Professional Documents
Culture Documents
TES
Prepared by:
Bati, Charrysse Bernadette
Cai, Delia Joyce
BSP3F
Definition
Antimetabolite
-a
substance that interferes
with the normal
metabolic processes
within cells, typically by
combining with enzymes.
Characteristics
Structural analogs of naturally
occurring compounds
Work via a variety of mechanisms
that include competitive inhibition
and incorporation into nucleic acids
S-phase-specific that interfere with
DNA synthesis
Myelosuppression is the dose
toxicity for all drugs in this class
Structure Activity
Relationship
5
1
2
Uracil
5Fluorouraci
l
1
2
5
6
7
4 9
3
Pteridine
ring
Para-amino
benzoic
acid
Glutamic
acid
Mechanism of Action
Classes of
Antimetabol
ites
Chemistry
Pyrimidine
These
drugs
drugs resemble
cytosine, thymine or uracil
Pyrimidine is a 6membered ring consisting
of four carbon atoms and
two nitrogen centers at
the 1- and 3- ring
positions
Pyrimidine drugs
Examples
Chemical Structure
Clinical Uses
5-Fluorouracil
Tx of several
carcinoma types
breast cancer,
stomach cancer,
pancreatic cancer,
Topical use basal cell
cancer of the skin
Floxuridine
Tx metastatic GI
adrenocarcinoma
Examples
Chemical Structure
Clinical Uses
Capecitabine
Gemcitabine
Tx of bladder cancer,
Pancreatic cancer,
And NSCLC (non-small
cell lung cancer)
Cytarabine
Tx of acute
myelogenous leukemia
and CML (Chronic
Myelogenous
Leukemia)
Examples
Chemical structure
Clinical Uses
Tegafur
is achemotherapeutic
fluorouracil prodrug
used in the treatment
of the ff cancers:
Stomach
Breast
Gallbladder
Lung
Colorectal
Head and neck
Liver
Pancreatic
Decitabine
Chemistry
Purine
drugs
These drugs resemble
guanine or adenine. A
purine is a
heterocyclic aromatic
organic compound. It
consists of a
pyrimidine ring fused
to an imidazole ring
Purine Drugs
Examples
Chemical structure
Clinical Uses
6-Mercaptopurine
Tx of lymphoblastic
leukemia
Acute lymphocytic
leukemia
Crohns disease
Thioguanine
Tx acute
nonlymphocytic
leukemia
Cladribine
Examples
Chemical Structure
Clinical Uses
Pentostatin
Fludarabine
Tx chronic
lymphocytic leukemia
and non-Hodgkins
lymphoma
Clofarabine
treat acute
lymphoblastic
leukemia in children
and young adults up
to 21 years old
Chemistry
Folates
Folate
Folate
drugs
Examples
Chemical structure
Clinical Uses
Methotrexate
Tx breast cancer
Bladder cancer
Colorectal cancer
Head and neck
cancer
Pemetrexed
Effective against
mesothelioma,
NSCLC, colorectal
cancer, bladder
cancer and lung
cancer
Trimetrexate
Tx colorectal cancer,
head and neck
cancer as well as
NSCLC
Adverse Effects