Core Medication List
Blocking the cell cycle by cytostatic drugs
General toxic effects: hair loss, bone marrow toxicity, impaired wound healing, damage to
gastrointestinal epithelium, nausea and vomiting, depression of growth in children, sterility,
teratogenicity.
Alkylating and related agents: cyclophosphamide, cisplatin, oxaliplatin
→ Affect the cell cycle (not phase dependent).
Mechanism of action: reactive covalent binding between alkylgroup and nucleic acid.
Inhibition of DNA replication and RNA transcription. Bifunctional alkylating agents can cause
intrastrand linking and crosslinking. This is a trigger for apoptosis. Indication: solid tumors.
Cisplatin and oxaliplatin have a much higher toxicity: severe nausea and vomiting,
myelosuppression, neurotoxicity and acute nephrotoxicity.
Antimetabolites: methotrexate, fluorouracil (5-FU), cytarabine (not (yet) in TRC database)
→ affect the S-phase of the cell cycle.
Mechanism of action (methotrexate and 5-FU): compete with the natural substrate for the
active site of an enzyme. Inhibition of DNA synthesis and cell death.
Methotrexate: IV is preferred as the bioavailability is unpredictable.
Fluorouracil: pro-drug for 5-FDMP
Common side effects: mucositis, diarrhea, myelosuppression.
Mechanism of action (cytarabine): blocking the function of DNA polymerases. Inhibition DNA
replication. IV administration (in combination with cisplatin)
Common side effects: myelosuppression, nausea, diarrhea.
Antimitotics: paclitaxel, docetaxel
→ affect the M-phase of the cell cycle
Mechanism of action: causes dysfunction in the formation of microtubules. Inhibition of cell
division.
Common side effects: peripheral edema, alopecia, myelosuppression, hypersensitivity
reactions, cardiac disturbances. Administration by IV.
Topoisomerase-inhibitors: doxorubicin
→ affects the cell cycle (not phase dependent)
Mechanism of action: Inhibition of topoisomerases (inhibition of unwinding, cutting and
ligation of DNA). Decreased capacity of DNA repair and inhibited DNA replication.
Common side effects: myelosuppression, vomiting, nausea, alopecia, cardiotoxicity.
Hormonal drugs
Anti-hormones: tamoxifen
Mechanism of action: competes with estradiol. Indication: breast cancer.
Aromatase-inhibitors: anastrozol
Mechanism of action: inhibits the aromatase enzyme.
Blocking the cell cycle by cytostatic drugs
General toxic effects: hair loss, bone marrow toxicity, impaired wound healing, damage to
gastrointestinal epithelium, nausea and vomiting, depression of growth in children, sterility,
teratogenicity.
Alkylating and related agents: cyclophosphamide, cisplatin, oxaliplatin
→ Affect the cell cycle (not phase dependent).
Mechanism of action: reactive covalent binding between alkylgroup and nucleic acid.
Inhibition of DNA replication and RNA transcription. Bifunctional alkylating agents can cause
intrastrand linking and crosslinking. This is a trigger for apoptosis. Indication: solid tumors.
Cisplatin and oxaliplatin have a much higher toxicity: severe nausea and vomiting,
myelosuppression, neurotoxicity and acute nephrotoxicity.
Antimetabolites: methotrexate, fluorouracil (5-FU), cytarabine (not (yet) in TRC database)
→ affect the S-phase of the cell cycle.
Mechanism of action (methotrexate and 5-FU): compete with the natural substrate for the
active site of an enzyme. Inhibition of DNA synthesis and cell death.
Methotrexate: IV is preferred as the bioavailability is unpredictable.
Fluorouracil: pro-drug for 5-FDMP
Common side effects: mucositis, diarrhea, myelosuppression.
Mechanism of action (cytarabine): blocking the function of DNA polymerases. Inhibition DNA
replication. IV administration (in combination with cisplatin)
Common side effects: myelosuppression, nausea, diarrhea.
Antimitotics: paclitaxel, docetaxel
→ affect the M-phase of the cell cycle
Mechanism of action: causes dysfunction in the formation of microtubules. Inhibition of cell
division.
Common side effects: peripheral edema, alopecia, myelosuppression, hypersensitivity
reactions, cardiac disturbances. Administration by IV.
Topoisomerase-inhibitors: doxorubicin
→ affects the cell cycle (not phase dependent)
Mechanism of action: Inhibition of topoisomerases (inhibition of unwinding, cutting and
ligation of DNA). Decreased capacity of DNA repair and inhibited DNA replication.
Common side effects: myelosuppression, vomiting, nausea, alopecia, cardiotoxicity.
Hormonal drugs
Anti-hormones: tamoxifen
Mechanism of action: competes with estradiol. Indication: breast cancer.
Aromatase-inhibitors: anastrozol
Mechanism of action: inhibits the aromatase enzyme.
