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MS 2 - Unit 1 > Pharmacology - Cancer III Lecture > Flashcards

Pharmacology - Cancer III Lecture Flashcards

1
Q

MOA - DNA Intercalating Agents (general)

A

Bind DNA through intercalation between specific bases, blocking DNA, RNA synthesis, or both Causes DNA strands to break and interfere with cell replication

anti-tumor antibiotics produced by Streptomyces

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2
Q

Class - Dactinomycin (Actinomycin-D, Cosmegen)

A

DNA intercalating agent

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3
Q

What are the side effects of Dactinomycin?

A

Hematopoetic suppression with pancytopenia

Anorexia, nausea, vomiting

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4
Q

What cancers is Dactinomycin used for?

A

Pediatric tumors, ie Wilm’s tumor,

rhabdomyosarcoma,

Ewing’s sarcoma

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5
Q

MOA - Dactinomycin (Actinomycin D, Cosmegen)

A

Intercalates C-G pairs of DNA interfering with DNA-dependent RNA polymerase

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6
Q

Class - Daunorubicin (Cerubidine)

A

DNA intercalating agents: anthracyclines

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7
Q

What cancer is Daunorubicin used for?

A

Daunorubicin and Idarubicin

  • used in combination with Ara-C for treatment of AML
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8
Q

MOA - Daunorubicin (Cerubidine)

A

Intercalate in DNA Donates electrons to O2 to form superoxide –> H2O2 –> OH radical cleaves DNA

same MOA as all anthracyclines: Daunirubicin, Idarubicin, Epirubicin and Doxorubicin

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9
Q

What are the side effects of Daunorubicin?

A

Irreversible dose-dependent cardiac toxicity –dexrazoxane is cardio-protective Mylosuppression Stomatitis and GI disturbances Alopecia same effects as Idarubicin, Doxorubicin, Epirubicin

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10
Q

Class: Idarubicin (Idamycin)

A

DNA intercalating agents: anthracyclines

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11
Q

Class: Doxorubicin (Adriamycin, Doxil)

A

DNA intercalating agents: anthracyclines

**one of the most widely used cancer drugs** broad clinical application

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12
Q

Class: Epirubicin (Ellence)

A

DNA intercalating agents: anthracyclines

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13
Q

Class: Bleomycin (Blenoxane)

A

DNA intercalating agent

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14
Q

Class: Vinblastine (Velban)

A

Microtubule inhibitors: Vinca alkaloids

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15
Q

Class: Vincristine (Oncovin)

A

Microtubule inhibitors: Vinca alkaloids

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16
Q

Class: Paclitaxil (Taxol, Abraxane)

A

Microtubule inhibitors: Taxanes

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17
Q

Class: Docetaxel (Taxotere)

A

Microtubule inhibitors: Taxanes

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18
Q

MOA - Idarubicin (Idamycin)

A

Intercalate in DNA Donates electrons to O2 to form superoxide –> H2O2 –> OH radical cleaves DNA same MOA as all anthracyclines: Daunirubicin, Idarubicin, Epirubicin and Doxorubicin

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19
Q

What cancer is Idarubicin used to treat?

A

Daunorubicin and Idarubicin

  • used in combination with Ara-C for treatment of AML
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20
Q

What are the side effects of Idarubicin?

A

Irreversible dose-dependent cardiac toxicity –dexrazoxane is cardio-protective Mylosuppression Stomatitis and GI disturbances Alopecia same side effects as Daunorubicin, Doxorubicin, Epirubicin

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21
Q

What are the side effects of Doxorubicin?

A

Irreversible dose-dependent cardiac toxicity –dexrazoxane is cardio-protective Mylosuppression Stomatitis and GI disturbances Alopecia same side effects as Daunorubicin, Idarubicin, and Epirubicin

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22
Q

What are the side effects of Epirubicin?

A

Irreversible dose-dependent cardiac toxicity –dexrazoxane is cardio-protective Mylosuppression Stomatitis and GI disturbances Alopecia same side effects as Daunorubicin, Idarubicin, and Doxorubicin

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23
Q

What are the side effects of Bleomycin?

