Pharmacology 2

Anticancer
Drugs
Presented by
D r. Vi v i a n L a p u t
Lecture Outline Cancer

To d a y ' s To p i c s Etiology

Carcinogenesis

Anticancer Drugs

Classifications

Nursing Responsibilities

PHARMACOLOGY
General Considerations

Cancer can be considered a chronic disease requiring ongoing

management, rather than a terminal illness. It consists of more than
100 different conditions characterized by uncontrolled growth and
spread of abnormal cells. Normal mechanisms of growth and

PHARMACOLOGY
proliferation are disturbed, which results in distinctive morphologic
alterations of the cell and aberrations in tissue pattern.
General Considerations

The malignant cell is able to invade the surrounding tissue and

regional lymph nodes. Primary cancer usually has a predictable
natural history and pattern of spread.
Metastasis is the secondary growth of the primary cancer in another

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organ. The cancer cell migrates through a series of steps to another
area of the body. This is the reason that cancer cannot always be
cured by surgical removal alone.
Etiology

Cancer arises as a result of a series of genetic and epigenetic

changes, the main genetic lesions being:
• Inactivation of tumor suppressor genes
• The activation of oncogenes (mutation of the normal genes

PHARMACOLOGY
controlling cell division and other processes).
 Acquired (environmental
Normal Cell
DNA damaging agents)
• Chemicals
• Radiation
• Viruses Successful DNA Repair
DNA Damage

Failure of DNA Repair

Mutations in the genomes of

somatic cells

Activation of growth promoting Alteration of genes that regulate Inactivation of cancer supression
oncogene apoptosis genes

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Expression of altered gene products, Loss of
regulatory gene product
• Clonal expansion
• Additional mutations
• Heterogeneity
MALIGNANT NEOPLASM
CARCINOGENESIS
Anticancer Drugs

Anticancer drug, also called antineoplastic

drug,  any drug that is effective in the
treatment of malignant, or cancerous,
disease. There are several major classes of
anticancer drugs; these include alkylating
agents, antimetabolites, natural products,
and hormones.

PHARMACOLOGY
Anticancer Drugs

In addition, there are a number of drugs that do

not fall within those classes but that demonstrate
anticancer activity and thus are used in the
treatment of malignant disease. The
term chemotherapy frequently is equated with the
use of anticancer drugs, although it more
accurately refers to the use of chemical
compounds to treat disease generally.

PHARMACOLOGY
Anticancer Drugs

One of the first drugs that was used

clinically in modern medicine for the
treatment of cancer was the alkylating
agent mechlorethamine, a nitrogen mustard
that in the 1940s was found to be effective
in treating lymphomas.

PHARMACOLOGY
Anticancer Drugs

In 1956 the antimetabolite methotrexate became

the first drug to cure a solid tumour, and the
following year 5-fluorouracil was introduced as
the first of a new class of tumour-fighting
compounds known as pyrimidine analogs. Since
then many anticancer drugs have been
developed and used with much success.

PHARMACOLOGY
Anticancer Drugs

The decision to use a certain anticancer drug depends

on many factors, including the type and location of
the cancer, its severity, whether surgery or radiation
therapy can or should be used, and the side effects
associated with the drug. Most anticancer drugs are
administered intravenously; however, some can be
taken orally, and others can be injected
intramuscularly or intrathecally (within the spinal
cord).

PHARMACOLOGY
Classification of Anticancer Drugs
Cell cycle-specific
CCS drugs acts on
proliferating cells, are the
most effective in
hematologic malignancies
and in solid tumors in
which a relatively large
proportion of the cells are
proliferating
Cell cycle-nonspecific
CCNS drugs can kill
both G0 and cycling
cells (although cycling
cells are more
sensitive). They are
used in slow growing
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tumors
Classification of Anticancer Drugs: Alkylating
Agents

Alkylating agents (cell cycle-nonspecific) are a class of antineoplastic or anticancer

drugs which act by inhibiting the transcription of DNA into RNA and thereby
stopping the protein synthesis. Alkylating agents substitute alkyl groups for hydrogen
atoms on DNA, resulting in the formation of cross links within the DNA chain and
thereby resulting in cytotoxic, mutagenic, and carcinogenic effects. This action occurs
in all cells, but alkylating agents have their primary effect on rapidly dividing cells
which do not have time for DNA repair. Cancer cells are among the most affected

