List of antineoplastic agents

This is an alphabetic list of approved antineoplastic agents used to directly treat cancer. For inclusion on this list, agents are approved by a recognized governmental agency such as the United States Food and Drug Administration, European Medicines Agency (EMA), or the equivalent agency in Australia, Canada, China or Japan.

Background

• This alphabetic list restricts itself to the medication name, and a brief explanation of its mechanism of action.
• Double entry of an agent on this table is permitted when two widely accepted generic names are in use in different international jurisdictions. For example, trastuzumab emtansine is ado-trastuzumab emtansine in the US. However, entries are based only on these INN or widely accepted generic names, and should not be added for brand names.
• In practice, some agents are used in combination chemotherapy regimens.
• Previous versions of this list attempted to include both approved (labeled) and unlabeled indications, as well as the most important side effects. However, this list now restricts itself to name, and mechanism of action. Additional information such as side effects may be available in the medication article, but for details of labeled uses, see the relevant package insert, which may vary by jurisdiction. For unlabeled uses, sources such as AHFS and oncology textbooks may be consulted. Additionally, HemOnc.org is an external wiki, which links each medication to its US package insert and to patient information sources.
• These agents can be sorted into therapeutic subgroups. One scheme for this is ATC code L01.

Not included

Additional agents that are used in oncology but which are not included here include:^[1]

1. antiemetics
2. hematopoietic growth factors: erythropoietin, GCSF, oprelvekin, pegfilgrastim, GMCSF
3. other marrow stimulating agents: eltrombopag, plerixafor, romiplostim
4. immunosuppressants (post-BMT): basiliximab, cyclosporine, mycophenolic acid
5. anti-complement therapy: eculizumab
6. bone resorption modifiers: calcitonin, cinacalcet, denosumab, pamidronate, zoledronate
7. toxicity modifiers: allopurinol, amifostine, dexrazoxane, glucarpidase, methylene blue, mesna, palifermin, rasburicase
8. medications for infections
9. anticoagulants and thrombolytic agents, such as alteplase for central venous access device clearance
10. replacement therapies: folate, intravenous iron, vitamin B₁₂
11. iron binding agents: deferasirox, deferiprone, deferoxamine
12. diagnostic agents, such as fluciclovine

Medications

mechlorethamine (widely used in the US, not the USAN, however) also known as mustine and HN2 and in former USSR as Embichin

