Drug Class Drug Name(s) Cell Cycle Mecanism of Action Specific Indications Important Side Resistance
Specificity (if any) Effects Mechanisms
Antimetabolites (folate Methotrexate, S Phase Inhibits DHFR (blocks Multiple Myelosuppression Drug efflux pump
antagonists) Pemetrexed DNA synthesis by malignancies (give Leucovorin to (MDR)
inhibiting THF (choriocarcinoma, alleviate severe BM
production). ALL, breast cancer, suppression),
Pemetrexed also lung cancer, NHL), hepatotoxicity, renal
inhibits thymydilate autoimmune toxicity.
synthase. disorders, abortion *IT Admin: Causes
arachnoiditis and
chronic demyelinating
encephalopathy.
Pyrimidine antagonist 5-FU, Capecitabine S Phase Inhibits thymydilate Liver, head/neck, Myleosuppression. In
synthase to prevent Ovarian, Cervical those with
nucleotide synthesis cancers dihydropyrimidine
and therefore DNA dehydrogenase
synthesis deficiency, life
threatening toxicity
can occur
Pyrimidine Antagonist Cytarabine (Ara-C) S Phase Competitively inhibits AML, ALL, CML, CNS Myelosuppression,
DNA polymerase and leukemia, NHL cerebellar dysfunction
terminates DNA (with high doses)
elongation by
incorporation
Pyrimidine Antagonist Gemcitabine S Phase Incorporates into the Bladder, breast, Myelosuppression
DNA strand and ovarian,
prevents elongation mesothelioma,
and repair NSCLC
Pyrimidine Antagonist Azacitidine, S Phase Hypomethylation of MDS Myelosuppression,
Decitabine DNA with some direct cardiac complications
toxicity on abnormal (decitabine)
cells
Purine Antagonist Fludarabine, S Phase Adenosine analogs CLL, NHL, AML, Hairy Myelosuppression
Cladribine, that inhibit DNA Cell Leukemia w/OI, tumor lysis
Pentostatin synthesis and repair syndrome, peripheral
& RNA function neuropathy
(fludarabine),
Purine Antagonist 6-mercaptopurine, 6- S Phase Converted to active ALL, CML, AML, NHL Myelosuppression. HGPRT Deficiency
TG form by HGPRT When given with
(purine salvage allopurinol can cause
enzyme) Inhibits de- overdose. VOD
novo purine (severe liver failure)
synthesis.
Antimetabolites Hydroxyurea S Phase Inhibits AML, sickle cell Myelosuppression
ribonucleotide anemia
reductase leading to
decreased DNA
synthesis
Antimicrotubules/ Vincristine, Metaphase Binds to tubulin and Multiple Peripheral Efflux Pump
vinca alkaloids. Vinblastine, inhibits microtubule hematologic neuropathy, (MDR), alterations
(Metabolized by Vinorelbine assembly which leads malignancies and myelosuppression, if in and β tubulin
CYP450) to cell arrest some solid tumors given IT causes severe
fatal ascending
paralysis.
Taxanes Paclitaxel, docetaxel, Metaphase Enhances tubulin Multiple solid Hypersensitivity Efflux Pump
(Metabolized by abraxane (albumin cross linking which tumors Reactions (decreased (MDR)
CYP450) bound paclitaxel) blocks normal cell with use of abraxane),
reproduction fluid retention,
peripheral
neuropathy
Epothilones-LOW Ixabepilone G2-M Binds B tubulin to Multidrug resistant Peripheral LOW
SUSCEPTIBILITY TO Arrest promote proliferation metastatic breast neuropathy, alopecia SUSCEPTIBILITY
RESISTANCE and prevent cancer TO MDR
breakdown of mitotic
spindles
Asparaginase G1 Hydrolyzes L- ALL Hypersensitivity
asparagine causing reactions, decreased
dysfunctional protein clotting factors
synthesis
Topoisomerase Irinotecan, G2 Stabilizes a cleavable Ovarian cancer Myelosuppression, Topoisomerase
Inhibitor topotecan topoisomerase1-DNA (topotecan), dose limiting diarrhea. alterations, MDR.
