II. Definitions

  1. Antimetabolite Chemotherapy
    1. Agents (typically analogs) that block DNA, RNA or Protein synthesis
    2. Suppress cancer cell expression, growth and replication

III. Medications Purine Analogs

  1. Mechanism
    1. Purine Analogs, resembling adenine or guanine, and incorporate into DNA
    2. Result in DNA cross-linking and inhibition of synthesis and repair of DNA
  2. Purine Analogs
    1. Azathioprine (Imuran)
    2. Cladribine (Leustatin)
    3. Clofarabine
    4. Fludarabine (Fludara)
    5. Mercaptopurine (6-MP, Purinethol)
    6. Nelarabine
    7. Pentostatin (Nipent)
    8. Thioguanine (6-TG)

IV. Medications: Pyrimidine Analogs

  1. Mechanism
    1. Pyrimidine Analogs, resembling cytosine, uracil or thymine, and incorporate into DNA and RNA
    2. Inhibits DNA and RNA synthesis
    3. Cytidine Analogs are described in a separate category below
  2. Pyrimidine Analogs
    1. Capecitabine (Xeloda)
    2. Floxuridine
    3. Fluorouracil (5-FU)
    4. Trifluridine

V. Medications: Cytidine Analogs

  1. Mechanism
    1. Antineoplastic, PyrimidineNucleoside analogs of cytidine
    2. By binding DNA at cytidine binding sites, these analogs block DNA methyltransferase, and in turn DNA methylation
  2. Cytidine Analogs
    1. Azacitidine (5-azacytidine)
    2. Cytarabine (cytosine arabinoside, ara-C)
    3. Decitabine
    4. Gemcitabine

VI. Medications: Folic Acid Antagonist

  1. Mechanism
    1. Folic Acid analogs that resemble its structure, binding Folate-dependent enzymes, and block their activity
    2. As an example, inhibition of dihydrofolate reductase results in a failed synthesis of Tetrahydrofolate (FH4)
    3. Result in decreased DNA, RNA and Protein synthesis
  2. Folic Acid Antagonists
    1. Methotrexate
    2. Pemetrexed
    3. Pralatrexate

VII. Medications: Histone Deacetylase Inhibitor (HDAC Inhibitor)

  1. Mechanism
    1. Histones are the spools around which DNA are wrapped, and which play a role in gene expression
      1. Cancers may be facilitated by abnormally expressed genes in specific histone regions
    2. HDAC Inhibitors block histone deacetylase
      1. Histone deacetylase is an enzyme that catalyzes removal of acetyl groups from core histones
      2. Results in hyperacetylation of histones, suppressing gene expression and cell differentiation
  2. HDAC Inhibitors
    1. Belinostat (Beleodaq)
    2. Romidepsin (Istodax)
    3. Panobinostat (Farydak)
    4. Vorinostat (Zolinza)

VIII. Medications: Miscellaneous

  1. Various mechanisms that interfere with DNA, RNA or Protein synthesis
  2. Agents
    1. Hydroxyurea

Images: Related links to external sites (from Bing)

Related Studies

Ontology: Folic Acid Antagonists (C0016411)

Definition (NCI_NCI-GLOSS) A substance that blocks the activity of folic acid. Folate antagonists are used to treat cancer.
Definition (NCI) A compound with a chemical structure similar to folic acid. Folate antagonists inhibit one or more folate-dependent enzymes, resulting in decreased DNA, RNA and protein synthesis.
Definition (MSH) Inhibitors of the enzyme, dihydrofolate reductase (TETRAHYDROFOLATE DEHYDROGENASE), which converts dihydrofolate (FH2) to tetrahydrofolate (FH4). They are frequently used in cancer chemotherapy. (From AMA, Drug Evaluations Annual, 1994, p2033)
Definition (CSP) inhibitors of the enzyme, dihydrofolate reductase, which converts dihydrofolate to tetrahydrofolate; frequently used in cancer chemotherapy.
Concepts Pharmacologic Substance (T121)
MSH D005493
SnomedCT 349846008, 372612001
English Acid Antagonists, Folic, Antagonists, Folic Acid, Antifolates, FOLIC ACID ANTAG, folic acid inhibitors (medication), folic acid inhibitors, Folic Acid Antagonists, antifolate, antagonists folate, antifolates, folic acid antagonists, Folic acid--Antagonists, folate antagonist, Inhibitors, Dihydrofolate Reductase, Dihydrofolate Reductase Inhibitors, Reductase Inhibitors, Dihydrofolate, Antifolate, Antifolate (product), Antifolate (substance), folic acid antagonist, Folate Analog, Folate Antagonist, Folate Inhibitors, Folic Acid Analog, Folic Acid Antagonist, Folic Acid Inhibitors
Swedish Folsyraantagonister
Czech kyselina listová - antagonisté
Finnish Foolihapon vastavaikuttajat
French Antagonistes de l'acide folique, Anti-folates, Antifolates, Anti-foliques, Antifoliques
Italian Antifolati, Antagonisti dell'acido folico
Russian ANTAGONISTY FOLIEVOI KISLOTY, FOLIEVOI KISLOTY ANTAGONISTY, АНТАГОНИСТЫ ФОЛИЕВОЙ КИСЛОТЫ, ФОЛИЕВОЙ КИСЛОТЫ АНТАГОНИСТЫ
Polish Antagoniści kwasu foliowego
Japanese 抗葉酸塩, 葉酸拮抗物質, 抗葉酸剤, 葉酸きっ抗剤, 葉酸拮抗剤, 葉酸代謝拮抗剤, 葉酸拮抗体
Spanish antifolato (producto), antifolato (sustancia), antifolato, Antifolatos, Antagonistas del Ácido Fólico
German Antignosten, Folsäure-, Folsäureantagonisten
Portuguese Antagonistas do Ácido Fólico, Antifolatos