PHARMACOLOGY
because they are among the most rapidly dividing cells.
Classification of Anticancer Drugs: Alkylating
Agents

However, hematopoetic, reproductive, and endothelial cells also divide rapidly

which accounts for the common side effects of the alkylating agents: anemia,
pancytopenia, amenorrhea, impaired spermatogenesis, intestinal mucosal
damage, alopecia, and increased risk of malignancy. The end result of the
alkylation process results in the misreading of the DNA code and the inhibition
of DNA, RNA, and protein synthesis and the triggering of programmed cell

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death (apoptosis) in rapidly proliferating tumor cells.
Classification of Anticancer Drugs: Alkylating
Agents

The alkylating agents are generally separated into six classes:

• The nitrogen mustards [mechlorethamine, cyclophosphamide, ifosfamide, melphalan
andchlorambucil]
• Ethylenamine and methylenamine derivatives [altretamine, thiotepa]
• Alkyl sulfonates [busulfan]
• Nitrosoureas [carmustine, lomustine]
• Triazenes [dacarbazine, procarbazine, temozolomide]
• The platinum-containing antineoplastic agents [cisplatin, carboplatin, oxaliplatin], whichare

PHARMACOLOGY
referred to as platinum coordination complexes. These antineoplastic drugs are usually
classified as alkylating agents, although they do not alkylate DNA, but cause covalent DNA
adducts by a different means.
Classification of Anticancer Drugs: Alkylating
Agents

Indications:
• Treatment of slow-growing cancers, like lymphomas, leukemias,
myelomas, some ovarian, testicular, and breast cancers, and pancreatic
cancers.

PHARMACOLOGY
Classification of Anticancer Drugs: Alkylating
Agents

Contraindications:
• Pregnancy and lactation. Severe effects to fetus and neonate.
• Known allergy to drugs. Caution is exercised to prevent hypersensitivity
reactions.
• Bone marrow suppression. The index for redosing and dosing levels
• Suppressed renal or hepatic function. Interfere with drug metabolism and

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excretion.
Classification of Anticancer Drugs: Alkylating
Agents

Adverse Effects:
• GI: nausea, vomiting, anorexia, diarrhea, and mucous membrane
deterioration, hepatic toxicity
• GU: renal toxicity, potentially toxic increase in uric acid levels
• Hematological: bone marrow suppression

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• Alopecia or hair loss
PHARMACOLOGY
Classification of Anticancer Drugs:
Antimetabolites

Antimetabolites (cell cycle-specific) are drugs that have chemical structures

similar to those of various natural metabolites that are necessary for growth and
division of rapidly growing neoplastic cells and normal cells. They inhibit DNA
production in cells that depend on certain natural metabolites to produce their
DNA. They replace these needed metabolites and thereby prevent normal cellular
function. Considered to be S phase specific in the cell cycle, they are most

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effective in rapidly dividing cells, preventing cell replication, and leading to cell
death.
Classification of Anticancer Drugs:
Antimetabolites

Drugs in the Subclass, Antimetabolites: 

• Cytosine: azacitidine, decitabine, cytarabine,
gemcitabine
• Uracil: capecitabine, floxuridine, fluorouracil

PHARMACOLOGY
• Trifluridine/Tipracil
Classification of Anticancer Drugs:
Antimetabolites

Azacitidine and decitabine have unique actions in that they block or

decrease the methylation of cytosine and, thus, cause hypomethylation of
DNA and increased gene expression. Because some cancers are marked
by hypermethylation of tumor suppressor genes, azacitidine and
decitabine have a potential for specific anticancer activity in these

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conditions. These two agents are used predominantly in the therapy of
myelodysplasia.
Classification of Anticancer Drugs:
Antimetabolites

In contrast, fluorouracil (5-FU) and floxuridine (FUDR) have more

typical antineoplastic activity and are important agents in regimens for
several solid tumors. Capecitabine is an orally available, prodrug of
fluorouracil and has activity against a similar spectrum of cancers as
fluorouracil. Cytarabine (Ara-C) and gemcitabine are cytosine analogues,
but are used in different forms of cancer, cytarabine for leukemias and

