List of antineoplastic agents

This article is a list of agents used to treat cancer. For overview material on chemotherapy, see Chemotherapy. For multiagent antineoplastic protocols, see Chemotherapy regimen.

This is a 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. Information herein may point to potential applications beyond the approved labeled use. In practice, some agents are used in combination chemotherapy regimens.

Additional agents that are used in oncology but which are not included here include antiemetics, hematopoietic growth factors and plerixafor, immunosuppressants (post-BMT), bone resorption modifiers, and toxicity modifiers (dexrazoxane, methylene blue, amifostine, rasburicase, palifermin, glucarpidase).

Overview

Within the tabulation sections below, each medication in the following sections is summarized with the following information.

Antineoplastic agents
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]

Abbreviations and acronyms

IA – Intra-arterial
IB – Intrabladder
IM – Intramuscular
IP – Intrapleural
IV – Intravenous
PO – Per os, oral
SC – Subcutaneous

Pregnancy category

The traditionally proferred pregnancy category here has been Australian (Au), but if it was unavailable the pregnancy category was given as American (US). The tables are being updated and will convert to FDA categories. Updated entries are marked with date of update.

Incomplete tables

Cytotoxic antineoplastics

Nucleoside analogs

nucleoside analogs
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
azacitidine [6][7][8][9]
[10][11][12]
[13][14][15] 		cytidine analog D (US December 2015) SC, IV DNA methyltransferase inhibitor and incorporates itself into RNA, hence inhibiting gene expression[16] myelodysplastic syndromes, acute myeloid leukemia, chronic myeloid leukemia myelosuppression, kidney failure (uncommon/rare), renal tubular acidosis, hypokalemia
capecitabine [17][18][19]
[20][21][22]
[23][24][25] 		uracil analog D (Au) PO fluorouracil prodrug breast, colorectal, gastric and esophageal cancer myelosuppression, cardiotoxicity, hypertriglyceridemia, GI hemorrhage (uncommon), cerebellar syndrome (uncommon), encephalopathy (uncommon), diarrhea
carmofur N/A uracil analog N/A PO fluorouracil prodrug colorectal, breast cancer, ovarian cancermyelosuppression, neurotoxicity, diarrhea
cladribine multiple sclerosis:
[26][27][28]
[29][30][31]
[32][33][34]
[35]
cancer:
[27][36][37]
[38] 		adenosine analog D (Au) PO, SC, IV DNA methyltransferaseinhibitor, metabolites incorporate themselves into DNA[34] hairy cell leukemia, chronic lymphocytic leukemia, Waldenstrom macroglobulinemia, multiple sclerosis myelosuppression, hemolytic anemia (uncommon), neurotoxicity (rare), renal impairment (rare), pulmonary interstitial infiltrates (rare), Stevens-Johnson syndrome (rare), toxic epidermal necrolysis (rare)
clofarabine [39][40][41]
[42][43][44]
[45][46][47] 		deoxyadenosine analog D (Au) IV ribonucleotide reductase and DNA polymerase inhibitor[48] acute lymphoblastic leukemia, acute myeloid leukemia myelosuppression, hypokalemia, cytokine release syndrome, Stevens-Johnson syndrome(uncommon), toxic epidermal necrolysis (uncommon), pancreatitis (uncommon)
cytarabine [49][50][51] cytidine analog D (Au) SC, IM, IV, IT DNA polymerase inhibitor, S-phase specific; incorporates its metabolites into DNA acute myeloid leukemia, acute lymphoblastic leukemia, chronic myeloid leukemia, lymphomas, progressive multifocal leucoencephalopathy and meningeal leukemia myelosuppression, GI bleeds, pancreatitis (uncommon/rare), anaphylaxis (uncommon/rare), pericarditis (uncommon/rare) and conjunctivitis (uncommon/rare). High dose: cerebral and cerebellar dysfunction, ocular toxicity, pulmonary toxicity, severe GI ulceration and peripheral neuropathy (rare)
decitabine [6][7][52]
[53][54][55]
[56][57][58]
[59][60]		cytidine analog D (US) IV DNA methyltransferase inhibitor myelodysplastic syndrome, sickle cell anemia (orphan), acute myeloid leukaemia and chronic myeloid leukemia myelosuppression, hyperglycemia, hypoalbuminemia, hypomagnesemia, hypokalemia, hyperkalemia, thrombocythemia
floxuridine [61] uracil analog D (US) IA fluorouracil analog metastatic GI adenocarcinoma, stomach cancer myelosuppression
fludarabine [62][63][64]
[64][65][66]
[67] 		adenosine analog D (Au) PO, IV DNA polymerase and ribonucleotide reductase inhibitor acute myeloid leukemia, chronic lymphocytic leukemia, non-Hodgkin lymphoma, Waldenstrom macroglobulinemia myelosuppression, hyperglycemia, GI bleeds (uncommon), pneumonitis (uncommon), hemolytic anemia (uncommon), severe neurotoxicity (rare), hemorrhagic cystitis (rare), Stevens-Johnson syndrome (rare), toxic epidermal necrolysis (rare)
fluorouracil [68][69][70] uracil analog D (Au) IV thymidylate synthase inhibitor anal cancer, breast cancer, colorectal cancer, gastric cancer, head and neck cancer, esophageal cancer, pancreatic cancer, Bowen's disease, actinic keratoses myelosuppression, diarrhea, cardiotoxicity, GI ulceration and bleeding (uncommon), cerebellar syndrome (uncommon), encephalopathy (uncommon), anaphylaxis (rare)
gemcitabine [71][72][73]
[74][75][76]
[77] 		deoxycytidine analog D (Au) IV DNA synthesis inhibitor, induces apoptosis specifically in S-phase bladder cancer, breast cancer, nasopharyngeal cancer, non-small cell lung cancer, ovarian cancer, pancreatic cancer, lymphomas, inflammatory bowel disease myelosuppression, pulmonary toxicity, kidney failure (rare), hemolytic uremic syndrome(rare), thrombotic thrombocytopenic purpura (rare), anaphylactoid reaction (rare), reversible posterior leucoencephalopathy syndrome (rare), myocardial infarction (rare), heart failure (rare)
mercaptopurine [78][79] hypoxanthine analog D (Au) PO purine synthesis inhibitor acute lymphoblastic leukemia, acute promyelocytic leukemia, lymphoblastic lymphoma, inflammatory bowel disease[80] myelosuppression, hepatotoxicity, GI ulceration (rare), pancreatitis (rare), secondary leukemia (rare) or myelodysplasia (rare)
nelarabine[81][82][83]
[84][85][86]
[87][88] 		adenosine analog D (US) IV purine synthesis inhibitor acute lymphoblastic leukemia, chronic lymphocytic leukemia myelosuppression, pleural effusion, seizures, tumor lysis syndrome, a condition similar to Guillain-Barré syndrome
pentostatin [89][90][91]
[92][93][94] 		adenosine analog D (US) IV adenosine deaminase inhibitor. hairy cell leukemia, peripheral T-cell lymphoma (orphan), cutaneous T cell lymphoma (orphan), chronic lymphocytic leukemia (orphan) myelosuppression, neurotoxicity, immune hypersensitivity, hyponatremia, thrombotic thrombocytopenic purpura, microangiopathic hemolytic anemia
tegafur [95][96][97]
[98][99][100]
[101] 		fluorouracil analog D (Au) PO thymidylate synthase inhibitor breast, colorectal cancer, gallbladder, gastrointestinal tract, head and neck, liver and pancreas cancer myelosuppression, diarrhea, neurotoxicity and hepatitis (rare)
tioguanine [102][103][104]
[105][106] 		guanine analog D (Au) PO Purine synthesis inhibitor acute lymphoblastic leukemia, acute myeloid leukemia myelosuppression, hepatotoxicity, peripheral neuropathy (uncommon), intestinal necrosis (rare) and perforation (rare)
trifluridine/tipiracil add add PO combination thymidine phosphorylase inhibitor and thymidylate synthetase inhibitor colorectal cancer add