Ontology: Pyrimidine analog (C0280039)

Definition (NCI) An antimetabolite that affects the metabolism and utilization of pyrimidines.
Definition (CSP) synthetic or natural chemical compounds which resemble pyrimidine in structure and/or function.
Concepts Nucleic Acid, Nucleoside, or Nucleotide (T114) , Pharmacologic Substance (T121)
SnomedCT 108812001, 372544007
English analogs pyrimidine, pyrimidine analog, Pyrimidine antagonist, Pyrimidine analog (product), Pyrimidine analog (substance), Pyrimidine analogue, Pyrimidine analog, pyrimidine antagonist, Pyrimidine Antagonist
Spanish análogo de pirimidina (producto), análogo de pirimidina (sustancia), análogo de pirimidina

Ontology: Purine analog (C1268902)

Definition (CSP) synthetic or natural chemical compounds which resemble naturally occurring purine in structure and/or function.
Concepts Nucleic Acid, Nucleoside, or Nucleotide (T114) , Biologically Active Substance (T123)
SnomedCT 108799004, 372543001
English analogs purine, purine analog, analogues purine, Purine analog (product), Purine analog (substance), Purine analogue, Purine analog
Spanish análogo de purina (producto), análogo de purina (sustancia), análogo de purina

Ontology: Histone deacetylase inhibitor (C1512474)

Definition (MSH) Compounds that inhibit HISTONE DEACETYLASES. This class of drugs may influence gene expression by increasing the level of acetylated HISTONES in specific CHROMATIN domains.
Definition (NCI) Any substance that inhibits histone deacetylase, an enzyme that catalyzes the removal of acetyl groups from core histones. Inhibition of histone deacetylase can result in hyperacetylation of histones, with an effect on gene expression and cell differentiation.
Definition (NCI_NCI-GLOSS) A substance that causes a chemical change that stops tumor cells from dividing. HDAC inhibitors are being studied in the treatment of cancer.
Concepts Pharmacologic Substance (T121) , Amino Acid, Peptide, or Protein (T116) , Enzyme (T126)
MSH D056572
SnomedCT 423081009, 423078004
English Histone deacetylase inhibitor (product), Histone deacetylase inhibitor (substance), Histone deacetylase inhibitor, Inhibitors, HDAC, Inhibitors, Histone Deacetylase, Deacetylase Inhibitor, Histone, Deacetylase Inhibitors, Histone, HDAC Inhibitors, Histone Deacetylase Inhibitors, Inhibitor, Histone Deacetylase, Histone Deacetylase Inhibitor, histone deacetylase inhibitor, HDAC inhibitor, HDAC Agent
Spanish inhibidor de desacetilasa de histona (sustancia), inhibidor de desacetilasa de histona, inhibidor de histona desacetilasa, inhibidor de desacetilasa de histona (producto), Inhibidores de Histona Desacetilasas, Inhibidores de la Histona Desacetilasa
French Inhibiteurs de désacétylases d'histones, Inhibiteurs de désacétylases d'histone, Inhibiteurs de désacétylase d'histone, Inhibiteurs d'histone désacétylase, Inhibiteurs d'histone désacétylases, Inhibiteurs de la désacétylase des histones, Inhibiteurs de HDAC
German Histondeacetylase-Inhibitoren, Histondeacetylase-Inhibitor, Histondeacetylaseinhibitor, Histondeacetylaseinhibitoren, Histon-Deacetylase-Inhibitor, HDAC-Inhibitoren, Histon-Deacetylase-Inhibitoren
Italian Inibitori delle istone deacetilasi
Portuguese Inibidores de Histona Desacetilases
Russian DEATSETILAZY GISTONOV INGIBITORY, ГИСТОН-ДЕАЦЕТИЛАЗЫ ИНГИБИТОРЫ, GISTON-DEATSETILAZY INGIBITORY, ДЕАЦЕТИЛАЗЫ ГИСТОНОВ ИНГИБИТОРЫ
Czech histondeacetylasy - inhibitory, inhibitory HDAC
Swedish Histondeacetylashämmare
Polish Inhibitory deacetylazy histonów, Inhibitor deacetylazy histonowej, Inhibitory deacetylazy histonowej, Inhibitory HDAC
Japanese ヒストン脱アセチル化阻害剤, ヒストンデアセチラーゼインヒビター, ヒストンデアセチラーゼ阻害剤, ヒストン脱アセチル化酵素阻害剤, HDAC阻害剤, ヒストン脱アセチル化酵素阻害薬
Croatian Histon deacetilaza, inhibitori

Ontology: Antimetabolite Chemotherapy (C1516020)

Definition (NCI) Treatment of cancer that utilizes antimetabolite substances to disrupt DNA, RNA, or protein synthesis.
Concepts Pharmacologic Substance (T121)
English Chemotherapy, Antimetabolites, Chemotherapy, Cancer, Antimetabolites, Antimetabolite Chemotherapy

Ontology: Purine analogs, antimetabolites antineoplastic (C3653380)

Concepts Pharmacologic Substance (T121) , Nucleic Acid, Nucleoside, or Nucleotide (T114)
English Purine analogs, antimetabolites antineoplastic, Purine analogues