List of antineoplastic agents

This is a list of antineoplastic agents used to treat cancer. See also: List of chemotherapeutic agents

Antineoplastic agents INN Route Mechanism of action Indications Major toxicities 1. Cytotoxic antineoplastics 1.01 Nucleoside analogues Azacitidine SC, IV DNA methyltransferase inhibitor and incorporates itself into RNA, hence inhibiting gene expression. Myelodysplastic syndromes, acute myeloid leukaemia and chronic myeloid leukaemia Myelosuppression, kidney failure (uncommon/rare), renal tubular acidosis and hypokalaemia. Capecitabine PO Fluorouracil prodrug Breast, colorectal, gastric and oesophageal cancer Myelosuppression, cardiotoxicity, hypertriglyceridaemia, GI haemorrhage (uncommon), cerebellar syndrome (uncommon), encephalopathy (uncommon) and diarrhoea. Carmofur PO Fluorouracil prodrug Colorectal, breast and ovarian cancerMyelosuppression, neurotoxicity and diarrhoea. Cladribine SC, IV DNA methyltransferase inhibitor, metabolites incorporate themselves into DNA. Hairy cell leukaemia, chronic lymphocytic leukaemia Myelosuppression, haemolytic anaemia (uncommon), neurotoxicity (rare), renal impairment (rare), pulmonary interstitial infiltrates (rare), Stevens–Johnson syndrome (rare) and toxic epidermal necrolysis (rare). Clofarabine IV Ribonucleotide reductase and DNA polymerase inhibitor. Acute lymphoblastic leukaemia and acute myeloid leukaemia Myelosuppression, hypokalaemia, cytokine release syndrome, Stevens–Johnson syndrome (uncommon), toxic epidermal necrolysis (uncommon) and pancreatitis (uncommon) Cytarabine SC, IM, IV, IT DNA polymerase inhibitor, S-phase specific. Incorporates its metabolites into DNA. Acute myeloid leukaemia, acute lymphoblastic leukaemia, chronic myeloid leukaemia, lymphomas, progressive multifocal leucoencephalopathy and meningeal leukaemia 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 IV DNA methyltransferase inhibitor. Myelodysplastic syndrome, sickle cell anaemia (orphan), acute myeloid leukaemia and chronic myeloid leukaemia. Myelosuppression, hyperglycaemia, hypoalbuminaemia, hypomagnesaemia, hypokalaemia, hyperkalaemia and thrombocythaemia. Floxuridine IA Fluorouracil analogue. Metastatic GI adenocarcinoma and stomach cancer Myelosuppression. Fludarabine PO, IV DNA polymerase and ribonucleotide reductase inhibitor. Acute myeloid leukaemia, chronic lymphocytic leukaemia, non-Hodgkin lymphoma and Waldenstrom macroglobulinaemia. Myelosuppression, hyperglycaemia, GI bleeds (uncommon), pneumonitis (uncommon), haemolytic anaemia (uncommon), severe neurotoxicity (rare), haemorrhagic cystitis (rare), Stevens–Johnson syndrome (rare) and toxic epidermal necrolysis (rare). Fluorouracil IV, Topical Thymidylate synthase inhibitor. Anal, breast, colorectal, gastric, head and neck, oesophageal and pancreatic cancer. Bowen's disease and actinic keratoses. Myelosuppression, diarrhoea, cardiotoxicity, GI ulceration and bleeding (uncommon), cerebellar syndrome (uncommon), encephalopathy (uncommon) and anaphylaxis (rare). Gemcitabine IV DNA synthesis inhibitor, induces apoptosis specifically in S-phase. Bladder, breast, nasopharyngeal, non-small cell lung, ovarian and pancreatic cancer, lymphomas and inflammatory bowel disease. Myelosuppression, pulmonary toxicity, kidney failure (rare), haemolytic uraemic syndrome (rare), thrombotic thrombocytopenic purpura (rare), anaphylactoid reaction (rare), reversible posterior leukoencephalopathy syndrome (rare), myocardial infarction (rare) and heart failure (rare). Mercaptopurine PO Purine synthesis inhibitor. Acute lymphoblastic leukaemia, acute promyelocytic leukaemia, lymphoblastic lymphoma and inflammatory bowel disease. Myelosuppression, hepatotoxicity, GI ulceration (rare), pancreatitis (rare) and secondary leukaemia (rare) or myelodysplasia (rare). Nelarabine IV Purine synthesis inhibitor. Acute lymphoblastic leukaemia and chronic lymphocytic leukaemia. Myelosuppression, pleural effusion, seizures, tumour lysis syndrome and a condition similar to Guillain-Barré syndrome. Pentostatin IV Adenosine deaminase inhibitor. Hairy cell leukaemia, peripheral T-cell lymphoma (orphan), cutaneous T cell lymphoma (orphan) and chronic lymphocytic leukaemia (orphan). Myelosuppression, neurotoxicity, immune hypersensitivity, hyponatraemia, thrombotic thrombocytopenic purpura and microangiopathic hemolytic anaemia. Tegafur PO Thymidylate synthase inhibitor. Breast, colorectal cancer, gallbladder, gastrointestinal tract, head and neck, liver and pancreas cancer. Myelosuppression, diarrhoea, neurotoxicity and hepatitis (rare). Tioguanine PO Purine synthesis inhibitor. Acute lymphoblastic leukaemia and acute myeloid leukaemia Myelosuppression, hepatotoxicity, peripheral neuropathy (uncommon), intestinal necrosis (rare) and perforation (rare). 