PHARMACOLOGY
lymphomas and gemcitabine in solid tumor chemotherapy.
Classification of Anticancer Drugs:
Antimetabolites

Indications:
• Treatment of various leukemias and some GI and basal cell
cancers.
• Use has been somewhat limited because neoplastic cells rapidly
develop resistance to these agents. Therefore, they are

PHARMACOLOGY
commonly administered as part of combination therapy.
Classification of Anticancer Drugs:
Antimetabolites

Contraindications:
• Known allergy to drug. Prevent hypersensitivity reactions
• Pregnancy and lactation. Severe effects on the fetus and neonate
• Bone marrow suppression. Index of redosing and dosing levels
• Renal and hepatic dysfunction. Interfere with drug metabolism and
excretion

PHARMACOLOGY
• Known GI ulceration or ulcerative diseases. Can be exacerbated by the
effects of the drug
Classification of Anticancer Drugs:
Antimetabolites

Adverse Effects:
• CNS: headache, drowsiness, aphasia, fatigue, malaise, dizziness
• Respiratory: pulmonary toxicity, interstitial pneumonitis
• Hematological: bone marrow suppression
• GI: nausea, vomiting, anorexia, diarrhea, mucous membrane deterioration, hepatic
toxicity
• GU: renal toxicity

PHARMACOLOGY
• Leucovorin is an active form of folic acid that is used to rescue normal cells from the
adverse effects of methotrexate therapy in the treatment of osteosarcoma.
PHARMACOLOGY
Classification of Anticancer Drugs: Cytotoxic
Antibiotics

Several naturally occurring compounds with antibiotic activity also have

potent antitumor activity and were developed as anticancer agents. These
cytotoxic antibiotics are often grouped together, even though they have
diverse mechanisms of action, widely different indications, a range of
efficacies and distinctive toxicities. They interfere with cellular DNA
synthesis by inserting themselves between base pairs in the DNA chain.

PHARMACOLOGY
This causes a mutant DNA molecule, leading to cell death.
Classification of Anticancer Drugs: Cytotoxic
Antibiotics

Cytotoxic antibiotics in current use:

• Bleomycin
• Dactinomycin
• Daunorubicin
• Doxorubicin
• Epirubicin
• Idarubicin
• Mitomycin

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• Mitoxantrone
• Plicamycin
• Valrubicin
Classification of Anticancer Drugs: Cytotoxic
Antibiotics

Bleomycin:
Bleomycin is a cystotoxic antibiotic that is used as an anticancer agent in the therapy of testicular
and germ cell cancers, Hodgkin disease, lymphomas and tumors of the head and neck. Therapy with
bleomycin in combination with other agents is often associated with mild-to-moderate serum
enzyme elevations.

Dactinomycin:
Dactinomycin is an intravenously administered, antineoplastic antibiotic that is used in the

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treatment of solid tumors in children and choriocarcinoma in adult women. In high doses,
dactinomycin can cause severe liver injury including sinusoidal obstruction syndrome.
Classification of Anticancer Drugs: Cytotoxic
Antibiotics

Daunorubicin:
Daunorubicin is an anthracycline antibiotic that has antineoplastic activity and is used
in the therapy of acute leukemia and AIDS related Kaposi sarcoma.

Doxorubicin, Epirubicin, Idarubicin, Valrubicin:

Doxorubicin, epirubicin, idarubicin and valrubicin are structurally related cytotoxic
antineoplastic antibiotics used in the therapy of several forms of lymphoma,

PHARMACOLOGY
leukemia, sarcoma and solid organ cancers.
Classification of Anticancer Drugs: Cytotoxic
Antibiotics

Mitomycin:
Mitomycin is a cytotoxic antibiotic which is used as anticancer therapy of advanced cancers of the stomach and
pancreas.

Mitoxantrone:
Mitoxantrone is an antineoplastic antibiotic that is used in the treatment of acute leukemia, lymphoma, and
prostate and breast cancer, but also for late stage, severe multiple sclerosis.

