How do alkylating agents work to treat cancer?
Mar 10, 2015 · Alkylating agents 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 chai …
Are alkylating agents bifunctional?
Melphalan is an alkylating agent that is used in the treatment of multiple myeloma,21,22ovarian cancer,23,24and breast cancer.25,26Melphalan is an amino acid analog that enters cells and crosses the blood–brain barrier through active transport systems.
Why is resistance to alkylating agents important for tumor cells?
Oct 27, 2021 · Alkyl sulfonates (busulfan) Busulfan is an injectable alkylating agent mainly used in the treatment of chronic myeloid leukemia (CML). This is a strong drug that causes myelosuppression, a side...
Why are alkylating agents used in bone marrow transplantation?
Oct 27, 2021 · Alkyl sulfonates (busulfan) Busulfan is an injectable alkylating agent mainly used in the treatment of chronic myeloid leukemia (CML). This is a strong drug that causes myelosuppression, a side effect that lowers platelets and blood cell counts.
Which alkylating agent is used in cancer treatment?
Nitrogen Mustards. The most frequently used alkylating agents are the nitrogen mustards. Although thousands of nitrogen mustards have been synthesized and tested, only five are commonly used in cancer therapy today.
What is the role of alkylating agents in cancer treatment?
Alkylating agents keep the cell from reproducing (making copies of itself) by damaging its DNA. These drugs work in all phases of the cell cycle and are used to treat many different cancers, including cancers of the lung, breast, and ovary as well as leukemia, lymphoma, Hodgkin disease, multiple myeloma, and sarcoma.Nov 22, 2019
Which chemotherapy drug is an alkylating agent?
Examples of alkylating agents include chlorambucil, cyclophosphamide, thiotepa, and busulfan.
What is an example of alkylating agent?
Some examples of alkylating agents are nitrogen mustards (chlorambucil and cyclophosphamide), cisplatin, nitrosoureas (carmustine, lomustine, and semustine), alkylsulfonates (busulfan), ethyleneimines (thiotepa), and triazines (dacarbazine).Mar 28, 2022
What do you mean by alkylating agents?
Listen to pronunciation. (AL-kuh-LAY-ting AY-jent) A type of drug that is used in the treatment of cancer. It interferes with the cell's DNA and inhibits cancer cell growth.
Do alkylating agents cause cancer?
However, they are also toxic to normal cells (cytotoxic), particularly cells that divide frequently, such as those in the gastrointestinal tract, bone marrow, testicles and ovaries, which can cause loss of fertility. Most of the alkylating agents are also carcinogenic.
What do alkylating agents interfere with?
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.
Which of these are examples of alkylating agents quizlet?
Nitrogen mustard.Alkylsulfonates.Nitrosoureas.Triazines.Ethylenimines.Methylhyderazine.
What is the main ingredient in chemotherapy?
There are several types of alkylating agents used in chemotherapy treatments: Mustard gas derivatives: Mechlorethamine, Cyclophosphamide, Chlorambucil, Melphalan, and Ifosfamide. Ethylenimines: Thiotepa and Hexamethylmelamine. Alkylsulfonates: Busulfan.
Which describes the main mechanism of action of alkylating agents?
The primary mode of action for most alkylating drugs is via cross-linking of DNA strands.
Alkyl sulfonates (busulfan)
Busulfan is an injectable alkylating agent mainly used in the treatment of chronic myeloid leukemia (CML). This is a strong drug that causes myelosuppression, a side effect that lowers platelets and blood cell counts.
Ethylenimine and methylenamine derivatives (altretamine, thiotepa)
Also used as injections, these types of alkylating agents are primarily used in the treatment of breast and ovarian cancers. Thiotepa, one brand-name drug in this type, may also be used to treat bladder cancer.
Nitrogen mustards (cyclophosphamide, and others)
Nitrogen mustards are primarily used in the treatment of lymphoma. This includes Hodgkin’s disease.