1.02 Antifolates Methotrexate SC, IM, IV, IT, PO Dihydrofolate reductase inhibitor. Bladder and breast cancer. squamous cell carcinoma of head and neck, gestational trophoblastic disease, acute leukaemias, non-Hodgkin lymphoma, osteosarcoma, brain tumours, graft-versus-host disease and 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) and macrocytic anaemia (rare). Pemetrexed IV Dihydrofolate reductase, thymidylate synthase and glycinamide ribonucleotide formyltransferase inhibitors. Malignant mesothelioma and 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) and toxic epidermal necrolysis (rare).PralatrexateIVDihydrofolate reductase, thymidylate synthase and glycinamide ribonucleotide formyltransferase inhibitors.Peripheral T cell lymphomasFebrile neutropenia (uncommon) renal failure (uncommon), peripheral neuropathy (uncommon), hepatotoxicity (rare) Raltitrexed IV Dihydrofolate reductase and thymidylate synthase inhibitor. Colorectal cancer MyelosuppressionTrimetrexateIVDihydrofolate reductase, thymidylate synthase and glycinamide ribonucleotide formyltransferase inhibitors.Pneumocystis jiroveciiNeutropenia, febrile neutropenia (uncommon), renal failure (uncommon) peripheral neuropathy (uncommon)1.03 Other antimetabolites Hydroxycarbamide PO Inhibits DNA synthesis by inhibiting the enzyme ribonucleotide reductase. Chronic myeloid leukaemia, essential thrombocytosis, polycythaemia vera, myelofibrosis, acute myeloid leukaemia and sickle cell anaemia Myelosuppression, skin cancer (rare), oedema (rare), hallucinations (rare), seizures (rare) and pulmonary toxicity (rare). 1.04 Topoisomerase I inhibitor Irinotecan IV Inhibits topoisomerase I. Colorectal cancer Diarrhoea, myelosuppression, pulmonary infiltrates (uncommon), bradycardia (uncommon), ileus (rare) and colitis (rare). Topotecan IV Inhibits topoisomerase I. Small cell lung cancer, ovarian cancer and cervical cancer Diarrhoea, myelosuppression, interstitial lung disease and allergy. 1.05 Anthracyclines Daunorubicin IV Inhibits DNA and RNA synthesis by intercalating DNA base pairs. Inhibits DNA repair by inhibiting topoisomerase II. Acute leukaemias Myelosuppression, cardiotoxicity, anaphylaxis (rare), secondary malignancies (particularly acute myeloid leukaemia and myelodysplastic syndrome) and radiation recall. Doxorubicin IV As above. Breast cancer, lymphomas, sarcomas, bladder cancer, acute lymphoblastic leukaemia, Wilms' tumour, AIDS-related Kaposi's sarcoma, neuroblastoma and multiple myeloma As above. Epirubicin IV As above. Breast cancer, gastric cancer and bladder cancer As above. Idarubicin IV, PO As above. Acute leukaemias. As above. Mitoxantrone IV As above. Non-Hodgkin lymphoma, acute myeloid leukaemia, prostate cancer and multiple sclerosis As above. Valrubicin IV As above. Bladder cancer. As above. 1.06 Podophyllotoxins Etoposide IV, PO Topoisomerase II inhibitor. Testicular cancer, ovarian cancer, lung cancer, acute myeloid leukaemia, lymphomas and sarcomas Myelosuppression, hypersensitivity reactions, Stevens–Johnson syndrome (rare), peripheral neuropathy (uncommon) and secondary malignancies (especially acute myeloid leukaemia). Teniposide IV Topoisomerase II inhibitor. Lymphomas, acute lymphoblastic leukaemia and neuroblastoma As above. 1.07 Taxanes Cabazitaxel 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 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 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). 1.08 Vinca alkaloids Vinblastine IV Microtubule assembly inhibitor. Arrests cells in M phase. Hodgkin lymphoma, germ cell tumours, non-small cell lung cancer, bladder cancer and primary immune thrombocytopenia Neurotoxicity, myelosuppression, myocardial ischaemia (rare) and myocardial infarction (rare). Vincristine IV As above. Lymphomas, acute lymphoblastic leukaemia, multiple myeloma, sarcoma, brain tumours, Wilms' tumour, neuroblastoma and primary immune thrombocytopenia Neurotoxicity, anaphylaxis (rare), myocardial ischaemia (rare) and myocardial infarction (rare). Vindesine IV As above. Refractory metastatic melanoma, childhood acute lymphoblastic leukaemia, chronic myeloid leukaemia in blast crises, neuroblastoma, non-small cell lung cancer and breast cancer. Myelosuppression, neurotoxicity and paralytic ileus. Vinflunine IV As above. Bladder cancer As per vinblastine. Vinorelbine IV As above. Breast cancer and non-small cell lung cancer. As above. 1.09 Alkylating agentsAltretaminePOAlkylates DNA.Recurrent or advanced ovarian cancerMyelosuppression, peripheral neuropathy, seizures and hepatotoxicity (rare). Bendamustine IV Alkylates DNA. Chronic lymphocytic leukaemia, mantle cell lymphoma and non-Hodgkin's lymphoma. Myelosuppression, hypokalaemia and tachycardia. Busulfan IV, PO Alkylates DNA. Conditioning treatment before haematopoietic stem cell transplantation (high dose, IV), chronic myeloid leukaemia, myelofibrosis, polycythaemia vera and 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. Carmustine 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 infec