PHARMACOLOGY
Plicamycin:
Plicamycin, which was formerly known as mithramycin, is an antibiotic that is used as an anticancer agent in
the therapy of testicular and germ cell cancers. Plicamycin has not been approved for use as cancer
chemotherapy in the United States, but continues to be used on an investigational basis.
Classification of Anticancer Drugs: Cytotoxic
Antibiotics

Contraindications:
• Known allergy to drug. Prevent hypersensitivity reactions
• Pregnancy and lactation. Severe effects on the fetus and neonate
• Bone marrow suppression. Index of redosing and dosing levels
• Renal and hepatic dysfunction. Interfere with drug metabolism and excretion
• Known GI ulceration or ulcerative diseases. Can be exacerbated by the effects of the
drug

PHARMACOLOGY
• Pulmonary problems. Exacerbated by bleomycin or mitomycin
• Cardiac problems. Exacerbated by idarubicin or mitoxantrone
Classification of Anticancer Drugs: Cytotoxic
Antibiotics

Adverse Effects:
• CNS: headache, drowsiness, aphasia, fatigue, malaise, dizziness
• Respiratory: pulmonary toxicity, interstitial pneumonitis
• Hematological: bone marrow suppression
• GI: nausea, vomiting, anorexia, diarrhea, mucous membrane deterioration,
hepatic toxicity

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• GU: renal toxicity
• Alopecia
PHARMACOLOGY
Classification of Anticancer Drugs: Biologic
Response Modifiers

Biological response modifiers improve the body's ability to

fight cancer by immunostimulation. BRM's can act passively by
enhancing the immunologic response to tumor cells or actively
by altering the differentiation/growth of tumor cells.

PHARMACOLOGY
Classification of Anticancer Drugs: Biologic
Response Modifiers

Biological response modifiers improve the body's ability to

fight cancer by immunostimulation. BRM's can act passively by
enhancing the immunologic response to tumor cells or actively
by altering the differentiation/growth of tumor cells.

PHARMACOLOGY
Classification of Anticancer Drugs: Biologic
Response Modifiers

Aldesleukin
Aldesleukin is a recombinant form of human interleukin-2, a cytokine that stimulates the
proliferation and maturation of T cells, which is used in immune therapy of renal cell
cancer and malignant melanoma.

Denileukin Diftitox
Denileukin diftitox is a recombinant fusion protein of human interleukin-2 (IL-2)

PHARMACOLOGY
attached to diphtheria toxin fragments A and B that is used as an antineoplastic agent to
treat cutaneous T cell lymphomas that express IL-2 receptors.
Classification of Anticancer Drugs: Biologic
Response Modifiers

Interferon Gamma
Interferon gamma is a recombinant cytokine with a multitude of actions
including stimulation of T cell immunity, increase in innate immune responses,
induction of Class II major histocompatibility complex molecules, and
inhibition of fibrosis. Interferon gamma is used for its immune enhancing
properties as therapy of chronic granulomatous disease of childhood and is

PHARMACOLOGY
used experimentally for its anti-fibrotic actions.
Classification of Anticancer Drugs: Biologic
Response Modifiers

Contraindications:
Biologic response modifiers should not be taken by patients who have active
infections, demyelinating diseases, e.g., (multiple sclerosis, optic neuritis), and
immunodeficiency syndromes.
BRM should also be avoided in patients with chronic recurrent infections and
untreated latent TB. TNF inhibitors should be avoided or used with caution in

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a patient with CHF. It is advised to avoid pregnancy or breastfeeding while
taking BRMs.
Classification of Anticancer Drugs: Biologic
Response Modifiers

Adverse Effects:
The adverse effects of biologic response modifier therapy could be secondary to
stimulation, suppression, or disruption of immune homeostasis. Since T cell-
mediated response is involved in the destruction of pathogens, inhibition of
immune response by BRM increases the risk of asymptomatic to life-threatening
infection due to the virus, bacteria, mycobacteria, fungi, and protozoa. Infection

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risk is increased, notably in patients with advanced diseases and those who already
have received treatment with other immunosuppressants.
PHARMACOLOGY
Classification of Anticancer Drugs: Hormonal
Agents

Hormones are substances that function as chemical messengers in the body.

They affect the actions of cells and tissues at various locations in the body,
often reaching their targets through the bloodstream. Hormone therapy (also
called hormonal therapy, hormone treatment, or endocrine therapy) slows or
stops the growth of hormone-sensitive tumors by blocking the body’s ability
to produce hormones or by interfering with effects of hormones on cancer

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cells.
Classification of Anticancer Drugs: Hormonal
Agents

Antiandrogens
The antiandrogens are medications that act by binding to intracellular androgen
receptors, preventing the effects of endogenous androgens on target tissues such
as testes, hair follicles, hypothalamus, pituitary, ovaries and prostate gland. The
antiandrogens are used for a variety of hyperandrogenic states such as acne,
hirsutism, and paraphilias, but their major use is in therapy of prostate cancer.