A

Pulmonary toxicity (fibrosis)****

cutaneous toxicity (hyperpigmentation, hyperkeratosis, erythema) hyperthermia minimally myelo and immunosuppressive headache, nausea, vomiting

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24
Q

MOA - Bleomycin (Blenoxane)

A

a mixture of two peptides obtained from Streptomyces

Acts in G2 phase of cell cycle

Binds to DNA and makes ss and ds DNA breaks

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25
What cancers does Bleomycin treat?
- used as a component of PEB combo regimen for treatment of testicular carcinomas or as a component of ABVD regimen for Hodgkin’s disease squamous cell carcinomas
26
What cancers does Epirubicin treat?
Metastatic breast cancer gastric cancer - used in combo regimen (FEC) for treatment of metastatic breast cancer
27
MOA - Doxorubicin
Intercalate in DNA Donates electrons to O2 to form superoxide --\> H2O2 --\> OH radical cleaves DNA same MOA as all anthracyclines: Daunirubicin, Idarubicin, Epirubicin and Doxorubicin -has broad clinical spectrum; one of the most widely used anticancer drugs - used for treatment of sarcomas, breast and lung carcinomas, and lymphomas
28
MOA - Epirubicin
Intercalate in DNA Donates electrons to O2 to form superoxide --\> H2O2 --\> OH radical cleaves DNA same MOA as all anthracyclines: Daunirubicin, Idarubicin, Epirubicin and Doxorubicin
29
MOA - Vinblastine (Velban)
MT inhibitor - Vinca alkaloid Block tubulin polymerization into MTs same as Vincristine
30
MOA - Vincristine (Oncovin)
MT inhibitor - Vinca alkaloid Block tubulin polymerization into MTs same as Vinblastine
31
What cancers is Vinblastine used for?
part of ABVD for Hodgin's disease \*\*\* Metastatic testicular tumors (in combo with bleomycin, cisplatin)
32
What are the side effects of Vinblastine?
Myelosuppression, nausea, vomiting
33
What cancers is Vincristine used to treat?
Childhood ALL (with glucocorticoids) also a component of MOPP (as Oncovin) regimen for Hodgkin’s lymphoma
34
What are the side effects of Vincristine?
Dose-limiting neurotoxicity (peripheral neuropathy)\*\*\* Low myelosuppression
35
MOA - Paclitaxel and Docetaxel
MT inhibitor - Taxanes Block MT depolymerization into tubulin
36
What cancers is Paclitaxel used for?
Metastatic breast, ovarian, lung, head and neck cancers (like Docetaxel)
37
What cancers is Docetaxel used for?
Metastatic breast, ovarian, lung, head and neck cancers (like Paclitaxel) hormone refractory prostate cancer\*\*\*
38
What are the side effects of both Paclitaxel and Docetaxel?
Peripheral neuropathy \*\*\* Neutropenia Hypersensitivity reactions \*\*\* (during infusion) Peripheral edema
39
Name the Anthracyclines (DNA Intercalating Agents)
Daunorubicin, Doxorubicin, Epirubicin, Idarubicin
40
What is Dexrazoxane?
The Anthracyclines (ie doxyrubicin) have Dose-limiting cardiotoxicity (cardiomyopathy); Dexrazoxane is an iron-chelating agent that blocks the formation of free radicals and protects against cardiotoxicity of anthracyclines such as doxorubicin.
41
How does resistance to MT inhibitors like Vincristine and Vinblastine occur?
- amplification of P-glycoprotein - mutations in tubulin resulting in reduced binding of the drugs to their target
42
MOA - Topoisomerase Inhibitors
Topoisomerases mediate DNA strand breakage and resealing during replication or transcription of DNA. Topoisomerase I breaks and reseals single-stranded DNA, whereas topoisomerase II breaks and reseals double-stranded DNA. Inhibitors of topoisomerases cause permanent DNA strand breaks by preventing the resealing of nicked strands of DNA. 1. Epipodophyllotoxins: Etoposide, Teniposide 2. Camptothecin Analogs: Irinotecan, Topotecan
43