(camptothecin complex (ATP colorectal cancer
analogs) independent) leading (irinotecan)
to SS DNA strand
breakage upon
replication
Topoisomerase Etoposide G2 Inhibits Multiple Dose limiting
Inhibitor topoisomerase II (ATP malignancies myelosuppression,
(Epipodophyllotoxins- dependent) leading to secondary AML
plant alkaloid) DS DNA strand
breakage
Topoisomerase Mitoxantroene G2 Inhibits Refractory prostate Bluish sclera, urine,
Inhibitor topoisomerase II cancer, AML and fingernails
causing cross linking
and DS DNA breaks
Anthracyclines Doxorubicin, Doxil G2 Inhibits Dano: ALL, AML Arrhythmias, Efflux Pump
(topoisomerase (liposomal topoisomerase II, Doxo: Multiple cardiomyopathy, (MDR), point
inhibitor) doxorubicin) intercalates between hematologic and pericarditis, CHF. mutations on
Danorubicin, base pairs disrupting solid tumors Cardiac sideFx be topoisomerase II,
Epirubicin, Idarubicin DNA and RNA decreased by inactivation of
synthesis, produces administration of superoxide free
oxygen radicals, and dexrazoxane. radicals
disrupts ion and fluid
balance
Alkylating Agents Cisplatin, Nonspecific Alkylating agent that Multiple solid Peripheral Impaired influx or
(Platinums) Carboplatin, cross links and tumors (primarily neuropathies, enhanced efflux
Oxaliplatin alkylates DNA. Causes genitourinary and tinnitus, renal failure, pumps, cytosolic
fragmentation by gastric malignancies) SIADH, metallic taste drug inactivation,
repair enzymes and DNA repair,
prevention of DNA & altered apoptotic
RNA synthesis. processes
Alkylating Agents Cyclophosphamide, Nonspecific Alkylating agent that Breast, Ovarian, NHL, Hemorrhagic cystitis,
(Nitrogen Mustards) Ifosfamide, cross links and CLL, MM, myelosuppression
Melphalan, alkylates DNA. Causes Lymphomas
Chlorambucil fragmentation by
repair enzymes and
prevention of DNA &
RNA synthesis.
Alkylating Agents Carmustine Nonspecific Alkylating agent that Brain tumors Myelosuppression,
(nitrosureas) can cross the BBB pulmonary fibrosis
Alkylating Agents Busulfan Nonspecific Alkylating agent Bone marrow Myelosuppression,
transplant hepatotoxicity,
pulmonary fibrosis
Non-classical Temozolomide Nonspecific Methylates guanine GBM Leukopenia,
Alkylating Agent residues preventing thrombocytopenia
DNA and protein
synthesis
Antitumor Antibiotic Bleomycin G2 Causes production of Testicular cancers Pulmonary fibrosis
oxygen free radicals
that damage DNA
Arsenic Trioxide Arsenic Trioxide Nonspecific Causes apoptosis of APL Prolonged QT
cells syndrome
All-trans retinoic acid ATRA N/A Induces maturation of APL Vitamin A toxicity
(ATRA) blasts in APL
Hormonal Agents Tamoxifen N/A Competitive estrogen Estrogen receptor + Endometrial cancer,
receptor antagonist breast cancers, thromboembolism,
that blocks the effects osteoporosis hot flashes, vaginal
of estrogen in tumor bleeding
cells while
potentiating normal
estrogen function
elsewhere in the body
Hormonal Agents Fulvestrant N/A ER antagonist Metastatic ER+ Hot flashes,
breast cancer arthralgias, headache
Hormonal Agents Anastrozole, N/A Aromatase inhibitor ER+ breast cancer Hot flashes,
Letrozole, blocks the arthralgias, headache
Exemestane transformation of
testosterone into
estrogen
Hormonal Agents Leuprolide, Goserelin N/A GHRH Antagonists Breast and prostate Hot flashes,
cancers impotence, decreased
libido,
Hormonal Agents Bicalutimide, N/A Androgen receptor Prostate cancer Decreased libido,
Nilutamide, blocker gynecomastia,
Flutamide myalgias,
hepatotoxicity
Topoisomerases are enzymes that unwind and wind DNA, in order for DNA to control the synthesis of proteins, and to facilitate DNA replication
Topoisomerase I Topoisomerase II
Acts on one strand of DNA Acts on both strands of DNA
Removes negative supercoils Removes positive supercoils
No involvement in DNA replication Involved in DNA replication
Expression is continuous during G2 phase of the cell cycle and in Expression increases during S phase of the cell cycle & is almost absent in qu
quiescent cells cells
ATP independent ATP dependent