Antifolates

antifolates
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
methotrexate [107][108][109][110][111][112] folate analog D (Au) SC, IM, IV, IT, PO dihydrofolate reductase inhibitor bladder, breast cancer, squamous cell carcinoma of head and neck, gestational trophoblastic disease, acute leukemias, non-Hodgkin lymphoma, osteosarcoma, brain tumors, graft-versus-host disease, systemic sclerosis myelosuppression, pulmonary toxicity, hepatotoxicity, neurotoxicity (high dose or intrathecal administration), anaphylactic reactions (rare), Stevens-Johnson syndrome (rare), toxic epidermal necrolysis (rare), kidney failure (rare), osteoporosis (rare), skin and bone necrosis (rare), macrocytic anemia (rare)
pemetrexed [113][114][115][116][117][118]
[119][120][121][122][123][124]
[125][126][127][128][129][130]
[131][132][133][134][135][136]
[137] 		folate analog D (Au) IV inhibitor of dihydrofolate reductase, thymidylate synthase and glycinamide ribonucleotide formyltransferase malignant mesothelioma, non-squamous non-small cell lung cancer myelosuppression, renal impairment, peripheral neuropathy, supraventricular tachycardia (uncommon), hepatitis (rare), colitis (rare), pneumonitis (rare), radiation recall (rare), Stevens-Johnson syndrome (rare), toxic epidermal necrolysis (rare)
pralatrexate folate analog IV relapsed or refractory peripheral T-cell lymphoma, or PTCL[138]
raltitrexed [139][140][141][142][143][144]
[145] 		quinazolinone D (Au) IV dihydrofolate reductase and thymidylate synthase inhibitor colorectal cancer myelosuppression

Other antimetabolites

Other antimetabolites
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
hydroxycarbamide [146][147][148]
[149][150][151]
[152][153][154]
[155] 		Urea analog D (Au) PO Inhibits DNA synthesis by inhibiting the enzyme ribonucleotide reductase chronic myeloid leukemia, essential thrombocytosis, polycythemia vera, myelofibrosis, acute myeloid leukemia, sickle cell anemia myelosuppression, skin cancer (rare), edema (rare), hallucinations (rare), seizures (rare), pulmonary toxicity (rare)

Topoisomerase I inhibitors

topoisomerase I inhibitors
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
irinotecan[Note 1] camptothecin D (Au) IV inhibits topoisomerase I colorectal cancer diarrhea, myelosuppression, pulmonary infiltrates (uncommon), bradycardia (uncommon), ileus (rare), colitis (rare)
topotecan camptothecin D (Au) IV inhibits topoisomerase I small cell lung cancer, ovarian cancer,cervical cancer diarrhea, myelosuppression, interstitial lung disease, allergy

Anthracyclines

anthracyclines
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
daunorubicin anthracycline D (Au) IV inhibits DNA and RNA synthesis by intercalating DNA base pairs; inhibits DNA repair by inhibiting topoisomerase II acute leukemias myelosuppression, cardiotoxicity, anaphylaxis (rare), secondary malignancies (particularly acute myeloid leukaemia and myelodysplastic syndrome), radiation recall.
doxorubicin anthracycline D (Au) IV as above breast cancer, lymphomas, sarcomas, bladder cancer, acute lymphoblastic leukemia, Wilms' tumour, AIDS-related Kaposi's sarcoma, neuroblastoma, multiple myeloma as above
epirubicin anthracycline D (Au) IV as above breast cancer, gastric cancer, bladder cancer as above
idarubicin anthracycline D (Au) IV, PO as above acute leukemias as above
mitoxantrone anthracycline D (Au) IV as above Non-Hodgkin lymphoma, acute myeloid leukemia, prostate cancer, multiple sclerosis as above
valrubicin anthracycline C (US) IV as above bladder cancer as above

