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.

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, or Japan.

Background

Medications

  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 linked to emtansine (DM1)
  4. afatinib, a tyrosine kinase inhibitor of EGFR, HER2 and HER4[1]
  5. aflibercept, a recombinant fusion protein inhibitor of VEGF and PGF 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[2]
  6. alectinib, an anaplastic lymphoma kinase (ALK) inhibitor
  7. alemtuzumab, a monoclonal antibody that targets CD52 # 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
  8. altretamine, an antineoplastic agent with unclear mechanism, classified by MeSH as an alkylating agent; forms reactive intermediates that covalently bind to microsomal proteins and DNA, possibly causing DNA damage
  9. 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
  10. anagrelide, a phosphodiesterase 3 inhibitor
  11. anastrozole, a non-steroidal aromatase inhibitor, which inhibits the synthesis of estrogen
  12. arsenic trioxide[Note 1]
  13. asparaginase,[Note 2] an antineoplastic agent which catalyses the conversion of the amino acid 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
  14. axitinib, a tyrosine kinase inhibitor multikinase inhibitor[3]
  15. azacitidine, a DNA methyltransferase inhibitor, incorporates itself into RNA, hence inhibiting gene expression[4][5][6][7][8][9][10][11][12][13][14]
  16. 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
  17. belinostat, a histone deacetylase inhibitor, hence inducing alterations in gene expression
  18. bendamustine, a nitrogen mustard alkylating agent
  19. bevacizumab, a monoclonal antibody that targets VEGF inhibitor
  20. bexarotene, a retinoid RXR agonist[15]
  21. bicalutamide
  22. bleomycin inhibits DNA and to a lesser extent RNA synthesis, produces single and double strand breaks in DNA possibly by free radical formation
  23. 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
  24. bortezomib, a proteasome inhibitor
  25. bosutinib, a tyrosine kinase inhibitor of Bcr-Abl and SRc family kinases (including Src, Lyn and Hck).[16][17]
  26. 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)
  27. busulfan, a dialkylsulfonate alkylating agent[18][19]
  28. cabazitaxel, a taxane microtubule disassembly inhibitor; arrests cells in late G2 phase and M phase
  29. cabozantinib, a tyrosine kinase inhibitor of c-Met and VEGFR2
  30. capecitabine, a fluorouracil-analog inhibitor of thymidylate synthase[20][21][22][23][24][25][26][27][28]
  31. carboplatin, a platinum-based antineoplastic that reacts with DNA, inducing non-cell cycle specific apoptosis
  32. carfilzomib, a proteasome inhibitor
  33. carmofur, a fluorouracil-analog inhibitor of thymidylate synthase and inhibitor of acid ceramidase (AC)
  34. carmustine, a nitrosourea alkylating agent
  35. chlorambucil, a nitrogen mustard alkylating agent[18][19]
  36. chlormethine, a nitrogen mustard alkylating agent[19]
  37. ceritinib, an anaplastic lymphoma kinase (ALK) inhibitor
  38. cetuximab, a monoclonal antibody that targets EGFR
  39. cisplatin, a platinum-based antineoplastic that reacts with DNA, inducing non-cell cycle specific apoptosis
  40. cladribine, adenosine analog DNA methyltransferaseinhibitor, metabolites incorporate themselves into DNA[29] used in multiple sclerosis[29][30][31][32][33][34][35][36][37][38]cancer:[30][39][40][41]
  41. clofarabine, a deoxyadenosine analog ribonucleotide reductase and DNA polymerase inhibitor[42][43][44][45][46][47][48][49][50][51]
  42. cobimetinib, a tyrosine kinase inhibitor [52] melanoma that expresses a BRAF V600E or V600K mutation[52]|| diarrhea, nausea, vomiting, rash, photosensitivity, pyrexia[53][53]
  43. crizotinib, a tyrosine kinase inhibitor of ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), and Recepteur d'Origine Nantais (RON)[54][55][56][57][58]
  44. cyclophosphamide, an alkylating agent nitrogen mustard[19]
