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Repro > week 6 - cancer pharmacology > Flashcards

week 6 - cancer pharmacology Flashcards

1
Q

These 8 things are known as the ________ of __________

Sustaining cell proliferation
Resisting cell death (apoptosis)
Inducing angiogenesis
Enabling replicative immortality
Activating invasion and metastasis
Evading growth suppressors
Reprogramming of energy metabolism
Evading immune destruction

A

hallmarks of cancer

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2
Q

Slowly growing tumors are less responsive to cytotoxic drugs, what are two examples of these?

A

colon and non small cell lung cancer

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3
Q

Most act by causing DNA damage. Cancers with high percentage of proliferating cells are susceptible to what type of intervention?

A

Cytotoxic Agents

target DNA mean they target proliferation

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4
Q

What are the two main classes for chemotherapy drugs?

A

Cell cycle specific and cell cycle non specific drugs

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5
Q

What normally rapidly dividing cells are seceptible to chemotherapy cytotoxic drugs?

A

•Bone marrow

Hair follicles

Intestinal epithelium

side effects/ adverse effects

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6
Q

-Staging (T-size of main tumor, M-metastasis, N- # of nearby lymph nodes with cancer)-Age-Comorbid factors-Compliance issues-Patient input-Pretreatment testing (KRas gene mutation, EGFR, HER2) are all important in what clinically

?

A

Determining therapy for cancer

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7
Q

Pretreatment testing (KRas gene mutation, EGFR, HER2) helps with what type of therapy for cancer?

A

Targeted therapy - decreases potential adverse effect

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8
Q

Paclitaxel (Taxol) and Docetaxel (Taxotere) are what class of drugs?

A

Taxanes - natural products

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9
Q

What drug is a natural taxane that was isolated from the Yew tree?

A

Paclitaxel

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10
Q

What class of drugs are potent inhibitors of mitosis (anti-mitotic) - inhibits spindle fibers assembly - act on specific phase of cell cycle meaning they are cell cycle specific drugs. This class Binds specifically to the β-tubulin subunit of microtubules and antagonizes disassembly of this key cytoskeletal protein. It stabilizes the microtubules and results in arrest in mitosis. Efficacy is dependent on both drug concentration and duration of cell exposure.

A

Natural products Taxanes

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11
Q

What drug class side effects include bone marrow toxicity (most common and severe), peripheral neuropathy (dose-limiting toxicity) and nausea/vomiting/diarrhea

A

Natural products - taxanes

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12
Q

Drugs that block cell cycle progression before mitosis antagonize the effect of ____________

A

Taxanes

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13
Q

What drug class was Isolated from the Madagascar periwinkle plant, Catharanthus roseus (formerly called Vinca rosea?

A

Vinca Alkaloids - treated leukemias early on

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14
Q

What two natural products are cell-cycle–specific and block cells in mitosis by binding specifically to β tubulin and to block polymerization with α tubulin into microtubules.

A
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15
Q

Paclitaxal class and MAO

A

taxane prevents depolymerization of microtubules

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16
Q

Docetaxel class and MOA

A

Taxane and inhibits depolymerization

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17
Q

Vincristine class and MOA

A

Vinca Alkaloids and prevents polymerization of microtubules

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18
Q

vinblastine class and Mao

A

Vinca alkaloid, prevents microtubule polymerization (assembly)

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19
Q

what drug class Side effects include Mild neurotoxicity and SIADH (syndrome of inappropriate antidiuretic hormone secretion)?

A

Vinca Alkaloids (Vincristine and Vinblastine)

20
Q

What is doxorubicin class and MOA (3 things)?

A

Antibiotic – member of the anthracycline class

  1. Inhibit DNA and RNA synthesis by intercalating into DNA base pairs and trigger DNA breaks

2. Inhibit topoisomerase II and prevents DNA uncoiling and subsequent transcription and replication

  1. Generate free radicals that damage protein, cell membrane and DNA

These drugs also generate free radicals – cardio toxic effect•Use – Breast and ovarian cancer, sarcomas and lymphoma

21
Q

What drug is a flat planar molecules that inhibit DNA and RNA synthesis by intercalating into DNA base pairs and trigger DNA breaks. thus inhibits topoisomerase II and prevents DNA uncoiling and subsequent transcription and replication. It also generate free radicals that damage protein, cell membrane and DNA. These drugs also generate free radicals – cardio toxic effect

A

Doxorubicin

22
Q

What class of drugs work to inhibit DNA synthesis and are analogues of cytidine and pyrimidine?