Podophyllotoxins

podophyllotoxins
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
etoposide podophyllotoxin D (Au) IV, PO topoisomerase II inhibitor testicular cancer, ovarian cancer, lung cancer, acute myeloid leukemia, lymphomas, sarcomas myelosuppression, hypersensitivity reactions, Stevens-Johnson syndrome (rare), peripheral neuropathy (uncommon), secondary malignancies (especially acute myeloid leukemia)
teniposide podophyllotoxin D (Au) IV topoisomerase II inhibitor lymphomas, acute lymphoblastic leukemia, neuroblastoma as above

Taxanes

taxanes
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
cabazitaxel taxane D (Au) IV Microtubule disassembly inhibitor. Arrests cells in late G2 phase and M phase. Prostate cancer Myelosuppression, diarrhoea, kidney failure, hypersensitivity, severe GI reactions (including perforation, ileus, colitis, etc.; all rare) and peripheral neuropathy
docetaxel taxane D (Au) IV As above. Breast cancer, non-small cell lung cancer, ovarian cancer, prostate cancer, squamous cell head and neck cancer and gastric cancer. Myelosuppression, peripheral neuropathy, hypersensitivity, fluid retention, heart failure (uncommon), pulmonary toxicity (rare), radiation recall (rare), scleroderma-like skin changes (rare), Stevens-Johnson syndrome (rare), toxic epidermal necrolysis (rare), seizures (rare) and encephalopathy (rare)
paclitaxel taxane D (Au) IV As above. Ovarian cancer, breast cancer, non-small cell lung cancer, AIDS-related Kaposi's sarcoma, cervical cancer, germ cell cancer and endometrial cancer Hypersensitivity, myelosuppression, peripheral neuropathy, myocardial infarction (uncommon), arrhythmias (uncommon), pulmonary toxicity (rare), radiation recall (rare), scleroderma-like skin changes (rare), Stevens-Johnson syndrome (rare), toxic epidermal necrolysis (rare), seizures (rare) and encephalopathy (rare).

Vinca alkaloids

vinca alkaloids
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
vinblastine vinca alkaloid D (Au) IV microtubule assembly inhibitor, arrests cells in M phase Hodgkin lymphoma, germ cell tumors, non-small cell lung cancer, bladder cancer and primary immune thrombocytopenia neurotoxicity, myelosuppression, myocardial ischemia (rare) and myocardial infarction (rare)
vincristine vinca alkaloid D (Au) IV as above lymphomas, acute lymphoblastic leukemia, multiple myeloma, sarcoma, brain tumurs, Wilms' tumor, neuroblastoma, primary immune thrombocytopenia neurotoxicity, anaphylaxis (rare), myocardial ischemia (rare) and myocardial infarction (rare).
vindesine vinka alkaloid D (Au) IV as above refractory metastatic melanoma, childhood acute lymphoblastic leukaemia, chronic myeloid leukaemia in blast crises, neuroblastoma, non-small cell lung cancer, breast cancer myelosuppression, neurotoxicity, paralytic ileus
vinflunine vinca alkaloid D (Au) IV as above bladder cancer as per vinblastine
vinorelbine vinca alkaloid D (Au) IV as above breast cancer and non-small cell lung cancer as above

Alkylating agents

Alkylating agents
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
bendamustine nitrogen mustard D (Au) IV alkylates DNA chronic lymphocytic leukemia, mantle cell lymphoma, non-Hodgkin's lymphoma myelosuppression, hypokalemia, tachycardia
busulfan dialkylsulfonate D (Au) IV, PO alkylates DNA conditioning treatment before hematopoietic stem cell transplantation (high dose, IV), chronic myeloid leukemia, myelofibrosis, polycythemia vera, essential thrombocytosis myelosuppression, seizures (high dose), tachycardia (high dose), hepatic sinusoidal obstruction syndrome (high dose), Addison-like syndrome (rare), pulmonary fibrosis (rare), cataracts (rare) and hepatitis (rare), secondary malignancies[1][156]
carmustine nitrosourea D (Au) IV alkylates DNA Anaplastic astrocytoma, glioblastoma multiforme and mycosis fungoides (topical) myelosuppression, pulmonary fibrosis, pulmonary infiltrates, seizure, brain oedema, cerebrospinal leaks, subdural fluid collection, intracranial infection, hypotension (uncommon), tachycardia (uncommon), decrease in kidney size (reversible), uremia (uncommon), kidney failure (uncommon), severe hepatic toxicity (rare), thrombosis (rare), neuroretinitis (rare), secondary malignancies.[1][156]
chlorambucil nitrogen mustard D (Au) IV alkylates DNA lymphoma, chronic lymphocytic leukemia and Waldenström's macroglobulinemia myelosuppression, hallucinations (rare), seizures (rare), sterile cystitis (rare), hepatotoxicity (rare), severe pneumonitis (rare), Stevens-Johnson syndrome (rare), toxic epidermal necrolysis (rare), drug fever (rare), secondary malignancies[1][156]
chlormethine nitrogen mustard D (Au) IV, topical alkylates DNA cutaneous T-cell lymphoma, metastatic carcinoma, leukemias, lymphomas, polycythemia vera and bronchogenic carcinoma Thrombosis, myelosuppression (common), hyperuricaemia, erythema multiforme, haemolytic anemia, nausea and vomiting (severe) and secondary malignancies.[156]
cyclophosphamide Nitrogen mustard D (Au) IV alkylates DNA Breast cancer, lymphoma, acute lymphoblastic leukaemia, chronic lymphocytic leukaemia, sarcoma, multiple myeloma, Waldenström's macroglobulinaemia, systemic lupus erythematosus, glomerulonephritis, systemic vasculitis and Wegener's granulomatosis Myelosuppression, nausea and vomiting (>30%), haemorrhagic cystitis, heart failure (rare), pulmonary fibrosis (rare), hepatic sinusoidal obstruction syndrome (rare), water retention resembling SIADH (rare) and seizures (rare). Secondary malignancies.[156]
dacarbazine Triazene D (Au) IV alkylates DNA Hodgkin lymphoma, metastatic malignant melanoma and soft tissue sarcoma Myelosuppression, agranulocytosis (uncommon), hepatic vein thrombosis (rare) and hepatocellular necrosis (rare). Secondary malignancies.[156]
Fotemustine nitrosourea D (Au) IV alkylates DNA. Metastatic malignant melanoma. Myelosuppression.
Ifosfamide nitrogen mustard D (Au) IV alkylates DNA Sarcomas, testicular cancer and lymphomas.Myelosuppression, haemorrhagic cystitis, nephrotoxicity, neurotoxicity and cardiac toxicity (rare). Secondary malignancies.[156]
lomustine nitrosourea D (Au) PO alkylates DNA glioma, medulloblastoma myelosuppression, pulmonary infiltration and fibrosis, secondary malignancies[156]
melphalan nitrogen mustard D (Au) IV, PO alkylates DNA malignant melanoma of the extremities, multiple myeloma, conditioning treatment before hematopoietic stem cell transplant myelosuppression, pulmonary fibrosis and pneumonitis (uncommon), skin necrosis (uncommon), anaphylaxis, hepatic sinusoidal obstruction syndrome, SIADH, secondary malignancies[156]
streptozotocin nitrosourea D (Au) IV, PO alkylates DNA pancreatic cancer, carcinoid syndromenephrotoxicity, hypoglycaemia, myelosuppression, nausea and vomiting (>90%), jaundice and nephrogenic diabetes insipidus (rare)
temozolomide triazene D (US) PO alkylates DNA anaplastic astrocytoma, glioblastoma multiforme, metastatic malignant melanoma myelosuppression, Stevens-Johnson syndrome (rare), pneumonitis (rare) and hepatitis (rare)
trabectedin add add add alkylates DNA liposarcoma, leiomyosarcoma add