  45. cyproterone
  46. cytarabine, a cytidine analog DNA polymerase inhibitor, S-phase specific; incorporates its metabolites into DNA [59][60][61]
  47. dabrafenib
  48. dacarbazine, an alkylating agent[19]
  49. dactinomycin complexes with DNA interfering with DNA-dependent RNA synthesis
  50. daratumumab, a monoclonal antibody inhibitor that targets CD38
  51. daunorubicin, an anthracycline: inhibits DNA and RNA synthesis by intercalating DNA base pairs; inhibits DNA repair by inhibiting topoisomerase II
  52. dasatinib, a tyrosine kinase inhibitor of BCR-ABL, SRC family, c-Kit, EPHA2 and PDGFR-β kinase
  53. decitabine, a DNA methyltransferase inhibitor [5][6][62][63][64][65][66][67][68][69][70]
  54. degarelix
  55. 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[71][72][73][74]
  56. dinutuximab, a monoclonal antibody that targets glycolipid GD2[75]
  57. docetaxel, a taxane microtubule disassembly inhibitor; arrests cells in late G2 phase and M phase
  58. doxorubicin, an anthracycline: inhibits DNA and RNA synthesis by intercalating DNA base pairs; inhibits DNA repair by inhibiting topoisomerase II
  59. elotuzumab antiSLAMF7 (CD319)
  60. enzalutamide (androgen receptor (AR) antagonist and also signaling inhibitor[76])
  61. epirubicin, an anthracycline: inhibits DNA and RNA synthesis by intercalating DNA base pairs; inhibits DNA repair by inhibiting topoisomerase II
  62. etoposide, a podophyllotoxin topoisomerase II inhibitor
  63. eribulin
  64. erlotiniba tyrosine kinase inhibitor of EGFR
  65. estramustine, a nitrogen mustard and estrogen analog
  66. everolimus, a sirolimus-analog mammalian target of rapamycin (mTOR) inhibitor
  67. exemestane
  68. floxuridine, a fluorouracil analog thymidylate synthase inhibitor[77]
  69. fludarabine, an adenosine analog DNA polymerase and ribonucleotide reductase inhibitor[78][79][80][80][81][82][83]
  70. fluorouracil, uracil analog thymidylate synthase inhibitor[84][85][86]
  71. fluoxymesterone
  72. flutamide
  73. fotemustine, a nitrosourea alkylating agent
  74. 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
  75. gefitinib, a tyrosine kinase inhibitor of EGFR
  76. gemcitabine, deoxycytidine analog DNA synthesis inhibitor, induces apoptosis specifically in S-phase[87][88][89][90][91][92]
  77. gemtuzumab ozogamicin, a monoclonal antibody antibody-drug conjugate that targets CD33[93]
  78. goserelin
  79. histrelin
  80. hydroxycarbamide Inhibits DNA synthesis by inhibiting the enzyme ribonucleotide reductase[94][95][96][97][98][99][100][101][102][103]
  81. ibritumomab tiuxetan, a monoclonal antibody radioimmunotherapy which binds to the CD20 antigen
  82. ibrutinib, a Bruton's tyrosine kinase (BTK) inhibitor * ibritumomab tiuxetan, a CD20 antibody bound with the radioactive isotope, 90Y, induces radiation-dependent cell lysis [104][105]
  83. idarubicin, an anthracycline inhibitor of DNA and RNA synthesis, which intercalates DNA base pairs; inhibits DNA repair by inhibiting topoisomerase II
  84. idelalisib, a phosphoinositide 3-kinase inhibitor of P110δ, the delta isoform of the enzyme phosphoinositide 3-kinase
  85. ifosfamide, a nitrogen mustard alkylating agent[19]
  86. imatinib, a tyrosine kinase inhibitor (TKI) of Bcr-Abl kinase, and...
  87. imiquimod, an immune response modifier which signals to the innate arm of the immune system through the toll-like receptor 7 (TLR7)
  88. interferon (Interferon alfa-2b and also Peginterferon alfa-2b)
  89. iobenguane, a monoclonal antibody radioimmunotherapy; the iodine-131 variant is used for tissue destruction
  90. ipilimumab, a monoclonal antibody that targets CTLA4
  91. irinotecan, a topoisomerase I inhibitor[Note 4]
  92. isotretinoin retinoid|| RXR & RAR agonist || neuroblastoma[106][107][108]
  93. ixabepilone, an epothilone B analog promotes tubulin polymerisation and stabilises microtubular function, causing cell cycle arrest at G2/M phase and subsequently induces apoptosis