A

Antimetabolites

23
Q

Fluorouracil (5-FU) and Capecitabine are what class of drugs

A

Antimetabolites Fluoropyrimidine analogues - 5-FU

24
Q

what drug uses deoxycytidine kinase intracelluarly to phosphorylate it producing difluorodeoxycytidinemonophosphate (dFdCMP), once phosphorylated and incorporated into DNA results in strand termination. It Inhibits DNA synthesis by inhibiting the action of ribonucleoside diphosphate reductase (results in depletion of deoxyribonucleotides for DNA synthesis)

A

Gemcitabine - deoxycytidine analogue

25
Q

Gemcitabine class and MOA

A

Deoxycytidine analogue results in DNA termination by inhibiting ribonucleoside diphosphate reductase

26
Q

What drug has the two main side effects of Myelosuppression and Flu-like symptoms?

A

Gemcitabine - deocycytidine analouge

27
Q

Capecitabine MAO and class

A

Fluoropyrimidine analogues - 5-FU, incoperated into both DNA and RNA (triphosphate form) causing toxicity

28
Q

what enzyme does 5-fluorouricil (5-FU) inhibits dTMP synthesis and needs folate to stabilize bond with enzyme?

A

Thymidylate synthase

29
Q

What drug can be used in addition to 5-fluorouricil (5-FU) to increase folate concentrations to effectively inhibits thymidylate synthase?

A

Leucovorin

30
Q

What is the oral form of the 5-fluoruricil?

A

Capecitabine

31
Q

Along with myelosuppression, what is the additional side effect is seen in Capecitabine vs. 5-FU?

A

Hand-foot syndrome - redress, swelling and blistering of the palms and soles of feet

32
Q

Small molecule targeted therapy are inhibitors of….

A

protein tyrosine kinases (TKIs)

intracellular target

33
Q

Monoclonal antibodies (mab) are inhibitors of …

A

EGFR - target outside receptor (do not need to enter cell)

34
Q

inhibitors of human epidermal growth factor ________ receptor

A

(HER2/NEU)

35
Q

What agents hit specific targets, and are not cell-cycle specific and Typically, these produce fewer side effects?

A
36
Q

What drug is a humanized monoclonal antibody that binds to the external domain of HER2/neu (ErbB2) that 30% of breast cancers overexpress HER2/neu(ErbB2) due to gene amplification on chromosome 17?

A

Trastuzumab (HERCEPTIN)

37
Q

Trastuzumab (HERCEPTIN) class and MOA

A

humanized monoclonal antibody that binds to the external domain of HER2/neu (ErbB2).

38
Q

what drug causes the side effects -

infusion effects (serum sickness) include fever, chills, nausea, dyspnea, and rashes (why?)

Cardiotoxicity (which other drug should we be careful of when combining with this?)

A

•Trastuzumab (HERCEPTIN) - humanized monoclonal antibody that binds to the external domain of HER2/neu (ErbB2).

Why - serum sickness

Cardiotoxicity is reversible should not be combined with doxorubicin also causing cardiac toxicity

39
Q

What two drugs can cause cardiac toxicity?

A

Trastuzumab (mAb) and Doxorubicin (anthracycline - Ab)

40
Q

What small molecular drug is a Dual EGFR/HER2 inhibitor

and its MOA is to Inhibit EGFR and HER2 tyrosine kinases

A

Lapatinib (TYKERB) is FDA-approved for HER2-amplified, trastuzumab-refractory breast cancer

41
Q

What drug presents with a Acneform rash in one-third of patients, but means they will have a good response?

Side effects include Diarrhea

Use with caution in patients with heart disease

A

Lapatinib - small molecule

42
Q

what small molecule drug Competitively blocks ATP by binding to the active site of the kinase inhibiting EGFR RTK?

A

Gefitinib

43
Q

What small molecule drug is a dual EGFR/HER2 inhibitor?

A

Lapatinib

44
Q

What class of drugs causes… In the cell, the chloride, cyclohexane, or oxalate ligands of the three analogs are displaced by water molecules, yielding a positively charged and highly reactive molecule. This positive charge is looking for electron. In the primary cytotoxic reaction, the aquated species of the drug then reacts with nucleophilic sites on DNA and proteins (guanine is preferred resulting in cross-linking of DNA and apoptosis

A

Platinum analogues

Cisplatin and carboplatinm

45
Q

what is the main side effect of platinum analogues?

A

Nephrotoxicity

  • in some cases hydration can help

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