Which medications in the drug class Antineoplastics, Alkylating are used in the treatment of Small Cell Lung Cancer (SCLC)?

Updated: May 07, 2021
  • Author: Winston W Tan, MD, FACP; Chief Editor: Nagla Abdel Karim, MD, PhD  more...
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Antineoplastics, Alkylating

Cyclophosphamide (Cytoxan, Neosar)

Cyclophosphamide is chemically related to the nitrogen mustards. As an alkylating agent, the mechanism of action of its active metabolites may involve cross-linking of DNA, which may interfere with the growth of normal and neoplastic cells. Fatal cardiotoxicity has been reported with coadministration of pentostatin.

Carboplatin (Paraplatin)

Carboplatin is a platinum alkylating agent that interferes with the function of DNA by producing interstrand DNA cross-links. It can be used for the treatment of small cell lung cancer (SCLC), which is an off-label indication. Carboplatin has black box warnings, including bone marrow suppression, anaphylactic reactions, and vomiting.


Cisplatin is a platinum-containing compound that exerts an antineoplastic effect by covalently binding to DNA, with preferential binding to the N-7 position of guanine and adenosine. It can react with 2 different sites on DNA to produce cross-links. The platinum complex can also bind to nuclear and cytoplasmic protein. Cisplatin has black box warnings, including anaphylacticlike reactions, ototoxicity, and renal toxicity.

Ifosfamide (Ifex)

Ifosfamide is a nitrogen mustard alkylating agent that inhibits DNA and protein synthesis. Although not FDA approved, ifosfamide is often used as a treatment for relapsed SCLC.

Lurbinectedin (Zepzelca)

Lurbinectedin is an alkylating drug. It binds guanine residues in the minor groove of DNA, forming adducts and resulting in a bending of the DNA helix towards the major groove. The adduct formation triggers a cascade of events that can affect the subsequent activity of DNA-binding proteins, including some transcription factors, and DNA repair pathways. FDA granted accelerated approval for adults with metastatic SCLC with disease progression on or after platinum-based chemotherapy. 

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