1. abarelix, a gonadotropin-releasing hormone antagonist (GnRH antagonist), primarily used in oncology to reduce the amount of testosterone
2. abiraterone, a CYP17A1 androgen biosynthesis inhibitor, used in oncology to reduce the amount of testosterone
3. ado-trastuzumab emtansine (US name, otherwise known as trastuzumab emtansine), an antibody-drug conjugate of the monoclonal antibody trastuzumab, that targets HER2, linked to emtansine (DM1), a tubulin inhibitor, that inhibits the assembly of microtubules
4. afatinib, a tyrosine kinase inhibitor of EGFR, HER2 and HER4^[2]
5. aflibercept (US name is ziv-aflibercept), a recombinant fusion protein consisting of vascular endothelial growth factor (VEGF)-binding portions from the extracellular domains of human VEGF receptors 1 and 2, that are fused to the Fc portion of the human IgG1 immunoglobulin, which acts as a decoy inhibitor of VEGF and PGF^{[1]:1788[3][4]}
6. aldesleukin, a recombinant form of interleukin-2 (IL-2), which is an immune system signaling cytokine with direct effects on immune cells, particularly T cells
7. alectinib, an anaplastic lymphoma kinase (ALK) inhibitor
8. alemtuzumab, a monoclonal antibody that targets CD52
9. alitretinoin, a retinoid agonist that binds to and activates all known intracellular retinoic acid receptor (RAR) and retinoid X receptor (RXR) subtypes (RAR-α, RAR-β, and RAR-γ, RXR-α, RXR-β, RXR-γ
10. altretamine, an antineoplastic agent with an unclear mechanism of action, classified by MeSH as an alkylating agent due to structural similarity, but which has exhibited activity in some tumors resistant to classic alkylators;^[1]:84 forms reactive intermediates that covalently bind to microsomal proteins and DNA, possibly causing DNA damage
11. amsacrine, an antineoplastic agent that intercalates into the DNA of tumor cells, thereby altering the major and minor groove proportions, and thus inhibiting both DNA replication and transcription by reducing association between the affected DNA and: DNA polymerase, RNA polymerase and transcription factors; also expresses topoisomerase inhibitor activity, inhibiting topoisomerase II
12. anagrelide, a phosphodiesterase 3 inhibitor
13. anastrozole, a non-steroidal aromatase inhibitor, which inhibits the synthesis of estrogen
14. antithymocyte globulin
15. arsenic trioxide,^{[Note 1]} an antineoplastic agent which induces apoptosis in APL cells via morphological changes and DNA fragmentation; also damages or degrades the fusion protein formed the commonest subtype of APL, the reciprocal translocation of the promyelocytic leukemia gene (PML) on chromosome 15 with the retinoic acid receptor-alpha gene on chromosome 17 (RARA)^[1]:142
16. asparaginase,^{[Note 2]} an antineoplastic enzyme agent which catalyses the hydrolysis conversion of the amino acid of L-asparagine to aspartic acid and thereby reduces the availability of L-asparagine to leukemic cells; unlike normal cells, certain types of leukemic cells do not synthesise L-asparagine, which is essential for cell growth and survival
17. atezolizumab, a monoclonal antibody that blocks the interaction of
18. axitinib, a tyrosine kinase inhibitor multikinase inhibitor^[5]
19. azacitidine, a DNA methyltransferase inhibitor, incorporates itself into RNA, hence inhibiting gene expression^{[6][7][8][9][10][11][12][13][14][15][16]}
20. BCG^{[Note 3]} a live, attenuated Mycobacterium bovis vaccine, which produces a local inflammatory reaction, resulting in elimination or reduction of superficial tumor lesions of the bladder
21. belinostat, a histone deacetylase inhibitor, hence inducing alterations in gene expression
22. bendamustine, a nitrogen mustard alkylating agent
23. bevacizumab, a monoclonal antibody that targets VEGF inhibitor
24. bexarotene, a retinoid RXR agonist^[17]
25. bicalutamide, a synthetic, non-steroidal, pure antiandrogen
26. bleomycin inhibits DNA and to a lesser extent RNA synthesis, produces single and double strand breaks in DNA possibly by free radical formation
