From: A systematic analysis of FDA-approved anticancer drugs
Drug | Approval year | Therapeutic class | Target gene | Delivery type |
---|---|---|---|---|
Cytotoxic | ||||
 Mechlorethamine | 1949 | Lung cancer; Leukemia; Lymphoma | DNA synthesis | Single |
 Leucovorin | 1952 | Colorectal cancer; Bone cancer | TYMS | Both |
 Methotrexate | 1953 | Leukemia; Breast cancer; Head and neck cancer; Lung cancer; Lymphoma; Bone cancer; Gestational trophoblastic disease | DHFR | Both |
 Mercaptopurine | 1953 | Leukemia | HPRT1 | Combination |
 Busulfan | 1954 | Leukemia | DNA synthesis | Combination |
 Chlorambucil | 1957 | Leukemia; Lymphoma | DNA synthesis | Single |
 Cyclophosphamide | 1959 | Lymphoma; Multiple myeloma; Leukemia; Brain cancer; Ovarian cancer; Retinoblastoma; Breast cancer | DNA synthesis | Both |
 Vincristine sulfate | 1963 | Leukemia | TUBA4A; TUBB | Single |
 Dactinomycin | 1964 | Sarcoma; Gestational trophoblastic disease; Testicular cancer; Kidney cancer | RNA synthesis | Both |
 Vinblastine sulfate | 1965 | Lymphoma; Testicular cancer; Choriocarcinoma; Breast cancer | TUBA1A; TUBB; TUBD1; TUBE1; TUBG1 | Combination |
 Thioguanine | 1966 | Leukemia | DNA synthesis | Combination |
 Procarbazine hydrochloride | 1969 | Lymphoma | DNA synthesis | Combination |
 Floxuridine | 1970 | Stomach cancer | DNA synthesis | Single |
 Fluorouracil | 1970 | Breast cancer; Colorectal cancer; Stomach cancer; Pancreatic cancer | DNA synthesis | Single |
 Mitotane | 1970 | Adrenal cortical carcinoma | Unknown | Single |
 Bleomycin | 1973 | Head and neck cancer; Lymphoma; Penile cancer; Cervical cancer; Vulvar cancer; Testicular cancer | DNA synthesis | Both |
 Doxorubicin hydrochloride | 1974 | Leukemia; Breast cancer; Stomach cancer; Lymphoma; Ovarian cancer; Lung cancer; Sarcoma; Thyroid cancer; Bladder cancer; Kidney cancer; Brain cancer | TOP2A; DNA synthesis | Single |
 Dacarbazine | 1975 | Melanoma; Lymphoma | DNA synthesis | Both |
 Lomustine | 1976 | Brain cancer; Lymphoma | DNA synthesis | Both |
 Carmustine | 1977 | Brain cancer; Lymphoma; Multiple myeloma | DNA synthesis | Both |
 Cisplatin | 1978 | Testicular cancer; Ovarian cancer; Bladder cancer | DNA synthesis | Both |
 Asparaginase | 1978 | Leukemia | Unknown | Combination |
 Streptozocin | 1982 | Pancreatic cancer | DNA synthesis; SLC2A2 | Single |
 Etoposide | 1983 | Testicular cancer; Lung cancer | TOP2A; TOP2B | Combination |
 Ifosfamide | 1988 | Testicular cancer | DNA synthesis | Combination |
 Carboplatin | 1989 | Ovarian cancer | DNA synthesis | Both |
 Altretamine | 1990 | Ovarian cancer | DNA synthesis | Single |
 Fludarabine | 1991 | Leukemia | DNA synthesis | Single |
 Pentostatin | 1991 | Leukemia | ADA | Single |
 Paclitaxel | 1992 | Breast cancer; Lung cancer; Pancreatic cancer; Ovarian cancer; Sarcoma | TUBA4A; TUBB1 | Both |