  94. ixazomib, a proteasome inhibitor; reversibly inhibits the protein proteasome subunit beta type-5 (PSMB5), which is part of the 20S proteasome complex
  95. lanreotide, a long-acting analogue of somatostatin
  96. lapatinib, a tyrosine kinase inhibitor of HER2
  97. 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
  98. lentinan, an anti-tumor polysaccharide
  99. lenvatinib, a tyrosine kinase inhibitor (TKI) of...
  100. letrozole, an antihormone non-steroidal aromatase inhibitor, thus inhibiting the synthesis of estrogen
  101. leuprolide
  102. lomustine, a nitrosourea alkylating agent[19]
  103. melphalan, a nitrogen mustard alkylating agent[19]
  104. methotrexate, an antifolate dihydrofolate reductase inhibitor[109][110][111][112][113][114]
  105. mercaptopurine, a hypoxanthine-analog inhibitor of purine synthesis[115][116][117]
  106. mifepristone
  107. mitomycin cross-links DNA
  108. mitotane, an isomer of DDD and a derivative of DDT, which alters steroid peripheral metabolism, directly suppresses the adrenal cortex
  109. mitoxantrone, an anthracycline: inhibits DNA and RNA synthesis by intercalating DNA base pairs; inhibits DNA repair by inhibiting topoisomerase II
  110. nab-paclitaxel, a taxane microtubule disassembly inhibitor; arrests cells in late G2 phase and M phase
  111. necitumumab, a recombinant human IgG1 monoclonal antibody that binds to the epidermal growth factor receptor (EGFR)
  112. nedaplatin, a platinum-based antineoplastic that reacts with DNA, inducing non-cell cycle specific apoptosis[118]
  113. nelarabine, an adenosine-analog inhibitor of purine synthesis [119][120][121][122][123][124][125][126]
  114. nilotinib, a tyrosine kinase inhibitor a tyrosine kinase inhibitor of Bcr-Abl kinase
  115. nilutamide, an antihormone agent
  116. nivolumab, a monoclonal antibody that targets
  117. obinutuzumab, a monoclonal antibody that targets CD20
  118. octreotide, an octapeptide analog (short and long acting forms) of somatostatin
  119. ofatumumab, a monoclonal antibody that targets CD20[127][128][129]
  120. olaparib, a PARP inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair
  121. omacetaxine, a natural product that acts as a protein translation inhibitor
  122. osimertinib, a third-generation tyrosine kinase inhibitor of T790M mutation-positive epidermal growth factor receptor (EGFR)
  123. oxaliplatin, a platinum-based antineoplastic that reacts with DNA, inducing non-cell cycle specific apoptosis
  124. palbociclib, a selective inhibitor of the cyclin-dependent kinases CDK4 and CDK6
  125. paclitaxel, a taxane microtubule disassembly inhibitor; arrests cells in late G2 phase and M phase
  126. panitumumab, a monoclonal antibody that targets EGFR
  127. panobinostat, a histone deacetylase inhibitor, hence inducing alterations in gene expression
  128. pazopanib, a tyrosine kinase inhibitor multikinase inhibitor of c-KIT, FGFR, PDGFR and VEGFR
  129. pembrolizumab, a monoclonal antibody that targets the programmed cell death 1 (PD-1) receptor
  130. pemetrexed, an antifolate inhibitor of dihydrofolate reductase, thymidylate synthase and glycinamide ribonucleotide formyltransferase[130][131][132][133][134][135][136][137][138][139][140][141][142][143][144][145][146][147][148][149][150][151][152][153][154]
  131. pertuzumab, a monoclonal antibody that targets HER2
  132. pentostatin, an adenosine analog adenosine deaminase inhibitor[155][156][157][158][159][160]
  133. plicamycin, an RNA synthesis inhibitor
  134. 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
  135. 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[161][162]
  136. pralatrexate, an antifolate for PTCL[163]
  137. procarbazine inhibits DNA, RNA and protein synthesis
  138. radium Ra 223 dichloride, a radiopharmaceutical
  139. raltitrexed, an antifolate dihydrofolate reductase and thymidylate synthase inhibitor[164][165][166][167][168][169][170]
