Name Cycle Major Tox Special Tox MOA Note

IH. DHFR
BMD Kidney: 7-OH D. Tetrahydrofolic acid
Methotrexate S Leucovorin Rescue
GI Ulcer Acidic Drugs D. Thymidine
Block DNA Syn

IH. DHFR
Kidney: 7-OH
BMD D. Tetrahydrofolic acid
Pemetrexed S Acidic Drugs Leucovorin Rescue
GI Ulcer D. Thymidine
Hepatoxicity
Block DNA Syn

BMD Converted to F-dUMP

FluoroURACIL
S GI Ulcer Skin Ulceration IH. Thymidylate Symthetase
5-FU
Diarrhea IC. Into DNA as abn nuc.
MercaptoPURINE Allopurinol
S BMD Interfers with Purine Biosynthesis
6-MP *IH. Xanthine Oxidase
2' OH cis to Pyrimidine Ring
Immunosuppressive
CytARABINE S BMD Hinders Rotation
Cerebellum Tox
Abn stacking of DNA

2' F cis to Pyrimidine Ring

GencitABINE BMD Hinders Rotation
Abn stacking of DNA & RNA

Arabinose Sterochem
2' OH cise to Purine Ring
FludARABINE S BMD Immunosuppressive Hinders Rotation
Abn Stacking of RNA & DNA
IH. DNA Polymerase

NO BMD
Asparaginase Postmitotic Allergic RXN Enzyme catalyzes Hydrolysis of Asparagine Use: ALL
G1 Hepatotoxicity which is req. for LYMPHOBLAST growth
Pancreatitis

NO BMD
Use: ALL
Postmitotic Allergic RXN Enzyme catalyzes Hydrolysis of Asparagine
Pegaspergase Less Frequ. SE
G1 Hepatotoxicity which is req. for LYMPHOBLAST growth
Peg= I. Lipophylicity
Pancreatitis
 Hemorrhagic Cystitis
Cyclophosphamide M. To Phosphoramide Mustard
CCNS BMD * Due to Acrolein formed from Mesna Prevents SE
X-link DNA via Aziridinium Ion
phosphoramide production

Hemorrhagic Cystitis Mesna Prevents SE

M. To Phosphoramide Mustard
Ifosfamide CCNS BMD * Due to Acrolein formed from
X-link DNA via Aziridinium Ion
phosphoramide production SE More Severe

Pulmonary Fibrosis
Lomustine CCNS BMD X-link DNA via Diazonium Ion
*Due to Isocyanate that attacks
Alkylates DNA
protein
Oxidatively Demethylated to form
Dacarbazine CCNS BMD Hepatic Necrosis
Triazene that Methylates DNA
Hydrolyzed to Triazene that Methylates
Temozolomide CCNS BMD
DNA

Sterility:
MAOI
D. M. of Sympathomimetics
Procarbazine CCNS BMD M. to Diazonium Ion that Methylates DNA
(pse, phenylproanolamine, red
wine, cheese)
Heart Arrhythmias

Alkylation of DNA via Imminium Ion

Hexamethylmelamine CCNS BMD
formed during N-Dealkylation
N/V
NO BMD DNA Intrastrand X-linking by Nucleophilic
CisPLATIN CCNS Acoustic Nerve Damage
Kidney Damage Displacement of Cis Chloride Ligands
Electrolyte Wasting

More Lipophilic
CarboPLATIN CCNS BMD Peripheral Neuropathy DNA Intrastrand X-linking by Nucleophilic
I. Tissue Penetration
Thrombocytopenia Kidney Damage Displacement of Cis Chloride Ligands
I. BMD

BMD DNA Intrastrand X-linking by Nucleophilic

OxaliPLATIN CCNS Peripheral Neuropathy
Kidney Damage Displacement of Cis Chloride Ligands

*Intercalation with DNA

NO BMD
*Chelation of Iron that binds O2 to form
Bleomycin G2 Pneumonitis
OxyRadicals leading to DNA Strand
Pulmonary Fibrosis
Scission
 Binds Topo II
Etoposide S & G2 BMD Hypersensitivity IH. Activity to nick & reseal
DNA strand breaks

Binds Topo II
Rubicin
IH. Activity to nick & reseal
Doxy CCNS
Cardiotoxicity DNA strand breaks
Epi (S-phase BMD
*Due to Radical Formation Intercalation with DNA
Dauno sensitive)
*Reduced to Radicals that leads to DNA
Ida
strand scission

Binds Topo I
BMD
Irinotecan S & G2 Hypersensitivity IH. Activity to nick & reseal
Diarrhea
DNA strand breaks

Bind Tubulin Dimers

VINcristine M NO BMD
Block Polymerization of MicroT.
Peripheral Neuropathy
IH. Mitosis at Metaphase

