Drugs and Interactions Flashcards by Photon Slinger

Erlotinib target and type

EGFR, small molecule

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Gefitinib target and type

EGFR, small molecule

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Cisplatin mechanism? sensitizer?

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

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Paclitaxel MOA

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

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Vincristine MOA

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

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Docetaxel MOA

disrupts microtubules

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Oxygen effect for chemo

True for BleOmycin

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Chemos that need hypoxia

Mitomycin C

Tirapazamine

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Drugs that radiosensitize hypoxic cells

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

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Cetuximab target and type

EGFR tki, mAb

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Panitumumab target and type

EGFR tki, mAb

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Sirolimus target

mTOR (FRAP1)

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Everolimus target

mTOR (FRAP1)

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Rapamycin target

mTOR (FRAP1)

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Bortezomib target

proteosome inhibitor (ubiq mediated proteins) in MM

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Nivolumab target

PD1

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Pembro target

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

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Atezolizumab target

PDL1

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Durvalumab target

PDL1

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Avelumab target

PDL1

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Ipilimumab

CTLA4

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Temozolamide sensitive

MGMT silencing

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Pemetrexed sensitivity in NSCLC

Thymidylate synthase downregulated

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NER overactivity chemo response

cisplatin-resistant (NSCLC)

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NER defects (ERCC2 mutated) chemo response

platinum-sensitive

HR defects (BRCA1/2) chemo response

platinum-sensitive

Infliximab target

TNF-alpha

Tipifarnib

RAS (farnesyl transferase)

Best radioprotectors

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

Imatinib target

BCR-ABL (TKI)

Rituxumab target

CD20

Vorinostat target

HDAC inhibitor (CTCL)

Alectanib target

ALK

Wee1 inhibitor target

block G2---> M checkpoint

Crizotinib target

ALK, ROS1

Trastuzumab/pertuzumab/lapatinib target

HER2

Sorafenib target

Raf

Vemurafenib

Raf

Bromodeoxyuridine MOA

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

Hsp90 inhibitor

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

Radiosensitizers

Taxanes, antiangiogenics, platinums

Tirapazamine

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

Radiation Mitigator (given after exposure

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

Other radioprotectors

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

Alkylating Agents, other pearl?

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

Antibiotics? Radiosensitizing?

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

anti-Metabolites, Cell cycle-dependent?

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

Vinka Alkaloid drugs? cell cycle-dependent?

Vincristine, Vinblastin, Vinorelabine, Vindesin Mitosis No CNS penetration

Taxane drugs, cell cycle-dependent? radiosensitizing?

Paclitaxel, Docetaxel, Cabazitaxel Mitosis Radiosensitizing

Topoisomerase inhibitors... Cell cycle dependence? radiosensitizing?

Partial S- cycle | not very sensitizing

Antibodies cross BBB?

No, too large

Tremelumimab target

CTLA4

Doxorubicin and Epirubicin MOA?

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

Doxil (liposomal doxorubicin)

preferenetial concentration to skin, designed for Kaposi sarc

Irinotecan, Topotecan MOA

Topoisomerase I inhibitor

Etoposide

Topoisomerase II inhibitor

5FU MOA

pyrimidine antimetabolite, stimulates thymidilate synthase (S-phase)

Gemcitabine

antimetabolite, nucleoside analog inhibits ribonucleotide reductase

MTX

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

Bleomycin MOA

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)

Dactinomycin

blocks RNA synthesis/transcription, antibiotics

Hydroxyurea

inhibits RNR

Drugs and Interactions Flashcards

(62 cards)