microtubule stabilizer

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18
Q

ixabepilone

A

microtubule stabilizer

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19
Q

enzalutamide

A

high affinity and binds to AR

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20
Q

abiraterone

A

CYP17 inhibitor

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21
Q

tamoxifen

A

SERM; raloxifene also in class

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22
Q

fulvestrant

A

SERD

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23
Q

letrozole, anastrozole

A

non-steroidal aromatase inhibitor

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24
Q

exemastene

A

steroidal aromatase inhibitor

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25
Q

leuprolide

A

GnRH analog

26
Q

imatinib

A

type II small molecule inhibitor of Abl tyrosine kinase

27
Q

ponatinib

A

type II small molecule inhibitor of Abl tyrosine kinase effective against T315I mutation– effective against all major BCR-ABL mutations

28
Q

midostaurin

A

first gen FLT3 inhibitor: broad kinase inhibitor

29
Q

quizartinib

A

Type II FLT3 inhibitor: specific for ITD mutations

30
Q

Crenolanib

A

second gen FLT3 inhibitor: specific kinase inhibitor

31
Q

sirolimus

A

inhibit the funciton of mTOR (serine-threonine kinase)

32
Q

alectinib

A

ALK inhibitor

33
Q

dabrafinib

A

inhibits BRAF-v600 to treat metastatic melanoma (used in combo with trametinib)

34
Q

trametinib

A

inhibits MEK1 and MEK2 kinase activity though type III allosteric inhibition (downstream of MET receptor tyrosine kinase)

35
Q

acalabrutinib

A

second gen covalent BTK (Bruton’s Tyrosine Kinase) inhibitor

36
Q

Gefitinib

A

EGFR tyrosine kinase inhibitor; type I TKI

37
Q

Lapatinib

A

small molecule TKI, reversible inhibitor of EGFR & HER2

38
Q

afatinib

A

covalent inhibitor of all ErbB receptors (used for EGFR mutations)

39
Q

Tucatanib

A

selective HER2 inhibitor

40
Q

Osimertinib

A

covalent EGFR inhibitor effective against T790M mutations (second line to Gefitinib)

41
Q

Pembrolizumab

A

Inhibits PD1 to block PD1+PDL1 interactions with T-cells

42
Q

atezolizumab

A

Inhibits PDL1 to block PD1+PDL1 interactions with T-cells

43
Q

Ipilimumab

A

Inhibits CTLA-4 on T-cells to enhance t-cell activation

44
Q

trastuzumab/pertuzimab

A

inhibits HER-2 to prohibit dimerization

45
Q

cetuximab

A

inhibits EGFR on B-cells – blocks activation of EGFR kinase

46
Q

Bevacizumab

A

inhibits VEGF on B-cells (binds ligand)

47
Q

Ramucirumab

A

inhibits VEGF on B-cells (binds receptor)

48
Q

rituximab

A

inhibits CD20 on B-Cells

49
Q

daratumumab

A

inhibits CD38 on B-Cells

50
Q

trastuzumab/emtansine

A

transtuzimab: binds & inhibits HER2; emtansine: inhibits microtubule assembly

51
Q

trastuzumab/daruxecan

A

transtuzimab: binds & inhibits HER2; deruxecan: type 1 topoisomerase inhibitor

52
Q

Blinatumomab

A

brings T cells (by binding to CD3) to CD19 on B cell tumors

53
Q

mosunetuzumab

A

brings T cells (by binding to CD3) to CD20 on B cell tumors

54
Q

Teclistamab

A

brings T cells (CD3) to BCMA on myelomas

55
Q

taquetamab

A

brings T cell to GPCR C5D on myelomas

56
Q

Sipulecel-T

A

antigens on prostate cancer

57
Q

CAR-T

A

will bind cells with CD19 and kill them

58
Q

Olaparib

A

PARP inhibitor - Primarily used in cancers with BRACA 1/2 mutations (traps PARP to DNA)

59
Q

Palbociclib

A

CDK 4/6 kinase inhibitor (used in cancers with BRCA 1/2 mutations)

60
Q

5-Azacytosine

A

DNMT (DNA methyltransferase) inhibitor: incorporates into DNA or RNA and covalently binds DNMT enzymes to inhibit their function

61
Q

Venetoclax

A

BCL-2 inhibitor: drives cell death via apoptosis (BCL-2 is and anti-apoptotic protein often overexpressed in cancers)

62
Q

Pomalidomide

A

binds cereblon to induce ubitquitination and degradation of IKZF TFs, (important for lymphocyte development and cell survival in multiple myeloma)

PHRM 864 (13 decks)

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