  140. ramucirumab, a monoclonal antibody that targets vascular endothelial growth factor receptor 2 (VEGFR2)
  141. 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[171][172][173][174]
  142. rituximab, a monoclonal antibody that targets CD20
  143. romidepsin, a histone deacetylase inhibitor, hence inducing alterations in gene expression[175]
  144. ruxolitinib, a tyrosine kinase inhibitor of JAK1 and JAK2[176][177][178][179]
  145. samarium (153Sm) lexidronam, a radiopharmaceutical
  146. sipuleucel-T, an immunostimulant activated blood product (APC8015)
  147. sonidegib, an inhibitor of the Hedgehog signaling pathway (via smoothened antagonism)# streptozotocin, an alkylating agent nitrosourea
  148. sorafenib, a tyrosine kinase inhibitor multikinase inhibitor, including VEGF and PDGF receptor kinases
  149. strontium-89, a radiopharmaceutical
  150. sunitinib, a tyrosine kinase inhibitor multikinase inhibitor, including VEGF and PDGF receptor kinases
  151. talimogene laherparepvec, an oncolytic virus
  152. tamibarotene, a retinoid which is a specific agonist for retinoic acid receptor RAR alpha/beta[180][181][182]
  153. tamoxifen, an antihormone agent
  154. tegafur/gimeracil/oteracil
  155. tegafur, fluorouracil analog thymidylate synthase inhibitor[183][184][185][186][187][188][189]
  156. 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
  157. temozolomide, an alkylating agent
  158. temsirolimus, a sirolimus-analog mammalian target of rapamycin (mTOR) inhibitor
  159. teniposide, a podophyllotoxin topoisomerase II inhibitor
  160. 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
  161. tioguanine, guanine analog Purine synthesis inhibitor[190][191][192][193][194]
  162. topotecan, a topoisomerase I inhibitor
  163. toremifene, an antihormone agent
  164. tositumomab, a radiopharmaceutical monoclonal antibody tagged with I131 that targets CD20[195][196]
  165. trabectedin, an alkylating agent
  166. trametinib, a tyrosine kinase inhibitor (TKI) of...
  167. trastuzumab, a monoclonal antibody that targets HER2
  168. trastuzumab emtansine (US name is ado-trastuzumab emtansine), an antibody-drug conjugate of the monoclonal antibody trastuzumab, which targets HER2, linked to emtansine (DM1)
  169. tretinoin, a retinoid RXR & RAR agonist
  170. trifluridine/tipiracil combination thymidine phosphorylase inhibitor and thymidylate synthetase inhibitor
  171. triptorelin, an antihormone agent
  172. valproate, which among other actions is a histone deacetylase inhibitor, hence inducing alterations in gene expression;[Note 5][197][198][199][200] orphan drug in fragile X syndrome and familial adenomatous polyposis
  173. valrubicin, an anthracycline: inhibits DNA and RNA synthesis by intercalating DNA base pairs; inhibits DNA repair by inhibiting topoisomerase II
  174. vandetanib, a tyrosine kinase inhibitor (TKI) with selective activity against RET, VEGFR-2 and EGFR[201]
  175. vemurafenib, a BRAF kinase inhibitor
  176. venetoclax, a BH3-mimetic which acts as a Bcl-2 inhibitor, leading to programmed cell death
  177. vinblastine, a vinca alkaloid microtubule assembly inhibitor, arrests cells in M phase
  178. vincristine, a vinca alkaloid microtubule assembly inhibitor, arrests cells in M phase
  179. vindesine, a vinca alkaloid microtubule assembly inhibitor, arrests cells in M phase
  180. vinflunine, a vinca alkaloid microtubule assembly inhibitor, arrests cells in M phase
  181. vinorelbine, a vinca alkaloid microtubule assembly inhibitor, arrests cells in M phase
  182. vismodegib
  183. vorinostat, a histone deacetylase inhibitor, hence inducing alterations in gene expression[202]

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. ↑ A liposomal formulation of irinotecan, Onivyde, is available.
  5. ↑ Its use in cancer treatment is purely investigational at present

References

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