Which medications in the drug class Antineoplastic Agents are used in the treatment of Renal Cell Carcinoma?

Updated: Feb 19, 2021
  • Author: Kush Sachdeva, MD; Chief Editor: E Jason Abel, MD  more...
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Antineoplastic Agents

Few options are available for the systemic therapy of renal cell carcinoma (RCC), and no hormonal or chemotherapeutic regimen is accepted as a standard of care to treat this disease. Objective response rates, either for single or combination chemotherapy, are usually lower than 15%. Multikinase inhibitors induce objective responses in up to 40% of patients, but they are not known to cure patients with metastatic disease.

Aldesleukin (Proleukin)

Aldesleukin is an interleukin (IL)–2 product that is also known as a T-cell growth factor and activator of T cells and natural killer cells. It has been approved for the treatment of adults with metastatic renal cell carcinoma. This agent affects tumor growth by activating lymphoid cells in vivo, without affecting tumor proliferation directly.

Caution must be exercised in patients with preexisting cardiac, pulmonary, central nervous system (CNS), hepatic, or renal impairment. The major toxic effect of high-dose IL-2 is a sepsislike syndrome, which includes a progressive decrease in systemic vascular resistance and an associated decrease in intravascular volume due to capillary leak.


Vinblastine is a vinca alkaloid with cytotoxic effects via mitotic arrest. This agent binds to a specific site on tubulin, preventing polymerization of tubulin dimers and inhibiting microtubule formation. Using the intrathecal route of administration may result in death.

Gemcitabine (Gemzar)

Gemcitabine is a cytidine analogue. After intracellular metabolism to active nucleotide, this agent inhibits ribonucleotide reductase and competes with deoxycytidine triphosphate for incorporation into DNA.


5-fluorouracil (5-FU) is a fluorinated pyrimidine antimetabolite that inhibits thymidylate synthase (TS) and interferes with RNA synthesis and function. This agent has cell-cycle specificity with activity in S phase. 5-FU metabolites can incorporate into DNA and RNA, resulting in changes in DNA synthesis and RNA processing that impair cell turnover.


Paclitaxel has a mechanism of action that involves tubulin polymerization and microtubule stabilization, which, in turn, inhibits mitosis and may result in breakage of chromosomes.


Carboplatin is an analog of cisplatin. This is a heavy metal coordination complex that exerts its cytotoxic effect by platination of DNA, a mechanism analogous to alkylation, leading to interstrand and intrastrand DNA cross-links and inhibition of DNA replication. Cytotoxicity can occur at any stage of the cell cycle, but the cell is most vulnerable to action of these drugs in the G1 and S phase. It has the same efficacy as cisplatin but with a better toxicity profile.

Ifosfamide (Ifex)

Ifosfamide inhibits DNA and protein synthesis and, thus, cell-proliferation, by causing DNA cross-linking and denaturation of the double helix.


Doxorubicin is a cytotoxic anthracycline antibiotic that blocks DNA and RNA synthesis by inserting between adjacent base pairs and binding to the sugar-phosphate backbone of DNA, which causes DNA polymerase inhibition. It binds to nucleic acids, presumably by specific intercalation of the anthracycline nucleus with the DNA double helix. Doxorubicin is also a powerful iron chelator. The iron-doxorubicin complex induces the production of free radicals that can destroy DNA and cancer cells.


Floxuridine is an antineoplastic antimetabolite that is most active during the S phase of the cell cycle. Floxuridine is catabolized to 5-fluorouracil when administered. Floxuridine inhibits DNA and RNA synthesis.

Interferon alfa-2a (Roferon A) and 2b (Intron A)

Interferons are natural glycoproteins with antiviral, antiproliferative, and immunomodulatory properties. These agents have a direct antiproliferative effect on renal tumor cells, stimulate host mononuclear cells, and enhance expression of major histocompatibility complex molecules.

Caution should be exercised when administering interferons in patients with brain metastases, severe hepatic or renal insufficiency, seizure disorders, multiple sclerosis, or a compromised CNS.

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