 Melphalan | 1992 | Multiple myeloma; Ovarian cancer | DNA synthesis | Combination |
 Teniposide | 1992 | Leukemia | TOP2A | Combination |
 Cladribine | 1993 | Leukemia | DNA synthesis | Single |
 Vinorelbine tartrate | 1994 | Lung cancer | TUBB | Both |
 Pegaspargase | 1994 | Leukemia | Biological | Combination |
 Thiotepa | 1994 | Breast cancer; Ovarian cancer; Bladder cancer | DNA synthesis | Single |
 Docetaxel | 1996 | Prostate cancer; Breast cancer; Head and neck cancer; Stomach cancer; Lung cancer; Brain cancer | TUBA4A; TUBB1 | Both |
 Gemcitabine | 1996 | Ovarian cancer; Pancreatic cancer; Lung cancer; Breast cancer | DNA synthesis; RRM1; TYMS | Both |
 Irinotecan | 1996 | Colorectal cancer | TOP1; TOP1MT | Both |
 Topotecan hydrochloride | 1996 | Ovarian cancer; Lung cancer; Cervical cancer | TOP1; TOP1MT | Both |
 Idarubicin | 1997 | Leukemia | DNA synthesis; TOP2A | Combination |
 Capecitabine | 1998 | Colorectal cancer; Breast cancer | DNA synthesis; RNA synthesis; Protein synthesis; TYMS | Both |
 Daunorubicin hydrochloride | 1998 | Leukemia | DNA synthesis; TOP2A; TOP2B | Combination |
 Valrubicin | 1998 | Bladder cancer | DNA synthesis; TOP2A | Single |
 Temozolomide | 1999 | Brain cancer | DNA synthesis | Both |
 Cytarabine | 1999 | Leukemia | DNA synthesis | Single |
 Epirubicin | 1999 | Breast cancer | CHD1; DNA synthesis; TOP2A | Single |
 Arsenic trioxide | 2000 | Leukemia | Unknown | Single |
 Mitomycin | 2002 | Stomach cancer; Pancreatic cancer | DNA synthesis | Both |
 Oxaliplatin | 2002 | Colorectal cancer | DNA synthesis | Combination |
 Pemetrexed disodium | 2004 | Lung cancer; Mesothelioma | DHFR; GART; TYMS | Both |
 Clofarabine | 2004 | Leukemia | DNA synthesis | Single |
 Nelarabine | 2005 | Leukemia; Lymphoma | DNA synthesis | Single |
 Ixabepilone | 2007 | Breast cancer | TUBB3 | Both |
 Bendamustine hydrochloride | 2008 | Leukemia; Lymphoma | DNA synthesis | Single |
 Pralatrexate | 2009 | Lymphoma | DHFR; TYMS | Single |
 Cabazitaxel | 2010 | Prostate cancer | TUBA4A; TUBB1 | Combination |
 Eribulin mesylate | 2010 | Breast cancer | TUBA4A; TUBB1 | Single |
 Asparaginase erwinia chrysanthemi | 2011 | Leukemia | Biological | Combination |
 Omacetaxine mepesuccinate | 2012 | Leukemia | RPL3 | Single |
 Radium 223 dichloride | 2013 | Prostate cancer | Unknown | Single |
Targeted | ||||
 Fluoxymesterone | 1956 | Breast cancer | AR; ESR1; NR3C1; PRLR | Single |
 Methyltestosterone | 1973 | Breast cancer | AR | Single |
 Tamoxifen citrate | 1977 | Breast cancer | ESR1; ESR2 | Single |
 Estramustine | 1981 | Prostate cancer | ESR1; ESR2; MAP1A; MAP2 | Single |
 Interferon Alfa-2b, recombinant | 1986 | Sarcoma; Leukemia; Melanoma; Lymphoma | IFNAR1; IFNAR2 | Single |
 Goserelin | 1989 | Prostate cancer; Breast cancer | GNRHR; LHCGR | Both |