27. blinatumomab, a bi-specific T-cell engager (BiTE) monoclonal antibody that targets the CD19 antigen present on B cells and the CD3 site on T cells
28. bortezomib, a proteasome inhibitor
29. bosutinib, a tyrosine kinase inhibitor of Bcr-Abl and SRc family kinases (including Src, Lyn and Hck).^[18][19]
30. brentuximab vedotin, an antibody-drug conjugate (ADC) that targets the protein CD30 on tumor cells, linked to the antimitotic agent monomethyl auristatin E (MMAE, reflected by the 'vedotin' in the drug's name)
31. busulfan, a dialkylsulfonate alkylating agent^[20][21]
32. cabazitaxel, a taxane microtubule disassembly inhibitor; arrests cells in late G2 phase and M phase
33. cabozantinib, a tyrosine kinase inhibitor of c-Met and VEGFR2
34. capecitabine, a fluorouracil-analog inhibitor of thymidylate synthase^{[22][23][24][25][26][27][28][29][30]}
35. carboplatin, a platinum-based antineoplastic that reacts with DNA, inducing non-cell cycle specific apoptosis
36. carfilzomib, a proteasome inhibitor
37. carmofur, a fluorouracil-analog inhibitor of thymidylate synthase and inhibitor of acid ceramidase (AC)
38. carmustine, a nitrosourea alkylating agent
39. chlorambucil, a nitrogen mustard alkylating agent^[20][21]
40. chlormethine, a nitrogen mustard alkylating agent^[21]
41. ceritinib, an anaplastic lymphoma kinase (ALK) inhibitor^{[Note 4]}
42. cetuximab, a monoclonal antibody that targets EGFR
43. chidamide, a histone deacetylase inhibitor, hence inducing alterations in gene expression
44. cisplatin, a platinum-based antineoplastic that reacts with DNA, inducing non-cell cycle specific apoptosis
45. cladribine, adenosine analog DNA methyltransferaseinhibitor, metabolites incorporate themselves into DNA^[31] used in multiple sclerosis^{[31][32][33][34][35][36][37][38][39][40]}cancer:^{[32][41][42][43]}
46. clofarabine, a deoxyadenosine analog ribonucleotide reductase and DNA polymerase inhibitor^{[44][45][46][47][48][49][50][51][52][53]}
47. cobimetinib, a tyrosine kinase inhibitor^[54] melanoma that expresses a BRAF V600E or V600K mutation^[54]|| diarrhea, nausea, vomiting, rash, photosensitivity, pyrexia^[55][55]
48. crizotinib, a tyrosine kinase inhibitor of ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), and Recepteur d'Origine Nantais (RON)^{[56][57][58][59][60]}
49. cyclophosphamide, an alkylating agent nitrogen mustard^[21]
50. cyproterone,
51. cytarabine, a cytidine analog DNA polymerase inhibitor, S-phase specific; incorporates its metabolites into DNA^[61][62][63]
52. dabrafenib
53. dacarbazine, an alkylating agent^[21]
54. dactinomycin complexes with DNA interfering with DNA-dependent RNA synthesis
55. daratumumab, a monoclonal antibody inhibitor that targets CD38
56. daunorubicin, an anthracycline: inhibits DNA and RNA synthesis by intercalating DNA base pairs; inhibits DNA repair by inhibiting topoisomerase II
57. dasatinib, a tyrosine kinase inhibitor of BCR-ABL, SRC family, c-Kit, EPHA2 and PDGFR-β kinase
58. decitabine, a DNA methyltransferase inhibitor^{[7][8][64][65][66][67][68][69][70][71][72]}
59. degarelix,
60. denileukin diftitox, interleukin 2 combined with diphtheria toxin which binds to the interleukin receptor on immune cells and introduces the diphtheria toxin into the cell^{[73][74][75][76]}
61. dinutuximab, a monoclonal antibody that targets glycolipid GD2^[77]
62. docetaxel, a taxane microtubule disassembly inhibitor; arrests cells in late G2 phase and M phase
63. doxorubicin, an anthracycline: inhibits DNA and RNA synthesis by intercalating DNA base pairs; inhibits DNA repair by inhibiting topoisomerase II
64. elotuzumab antiSLAMF7 (CD319)
65. enzalutamide (androgen receptor (AR) antagonist and also signaling inhibitor^[78])
66. epirubicin, an anthracycline: inhibits DNA and RNA synthesis by intercalating DNA base pairs; inhibits DNA repair by inhibiting topoisomerase II
67. etoposide, a podophyllotoxin topoisomerase II inhibitor
68. eribulin
69. erlotinib, a tyrosine kinase inhibitor of EGFR
70. estramustine, a nitrogen mustard and estrogen analog