Nitrosoureas (carmustine, lomustine)
There are two types of nitrosoureas: carmustine injections and lomustine (Gleostine) oral tablets. Oncologists may prescribe these to help treat brain tumors.
Platinum-containing antineoplastic agents (carboplatin, cisplatin, oxaliplatin)
Also called platinum coordinating complexes, these drugs work differently from other alkylating agents by destroying the DNA in cancer cells without the use of alkyl groups.
Triazenes (dacarbazine, procarbazine, temozolomide)
Triazenes are used to treat a variety of cancers, including brain tumors, melanoma, and Hodgkin’s disease. While dacarbazine and procarbazine are used in injection or intravenous (IV) solutions, temozolomide is a capsule taken by mouth.
How do alkylating agents stop cancer?
They stop the tumour growth by cross-linking guanine nucleobases in the double-helix strands of DNA, directly attacking DNA. This process makes the strands unable to separate and uncoil. As this is quite necessary for DNA replication, the cells may no longer divide. These particular drugs act nonspecifically.
What is alkylating agent used for?
Alkylating agents have been found to be used in the treatment of leukaemia, lymphoma, melanoma, testicular cancer, breast cancer, and brain cancer. Often, they are the most used ones in combination with other anticancer drugs.
What is the mechanism of action of busulfan?
Answer: Busulfan (alkylating agents mechanism of action) is a bifunctional alkylating agent that can be used to bind two labile methanesulfonate groups to opposite ends of a four-carbon alkyl chain. Busulfan hydrolyzes in aqueous media, releasing methanesulfonate groups.
How does Melphalan affect DNA?
Answer: Melphalan chemically changes the DNA nucleotide guanine via the alkylation process and causes the linkages between DNA strands. This chemical alteration inhibits the RNA synthesis and DNA synthesis, functions required for cells to survive. These particular changes cause cytotoxicity in the dividing and non-dividing tumour cells.
What happens if the MGMT promoter region gets methylated?
If the MGMT promoter region gets methylated, the cells will no longer produce the MGMT, and they are thus more responsive to the alkylating agents. In gliomas, methylation of the MGMT promoter is a valuable indicator of tumour responsiveness to alkylating agents.
What is the name of the drug group that is used to treat brain cancer?
Answer: A cancer drug group, which is called alkylating agents due for the reason they act by the process of alkylation to inhibit the DNA repair. The nitrosoureas may cross the blood-brain barrier and can be used in the treatment of brain tumours. The nitrosoureas include lomustine (CCNU), carmustine (BCNU), and semustine.
What are the types of molecular changes that are induced by the alkylating agents?
The types of molecular changes that are induced by the alkylating agents can be given as cross-linking between the DNA strands and the loss of a basic component (which is purine) from or the nucleic acid breaking. The result is, nucleic acid will not be replicated.
What Lomustine Is Used For
Treatment of brain tumors, both primary (developed in the brain) and metastatic (spread from another source).
How Lomustine Is Given
Lomustine is given by mouth in capsule form. Comes in 5mg, 10mg, 40mg, and 100mg sizes.
Precautions
Before starting lomustine treatment, make sure you tell your doctor about any other medications you are taking (including prescription, over-the-counter, vitamins, herbal remedies, etc.).
Self-Care Tips
Drink at least two to three quarts of fluid every 24 hours, unless you are instructed otherwise.
Monitoring and Testing While Taking Lomustine
You will be checked regularly by your health care professional while you are taking lomustine, to monitor side effects and check your response to therapy. Periodic blood work to monitor your complete blood count (CBC) as well as the function of other organs (such as your kidneys and liver) will also be ordered by your doctor.
How Lomustine Works
Cancerous tumors are characterized by cell division, which is no longer controlled as it is in normal tissue. "Normal" cells stop dividing when they come into contact with like cells, a mechanism known as contact inhibition. Cancerous cells lose this ability.