Bind Tubulin Dimers

Mild BMD
VINorelbine M Block Polymerization of MicroT.
Peripheral Neuropathy
IH. Mitosis at Metaphase

Bind Tubulin Dimers More Lipophilic

VINblastine M BMD Block Polymerization of MicroT. I. Tissue Penetration
IH. Mitosis at Metaphase I. BMD

1. Binds to polymerized Tubulin

Stabilizes MicroT.
BMD MicroT. Don't depolymerize
Taxol G2 & M Hypersensitivity
Peripheral Neuropathy Disruption of Mitosis
2.IH. BCL2 Protein leading to promotion of
apoptotic cell death

1. Binds to polymerized Tubulin

Stabilizes MicroT.
BMD Pulmonary Edema MicroT. Don't depolymerize
DoceTAXEL G2 & M
Peripheral Neuropathy Hypersensitivity Disruption of Mitosis
2.IH. BCL2 Protein leading to promotion of
apoptotic cell death
 1. Binds to polymerized Tubulin
Stabilizes MicroT.
BMD MicroT. Don't depolymerize
CabaziTAXEL G2 & M Hypersensitivity
Peripheral Neuropathy Disruption of Mitosis
2.IH. BCL2 Protein leading to promotion of
apoptotic cell death

Bind R in Lymphocytes that bind DNA

Cushings Syndrome
Produce Inhibitory Protein
Prednisone Endocrine *I. Infections
I. RNA & DNA syn
Steroid Psychosis
Cytotox of lympohcytes & lymph cell

Bind R in Lymphocytes that bind DNA

Cushings Syndrome
Produce Inhibitory Protein
Dexamethasone Endocrine *I. Infections
I. RNA & DNA syn
Steroid Psychosis
Cytotox of lympohcytes & lymph cell

*N/V, Hot Flashes, Vaginal

Binds Estrogen R
Bleeding, I. R. of clots & strokes
Tamoxifen Endocrine Abn DNA binding Use: Breast Cancer
*P450 I
D. Estrogen R req. for tumor growth
*Uterine Sarcoma

Tight-binding I. of Aromatase
N/V, Hot Flashes, I. R. of clots &
Anastrazole Endocrine *a enzyme req.for breast tumor grwt Use: Breast Cancer
stroke
D. Estrogen Syn

Tight-binding I. of Aromatase
N/V, Hot Flashes, I. R. of clots &
Letrazole Endocrine *a enzyme req.for breast tumor grwt Use: Breast Cancer
stroke
D. Estrogen Syn

LRH Analog that suppresses FSH & LH

Feminization
Leuprolide Endocrine D. Androgen Syn
Hot Flashes
I. Tumor Growth

Bicalutamide Endocrine Feminization 1.Blocks Androgen R.

Hot Flashes 2. Synergistically w/ Leuprolide

Anaphylaxis Binds Cellular R.

Interferon Modifier Hypotension p450 I. I. express of ezyms to activate RNAase
Tachycardia Degrade RNA made from oncogenes
 *G-CSF stimulates Granulocyte produc.
Fever
G-CSF Modifier Bone Pain *I. WBC produc. In chemo regimens that
Flu-like symptoms
cause BMD

Hypotension
IL-1: Enhance Platelet Recovery
Pulmonary Edema
Interleukins Cytokine Cappillary Leak Syndrome
Peripheral Edema
IL-2: T-cells --> Killer Cells
Flu-Like symp

Protects against
Hemorrhagic Cystitis
Mesna Protectant Thiol Group Scavenges Acrolein
after Ifosfamide or
Cyclophosphamide

Protects against
Protectant Methotrexate
Lecovorin
Enhancer
Enhances 5-FU

I. BCR-Abl tyrosine kinase protein

Edema
*typically phosphorylates effector
N/V/D P450 I., primarly CYP3A4
Imatinib Kinase proteins that cause (therefore decreases) Use: CML
BMD *inducers of CYP3A4 Decrease
(Gleevec) cell proliferation in myeloid cells what
Cardiotox [Drug]
contain mutated Philadelphia
Rare Hepatotoxicity
chromosome

*Heart Failure
P450 I. & metabolized by
*QT-Prolongation
CYP3A4 I. multiple Intracellular Tyrosine Kinases in
Lapatinib Kinase *Swelling & Numb in Use: Breast Cancer
*incucers of CYP3A4 Decrease HER2 cancer cells
Hands & Feet
[Drug]
*N/V/D

Use:
*I. [Warfarin]
Intersitial Lung Disease *I. phosporylation of EGFR tyrosine kinase *Non-sm cell
*Metab. By CYP3A4
Erlotinib Kinase Rash *Blocks invasion of tumors & lung cancer
*Inducers & Inhibitors of P450
N/V/D angiogenesis(blood vessel growth) *Pancreatic Cancer
affect [Erlotinib]