Platinum compounds

platinum compounds
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
carboplatin platinum complex D (Au) IV reacts with DNA, inducing apoptosis, non-cell cycle specific ovarian cancer, lung cancer, squamous cell head and neck cancer myelosuppression, nausea and vomiting (30-90%), peripheral neuropathy, ototoxicity, anaphylaxis, acute kidney failure (rare), haemolytic uraemic syndrome (rare) and loss of vision (rare).
cisplatin platinum complex D (Au) IV as above germ cell tumors (including testicular cancer), ovarian cancer, cervical cancer, small cell and non-small cell lung cancer, mesothelioma, squamous cell head and neck cancer, esophageal cancer, gastric cancer, bladder cancer, osteosarcoma nephrotoxicity, nausea and vomiting (30-100%), myelosuppression, electrolyte anomalies, peripheral neuropathy, ototoxicity and anaphylaxis, hemolytic anemia (rare), optic neuritis (rare), reversible posterior leucoencephalopathy syndrome (rare), seizures (rare), ECG changes (rare), heart failure (rare)
nedaplatin [157] platinum complex N/A IV as above non-small cell lung cancer, esophageal cancer, uterine cervical cancer, head and neck cancer and urothelial cancer nephrotoxicity, myelosuppression, nausea and vomiting (30-90%)
oxaliplatin platinum complex D (Au) IV as above colorectal cancer, oesophageal cancer and gastric cancermyelosuppression, peripheral neuropathy, anaphylaxis, nausea and vomiting (30-90%), hypokalaemia, metabolic acidosis, interstitial lung disease (uncommon), ototoxicity (rare), reversible posterior leucoencephalopathy syndrome (rare), immune-mediated cytopenias (rare), hepatic sinusoidal obstruction syndrome (rare)

Miscellaneous others

miscellaneous others
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
altretamine triazine D (Au) PO unclear, reactive intermediates covalently bind to microsomal proteins and DNA, possibly causing DNA damage recurrent ovarian cancer myelosuppression, peripheral neuropathy, seizures, hepatotoxicity (rare)
bleomycin glycopeptide D (Au) IM, SC, IA, IV or IP inhibits DNA and to a lesser extent RNA synthesis, produces single and double strand breaks in DNA possibly by free radical formation germ cell tumors, squamous cell carcinoma, pancreatic cancer, non-Hodgkin's lymphoma, Hodgkin's lymphoma pulmonary toxicity, hypersensitivity, scleroderma, Raynaud's phenomenon
bortezomib bipeptidyl boronic acid C (Au) IV, SC proteasome inhibitor multiple myeloma, mantle cell lymphoma, follicular lymphoma (orphan) peripheral neuropathy, neutropenia, thrombocytopenia, anemia, orthostatic hypotension, hepatitis (uncommon/rare), haemorrhage (uncommon/rare), heart failure (uncommon/rare), seizures (uncommon/rare), progressive multifocal leucoencephalopathy (PML), hearing loss
carfilzomib add add add proteasome inhibitor multiple myeloma add
dactinomycin polypeptide D (Au) IV complexes with DNA interfering with DNA-dependent RNA synthesis gestational trophoblastic disease, Wilms' tumor, rhabdomyosarcoma myelosuppression, anaphylaxis, radiation recall, hepatotoxicity, hepatic sinusoidal obstruction syndrome (common in Wilms' tumor)
eribulin IV
estramustine nitrogen mustard and estrogen analog D (Au) PO antimicrotubule and estrogenic actions prostate cancer cardiovascular complications, such as ischemic heart disease, venous thromboembolism, congestive heart failure, pulmonary embolism, myocardial infarction, cerebrovascular failure
ixabepilone epothilone B analog D (US) IV promotes tubulin polymerisation and stabilises microtubular function, causing cell cycle arrest at G2/M phase and subsequently induces apoptosis locally advanced or metastatic breast cancermyelosuppression, peripheral neuropathy, myocardial ischemia (uncommon/rare), supraventricular arrhythmia (uncommon/rare), hypersensitivity reaction (uncommon/rare)
mitomycin aziridine D (Au) IV cross-links DNA anal cancer, bladder cancer myelosuppression, pulmonary toxicity, hemolytic uremic syndrome (rare)
procarbazine methylhydrazine D (Au) IM, IV inhibits DNA, RNA and protein synthesis glioma, Hodgkin's lymphoma myelosuppression, neurotoxicity, pulmonary fibrosis (uncommon/rare), pneumonitis (uncommon/rare), hemolysis (uncommon/rare), hepatic dysfunction (uncommon/rare)