MOA - Epipodophyllotoxins
Epipodophyllotoxins: Etoposide, Teniposide - inhibit topoisomerase II
44
What are the therapeutic uses for Etoposide?
Etoposide has broad clinical spectrum; used for treatment of testicular carcinoma, lung cancer, and non-Hodgkin’s lymphoma Topoisomerase inhibitor - epipodophyllotoxin - inhibits top II
45
What is the main therapeutic use for Teniposide?
Teniposide mainly used for acute lymphoblastic leukemia (ALL)
46
What are the side effects of Teniposide/Etoposide?
- dose-limiting myelosuppression (neutropenia) - oral mucositis
47
MOA - Camptothecin analogs
Camptothecin Analogs: Irinotecan, Topotecan - inhibit topoisomerase I
48
What cancers does Irinotecan treat?
- Irinotecan is approved for treatment of advanced colorectal cancer; also used for lung, ovarian, cervical and brain tumors Camptothecin analog - topoisomerase inhibitor - inhibits top I
49
What cancers does Topotecan treat?
Topotecan is indicated for treatment of ovarian and small cell lung cancer Topoisomerase inhibitor - Camptothecin analog - inhibits top I
50
What are the side effects of the Camptothecin analogs (Irinotecan, Topotecan)?
Severe neutropenia Severe diarrhea
51
Hormone therapy may be useful for what cancers?
Hormonal therapy is useful in three clinical settings: 1. Lymphomas and leukemias 2. Breast cancer 3. Prostate cancer
52
MOA - glucocorticoids
Glucocorticoids: Prednisone, Dexamethasone cytotoxic effects on lymphocytes; inhibit mitosis in lymphocytes
53
Give three therapeutic uses for glucocorticoids in cancer.
- Prednisone plus vincristine produce remission in patients with ALL - Prednisone is also a component of combination regimens (MOPP and CHOP) for Hodgkin’s and non-Hodgkin’s lymphomas - Dexamethasone is used to reduce edema following radiation therapy of brain tumors
54
Give an example of a Selective Estrogen-Receptor Modulators (SERMs)
Tamoxifen competes with natural hormone for intracellulr receptor
55
Give an example of a Selective Estrogen-Receptor Downregulators (SERDs).
Fulvestrant
56
Give an example of an Aromatase Inhibitor (AI).
Aromatase Inhibitors (AIs): Aminoglutethamide, Anastrozole, Letrozole, Exemestane
57
What is Tamoxifen used for?
Therapeutic Uses - used for treatment of ER-positive early-stage and metastatic breast cancer - used for prevention of breast cancer in high risk women (family history) Toxicity - hot flushes, hair loss, nausea and vomiting - weak agonist of ER in endometrium; increased risk of endometrial cancer and thromboembolism
58
How is Fulvestrant used?
- Fulvestrant is the first FDA approved SERD - binds to ER with a much higher affinity (\>100 fold) than tamoxifen and inhibits hormone-receptor complex formation - also reduces ER expression Therapeutic Uses - approved for postmenopausal women with ER-positive metastatic breast cancer
59
Why is Aminoglutethamide not used anymore?
First generation AI significant toxicity Replaced by third generation AIs like Anastrozole, Letrozole, Exemestane
60
What are the third generation AIs?
Anastrazole, Exemastane, Letrozole ## Footnote - third-generation AI; potent and selective inhibitor of aromatase - Anastrozole and Letrozole are non-steroidal reversible inhibitors of aromatase - Exemestane is a steroidal inhibitor of aromatase; it competes with the natural substrate androstenedione; irreversibly inactivates aromatase Therapeutic Uses - third generation AIs are most commonly used for the treatment of early- stage and advanced breast cancer - have replaced tamoxifen as first-line therapy for postmenopausal ER+ breast cancer
61
What are Leuprolide, Goserelin used for?
