Anticancer Drugs

Anticancer Drugs
Anticancer, or antineoplastic, drugs are used to treat malignancies, or cancerous growths.

There are several major classes of anticancer drugs - alkylating agents, antimetabolites and
anthracycline antibiotics. 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.
Drug treatment for cancer is called chemotherapy. It targets cells that grow and divide
quickly, as cancer cells do. Unlike radiation or surgery, which target specific areas, chemo can
work throughout your body. But it can also affect some fast-growing healthy cells, like those of
the skin, hair, intestines, and bone marrow. That’s what causes some of the side effects from the
treatment.
When fighting cancer, the entire population of neoplastic cells - abnormal growth of cells
must be eradicated in order to obtain desired results. The concept of "total cell-kill" applies to
chemotherapy as it does to other means of treatment: total excision of the tumor is necessary for
surgical care, and complete eradication of all cancer cells is required for a cure with radiation
therapy. By investigation of a model tumor system, the L1210 leukemia of mice, a number of
important principles have been established as follows:
1. a single clonogenic malignant cell can give rise to sufficient progeny to kill the host; to
achieve cure it is thus necessary to destroy every such cell. Since the doubling-time of most
tumors is relatively constant during logarithmic growth, the life-span of the host is inversely
related to the number of malignant cells that are inoculated or that survive therapeutic
measures;
2. The cell-kill caused by antineoplastic agents follows first-order kinetics, that is, a constant
percentage, rather than a constant number, of cells is killed by a given therapeutic maneuver,
this finding has had a profound impact on clinical cancer chemotherapy. For example, a
patient with advanced acute lymphocytic leukemia might harbor 1012 or about 1 kg of
malignant cells. A drug killing 99.99% of these cells would reduce the tumor mass to about
100mg, and this would be apparent as a complete 5 clinical remission. However, 108
malignant cells would remain, any of which could cause a relapse in the disease.
Major classes of anticancer drugs
1. Alkylating agents. Classic alkylating agents interfere with DNA replication by

crosslinking DNA strands, DNA strand breaking, and abnormal pairing of base pairs. They
exert their lethal effects on cells throughout the cell cycle but tend to be more effective
against rapidly dividing cells.
Because alkylating agents are active against cells in G 0, they can be used to debulk
tumours, causing resting cells to be recruited into active division. At this point, those cells
are vulnerable to the cell cycle-specific agents. These agents are active against
lymphomas, Hodgkin's disease, breast cancer, and multiple myeloma.
Major toxicities occur in the haematopoietic, gastrointestinal and reproductive systems.
Individuals treated with these agents are also placed at a higher risk of developing
secondary malignancies. Examples include Cyclophosphamide, Ifosfamide, Chlorambucil,
Busulfan and Melphalan.
The nitrosureas are a subgroup of the alkylating agents. They also interfere with DNA
replication and repair. They are highly lipid soluble and readily cross the blood-brain
barrier. An example is Carmustine.
Another subgroup of alkylators called Platinum-containing compounds include agents
such as Cisplatin, Carboplatin and Oxaliplatin. Their cytotoxic properties also extend to
alteration of the cell membrane transport systems and suppression of mitochondrial
function.
2. Antimetabolites. Antimetabolites interfere with DNA and RNA synthesis by acting as

false metabolites, which are incorporated into the DNA strand or block essential enzymes,
so that DNA synthesis is prevented. Most agents are cell cycle phase specific for S phase.
These agents are most effective when used against rapidly cycling cell populations and
are consequently more effective against fast-growing tumors than slow-growing tumors.
Major toxicities occur in the haematopoietic and gastrointestinal systems. Examples
include Methotrexate, 5-Fluorourocil and Cytosine Arabinoside.
Hypomethylating agents represent a class of drugs that may restore normal gene function
to genes responsible for cell division and differentiation. Hypomethylating agents may
function as biological response modifiers by affecting cytokine cell signaling. These
agents may be identified as antimetabolites and they include 5-azacytidine and
Decitabine.
3. Anthracyclines. or anthracycline antibiotics are a class of drugs used in cancer

chemotherapy derived from Streptomyces bacteria (more specifically, Streptomyces
peucetius var. caesius). These compounds are used to treat a wide range of cancers,
including leukemias, lymphomas, and breast, uterine, ovarian, and lung cancers.
Examples include Bleomycin, Daunorubicin, and Doxorubicin. Anthracycline has three
mechanisms of action:
1. inhibits DNA and RNA synthesis by intercalating between base pairs of the
DNA/RNA strand, thus preventing the replication of rapidly-growing cancer cells;
2. inhibits topoisomerase II enzyme, preventing the relaxing of supercoiled DNA and
thus blocking DNA transcription and replication; and
3. creates iron-mediated free oxygen radicals that damage the DNA and cell
membranes.
Patients treated with doxorubicin have been described in acute and chronic
cardiovascular effects. The first, which can develop within a few minutes after
administration and include hypotension and rhythm disturbances are usually reversible
and easily treatable. However, doxorubicin is also able to induce chronic myocardial
damage, depending on the cumulative dose of drug administered and clinically
characterized by hypotension, tachycardia, ventricular dilation and congestive heart
failure. It has been calculated that, from 27 to 60% of patients who undergo this event by
doxorubicin die because of it.
SOME COMMON CHEMOTHERAPY DRUGS:

• Doxorubicin (Adriamycin) is one of the most powerful chemotherapy drugs ever
invented. It can kill cancer cells at every point in their life cycle, and it's used to
treat a wide variety of cancers. Unfortunately, the drug can also damage heart
cells, so a patient can't take it indefinitely.
• Cyclophosphamide (Cytotoxan) is a drug that can treat many different cancers.
Like many other chemotherapy drugs, it scrambles the DNA of cancer cells.
Because it damages healthy DNA too, it can also cause long term injury to the bone
marrow, which, in a few rare cases, can lead to a new case of leukemia (cancer of
certain white blood cells).
• Paclitaxel (Taxol) is an effective drug used for treating some cases of breast cancer
and ovarian cancer, but it can damage nerves over time, leaving some people with
decreased sensation in their hands and feet. The anticancer compound in this drug
was first discovered in the bark of Pacific yew trees.
• Fluorouracil (Adrucil) was first approved as a chemotherapy drug in 1962 and is

one of the oldest chemotherapy drugs still prescribed today. It's primarily used to
treat gastrointestinal cancers (including colon, rectal, stomach) and certain types
of breast cancer.
• Gemcitabine (Gemzar) is a relatively new chemotherapy drug that is effective at

slowing the growth of several types of cancer. Used alone, it's a first-line treatment
for pancreatic cancer that has spread or is inoperable. It's also used in
combination to treat certain types of breast, ovarian, and lung cancers

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Anticancer Drugs

Anticancer, or antineoplastic, drugs are used to treat malignancies, or cancerous growths.

Major classes of anticancer drugs

1. Alkylating agents. Classic alkylating agents interfere with DNA replication by

2. Antimetabolites. Antimetabolites interfere with DNA and RNA synthesis by acting as

3. Anthracyclines. or anthracycline antibiotics are a class of drugs used in cancer

SOME COMMON CHEMOTHERAPY DRUGS:

• Fluorouracil (Adrucil) was first approved as a chemotherapy drug in 1962 and is

• Gemcitabine (Gemzar) is a relatively new chemotherapy drug that is effective at

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