What is the mechanism of action of cladribine?
Cladribine-phosphates interfere with DNA synthesis and repair through incorporation into DNA and through inhibition of enzymes involved in DNA metabolism, including DNA polymerase and ribonucleotide reductase. This in turn leads to DNA strand breaks and ultimately cell death.
What enzyme does cladribine inhibit?
Cladribine is a purine nucleoside analog that inhibits DNA synthesis and ribonucleotide reductase, which is used for the treatment of leukemia and lymphoma (Roback et al., 2006).
What type of drug is cladribine?
Cladribine is used to treat hairy cell leukemia (cancer of a certain type of white blood cell). Cladribine is in a class of medications known as purine analogs. It works by stopping or slowing the growth of cancer cells.
Is cladribine cell cycle specific?
Cladribine belongs to the class of chemotherapy drugs called antimetabolites. Antimetabolites are very similar to normal substances within the cell. When the cells incorporate these substances into the cellular metabolism, they are unable to divide. Antimetabolites are cell-cycle specific.
Is cladribine a purine analogue?
Cladribine was synthesized as a purine analogue drug that inhibited adenosine deaminase. It received FDA approval in the 1980s for treatment of hairy cell leukemia.
Is teriflunomide an immunosuppressant?
Yes, Aubagio (teriflunomide) may lower your white blood cell (WBC) count and possibly suppress your immune system. White blood cells are found in your blood and are used to fight infection.
Does Tecfidera cross the blood brain barrier?
This molecule interacts with the immune cells in the blood circulation and crosses the blood–brain barrier (BBB) to the central nervous system (CNS) (10).
Is cladribine an antimetabolite?
Drug type: Cladribine is an anti-cancer (“antineoplastic” or “cytotoxic”) chemotherapy drug. This medication is classified as an “antimetabolite.” (For more detail, see “How this drug works” section below).
What part of the cell cycle does chemotherapy affect?
The cell cycle goes from the resting phase, through active growing phases, and then to mitosis (division). The ability of chemotherapy to kill cancer cells depends on its ability to halt cell division. Usually, cancer drugs work by damaging the RNA or DNA that tells the cell how to copy itself in division.
What happens when cladribine is activated in a cell?
Activated cladribine is incorporated into the DNA synthesis pathway, where it disrupts DNA repair and synthesis, resulting in an accumulation of DNA strand breaks This is followed by the activation of transcription factor p53, the release of cytochrome c from mitochondria and eventual programmed cell death (apoptosis).
What kind of drug is cladribine used for?
Drug type: Cladribine is an anti-cancer (“antineoplastic” or “cytotoxic”) chemotherapy drug. This medication is classified as an “antimetabolite.” (For more detail, see “How this drug works” section below). What Cladribine Is Used For:
How is cladribine resistant to breakdown by Ada?
However, unlike adenosine, cladribine has a chlorine molecule at position 2, which renders it partially resistant to breakdown by ADA. This causes it to accumulate in cells and interfere with the targeted cell’s ability to process DNA. Cladribine is taken up via specific nucleoside transporter proteins.
How is the accumulation of cladribine dependent on the ratio?
Accumulation of cladribine into cells is dependent on the ratio of 2-CdATP and 5′-nucleotidase (5′-NT), which breaks down and inactivates the compound. This ratio differs between cell types, with high levels in T and B lymphocytes, resulting in selective targeting of these cells.