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Rad Bio > Drugs and Interactions > Flashcards

Drugs and Interactions Flashcards

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Biology 101 flashcards
1
Q

Erlotinib target and type

A

EGFR, small molecule

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2
Q

Gefitinib target and type

A

EGFR, small molecule

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3
Q

Cisplatin mechanism? sensitizer?

A

Interstrand cross-links, cell cycle non-specific, inhibits DNA>RNA, radiosensitizer

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4
Q

Paclitaxel MOA

A

stabilizes microtubules and protects from disassembly so MITOSIS is blocked and apoptosis is activated

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5
Q

Vincristine MOA

A

stabilizes microtubules and protects from disassembly so MITOSIS is blocked and apoptosis is activated

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6
Q

Docetaxel MOA

A

disrupts microtubules

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7
Q

Oxygen effect for chemo

A

True for BleOmycin

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8
Q

Chemos that need hypoxia

A

Mitomycin C

Tirapazamine

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9
Q

Drugs that radiosensitize hypoxic cells

A

Misonidazole
Etanodazole
Nimorazole (only clinically used one, in HNSCC)

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10
Q

Cetuximab target and type

A

EGFR tki, mAb

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11
Q

Panitumumab target and type

A

EGFR tki, mAb

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12
Q

Sirolimus target

A

mTOR (FRAP1)

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13
Q

Everolimus target

A

mTOR (FRAP1)

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14
Q

Rapamycin target

A

mTOR (FRAP1)

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15
Q

Bortezomib target

A

proteosome inhibitor (ubiq mediated proteins) in MM

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16
Q

Nivolumab target

A

PD1

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17
Q

Pembro target

A

PD1 (improved OS/PFS PDL1 expression > 50%)

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18
Q

Atezolizumab target

A

PDL1

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19
Q

Durvalumab target

A

PDL1

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20
Q

Avelumab target

A

PDL1

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21
Q

Ipilimumab

A

CTLA4

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22
Q

Temozolamide sensitive

A

MGMT silencing

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23
Q

Pemetrexed sensitivity in NSCLC

A

Thymidylate synthase downregulated

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24
Q

NER overactivity chemo response

A

cisplatin-resistant (NSCLC)

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25
Q

NER defects (ERCC2 mutated) chemo response

A

platinum-sensitive

26
Q

HR defects (BRCA1/2) chemo response

A

platinum-sensitive

27
Q

Infliximab target

A

TNF-alpha

28
Q

Tipifarnib

A

RAS (farnesyl transferase)

29
Q

Best radioprotectors

A

Thiols, need to be in the cell during the radiation
Amifostine
Sulfydryl
They might put an H back on free radicals

30
Q

Imatinib target

A

BCR-ABL (TKI)

31
Q

Rituxumab target

A

CD20

32
Q

Vorinostat target

A

HDAC inhibitor (CTCL)

33
Q

Alectanib target

A

ALK

34
Q

Wee1 inhibitor target

A

block G2—> M checkpoint

35
Q

Crizotinib target

A

ALK, ROS1

36
Q

Trastuzumab/pertuzumab/lapatinib target

A

HER2

37
Q

Sorafenib target

A

Raf

38
Q

Vemurafenib

A

Raf

39
Q

Bromodeoxyuridine MOA

A

incorp into DNA in place of thymidine during S phase (decrease or removal of shoulder of survival curve); also increased sensitivity to light, radiosensitizer

40
Q

Hsp90 inhibitor

A

reassortment int G2-M, and other mechs including inhibition of DNA Damage Response, radiosensitizer

41
Q

Radiosensitizers

A

Taxanes, antiangiogenics, platinums

42
Q

Tirapazamine

A

bioreductive drug (undergoes reduction to form a cytotoxic species) selectively toxic to hypoxic cells; higher esophagitis SWOG), radiosensitizer

43
Q

Radiation Mitigator (given after exposure

A

Growth factors/cytokines (keratinocyte growth factor palfermin, G-CSF, IL-11)
Antioxidants

44
Q

Other radioprotectors

A

superoxide dismutase (SOD) (Converts )2 > H2O2
Cysteine
WR2721
WR638 (both cover sulfhydryl with phosphate, not useful)

45
Q

Alkylating Agents, other pearl?

A

“ides” nad “ines”: (cyclophosphamide, TMZ, Lomustine, ifosfamide, dacarbazine),
CNS penetration
(adds alkyl group to guanine, preventing strands of DNA from linking)

46
Q

Antibiotics? Radiosensitizing?

A

Doxorubicin(Adriamycin) Epirubicin, Mitomycin C, Bleomycin, Daunorubicin, Actinomycin D
Very Radiosensitizing

47
Q

anti-Metabolites, Cell cycle-dependent?

A

“abine”
5FU, gemcitabine, capecitabine, Methotrexate, 6-MP, cytarabine, hydroxyurea
Cell cycle - S phase

48
Q

Vinka Alkaloid drugs? cell cycle-dependent?

A

Vincristine, Vinblastin, Vinorelabine, Vindesin
Mitosis
No CNS penetration

49
Q

Taxane drugs, cell cycle-dependent? radiosensitizing?

A

Paclitaxel, Docetaxel, Cabazitaxel
Mitosis
Radiosensitizing

50
Q

Topoisomerase inhibitors… Cell cycle dependence? radiosensitizing?

A

Partial S- cycle

not very sensitizing

51
Q

Antibodies cross BBB?

A

No, too large

52
Q

Tremelumimab target

A

CTLA4

53
Q

Doxorubicin and Epirubicin MOA?

A

intercalation and inhibition of DNA biosynthesis; stabilizes topoisomerase II (prevents progression of relaxing supercoils for transcription) thereby preventing replication; most active during S-phase

54
Q

Doxil (liposomal doxorubicin)

A

preferenetial concentration to skin, designed for Kaposi sarc

55
Q

Irinotecan, Topotecan MOA

A

Topoisomerase I inhibitor

56
Q

Etoposide

A

Topoisomerase II inhibitor

57
Q

5FU MOA

A

pyrimidine antimetabolite, stimulates thymidilate synthase (S-phase)

58
Q

Gemcitabine

A

antimetabolite, nucleoside analog inhibits ribonucleotide reductase

59
Q

MTX

A

antimetabolite, inhibits dihydrofolate reductase blocking DNA/RNA synthesis through similarity to folic acid

60
Q

Bleomycin MOA

A

induction of DNA strand breaks (may also inhibit thymidine incorp in DNA strands)
may act via free radicals formed from 02, therefore more tox w/02 (lung tox)

61
Q

Dactinomycin

A

blocks RNA synthesis/transcription, antibiotics

62
Q

Hydroxyurea

A

inhibits RNR

Rad Bio (6 decks)

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