List of antineoplastic agents

This article is an alphabetic list of agents used to treat cancer. For overview material on chemotherapy, see Chemotherapy. For multiagent antineoplastic protocols, see Chemotherapy regimen. For therapeutic subgroup information for these agents, see ATC code L01. For antineoplastic brand names, see List of antineoplastic agent brand names (in process)

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

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

References

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  15. ↑ Vigil CE, Martin-Santos T, Garcia-Manero G (24 September 2010). "Safety and efficacy of azacitidine in myelodysplastic syndromes". Drug Design, Development and Therapy. 4: 221–9. doi:10.2147/DDDT.S3143. PMC 2948932Freely accessible. PMID 20957213.
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  18. ↑ "Bosulif (bosutinib) dosing, indications, interactions, adverse effects, and more". Medscape Reference. WebMD. Retrieved 9 February 2014.
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