Antihormones

Radiopharmaceutics

Targeted antineoplastics

Monoclonal antibodies and antibody-drug conjugates

monoclonal antibodies
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
ado-trastuzumab emtansine add add add add add
alemtuzumab protein B2 (Au) IV CD52 antibody induces apoptosis in the tagged cells chronic lymphocytic leukemia pancytopenia, pneumonitis, arrhythmias and hypersensitivity reactions (rare), autoimmune hemolytic anemia (rare), autoimmune thrombocytopenia (rare), progressive multifocal leucoencephalopathy (rare)
bevacizumab protein D (Au) IV VEGF inhibitor colorectal, breast, ovarian, renal cell and non-squamous non-small cell lung cancer and glioblastoma hypertension, thromboembolisms, heart failure, bleeding, neutropenia, thrombocytopenia, GI perforation, fistula formation, hypertensive encephalopathy, pulmonary hypertension, reversible posterior leucoencephalopathy syndrome, nasal septum perforation and osteonecrosis of the jaw
blinatumomab add add add add add
brentuximab vedotin antibody-drug conjugate (ADC) directed to the protein CD30 add add add add add
cetuximab protein D (Au) IV EGFR inhibitor squamous cell head and neck cancer or EGFR-positive and KRAS wild-type metastatic colorectal cancer. Infusion-related reactions, skin reactions, hypomagnesaemia, hypocalcemia, hypokalemia, blood clots, interstitial lung disease, aseptic meningitis
daratumumab[159][160] protein (anti-CD38) add add add add add
denosumab protein X (US) SC RANKL inhibitor osteoporosis, including drug- and cancer-related osteoporosis, giant cell tumor of bone, hypercalcemia of malignancies hypercholesterolemia, cataract, urinary retention, hypocalcemia, osteonecrosis of the jaw, anaphylaxis
dinutuximab [161] protein IV binds to glycolipid GD2 pediatric neuroblastoma infections, infusion reactions, hypokalemia, hypotension, pain, fever, capillary leak syndrome[162]
gemtuzumab ozogamicin [163] protein D (US) IV CD33 antibody that induces apoptosis of the tagged cell acute myeloid leukemia hepatic veno-occlusive disease, myelosuppression, cytokine release syndrome, hypersensitivity, electrolyte anomalies
ibritumomab tiuxetan [164][165] protein D (US) IV CD20 antibody bound with the radioactive isotope, 90Y, induces radiation-dependent cell lysis. Non-Hodgkin's lymphoma and follicular lymphomathrombocytopenia, neutropenia, anemia, hypotension, secondary malignancies
ipilimumab protein C (Au) IV CTLA4 antibody that causes immune system-mediated lysis of the tagged cellunresectable or metastatic malignant melanoma life-threatening immune mediated reactions, fever
nivolumab add add add add add add
obinutuzumab add add add add add add
ofatumumab [166][167][168] Protein C (US) IV anti-CD20 antibody chronic lymphocytic leukemia neutropenia, pneumonia, infusion reactions, cytopenias
panitumumab protein C (Au) IV EGFR inhibitor. RAS (KRAS or NRAS) wild-type metastatic colorectal cancer skin reactions, electrolyte anomalies, anaphylaxis, angioedema (rare)
pembrolizumab add add add add add add
pertuzumab protein D (Au) IV HER2 inhibitor HER2-positive breast cancer anaphylaxis, cardiac dysfunction, anemia
ramucirumab add add add add add add
rituximab protein C (Au) IV anti-CD20 antibody CD20-positive B cell non-Hodgkin lymphoma, chronic lymphocytic leukemia, rheumatoid arthritis, Wegener's granulomatosis and microscopic polyangiitis infusion-related reactions, neutropenia, arrhythmias, infection, thrombocytopenia (uncommon), anaemia (uncommon), angina (uncommon), myocardial infarction (uncommon), heart failure (uncommon), hemolytic anemia (rare), aplastic anaemia (rare), serum sickness (rare), severe skin conditions (rare), pulmonary infiltrates (rare), pneumonitis (rare), cranial neuropathy (vision or hearing loss; rare) and progressive multifocal leucoencephalopathy (rare)
tositumomab [169][170]Protein X (US) IV Anti-CD20 antibody which is tagged with I131. Non-Hodgkin's lymphoma grade 3-4 cytopenias, methemoglobinemia, acute myeloid leukemia or myelodysplastic syndrome, anaphylaxis and hyperthyroidism
trastuzumab protein B2 (Au) IV anti-HER2 antibody HER2-positive breast cancer, gastric cancer, pancreatic cancer (orphan) and gastro-esophageal junction cancer cardiac dysfunction, infusion-related reactions, peripheral neuropathy and pulmonary toxicity (rare)