PHARMACOLOGY
Chemically, antiandrogens are classified into steroidal (such as cyproterone
acetate) and nonsteroidal (including flutamide, nilutamide and bicalutamide).
Classification of Anticancer Drugs: Hormonal
Agents

Antiandrogens
• Abiraterone
• Apalutamide
• Bicalutamide
• Cyproterone
• Enzalutamide

PHARMACOLOGY
• Flutamide
• Nilutamide
Classification of Anticancer Drugs: Hormonal
Agents

Antiandrogens
The largest and longest clinical experience has been with flutamide
which has been shown to produce clinical remission in patients with
prostate cancer, and is also used in hyperandrogenic states including

PHARMACOLOGY
acne and hirsutism.
Classification of Anticancer Drugs: Hormonal
Agents

Aromatase Inhibitors/Antiestrogens
The aromatase inhibitors block estrogen synthesis and are used as
therapy of estrogen receptor positive breast cancer, usually after
resection and as a first line treatment or after failure of tamoxifen
(another antiestrogen that acts by blocking the estrogen receptor).

PHARMACOLOGY
The aromatase inhibitors include anastrozole, letrozole and
exemestane.
Classification of Anticancer Drugs: Hormonal
Agents

Aromatase Inhibitors/Antiestrogens
Aromatase is the enzyme responsible for the conversion of testosterone to estrone
(E1) and androstenedione to estradiol (E2). Highest levels of aromatase are found
in the ovary and placenta, which are the major sources of estrogen in
premenopausal women. However, aromatase is also found in other tissues, such as
liver, kidney, adrenals, brain, muscle and subcutaneous fat where it is also active in

PHARMACOLOGY
producing estrogens, although at low levels. These tissues are the major source of
estrogen after menopause or oopherectomy.
Classification of Anticancer Drugs: Hormonal
Agents

Aromatase Inhibitors/Antiestrogens
Inhibitors of aromatase were developed to block the synthesis of estrogen
in the peripheral tissues and, thus, as antiestrogen therapy of estrogen
receptor positive breast cancer in postmenopausal women. The first
aromatase inhibitor used in clinical medicine was aminoglutethimide,
which was initially developed as an anticonvulsant, but later found to

PHARMACOLOGY
inhibit adrenocorticoid steroid synthesis.
Classification of Anticancer Drugs: Hormonal
Agents

Aromatase Inhibitors/Antiestrogens
• Anastrozole
• Exemestane

PHARMACOLOGY
• Letrozole
Classification of Anticancer Drugs: Hormonal
Agents

Gonadotropin Releasing Hormone (GnRH) Analogues

The gonadotropin releasing hormone (GnRH) agonists and antagonists are short
peptide analogues of GnRH that cause a profound inhibition of estrogen and
androgen synthesis and are used predominantly as androgen deprivation therapy of
advanced prostate cancer. Some of these agents are also used to treat benign
conditions responsive to hormonal inhibition such as endometriosis, uterine

PHARMACOLOGY
fibroids, precocious puberty and infertility. Leuprolide, goserelin, triptorelin and
histrelin are considered GnRH agonists, whereas degarelix acts predominantly as
an antagonist.
Classification of Anticancer Drugs: Hormonal
Agents

Peptide Hormones
Anticancer Peptides or ACPs, as small peptides containing amino acid
sequences, are selective and toxic to cancer cells. CPs are a superior
choice of therapeutics compared with antibodies and small molecules
due to their high selectivity, high penetration and easy modifications.
Numerous anticancer peptides destroy cancer cells via apoptosis and

PHARMACOLOGY
necrosis by membrane lysis or pore formation.
Classification of Anticancer Drugs: Hormonal
Agents

Peptide Hormones
• Lanreotide  is a synthetic polypeptide analogue of somatostatin that
resembles the native hormone in its ability to suppress levels and activity
of growth hormone, insulin, glucagon and many other gastrointestinal
peptides. Because its half-life is longer than somatostatin, lanreotide can
be used clinically to treat neuroendocrine tumors that secrete excessive