71. everolimus, a sirolimus-analog mammalian target of rapamycin (mTOR) inhibitor
72. exemestane
73. floxuridine, a fluorouracil analog thymidylate synthase inhibitor^[79]
74. fludarabine, an adenosine analog DNA polymerase and ribonucleotide reductase inhibitor^{[80][81][82][82][83][84][85]}
75. fluorouracil, uracil analog thymidylate synthase inhibitor^[86][87][88]
76. fluoxymesterone,
77. flutamide
78. fotemustine, a nitrosourea alkylating agent
79. fulvestrant, is a selective estrogen receptor degrader (SERD), which results in complete estrogen receptor antagonist with no agonist effects, and which, in addition, accelerates the proteasomal degradation of the estrogen receptor
80. gefitinib, a tyrosine kinase inhibitor of EGFR
81. gemcitabine, deoxycytidine analog DNA synthesis inhibitor, induces apoptosis specifically in S-phase^{[89][90][91][92][93][94]}
82. gemtuzumab ozogamicin, a monoclonal antibody antibody-drug conjugate that targets CD33^[95]
83. goserelin
84. histrelin,
85. hydroxycarbamide, also known as hydroxyurea, an inhibitor of the enzyme ribonucleotide reductase, thus inhibiting DNA synthesis^{[96][97][98][99][100][101][102][103][104][105]}
86. hydroxyurea, also known as hydroxycarbamide, an inhibitor of the enzyme ribonucleotide reductase, thus inhibiting DNA synthesis
87. ibritumomab tiuxetan, a monoclonal antibody radioimmunotherapy which binds to the CD20 antigen
88. ibrutinib, a Bruton's tyrosine kinase (BTK) inhibitor * ibritumomab tiuxetan, a CD20 antibody bound with the radioactive isotope, 90Y, induces radiation-dependent cell lysis^[106][107]
89. idarubicin, an anthracycline inhibitor of DNA and RNA synthesis, which intercalates DNA base pairs; inhibits DNA repair by inhibiting topoisomerase II
90. idelalisib, a phosphoinositide 3-kinase inhibitor of P110δ, the delta isoform of the enzyme phosphoinositide 3-kinase
91. ifosfamide, a nitrogen mustard alkylating agent^[21]
92. imatinib, a tyrosine kinase inhibitor (TKI) of Bcr-Abl kinase, and...
93. imiquimod, an immune response modifier which signals to the innate arm of the immune system through the toll-like receptor 7 (TLR7)
94. interferon (Interferon alfa-2b and also Peginterferon alfa-2b)
95. iobenguane, a monoclonal antibody radioimmunotherapy; the iodine-131 variant is used for tissue destruction
96. ipilimumab, a monoclonal antibody that targets CTLA4
97. irinotecan, a topoisomerase I inhibitor^{[Note 5]}
98. isotretinoin retinoid|| RXR & RAR agonist || neuroblastoma^{[108][109][110]}
99. ixabepilone, an epothilone B analog promotes tubulin polymerisation and stabilises microtubular function, causing cell cycle arrest at G2/M phase and subsequently induces apoptosis
100. ixazomib, a proteasome inhibitor; reversibly inhibits the protein proteasome subunit beta type-5 (PSMB5), which is part of the 20S proteasome complex
101. lanreotide, a long-acting analogue of somatostatin
102. lapatinib, a tyrosine kinase inhibitor of HER2
103. lenalidomide, a thalidomide analog immunomodulatory drug (IMiD); anti-angiogenesis (via inhibition of VEGF release), anti-TNF, IL-6 and pro-IL-2, IFN-γ effects; also stimulates T cells and apoptosis in cancer cells
104. lentinan, an anti-tumor polysaccharide
105. lenvatinib, a tyrosine kinase inhibitor (TKI) of...
106. letrozole, an antihormone non-steroidal aromatase inhibitor, thus inhibiting the synthesis of estrogen
107. leuprolide
108. lomustine, a nitrosourea alkylating agent^[21]
109. melphalan, a nitrogen mustard alkylating agent^[21]
110. methotrexate, an antifolate dihydrofolate reductase inhibitor^{[111][112][113][114][115][116]}
111. mercaptopurine, a hypoxanthine-analog inhibitor of purine synthesis^{[117][118][119]}
112. mifepristone
113. mitomycin cross-links DNA
114. mitotane, an isomer of DDD and a derivative of DDT, which alters steroid peripheral metabolism, directly suppresses the adrenal cortex
115. mitoxantrone, an anthracycline: inhibits DNA and RNA synthesis by intercalating DNA base pairs; inhibits DNA repair by inhibiting topoisomerase II
