Cancer Drugs Flashcards

1
Q

The alkylating agents exert their effects by

A

on DNA and

protein synthesis by binding to DNA and preventing theunwinding of the DNA molecule.

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2
Q
  • Fluorouracil:
A

It is used for colon cancer, esophageal cancer, stomach
cancer, pancreatic cancer, breast cancer, and cervical
cancer.
Acts as thymidylatesynthase (TS) inhibitor. Interrupting the action of this enzyme blocks synthesis of the pyrimidine thymidylate (dTMP), which is a nucleotide required for DNA replication.

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3
Q

Capecitabine

A

Inhibit dTMP Synthesis

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4
Q

Cytarabine:

A

Cytarabine (ara-C) is an arabinose analog of cytosine.
Ara-CTP inhibits DNA polymerase, an enzyme responsible for strand elongation.
• Cytarabine is mainly used in the treatment of acute myeloid leukaemia, acute lymphocytic leukaemia (ALL) and in lymphomas
• The toxicity of cytarabine is dose dependent. The most characteristic toxicity of high-dose ara-C (>1 g/m2 per dose) regimens

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5
Q

Gemcitabine

A

Gemcitabine is a fluorine-substituted deoxycytidine
analog related structurally to cytarabine.
• Gemcitabine is incorporated into DNA, where it inhibits DNApolymerase activity.
• Compared with cytarabine gemcitabine achieves
intracellular concentrations about 20 times higher than
does ara-C, secondary to increased penetration of cell
membranes, and greater affinity for the activating
enzyme deoxycytidine kinase.

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6
Q

Azacytidine and Decitabine: •

A

Both of these agents are nucleoside analogs, and act by direct incorporation into DNA and inhibition of DNA
methyltransferase which cause hypomethylation of
DNA.
• Azacitidine, marketed as Vidaza, is used mainly in the
treatment of myelodysplastic syndrome

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7
Q
  • 6-Mercaptopurine and 6-Thioguanine:
A

6-Mercaptopurine (6-MP) is used to treat acute lymphocytic leukemia, Crohn’s disease, and
ulcerative colitis.
• Mercaptopurine (6-MP) competes with the purine derivatives hypoxanthine and guanine
for the enzyme HGPRT and is itself converted to thio inosine monophosphate (TIMP). • TIMP inhibits several chemical reactions
• In addition, 6-methylthioinosinate (MTIMP) is formed by the methylation of TIMP. • Both TIMP and MTIMP have been reported to inhibit glutamine-5-
phosphoribosylpyrophosphate amidotransferase,
Inhibit Purine BioSynthesis

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8
Q

Fludarabine Monophosphate

A

is an analog of the purine adenine.
Fludarabine interferes with DNA polymerase, causing chain termination.
• Fludarabine is also immunosuppressive, with associated opportunistic infections resulting from fludarabine’s effect on T cells and a subsequent decrease in CD4 counts; prophylactic antibiotics and antiviral medications are recommended.
• Fludarabine is highly effective in the treatment of chronic lymphocytic leukemia

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9
Q

Cladribine and pentostatin

A

are purine nucleoside analogs
.• Cladribine is resistant to inactivation by adenosine deaminase and triphosphorylated to an active form that is incorporated into DNA, resulting in inhibition of DNA synthesis and early chain termination.

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10
Q

Antifolates (Leucovorin

A

They carry one-carbon group in transfer
reactions that are required for purine and
thymidylic acid synthesis, and, in turn, for
formation of DNA and for cell division.
This drug bypasses the
metabolic block induced by DHFR inhibitors

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11
Q

Methotrexate

A

• It is effective for the treatment of a number of
cancers, including breast, head and neck,
leukemia, lymphoma, lung, osteosarcoma,
bladder, and trophoblastic neoplasms.

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12
Q

What’s Pemetrexed

A

It’s a multitargeted
antifolate that inhibits at least three biosynthetic
pathways in thymidine and purine synthesis.

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13
Q

Vinca alkaloids derived from, act as

A

Vincristine, vinblastine, and vinorelbine are natural alkaloids derived from the periwinkle (vinca) plant. They act as mitotic inhibitors, or “spindle poisons.”