PHARMACOLOGY
amounts of growth hormone (acromegaly) or other active hormones or
neuropeptides.
Classification of Anticancer Drugs: Hormonal
Agents

Peptide Hormones
• Octreotide is a synthetic somatostatin analogue that resembles the native
polypeptide in its activity in suppressing levels and activity of growth
hormone, insulin, glucagon and many other gastrointestinal peptides.
Because its half-life is longer than somatostatin, octreotide can be used
clinically to treat neuroendocrine tumors that secrete excessive amounts of

PHARMACOLOGY
growth hormone (acromegaly) or other active hormones or neuropeptides.
.
Classification of Anticancer Drugs: Hormonal
Agents

Peptide Hormones
• Pasireotide is a synthetic polypeptide analogue of somatostatin that resembles
the native hormone in its ability to suppress levels and activity of growth
hormone, insulin, glucagon and many other gastrointestinal peptides. Because
its half-life is longer than somatostatin, pasireotide can be used clinically to
treat neuroendocrine pituitary tumors that secrete excessive amounts of growth
hormone causing acromegaly, or adrenocorticotropic hormone (ACTH) causing

PHARMACOLOGY
Cushing disease.
.
Classification of Anticancer Drugs: Hormonal
Agents

Contraindications:
• Known allergy to drug. Prevent hypersensitivity reactions
• Hypercalcemia. Contraindication to the use of toremifene because the drug can
increase serum calcium levels.
• Pregnancy and lactation. Severe effects on the fetus and neonate
• Bone marrow suppression. Index of redosing and dosing levels
• Renal and hepatic dysfunction. Interfere with drug metabolism and excretion

PHARMACOLOGY
• Known GI ulceration or ulcerative diseases. Can be exacerbated by the effects of the
drug
Classification of Anticancer Drugs: Hormonal
Agents

Adverse Effects:
• Menopause-associated effects: hot flashes, vaginal spotting, vaginal
dryness, moodiness, and depression
• Hematological: bone marrow suppression
• GI: hepatic toxicity
• GU: renal toxicity

PHARMACOLOGY
• Hypercalcemia is encountered as the calcium is pulled out of
the bones without estrogen activity to promote calcium deposition.
PHARMACOLOGY
Classification of Anticancer Drugs: Vinca
Alkaloids

The vinca alkaloids are antineoplastic agents that act by binding to

intracellular tubulin, the basic protein subunit of microtubules which
are important in many intracellular processes including mitosis and cell
division. The vinca alkaloids inhibit cell division by blocking mitosis;
they also inhibit purine and RNA synthesis causing death of rapidly

PHARMACOLOGY
dividing cells.
Classification of Anticancer Drugs: Vinca
Alkaloids

They have become major components of many combination anticancer

regimens, used particularly in treatment of acute leukemia, Hodgkin
disease and other lymphomas, various sarcomas, Wilms tumor,
neuroblastoma, and breast and lung cancer. The vinca alkaloids are
given intravenously, typically at one or two week intervals in cycles

PHARMACOLOGY
with other agents.
Classification of Anticancer Drugs: Vinca
Alkaloids

• Vincristine
• Vinblastine
• Vinorelbine

PHARMACOLOGY
Classification of Anticancer Drugs: Taxanes

The taxanes or taxoids are a closely related group of antineoplastic agents that
have a unique mechanism of action as inhibitors of mitosis and which are
widely used in the therapy of ovarian, breast, lung, esophageal, prostate,
bladder and head and neck cancers. The taxanes are similar to the vinca
alkaloids in that they bind to tubulin and cause inhibition of mitosis. However,
the taxanes bind at a different site than the vinca alkaloids and cause inhibition

PHARMACOLOGY
of mitosis by prevention of degradation of microtubules, rather than prevention
of their assembly.
Classification of Anticancer Drugs: Taxanes

Drugs in the Subclass, Taxanes: 

• Cabazitaxel
• Docetaxel
• Paclitaxel

PHARMACOLOGY
Classification of Anticancer Drugs: Taxanes

Contraindications:
• Known allergy to drug. Prevent hypersensitivity reactions
• Pregnancy and lactation. Severe effects on the fetus and neonate
• Bone marrow suppression. Index of redosing and dosing levels
• Renal and hepatic dysfunction. Interfere with drug metabolism and
excretion