116. nab-paclitaxel, a taxane microtubule disassembly inhibitor; arrests cells in late G2 phase and M phase
117. necitumumab, a recombinant human IgG1 monoclonal antibody that binds to the epidermal growth factor receptor (EGFR)
118. nedaplatin, a platinum-based antineoplastic that reacts with DNA, inducing non-cell cycle specific apoptosis^[120]
119. nelarabine, an adenosine-analog inhibitor of purine synthesis^{[121][122][123][124][125][126][127][128]}
120. nilotinib, a tyrosine kinase inhibitor a tyrosine kinase inhibitor of Bcr-Abl kinase
121. nilutamide, an antihormone agent
122. nivolumab, a monoclonal antibody that targets
123. obinutuzumab, a monoclonal antibody that targets CD20
124. octreotide, an octapeptide analog (short and long acting forms) of somatostatin
125. ofatumumab, a monoclonal antibody that targets CD20^{[129][130][131]}
126. olaparib, a PARP inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair
127. olaratumab, a monoclonal antibody that targets platelet-derived growth factor (PDGF) receptor-alpha
128. omacetaxine, a natural product that acts as a protein translation inhibitor
129. osimertinib, a third-generation tyrosine kinase inhibitor of T790M mutation-positive epidermal growth factor receptor (EGFR)
130. oxaliplatin, a platinum-based antineoplastic that reacts with DNA, inducing non-cell cycle specific apoptosis
131. palbociclib, a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6
132. paclitaxel, a taxane microtubule disassembly inhibitor; arrests cells in late G2 phase and M phase
133. panitumumab, a monoclonal antibody that targets EGFR
134. panobinostat, a histone deacetylase inhibitor, hence inducing alterations in gene expression
135. pazopanib, a tyrosine kinase inhibitor multikinase inhibitor of c-KIT, FGFR, PDGFR and VEGFR
136. pembrolizumab, a monoclonal antibody that targets the programmed cell death 1 (PD-1) receptor
137. pemetrexed, an antifolate inhibitor of dihydrofolate reductase, thymidylate synthase and glycinamide ribonucleotide formyltransferase^{[132][133][134][135][136][137][138][139][140][141][142][143][144][145][146][147][148][149][150][151][152][153][154][155][156]}
138. pertuzumab, a monoclonal antibody that targets HER2
139. pentostatin, an adenosine analog adenosine deaminase inhibitor^{[157][158][159][160][161][162]}
140. plicamycin, an RNA synthesis inhibitor
141. pomalidomide, a thalidomide analog immunomodulatory drug (IMiD); anti-angiogenesis (via inhibition of VEGF release), anti-TNF, IL-6 and pro-IL-2, IFN-γ effects; also stimulates T cells and apoptosis in cancer cells
142. ponatinib, a tyrosine kinase inhibitor (TKI) multikinase inhibitor of BEGFR, PDGFR, FGFR, EPH receptors and SRC families of kinases, and KIT, RET, TIE2 and FLT3), that also inhibits T135I Bcr-Abl kinase^[163][164]
143. pralatrexate, an antifolate for PTCL^[165]
144. procarbazine inhibits DNA, RNA and protein synthesis
145. radium Ra 223 dichloride, a radiopharmaceutical
146. raltitrexed, an antifolate dihydrofolate reductase and thymidylate synthase inhibitor^{[166][167][168][169][170][171][172]}
147. ramucirumab, a monoclonal antibody that targets vascular endothelial growth factor receptor 2 (VEGFR2)
148. regorafenib, a tyrosine kinase inhibitor multikinase inhibitor for RET, VEGFR1, VEGFR2, VEGFR3, KIT, PDGFR-alpha, PDGFR-beta, FGFR1, FGFR2, TIE2, DDR2, Trk2A, Eph2A, RAF-1, BRAF, BRAFV600E, SAPK2, PTK5, and Bcr-Abl^{[173][174][175][176]}
149. rituximab, a monoclonal antibody that targets CD20
150. romidepsin, a histone deacetylase inhibitor, hence inducing alterations in gene expression^[177]
151. ruxolitinib, a tyrosine kinase inhibitor of JAK1 and JAK2^{[178][179][180][181]}
152. samarium (153Sm) lexidronam, a radiopharmaceutical
153. siltuximab
154. sipuleucel-T, an immunostimulant activated blood product (APC8015)
155. sonidegib, an inhibitor of the Hedgehog signaling pathway (via smoothened antagonism)# streptozotocin, an alkylating agent nitrosourea
156. sorafenib, a tyrosine kinase inhibitor multikinase inhibitor, including VEGF and PDGF receptor kinases
157. strontium-89, a radiopharmaceutical
