Which medications in the drug class Antineoplastics, Antimetabolite are used in the treatment of Bladder Cancer?

Updated: Feb 23, 2021
  • Author: Kara N Babaian, MD, FACS; Chief Editor: Bradley Fields Schwartz, DO, FACS  more...
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Answer

Antineoplastics, Antimetabolite

These agents inhibit cell growth and proliferation. They interfere with DNA synthesis by blocking the methylation of deoxyuridylic acid.

Fluorouracil (Adrucil)

Fluorouracil is a pyrimidine antimetabolite. Several mechanisms of action have been proposed, including inhibition of thymidylate synthase and inhibition of RNA synthesis. This agent is also a potent radiosensitizer. Although not approved by the FDA for this indication, it is often used as a treatment for bladder cancer,., commonly in Cisplatin/Fluorouracil combinations.

Methotrexate (Trexall, Rasuvo, Otrexup, Xatmep)

Methotrexate inhibits dihydrofolate reductase (DHFR), causing a block in the reduction of dihydrofolate to tetrahydrofolate. This inhibits the formation of thymidylate and purines and arrests DNA, RNA, and protein synthesis.Common toxicities include mucositis and myelosuppression. It is often used as a treatment for bladder cancer, although that is not an FDA-approved indication.

Gemcitabine (Gemzar)

Gemcitabine is a pyrimidine analog. After intracellular metabolism to its active nucleotide, it inhibits ribonucleotide reductase and competes with deoxycytidine triphosphate for incorporation into DNA. Although it does not have FDA approval for this indication, it is often used as a treatment for bladder cancer. Gemcitabine is used in combination with cisplatin for the treatment of advanced or metastatic bladder cancer. It is also used as an intraveiscal treatment.

Pemetrexed (Alimta)

Pemetrexed disrupts the folate-dependant metabolic processes important for cell replication, inhibits the enzymes involved in folate metabolism and DNA synthesis, and inhibits protein synthesis. Although it does not have FDA approval for this indication, it is often used for the treatment of metastatic bladder cancer. Folic acid and vitamin B12 are typically given prior to initiation of treatment. Dexamethasone is also given with pemetrexed, to minimize cutaneous reactions.


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