Tyrosine kinase inhibitors

tyrosine kinase inhibitors
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
afatinib [171] phenyl quinazolinamine D (US) PO EGFR, HER2 and HER4 inhibitor non-small cell lung cancer diarrhea, hypokalemia, interstitial lung disease, hepatotoxicity
aflibercept [172] protein C (US) IV VEGF and PGF inhibitor colorectal cancermyelosuppression, hypertension, dehydration, blood clots, GI perforation, reversible posterior leucoencephalopathy syndrome (uncommon)
axitinib [173] indazole and pyridine analog D (Au) PO multikinase inhibitor renal cell carcinoma hypertension, thyroid dysfunction, blood clots, electrolyte disturbances, GI perforation (rare), fistula formation (rare), reversible posterior leucoencephalopathy syndrome (rare), polycythemia (uncommon)
bosutinib [174][175] quinoline carbonitrile analog D (Au) PO Bcr-Abl and SRc kinase inhibitor chronic myeloid leukemia diarrhea, thrombocytopenia, neutropenia, hepatotoxicity, QT interval prolongation, kidney failure, pleural effusion, pericarditis (uncommon/rare), acute pancreatitis (uncommon/rare), GI hemorrhage (uncommon/rare), anaphylactic shock (uncommon/rare), acute pulmonary edema (uncommon/rare), respiratory failure (uncommon/rare), pulmonary hypertension(uncommon/rare), erythema multiforme (uncommon/rare)
cobimetinib[176] add add add melanoma that expresses a BRAF V600E or V600K mutation[176] diarrhea, nausea, vomiting, rash, photosensitivity, pyrexia[177][177]
crizotinib [178][179][180]
[181][182] 		aminopyridine D (US) PO ALK, Hepatocyte Growth Factor Receptor (HGFR, c-Met), and Recepteur d'Origine Nantais (RON) inhibitor non-small cell lung cancer lymphopenia, neutropenia, hypophosphatemia, hypokalemia, peripheral neuropathy, blood clots, QT interval prolongation, bradycardia, pneumonia, pneumonitis, kidney cyst, ARDS, liver failure
dasatinib piperazine D (Au) PO BCR-ABL, SRC family, c-Kit, EPHA2 and PDGFR-β kinase inhibitor.Philadelphia positive chronic myeloid leukaemia and acute lymphoblastic leukemia Fluid retention, myelosuppression, hemorrhage, hypertension, electrolyte anomalies, cardiac dysfunction (rare), heart failure (rare), myocardial infarction, arrhythmia (rare), prolonged QT interval (rare), kidney failure (rare), hypersensitivity (rare), hepatic failure (rare)
erlotinib quinazoline C (Au) PO EGFR inhibitor non-small cell lung cancer, pancreatic cancer skin reactions, diarrhea, GI bleeds, anemia, dehydration, interstitial lung disease (uncommon), hepatic failure (rare), hepatorenal syndrome (rare), GI perforation (rare), ulcerative keratitis (rare)
gefitinib quinazoline C (Au) PO EGFR inhibitor. EGFR-mutation positive non-small cell lung cancer skin reactions, diarrhea, dehydration, hemorrhage, interstitial lung disease (uncommon), pancreatitis (uncommon), hepatitis (uncommon), allergy (uncommon), hepatic failure (rare), toxic epidermal necrolysis (rare), Stevens-Johnson syndrome (rare)
imatinib pyrimidine and piperazine D (Au) PO Bcr-Abl kinase inhibitor Philadelphia chromosome-positive acute lymphoblastic leukemia, chronic myeloid leukemia, GI stromal tumor, myelodysplastic/myeloproliferative diseases myelosuppression, fluid retention, GI bleeding, electrolyte anomalies, left ventricular dysfunction (uncommon), heart failure (uncommon), pulmonary edema (uncommon), kidney failure (uncommon), angioedema (rare), anaphylaxis (rare), GI perforation (rare), hepatotoxicity (rare), avascular necrosis (rare), myopathy (rare), rhabdomyolysis (rare)
lapatinib quinazoline C (Au) PO HER2 inhibitor. HER2-positive breast cancer, stomach cancer (orphan), esophageal cancer (orphan) diarrhea, interstitial lung disease (uncommon), hepatotoxicity (uncommon), anaphylaxis (rare)
lenvatinib add add add add add
nilotinib imidazole D (Au) PO Bcr-Abl kinase inhibitor chronic myeloid leukemia myelosuppression, electrolyte disturbances, hyperglycemia, prolonged QT interval (uncommon), peripheral arterial occlusive disease (uncommon), pancreatitis (uncommon), pleural effusion (uncommon), pericardial effusion (uncommon)
osimertinib add add add add add
pazopanib indazole D (Au) PO multikinase inhibitor, including c-KIT, FGFR, PDGFR and VEGFR renal cell carcinoma, soft tissue sarcoma hypertension, QT interval prolongation, hemorrhage, blood clots, neutropenia, thrombocytopenia, neutropenia, thrombocytopenia, elevated thyroid-stimulating hormone, hypothyroidism, electrolyte disturbances, hypo- or hyperglycemia, torsades de pointes (uncommon), heart failure (uncommon), hepatic failure (uncommon), GI perforation (uncommon), fistula formation (uncommon), reversible posterior leucoencephalopathy syndrome (rare)
ponatinib [183][184] Imidazopyridazine D (US) PO Multikinase inhibitor (BEGFR, PDGFR, FGFR, EPH receptors and SRC families of kinases, and KIT, RET, TIE2 and FLT3), that also inhibits T135I Bcr-Abl kinase T135I positive chronic myeloid leukemia, Philadelphia chromosome positive acute lymphoblastic leukemia hypertension, neutropenia, leucopenia, anemia, thrombocytopenia, lymphopenia, pleural effusion, heart failure, peripheral neuropathy, hemorrhage, blood clots, pancreatitis, infection
regorafenib [185][186][187]
[188] 		4-phenoxypyridine D (US) PO 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 colorectal cancer, GI stromal tumors anemia, lymphopenia, thrombocytopenia, electrolyte anomalies, hepatotoxicity, hypertension, hypothyroidism, neutropenia, myocardial ischemia or infarction
ruxolitinib [189][190][191][192] pyrimidinylpyrazole C (Au) PO JAK1 and JAK2 inhibitor myelofibrosis, pancreatic cancer (orphan) anemia, thrombocytopenia
sorafenib 4-phenoxypyridine D (Au) PO multikinase inhibitor (including VEGF and PDGF receptor kinases) renal cell carcinoma, hepatocellular carcinoma hypertension, skin reactions, bleeding, neutropenia, thrombocytopenia, lymphopenia, peripheral neuropathy, thyroid dysfunction, electrolyte anomalies, myocardial ischemia or infarctions, heart failure (uncommon), GI perforation (uncommon), pancreatitis (uncommon), reversible posterior leucoencephalopathy syndrome (rare), hepatitis (rare), nephrotic syndrome (rare), prolonged QT interval (rare)
sunitinib oxindole D (Au) PO multikinase inhibitor (including VEGF & PDGF receptor tyrosine kinases) renal cell carcinoma, GI stromal tumor, pancreatic neuroendocrine tumour neutropenia, thrombocytopenia, lymphopenia, hypertension, left ventricular dysfunction, heart failure, blood clots, thyroid dysfunction, electrolyte anomalies, pancreatitis (uncommon), hepatic failure (uncommon), prolonged QT interval (rare), torsades de pointes (rare), GI perforation (rare), fistula formation (rare), seizures (rare), reversible posterior leucoencephalopathy syndrome (rare), hemolytic uremic syndrome (rare), thrombotic thrombocytopenic purpura (rare), nephrotic syndrome (rare), hypersensitivity (rare), angioedema (rare), toxic epidermal necrolysis (rare), Stevens-Johnson syndrome (rare)
trametinib add add add melanoma that expresses a BRAF V600E or V600K mutation
vandetanib[193] quinazoline D (US) PO tyrosine kinase inhibitor (TKI) with selective activity against RET, VEGFR-2 and EGFR medullary thyroid cancer diarrhea, hypertension, QT interval prolongation, depression, electrolyte anomalies, hypothyroidism, GI perforation (uncommon)

