Antineoplastic agent

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This editable Main Article is under development and subject to a disclaimer.

[edit intro]

## Contents

* 1 Classification
* 1.1 Alkylating agents
* 1.1.1 Nitrogen mustard analogues
* 1.1.2 Alkyl sulfonates
* 1.1.3 Ethylene imines
* 1.1.4 Nitrosoureas
* 1.1.5 Epoxides
* 1.1.6 Other alkylating agents
* 1.2 Antimetabolites
* 1.2.1 Folic acid analogues
* 1.2.2 Purine analogues
* 1.2.3 Pyrimidine analogues
* 1.3 Plant alkaloids and other natural products
* 1.3.1 Vinca alkaloids and analogues
* 1.3.2 Podophyllotoxin derivatives
* 1.3.3 Colchicine derivatives
* 1.3.4 Taxanes
* 1.3.5 Other plant alkaloids and natural products
* 1.4 Cytotoxic antibiotics and related substances
* 1.4.1 Actinomycines
* 1.4.2 Anthracyclines and related substances
* 1.4.3 Other cytotoxic antibiotics
* 1.5 Other antineoplastic agents
* 1.5.1 Platinum compounds
* 1.5.2 Methylhydrazines
* 1.5.3 Monoclonal antibodies
* 1.5.4 Sensitizers used in photodynamic/radiation therapy
* 1.5.5 Protein kinase inhibitors
* 1.5.6 Other antineoplastic agents
* 2 Dosing
* 3 References

In medicine, antineoplastic agents are "substances that inhibit or prevent the proliferation of neoplasms", otherwise known as cancers.[1] Generally, antineoplastic agents are for treating malignant neoplasms such as cancers and sarcomas.

## Classification[edit]

This classification is based on World Health Organization's Collaborating Centre for Drug Statistics Methodology.[2]

### Alkylating agents[edit]

ATC/DDD group L01A. Alkylating antineoplastic agents are a "class of drugs that differs from other alkylating agents used clinically in that they are monofunctional and thus unable to cross-link cellular macromolecules. Among their common properties are a requirement for metabolic activation to intermediates with antitumor efficacy and the presence in their chemical structures of N-methyl groups, that after metabolism, can covalently modify cellular DNA. The precise mechanisms by which each of these drugs acts to kill tumor cells are not completely understood."[3]

#### Nitrogen mustard analogues[edit]

ATC/DDD group L01AA. Examples include cyclophosphamide, chlorambucil, melphalan.

#### Alkyl sulfonates[edit]

ATC/DDD group L01AB.

#### Ethylene imines[edit]

ATC/DDD group L01AC.

#### Nitrosoureas[edit]

ATC/DDD group L01AD.

#### Epoxides[edit]

ATC/DDD group L01AG.

#### Other alkylating agents[edit]

ATC/DDD group L01AX.

### Antimetabolites[edit]

ATC/DDD group L01B. Antineoplastic antimetabolites are "antimetabolites that are useful in cancer chemotherapy."[4]

#### Folic acid analogues[edit]

ATC/DDD group L01BA. Examples include:

* Methotrexate "is an inhibitor of tetrahydrofolate dehydrogenase and prevents the formation of tetrahydrofolate, necessary for synthesis of thymidylate, an essential component of DNA."[5]
* Raltitrexed
* Pemetrexed

#### Purine analogues[edit]

ATC/DDD group L01BB. Examples include:

* mercaptopurine is an "antimetabolite antineoplastic agent with immunosuppressant properties. It interferes with nucleic acid synthesis by inhibiting purine metabolism and is used, usually in combination with other drugs, in the treatment of or in remission maintenance programs for leukemia."[6]
* tioguanine
* cladribine
* fludarabine
* clofarabine
* nelarabine

#### Pyrimidine analogues[edit]

ATC/DDD group L01BC. Examples include:

* cytarabine is a "pyrimidine nucleoside analog that is used mainly in the treatment of leukemia, especially acute non-lymphoblastic leukemia. Cytarabine is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA. Its actions are specific for the S phase of the cell cycle. It also has antiviral and immunosuppressant properties."[7]
* fluorouracil
* tegafur
* carmofur
* gemcitabine
* capecitabine
* azacitidine
* decitabine

### Plant alkaloids and other natural products[edit]

ATC/DDD group L01C.

#### Vinca alkaloids and analogues[edit]

ATC/DDD group L01CA.

#### Podophyllotoxin derivatives[edit]

ATC/DDD group L01CB. Examples include etoposide.

#### Colchicine derivatives[edit]

ATC/DDD group L01CC.

#### Taxanes[edit]

ATC/DDD group L01CD.

#### Other plant alkaloids and natural products[edit]

ATC/DDD group L01CX.

### Cytotoxic antibiotics and related substances[edit]

ATC/DDD group L01D.

#### Actinomycines[edit]

ATC/DDD group L01DA.

#### Anthracyclines and related substances[edit]

ATC/DDD group L01DB.

#### Other cytotoxic antibiotics[edit]

ATC/DDD group L01DC.

### Other antineoplastic agents[edit]

ATC/DDD group L01X.

