Which medications in the drug class Antineoplastic Agents are used in the treatment of Non-Small Cell Lung Cancer (NSCLC)?

Updated: Jul 15, 2021
  • Author: Winston W Tan, MD, FACP; Chief Editor: Nagla Abdel Karim, MD, PhD  more...
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Antineoplastic Agents

Antineoplastic agents are used either to prolong survival or to palliate symptoms in advanced or unresectable lung cancer.


Carboplatin has a mechanism of action similar to that of cisplatin. It is approved for ovarian cancer but is used commonly in squamous cell carcinoma (SCC) of the head, neck, cervix, and lungs. Its main advantages over cisplatin include less nephrotoxicity and ototoxicity (not requiring extensive prehydration) and reduced likelihood of inducing nausea and vomiting. It is more likely to induce myelotoxicity.

Vinorelbine (Navelbine)

Vinorelbine is a semisynthetic vinca alkaloid that inhibits tubulin polymerization during the G2 phase of cell division, thereby inhibiting mitosis. Vinorelbine alone or in combination with cisplatin is indicated as first-line treatment of ambulatory patients with unresectable, advanced NSCLC and for stage IV NSCLC. In stage III NSCLC, vinorelbine is indicated in combination with cisplatin.


Paclitaxel is a naturally occurring chemical derived from the Pacific yew tree (Taxus brevifolia). It inhibits tubulin depolymerization in the spindle during cell division. Paclitaxel is used in combination with cisplatin for the first-line treatment of NSCLC in patients who are not candidates for potentially curative surgery or radiation therapy.

Paclitaxel protein bound (Abraxane)

Protein-bound paclitaxel is a microtubular inhibitor (albumin-conjugated formulation). It is a natural taxane, and it prevents depolymerization of cellular microtubules, which results in DNA, RNA, and protein synthesis inhibition. It is indicated for locally advanced or metastatic non–small cell lung cancer (NSCLC), as first-line treatment in combination with carboplatin, in patients who are not candidates for curative surgery or radiation therapy.


Cisplatin is an alkylating agent that causes intrastrand and interstrand cross-linking of DNA, leading to strand breakage. It has a very broad range of antitumor activity and is approved for use in testicular, ovarian, and transitional cell carcinomas. It forms the basis of currently available approved combination chemotherapy regimens for NSCLC. Administer it as a single-dose intravenous (IV) infusion or in divided doses over several days; this can be repeated only after complete hematologic recovery; cycles are typically separated by 3-4 wk.

Gemcitabine (Gemzar)

Gemcitabine is an antimetabolite that acts as an inhibitor of DNA synthesis. It is cell-cycle specific for the S phase. Gemcitabine is used as first-line treatment of patients with inoperable, locally advanced (stage IIIA or IIIB), or metastatic (stage IV) NSCLC in combination with cisplatin.

Docetaxel (Taxotere)

Docetaxel is a semisynthetic taxane, a class of drugs that inhibits cancer cell growth by promoting assembly and blocking disassembly of microtubules, thereby preventing cancer cell division, leading to cell death. It is indicated for the treatment of patients with locally advanced or metastatic NSCLC after failure of prior platinum-based chemotherapy when used alone. It can be used in combination with cisplatin for the treatment of patients with unresectable, locally advanced, or metastatic NSCLC who have not previously received chemotherapy for this condition.

Pemetrexed disodium (Alimta)

Pemetrexed disrupts folate-dependent metabolic processes essential for cell replication. It specifically inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), which are folate-dependent enzymes involved in de novo biosynthesis of thymidine and purine nucleotides. It is indicated for nonsquamous NSCLC as follows:

1) Initial treatment in combination with pembrolizumab and platinum chemotherapy for patients with metastatic disease with no EGFR or ALK genomic tumor aberrations

2) Initial treatment in combination with cisplatin for patients with locally advanced or metastatic disease

3) Single agent for maintenance in patients with locally advanced or metastatic disease that has not progressed after 4 cycles of platinum-based first-line chemotherapy

4) Single agent for treatment of patients with recurrent metastatic disease after prior therapy


Cyclophosphamide is chemically related to nitrogen mustards; as an alkylating agent, the mechanism of action of active metabolites may involve cross-linking of DNA, which may interfere with growth of normal and neoplastic cells.


Doxorubicin is an anthracycline that inhibits topoisomerase II and produces free radicals, which may cause destruction of DNA; the combination of these 2 events can, in turn, inhibit the growth of neoplastic cells.


Vincristine is a vinca alkaloid whose mechanism of action is uncertain. It may involve a decrease in reticuloendothelial cell function or an increase in platelet production. However, neither of these mechanisms fully explains the effect in thrombotic thrombocytopenic purpura and hemolytic uremic syndrome. The antineoplastic effects of vincristine are related to its binding to tubulin and inhibition of microtubule formation.


Etoposide inhibits topoisomerase II and causes DNA strand breakage, causing cell proliferation to arrest in the late S or early G2 portion of cell cycle; do not administer IT.

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