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14
Q

Vinca alkaloids are used for treatment of

A

leukemias, lymphomas, sarcomas, and other solid tumors. Due to poor penetration of the BBB, vinca alkaloids are associated only occasionally with episodes of CNS toxicity.

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15
Q

Paclitaxel and docetaxel are

A

taxane plant alkaloids with

antimitotic activity.

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16
Q

How do DNA topoisomerase enzymes relieve torsional

strain?

A

during DNA unwinding by producing

strand breaks.

17
Q

Camptothecin?

A

A plant alkaloid derived from
Camptotheca acuminata, is a potent inhibitor
of DNA topoisomerase I.

18
Q

Doxorubicin, Daunorubicin, Idarubicin, and Epirubicin, what are they classified as

A

Anthracyclines have been classified as antitumor
antibiotics, but it is more accurate to refer to them as
intercalating topoisomerase inhibitors.

19
Q

Alkylating Agents MOA

A

All of the alkylating agents work through the
covalent bonding of highly reactive alkyl groups
or substituted alkyl groups with nucleophilic
groups of proteins and nucleic acids.
Clinical use in world war 1

20
Q

Cyclophosphamide and ifosfamide are

A

nitrogen mustard derivatives, and are widely

used alkylating agents.

21
Q

Acrolein,

A

a metabolite of both cyclophosphamide and ifosfamide, has little antitumor activity, but is responsible for the
hemorrhagic cystitis of these agents.

22
Q

The nitrosoureas are alkylating agents characterized by

A

lipophilicity and ability to cross the blood–brain barrier

23
Q

• Dacarbazine and Temozolomide Dacarbazine (DTIC)

and temozolomide are nonclassic alkylating agents.

A
Both compounds undergo demethylation to the same
active intermediate (monomethyl triazeno-imidazolecarboxamide [MTIC]) that interrupts DNA replication by causing methylation of guanine.
24
Q

The platinum derivatives—cisplatin, carboplatin,

and oxaliplatin—

A

• The cytotoxicity of the platinum derivatives
depends on platinum binding to DNA and the
formation of intrastrand cross-links or adducts
between neighboring guanines.

25
Q

Cisplatin adverse effects

A

Cisplatin is a highly toxic antineoplastic agent that
can cause serious nephrotoxicity, ototoxicity,
peripheral neuropathy, emesis, and anemia.

26
Q

Two main classes of MoABs are used in the

treatment of cancer,

A

the most common of which

are unconjugated or naked MoABs.

27
Q

The other class is immunoconjugates,

A

which are MoABs conjugated to a toxin (immunotoxin),
chemotherapy agent, or radioactive particle
(radioimmunoconjugate).

28
Q

Unconjugated MoABs MOA

A

that target antigens on the
cell surface of cancer cells may directly mediate
cell killing through complement activation
(complement-dependent cytotoxicity [CDC]),
antibody-dependent cellular toxicity (ADCC), or
signaling the cascade of events that lead to tumor
cell apoptosis.

29
Q

Gemtuzumab ozogamicin consists of

A

recombinant humanized anti-CD33 MoAB
conjugated to the calicheamicin derivative
Nacetyl- gamma calicheamicin, a cytotoxic
antitumor antibiotic, by the linker ozogamicin

30
Q

Rituximab

A

Rituximab is a chimeric MoAB directed against
the CD20 antigen found on the surface of
normal and malignant B cells.

31
Q

Cetuximab

A

is a recombinant chimeric MoAB that binds
specifically to the extracellular domain of EGFR. • Cetuximab is also approved for use in head and neck
cancer either by itself or in combination with radiation.

32
Q

Trastuzumab

A

is a recombinant humanized MoAB that

selectively binds to HER-2.

33
Q

Bevacizumab

A

Bevacizumab is a recombinant humanized MoAB
directed against circulating VEGF. • Bevacizumab binds to all biologically active circulating
isoforms of VEGF and prevents the activation and
promotion of angiogenesis.