Hormone Tx for Prostate cancer - are GnRH analogs - bind to GnRH receptor and inhibit the release of FSH and LH, resulting in reduced testicular production of testosterone - do not inhibit adrenal androgen synthesis
62
What are Flutamide, Bicalutamide used for?
Flutamide, Bicalutamide Hormone therapy for prostate cancer - are non-steroidal androgen-receptor (AR) blockers - compete with natural hormone testosterone for binding with the AR
63
MOA - Hydroxyurea
- inhibits ribonucleotide reductase, which catalyzes the conversion of ribonucleotides to deoxyribonucleotides Miscellaneous anticancer agent - useful for treatment of myeloproliferative neoplasms (polycythemia vera, essential thrombocythemia) - also approved for treatment of sickle cell disease
64
What is All-trans-retinoic acid used to treat?
All-trans retinoic acid (ATRA) Miscellaneous anticancer agent - approved for treatment of acute promyelocytic leukemia (APL) a.k.a. AML M3 - promotes differentiation of promyelocytes
65
What is Arsenic Trioxide?
Arsenic Trioxide Miscellaneous anticancer agent - a heavy metal toxin highly effective in the treatment of relapsed APL
66
MOA - Thalidomide
Miscellaneous anticancer agent ## Footnote - approved for treatment of multiple myeloma and MDS - inhibits the production of IL-6, which is a growth factor for myeloma cells - inhibits angiogenesis
67
What cancers can Interferon-alpha treat?
Interferon-alpha - approved for treatment of hairy cell leukemia, CML and AIDS-related Kaposi’s sarcoma
68
Tyrosine Kinase Inhibitors include:
- Imatinib (Abl inhibitor) for treatment of CML - Gefitinib/Erlotinib (EGFR inhibitor) for treatment of non-small cell lung cancer
69
Give two examples of monoclonal antibodies.
Monoclonal Antibodies - Trastuzumab for treatment of metastatic HER2+ breast cancer - Cetuximab (a mAb against ErbB1) for treatment of metastatic colon cancer
70
What drug can be administered to reduce efflux of anticancer agents and combat drug resistance?
Verapamil (a calcium channel antagonist) inhibits these drug transporters
71
Which of the following chemotherapeutic agents used in drug combination regimens to treat testicular carcinoma is most likely to cause nephrotoxicity? A. Bleomycin B. Cisplatin C. Etoposide D. Luprolide E. Vinblastine
B. Nephrotoxicity is a dose-limiting toxicity of Cisplatin
72
If allopurinol is used to offset hyperuricemia in a cancer patient, the dosage of which of the following drugs should be reduced to 25% of normal? A. Cytarabine B. 5-Fluorouracil C. 6-Mercaptopurine D. Etoposide E. Paclitaxel
C. The anti-metabolite 6-mercaptopurine is metabolized by the enzyme xanthine oxidase. Allopurinol inhibits xanthine oxidase. In the presence of allopurinol, plasma levels of mercaptopurine may increase rapidly to toxic levels. Therefore, the dosage of 6-MP should be reduced if the cancer patient is receiving allopurinol.
73
Which one of the following anticancer drugs induces mitotic arrest? A. Belomycin B. 5-Fluorouracil C. 6-Mercaptopurine D. Etoposide E. Paclitaxel
E. Paclitaxel binds to tubulin and prevents disassembly of microtubules, which is necessary for chromosome segregation during mitosis.
74
Resistance to which anticancer drug is associated with decreased expression of hypoxanthine-guanine phosphoribosyl transferase (HGPRT)? A. Methotrexate B. 5-Fluorouracil C. Gemcitabine D. 6-Mercaptopurine E. Cytarabine
D. 6-Mercaptopurine is a pro-dug. It is converted to the active metabolite 6-thioinosinic acid by the enzyme HGPRT. Decreased expression of HGPRT will result in reduced production of 6-thioinosinic acid, causing decreased inhibition of purine biosynthesis and resistance to 6-MP.

MS 2 - Unit 1 (12 decks)

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