PHARMACOLOGY
• Known GI ulceration or ulcerative diseases. Can be exacerbated by the
effects of the drug
Classification of Anticancer Drugs: Taxanes

Adverse Effects:
• CNS: headache, drowsiness, aphasia, fatigue, malaise, dizziness
• Respiratory: pulmonary toxicity, interstitial pneumonitis
• Hematological: bone marrow suppression
• GI: nausea, vomiting, anorexia, diarrhea, mucous membrane
deterioration, hepatic toxicity

PHARMACOLOGY
• GU: renal toxicity
• Can cause necrosis and cellulitis if extravasation occurs
PHARMACOLOGY
Classification of Anticancer Drugs:
Miscellaneous

Bexarotene
Bexarotene is a retinoid analogue that is used to treat the skin manifestations of
cutaneous T cell lymphoma (CTCL).

Asparaginase
Asparaginase is a bacterial enzyme that is used as an antineoplastic agent, largely in the
therapy of acute lymphocytic leukemia. L-asparaginase has many side effects, one of

PHARMACOLOGY
which is hepatic injury that is characterized by inhibition of hepatic protein synthesis
and steatosis, which can be severe and lead to death from hepatic failure.
Classification of Anticancer Drugs:
Miscellaneous

Eribulin
Eribulin mesylate is an inhibitor of microtubule function and is used as an antineoplastic
agent for refractory, metastatic breast cancer and liposarcoma.

Everolimus
Everolimus is an inhibitor of cell proliferation and immunosuppressive agent that is
used alone or in combination with calcineurin inhibitors to prevent cellular rejection

PHARMACOLOGY
after organ transplantation, and in combination with other anticancer agents as treatment
of advanced renal cell and other cancers.
Classification of Anticancer Drugs:
Miscellaneous

Hydroxyurea
Hydroxyurea is an antimetabolite that is used in the treatment of cancer and to
stimulate fetal hemoglobin production in sickle cell disease.

Ixabepilone
Ixabepilone is a semisynthetic epothilone analogue that acts to stabilize microtubules
thereby preventing mitosis and causing growth arrest in cancer cells. Ixabepilone is

PHARMACOLOGY
approved for use in refractory cases of advanced breast cancer.
Classification of Anticancer Drugs:
Miscellaneous

Thalidomide
Thalidomide and its analogue lenalidomide are immunomodulatory and
antineoplastic agents that are used in the therapy of multiple myeloma.

Temsirolimus
Temsirolimus is an inhibitor of cell proliferation and anticancer agent that is used

PHARMACOLOGY
as treatment of advanced renal cell cancer
Classification of Anticancer Drugs:
Miscellaneous

Telotristat
Telotristat is an oral, small molecule inhibitor of tryptophan hydroxylase that is
used in the treatment of symptoms of carcinoid syndrome.

Tagraxofusp
Tagraxofusp is a recombinant fusion protein consisting of the binding site of

PHARMACOLOGY
interleukin 3 [IL3] fused with diphtheria toxin and that is given by intravenous
infusion and used as an antineoplastic agent for patients with blastic
plasmacytoid dendritic cell neoplasm.
Classification of Anticancer Drugs:
Miscellaneous

Telotristat
Telotristat is an oral, small molecule inhibitor of tryptophan hydroxylase that is
used in the treatment of symptoms of carcinoid syndrome.

Tagraxofusp
Tagraxofusp is a recombinant fusion protein consisting of the binding site of

PHARMACOLOGY
interleukin 3 [IL3] fused with diphtheria toxin and that is given by intravenous
infusion and used as an antineoplastic agent for patients with blastic
plasmacytoid dendritic cell neoplasm.
Nursing
Responsibilities

• Watch for bleeding. If platelet count

is low, avoid giving I.M. injections and taking

rectal temperature.
• Stay alert for bone marrow
depression, neutropenia, and
anemia.
• Monitor fluid intake and output

PHARMACOLOGY
• Monitor for GI upset. Give
antiemetics as needed and
prescribed.
PHARMACOLOGY

THE END

DR. VIVIAN LAPUT

BIOTIN BENEFITS | AMC