Mammalian target of rapamycin (mTOR) inhibitors

mTOR inhibitors
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
everolimus Sirolimus analog C (Au) PO mTOR inhibitor renal cell cancer, pancreatic neuroendocrine tumor and breast cancer Pleural effusion, hyperglycemia, hypercholesterolemia, hypertriglyceridemia, neutropenia, lymphopenia, thrombocytopenia, anaemia, bleeding, kidney failure, hypokalemia, hypophosphataemia, pneumonitis, impaired wound healing (uncommon), anaphylaxis (rare) and angioedema (rare).
temsirolimus Sirolimus analog D (Au) IV mTOR inhibitor renal cell cancer, mantle cell lymphoma infusion reactions, impaired wound healing, hyperglycemia, hypercholesterolemia, hypertriglyceridemia, neutropenia, lymphopenia, thrombocytopenia, anemia, bleeding, kidney failure, hypokalemia, hypophosphatemia, pneumonitis, bowel perforation (uncommon), intracerebral bleeding, Stevens-Johnson syndrome (rare)

Retinoids

retinoids
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
alitretinoin 9-cis retinoic acid D (US) topical retinoic acid receptor (RAR) and retinoid X receptor (RXR) agonist. Kaposi's sarcoma. Edema, rashes
bexarotene[194] Phenethylnaphthalene X (US) PO, topical RXR agonist cutaneous T cell lymphoma Leucopenia, anaemia, lactic dehydrogenase increased, hypochromic anemia, hyperlipidemia, hypercholesteremia, hypothyroidism, hemorrhage, hypertension and kidney dysfunction.
isotretinoin 13-cis retinoic acid D (Au, topical), X (Au, oral) PO, topical RXR & RAR agonist neuroblastoma[195] and acne. topical: Skin reactions, blood lipid anomalies, increased platelet count and osteoporosis.[196] oral: anemia, red blood cell sedimentation rate increased, thrombocytopenia, thrombocytosis, neutropenia, anaphylaxis, hypersensitivity, diabetes mellitus, hyperuricemia, psychiatric disturbances (rare), convulsions (very rare), conjunctivitis, vasculitis (very rare), GI hemorrhage (very rare), hepatitis (very rare), erythema multiforme, Stevens-Johnson Syndrome, toxic epidermal necrolysis, arthritis (very rare), rhabdomyolysis, glomerulonephritis (very rare)[197]
tamibarotene [198][199][200] Naphthalene N/A PO RAR agonist. refractory acute promyelocytic leukemia and Alzheimer's disease hypercholesterolemia, hypertriglyceridemia, gastrointestinal disturbances, liver damage, leucocytosis, differentiation syndrome
tretinoin all-trans retinoic acid D (Au, topical), X (Au, oral) PO, topical RXR & RAR agonist acne, acute promyelocytic leukemia oral: differentiation syndrome, hyperleucocytosis, elevated cholesterol and triglycerides, arrhythmias, pancreatitis, elevated liver enzymes, thrombosis, intracranial hypertension and pseudotumour cerebri (mainly in children), anxiety, depression, genital ulceration (rare); topical: erythema