 Flutamide | 1989 | Prostate cancer | AR | Combination |
 Aldesleukin | 1992 | Melanoma; Kidney cancer | IL2RA; IL2RB; IL2RG | Single |
 Bicalutamide | 1995 | Prostate cancer | AR | Combination |
 Anastrozole | 1995 | Breast cancer | CYP19A1 | Single |
 Porfimer | 1995 | Esophageal cancer; Lung cancer | FCGR1A; LDLR | Single |
 Nilutamide | 1996 | Prostate cancer | AR | Combination |
 Imiquimod | 1997 | Basal cell carcinoma | TLR7; TLR8 | Single |
 Letrozole | 1997 | Breast cancer | CYP19A1 | Single |
 Rituximab | 1997 | Lymphoma; Leukemia | MS4A1 | Single |
 Toremifene | 1997 | Breast cancer | ESR1 | Single |
 Thalidomide | 1998 | Multiple myeloma | CRBN | Combination |
 Trastuzumab | 1998 | Breast cancer; Stomach cancer | ERBB2 | Single |
 Alitretinoin | 1999 | Kaposi’s sarcoma | RARA; RARB; RARG; RXRA; RXRB; RXRG | Single |
 Bexarotene | 1999 | Lymphoma | RXRA; RXRB; RXRG | Single |
 Denileukin diftitox | 1999 | Lymphoma | IL2RA; IL2RB; IL2RG; protein synthesis | Single |
 Exemestane | 1999 | Breast cancer | CYP19A1 | Single |
 Gemtuzumab ozogamicin | 2000 | Leukemia | CD33; DNA synthesis | Single |
 Triptorelin | 2000 | Prostate cancer | GNRH1 | Single |
 Alemtuzumab | 2001 | Leukemia | CD52 | Single |
 Imatinib mesylate | 2001 | Leukemia; Stomach cancer | BCR-ABL | Single |
 Peginterferon Alfa-2b | 2001 | Melanoma | IFNAR1; IFNAR2 | Single |
 Fulvestrant | 2002 | Breast cancer | ESR1 | Single |
 Ibritumomab tiuxetan | 2002 | Lymphoma | MS4A1 | Single |
 Leuprolide acetate | 2002 | Prostate cancer | GNRHR | Single |
 Abarelix | 2003 | Prostate cancer | GNRHR | Single |
 Bortezomib | 2003 | Multiple myeloma; Lymphoma | PSMB1; PSMB2; PSMB5; PSMD1; PSMD2 | Single |
 Gefitinib | 2003 | Lung cancer | EGFR | Single |
 Tositumomab and Iodine I 131 Tositumomab | 2003 | Lymphoma | MS4A1 | Single |
 Bevacizumab | 2004 | Colorectal cancer; Lung cancer; Brain cancer; Kidney cancer | VEGFA | Both |
 Cetuximab | 2004 | Head and neck cancer; Colorectal cancer | EGFR | Both |
 Erlotinib hydrochloride | 2004 | Pancreatic cancer; Lung cancer | EGFR | Both |
 Azacitidine | 2004 | Leukemia | DNMT1 | Single |
 Lenalidomide | 2005 | Multiple myeloma; Lymphoma | CRBN | Both |
 Sorafenib tosylate | 2005 | Liver cancer; Kidney cancer; Thyroid cancer | BRAF; FGFR1; FLT1; FLT3; FLT4; KDR; KIT; PDGFRB; RAF1; RET | Single |
 Dasatinib | 2006 | Leukemia | BCR-ABL | Single |
 Decitabine | 2006 | Leukemia | DNMT1 | Single |
 Panitumumab | 2006 | Colorectal cancer | EGFR | Single |
 Sunitinib malate | 2006 | Stomach cancer; Kidney cancer; Pancreatic cancer | CSF1R; FLT1; FLT3; FLT4; KDR; KIT; PDGFRA; PDGFRB | Single |
 Vorinostat | 2006 | Lymphoma | HDAC1; HDAC2; HDAC3; HDAC6 | Single |
 Lapatinib ditosylate | 2007 | Breast cancer | EGFR; ERBB2 | Combination |
 Nilotinib | 2007 | Leukemia | BCR-ABL | Single |