#### Platinum compounds[edit]

ATC/DDD group L01XA examples include cisplatin, carboplatin, oxaliplatin, and satraplatin.

#### Methylhydrazines[edit]

ATC/DDD group L01XB.

#### Monoclonal antibodies[edit]

ATC/DDD group L01XC. Examples include:

Anti-EpCAM

* Edrecolomab is monclonal antibody against EpCAM (Entrez protein). Edrecolomab is a "anticolorectal carcinoma antibody for treatment of advanced colorectal carcinoma".[8]

Anti-ErbB1

* Cetuximab (IMC-C225) is a recombinant, human/mouse chimeric monoclonal antibody that binds to epidermal growth factor receptor (ErbB1, EGFR) and may treat head and neck cancers, colorectal cancer, and non-small cell lung cancer in patients who do not have mutations in the KRAS gene.[9]

* Panitumumab is an "antibody that blocks receptors for epidermal growth factor receptor; approved for advanced colon cancer".[10]

Anti-ErbB2

* Trastuzumab is a "an antibody against the ErbB-2 receptor that lengthens remission time in metastatic breast cancer."[11]

Anti-CD3 and anti-EpCAM

* Catumaxomab. Is a monoclonal antibody against CD3 (Entrez protein)and EpCAM (Entrez protein). "Extracorporeal PBMNC coating with catumaxomab may be an option to control intravascular cytokine release induced by therapeutic antibodies".[12]

Anti-MS4A1 (CD20 antigen)

* Rituximab is a "genetically engineered anti-CD20 (Entrez protein) antibody for the treatment of B-cell lymphoma".[13]

Anti-SIGLEC3 (CD33)

* Gemtuzumab is an "anti-CD33 (Entrez protein) antibody calicheamicin conjugate".[14]

Anti-CD52

* Alemtuzumab is a "a therapeutic antibody directed against the CDw52 antigen (Entrez protein) expressed by the lymphocytes and has proven lytic abilities both in vitro and in vivo; has been sequenced".[15]

Anti-VEGF

* Bevacizumab is an "anti-VEGF (Entrez protein) monoclonal antibody consisting of humanized murine antibody with antigen-binding, complementary-determining regions from murine VEGF".[16]

#### Sensitizers used in photodynamic/radiation therapy[edit]

ATC/DDD group L01XD.

#### Protein kinase inhibitors[edit]

ATC/DDD group L01XE. Examples include imatinib, gefitinib, erlotinib, sunitinib, sorafenib, dasatinib, lapatinib, nilotinib, and temsirolimus.

#### Other antineoplastic agents[edit]

ATC/DDD group L01XX. Examples include hydroxycarbamide (hydroxyurea), tretinoin, and celecoxib.

## Dosing[edit]

Dosage may be by the area under the curve (AUC), expressed at mg/mL * min.

## References[edit]

1. ↑ Anonymous (2025), Antineoplastic agent (English). Medical Subject Headings. U.S. National Library of Medicine.
2. ↑ Anonymous. WHO Collaborating Centre for Drug Statistics Methodology. World Health Organization. Retrieved on 2009-02-04.
3. ↑ Anonymous (2025), Antineoplastic Agents, Alkylating (English). Medical Subject Headings. U.S. National Library of Medicine.
4. ↑ Anonymous (2025), Antineoplastic Agents, Alkylating (English). Medical Subject Headings. U.S. National Library of Medicine.
5. ↑ Anonymous (2025), Methotrexate (English). Medical Subject Headings. U.S. National Library of Medicine.
6. ↑ Anonymous (2025), Mercaptopurine (English). Medical Subject Headings. U.S. National Library of Medicine.
7. ↑ Anonymous (2025), cytarabine (English). Medical Subject Headings. U.S. National Library of Medicine.
8. ↑ Anonymous (2025), edrecolomab [Substance Name] (English). Medical Subject Headings. U.S. National Library of Medicine.
9. ↑ Van Cutsem E, Köhne CH, Hitre E, Zaluski J, Chang Chien CR, Makhson A et al. (2009). "Cetuximab and chemotherapy as initial treatment for metastatic colorectal cancer.". N Engl J Med 360 (14): 1408-17. DOI:10.1056/NEJMoa0805019. PMID 19339720. Research Blogging.
10. ↑ Anonymous (2025), Panitumumab [Substance Name] (English). Medical Subject Headings. U.S. National Library of Medicine.
11. ↑ Anonymous (2025), Trastuzumab [Substance Name] (English). Medical Subject Headings. U.S. National Library of Medicine.
12. ↑ Anonymous (2025), Catumaxomab [Substance Name] (English). Medical Subject Headings. U.S. National Library of Medicine.
13. ↑ Anonymous (2025), Rituximab [Substance Name] (English). Medical Subject Headings. U.S. National Library of Medicine.
14. ↑ Anonymous (2025), Gemtuzumab [Substance Name] (English). Medical Subject Headings. U.S. National Library of Medicine.
15. ↑ Anonymous (2025), Alemtuzumab [Substance Name] (English). Medical Subject Headings. U.S. National Library of Medicine.
16. ↑ Anonymous (2025), Bevacizumab [Substance Name] (English). Medical Subject Headings. U.S. National Library of Medicine.