Immunomodulatory agents

immunomodulatory drugs (IMiDs)
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
lenalidomide thalidomide analog X (Au) PO numerous actions; 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 multiple myeloma blood clots, neutropenia (dose-limiting), thrombocytopenia (dose-limiting), anemia, infection, hypotension, hypokalemia, hypothyroidism, Stevens-Johnson syndrome, toxic epidermal necrolysis, angioedema, pneumonitis, hepatotoxicity, secondary malignancies (mostly myelodysplastic syndrome and acute myeloid leukemia)
pomalidomide thalidomide analog X (US) PO as above multiple myeloma and systemic sclerosis (orphan)neutropenia, anemia, pneumonia, thrombocytopenia, hypercalcemia, hyperglycemia, kidney failure, lymphopenia, hyponatremia, hypocalcemia, hypokalemia, peripheral neuropathy, thromboembolism
thalidomide thalidomide X (Au) PO as above multiple myeloma, erythema nodosum leprosum and the following orphan indications: graft versus host disease, mycobacterial infection, recurrent aphthous ulcers, severe recurrent aphthous stomatitis, primary brain malignancies, HIV-associated wasting syndrome, Crohn's disease, Kaposi's sarcoma, myelodysplastic syndrome and hematopoietic stem cell transplantation. peripheral neuropathy, depression, thromboembolism, bradycardia, orthostatic hypotension, leucopenia, hypothyroidism, thrombocytopenia (uncommon), Stevens-Johnson syndrome (rare), toxic epidermal necrolysis (rare), pneumonitis (rare), hepatotoxicity (rare), hearing loss (rare)

Histone deacetylase inhibitors

histone deacetylase inhibitors
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
belinostat add add add add add add
panobinostat add add add add add add
romidepsin [201]depsipeptide D (US) IV histone deacetylase inhibitor, hence inducing alterations in gene expression in the affected cells peripheral and cutaneous T-cell lymphoma electrolyte anomalies, anemia, thrombocytopenia, neutropenia, lymphopenia, ECG anomalies
valproate[Note 2] [202][203][204]
[205]		 branched short-chain fatty acids D (Au) PO, IV as above migraine prophylaxis, mania, epilepsy, fragile X syndrome (orphan), familial adenomatous polyposis (orphan) and the following off-label uses: cervical cancer, melanoma, mesothelioma, acute myeloid leukemia, myelodysplastic syndrome hyperammonemia, thrombocytopenia, polycystic ovaries, SIADH (uncommon), hepatic failure (rare), pancreatitis (rare), leucopenia (rare), neutropenia (rare), pure red cell aplasia (rare), agranulocytosis (rare), extrapyramidal syndrome (rare), reduced BMD with long-term use, pleural effusion (rare), multiorgan hypersensitivity reaction (rare)
vorinostat [206]phenyloctanediamide D (US) PO as above as per romidepsin thrombocytopenia, anemia, QT interval prolongation, pulmonary embolism

Other agents

other agents
INN reviews chemical classification pregnancy category route[1] mechanism of action[1][2][3][4] indications[1][2][4] major toxicities[1][2][4][5]
anagrelide imidazoquinazoline B3 (Au) PO phosphodiesterase 3 inhibitor essential thrombocythemiafluid retention, palpitations, tachycardia, hepatotoxicity (uncommon), heart failure (uncommon), hypertension (uncommon), arrhythmia (uncommon), syncope (uncommon), cardiomyopathy (rare), cardiomegaly (rare), MI (rare), pulmonary hypertension (rare), interstitial lung disease (rare) and pancreatitis (rare)
arsenic trioxide[Note 3] arsenic compound X (Au) IVnot fully understood; induces partial differentiation and promotes apoptosis of leukemic cells and may also inhibit angiogenesisacute promyelocytic leukemia; orphan indications include: acute myeloid leukaemia, chronic lymphocytic leukemia, malignant glioma, myelodysplastic syndrome, multiple myeloma, liver cancer and chronic myeloid leukemia differentiation syndrome, hyperleucocytosis, neutropenia, thrombocytopenia, ventricular tachycardia, prolonged QT interval, torsades de pointes, complete atrioventricular block, peripheral neuropathy, hyperglycemia, hypokalemia, hypomagnesemia, elevation of bilirubin or aminotransferases, hepatotoxicity and secondary malignancies.
asparaginase
[Note 4] 		protein D (Au) IM, IV 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 acute lymphoblastic leukaemia and lymphoblastic lymphoma. allergic reactions, hemorrhagic and thrombotic events, uremia, pancreatitis, hyperglycemia, hyperammonaemia, acute kidney failure and diabetic ketoacidosis
BCG vaccine
[Note 5] 		protein B2 (Au) IB live, attenuated Mycobacterium bovis, which produces a local inflammatory reaction, resulting in elimination or reduction of superficial tumor lesions of the bladder bladder cancer cystitis, BCG infection and contracted bladder
ceritinib add add add add add add
dabrafenib add add add add add add
denileukin diftitox [207][208][209][210] protein C (US) IV interleukin 2 combined with diphtheria toxin which binds to the interleukin receptor on immune cells and introduces the diphtheria toxin into the cell. cutaneous T cell lymphoma and peripheral T cell lymphoma (orphan) infusion reactions, hypocalcemia, hypotension, thrombocytopenia, acute renal insufficiency (uncommon/rare), hyper/hypothyroidism (uncommon/rare), pancreatitis (uncommon/rare) and toxic epidermal necrolysis (uncommon/rare)
idelalisib add add add add add
ibrutinib inhibitor of Bruton's tyrosine kinase add add add add add
olaparib add add add add add add
palbociclib add add add add add add
sonidegib add add add add add add
talimogene laherparepvec add add add add add add
vemurafenib pyrrolopyridine D (Au) PO BRAF kinase inhibitor BRAF kinase mutation V600E-positive metastatic melanoma skin reactions, secondary malignancies (mostly squamous cell carcinoma), anaphylaxis (rare), hypotension (rare)
vismodegib add add add add add add

Notes

  1. ↑ A liposomal formulation of irinotecan, Onivyde, is available.
  2. ↑ Its use in cancer treatment is purely investigational at present
  3. ↑ There is no INN for arsenic trioxide, just the USAN
  4. ↑ There is no INN for asparaginase, only a USAN
  5. ↑ There is no INN for BCG

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