 Temsirolimus | 2007 | Kidney cancer | MTOR | Single |
 Degarelix | 2008 | Prostate cancer | GNRHR | Single |
 Everolimus | 2009 | Breast cancer; Brain cancer; Kidney cancer; Pancreatic cancer | MTOR | Both |
 Ofatumumab | 2009 | Leukemia | MS4A1 | Single |
 Pazopanib hydrochloride | 2009 | Kidney cancer; Sarcoma | FGF1; FGFR3; FLT1; FLT4; ITK; KDR; KIT; PDGFRA; PDGFRB; SH2B3 | Single |
 Romidepsin | 2009 | Lymphoma | HDAC1; HDAC2; HDAC3; HDAC6 | Single |
 Denosumab | 2010 | Bone cancer | TNFSF11 | Single |
 Hydroxyurea | 2010 | Melanoma; Leukemia; Ovarian cancer; Head and neck cancer | RRM1 | Single |
 Sipuleucel-T | 2010 | Prostate cancer | ACPP | Single |
 Abiraterone acetate | 2011 | Prostate cancer | CYP17A1 | Single |
 Brentuximab vedotin | 2011 | Lymphoma | TNFRSF8 | Single |
 Crizotinib | 2011 | Lung cancer | ALK; MET | Single |
 Ipilimumab | 2011 | Melanoma | CTLA4 | Single |
 Ruxolitinib phosphate | 2011 | Myelofibrosis | JAK1; JAK2 | Single |
 Vandetanib | 2011 | Thyroid cancer | EGFR; PTK6; TEK; VEGFA | Single |
 Vemurafenib | 2011 | Melanoma | BRAF | Single |
 Pertuzumab | 2012 | Breast cancer | ERBB2 | Both |
 Axitinib | 2012 | Kidney cancer | FLT1; FLT4; KDR | Single |
 Bosutinib | 2012 | Leukemia | BCR-ABL | Single |
 Cabozantinib | 2012 | Thyroid cancer | KDR; MET; RET | Single |
 Carfilzomib | 2012 | Multiple myeloma | PSMB1; PSMB10; PSMB2; PSMB5; PSMB8; PSMB9 | Single |
 Enzalutamide | 2012 | Prostate cancer | AR | Single |
 Ponatinib hydrochloride | 2012 | Leukemia | BCR-ABL | Single |
 Regorafenib | 2012 | Colorectal cancer; Stomach cancer | RET; FLT1; KDR; FLT4; KIT; PDGFRA; PDGFRB; FGFR1; FGFR2; TEK; DDR2; NTRK1; EPHA2; RAF1; BRAF; MAPK11; FRK; ABL1 | Single |
 Vismodegib | 2012 | Basal cell carcinoma | SMO | Single |
 Ziv-aflibercept | 2012 | Colorectal cancer | PGF; VEGFA; VEGFB | Single |
 Dabrafenib | 2013 | Melanoma | BRAF; LIMK1; NEK11; RAF1; SIK1 | Both |
 Trametinib | 2013 | Melanoma | MAP2K1; MAP2K2 | Both |
 Obinutuzumab | 2013 | Leukemia | MS4A1 | Combination |
 Ado-trastuzumab emtansine | 2013 | Breast cancer | ERBB2 | Single |
 Afatinib | 2013 | Lung cancer | EGFR; ERBB2; ERBB4 | Single |
 Ibrutinib | 2013 | Lymphoma | BTK | Single |
 Pomalidomide | 2013 | Multiple myeloma | CRBN | Single |
 Idelalisib | 2014 | Leukemia; Lymphoma | PIK3CD | Both |
 Belinostat | 2014 | Lymphoma | HDAC1; HDAC2; HDAC3; HDAC6 | Single |
 Ceritinib | 2014 | Lung cancer | ALK | Single |
 Pembrolizumab | 2014 | Melanoma | PDCD1 | Single |
 Ramucirumab | 2014 | Stomach cancer | KDR | Single |
 Lanreotide | 2014 | Gastroenteropancreatic neuroendocrine tumor | SSTR2; SSTR5 | Single |
 Blinatumomab | 2014 | Leukemia | CD19; CD3D | Single |
 Nivolumab | 2014 | Melanoma | PDCD1 | Single |
 Olaparib | 2014 | Ovarian cancer | PARP1; PARP2; PARP3 | Single |