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Table 1 Summary of FDA-approved anticancer drugs from 1949 to 2014

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