158. sunitinib, a tyrosine kinase inhibitor multikinase inhibitor, including VEGF and PDGF receptor kinases
159. talimogene laherparepvec, an oncolytic virus
160. tamibarotene, a retinoid which is a specific agonist for retinoic acid receptor RAR alpha/beta^{[182][183][184]}
161. tamoxifen, an antihormone agent
162. tegafur/gimeracil/oteracil
163. tegafur, fluorouracil analog thymidylate synthase inhibitor^{[185][186][187][188][189][190][191]}
164. tegafur/uracil, a first generation dihydropyrimidine dehydrogenase (DPD) inhibitory fluoropyrimidine (DIF), which combines uracil, a competitive inhibitor of DPD, with the 5-FU prodrug tegafur in a 4:1 molar ratio
165. temozolomide, an alkylating agent
166. temsirolimus, a sirolimus-analog mammalian target of rapamycin (mTOR) inhibitor
167. teniposide, a podophyllotoxin topoisomerase II inhibitor
168. thalidomide, an immunomodulatory drug (IMiD); anti-angiogenesis (via inhibition of VEGF release), anti-TNF, IL-6 and pro-IL-2, IFN-γ effects; also stimulates T cells and apoptosis in cancer cells
169. tioguanine, guanine analog Purine synthesis inhibitor^{[192][193][194][195][196]}
170. topotecan, a topoisomerase I inhibitor
171. toremifene, an antihormone agent
172. tocilizumab
173. tositumomab, a radiopharmaceutical monoclonal antibody tagged with I131 that targets CD20^[197][198]
174. trabectedin, an alkylating agent
175. trametinib, a tyrosine kinase inhibitor (TKI) of...
176. trastuzumab, a monoclonal antibody that targets HER2
177. trastuzumab emtansine (US name is ado-trastuzumab emtansine), an antibody-drug conjugate of the monoclonal antibody trastuzumab, that targets HER2, linked to emtansine (DM1), a tubulin inhibitor, that inhibits the assembly of microtubules
178. tretinoin, a retinoid RXR & RAR agonist
179. trifluridine/tipiracil combination thymidine phosphorylase inhibitor and thymidylate synthetase inhibitor
180. triptorelin, an antihormone agent
181. valproate, which among other actions is a histone deacetylase inhibitor, hence inducing alterations in gene expression;^{[Note 6][199][200][201][202]} orphan drug in fragile X syndrome and familial adenomatous polyposis
182. valrubicin, an anthracycline: inhibits DNA and RNA synthesis by intercalating DNA base pairs; inhibits DNA repair by inhibiting topoisomerase II
183. vandetanib, a tyrosine kinase inhibitor (TKI) with selective activity against RET, VEGFR-2 and EGFR^[203]
184. vemurafenib, a BRAF kinase inhibitor
185. venetoclax, a BH3-mimetic which acts as a Bcl-2 inhibitor, leading to programmed cell death
186. vinblastine, a vinca alkaloid microtubule assembly inhibitor, arrests cells in M phase
187. vincristine, a vinca alkaloid microtubule assembly inhibitor, arrests cells in M phase
188. vindesine, a vinca alkaloid microtubule assembly inhibitor, arrests cells in M phase
189. vinflunine, a vinca alkaloid microtubule assembly inhibitor, arrests cells in M phase
190. vinorelbine, a vinca alkaloid microtubule assembly inhibitor, arrests cells in M phase
191. vismodegib, a receptor antagonist of the smoothened receptor (SMO), part of the Hedgehog signaling pathway
192. vorinostat, a histone deacetylase inhibitor, hence inducing alterations in gene expression^[204]
193. ziv-aflibercept (US name, otherwise known as aflibercept), a recombinant fusion protein consisting of vascular endothelial growth factor (VEGF)-binding portions from the extracellular domains of human VEGF receptors 1 and 2, that are fused to the Fc portion of the human IgG1 immunoglobulin, which acts as a decoy inhibitor of VEGF and PGF^{[1]:1788[3][4]}

Notes

1. There is no INN for arsenic trioxide, just the USAN
2. There is no INN for asparaginase, only a USAN
3. There is no INN for BCG
4. not to be confused with an unapproved agent, cediranib, an inhibitor of vascular endothelial growth factor (VEGF) receptor
5. A liposomal formulation of irinotecan, Onivyde, is available.
6. Its use in cancer treatment is purely investigational at present

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