Antineoplastic Agents, Alkylating

A class of drugs that differs from other alkylating agents used clinically in that they are monofunctional and thus unable to cross-link cellular macromolecules. Among their common properties are a requirement for metabolic activation to intermediates with antitumor efficacy and the presence in their chemical structures of N-methyl groups, that after metabolism, can covalently modify cellular DNA. The precise mechanisms by which each of these drugs acts to kill tumor cells are not completely understood. (From AMA, Drug Evaluations Annual, 1994, p2026)
DrugDrug NameDrug Description
DB00236PipobromanFor the treatment of polycythaemia vera and refractory chronic myeloid leukaemia.
DB00262CarmustineAn alkylating agent used in the treatment of various malignancies, including brain tumours and multiple myeloma, among others.
DB00291ChlorambucilA chemotherapy agent used in the management of chronic lymphocytic leukemia and malignant lymphomas.
DB00488AltretamineAn antineoplastic agent used in palliative treatment of persistent or recurrent ovarian cancer.
DB00531CyclophosphamideA nitrogen mustard used to treat lymphomas, myelomas, leukemia, mycosis fungoides, neuroblastoma, ovarian adenocarcinoma, retinoblastoma, and breast carcinoma.
DB00791Uracil mustardUsed for its antineoplastic properties.
DB00851DacarbazineAn antineoplastic agent used to treat malignant melanoma and Hodgkin's disease.
DB00853TemozolomideAn alkylating agent used to treat glioblastoma multiforme and refractory anaplastic astrocytoma.
DB00888MechlorethamineAn antineoplastic agent used to treat Hodgkin's disease, lymphosarcoma, and chronic myelocytic or lymphocytic leukemia.
DB01008BusulfanAn alkylating agent used to treat chronic myelogenous leukemia.
DB01042MelphalanAn alkylating antineoplastic agent used to treat multiple myeloma and ovarian carcinoma.
DB01181IfosfamideAn alkylating and immunosuppressive agent used in chemotherapy for the treatment of cancers, including testicular cancer, ovarian cancer, cervical cancer, osteocarcinoma, bladder cancer, small cell lung cancer, and non-Hodgkin's lymphoma.
DB01196EstramustineAn antineoplastic agent used for the management of metastatic and/or progressive prostate cancer in palliative setting.
DB01206LomustineAn alkylating agent used as a part of chemotherapeutic regimens for the treatment of primary and metastatic brain tumors as well as refractory or relapsed Hodgkin's disease in addition to surgical and/or radiotherapeutic treatments.
DB04572ThiotepaAn alkylating agent used to prevent graft rejection in stem cell transplantation and to treat a variety of malignancies including certain types of adenocarcinoma and superficial bladder carcinomas.
DB05109TrabectedinAn alkylating agent approved for the treatment of unresectable or metastatic soft tissue sarcoma (liposarcoma or leiomyosarcoma).
DB05668PalifosfamideInvestigated for use/treatment in cancer/tumors (unspecified), lymphoma (unspecified), and sarcoma.
DB05786IrofulvenInvestigated for use/treatment in brain cancer, breast cancer, endometrial cancer, liver cancer, lung cancer, ovarian cancer, pancreatic cancer, pediatric indications, prostate cancer, and sarcoma.
DB06769BendamustineAn antineoplastic agent used for the treatment of chronic lymphocytic leukemia (CLL) and indolent B-cell non-Hodgkin lymphoma (NHL) that has progressed following rituximab therapy.
DB11678TreosulfanTreosulfan is under investigation in Allogeneic Haematopoietic Stem Cell Transplantation. Treosulfan has been investigated for the treatment of Lymphoblastic Leukemia, Acute, Childhood.
DB12025TriptolideTriptolide has been used in trials studying the treatment of HIV, Crohn's Disease, Intestinal Diseases, Gastrointestinal Diseases, and Digestive System Diseases, among others.
DB12352BizelesinBizelesin has been used in trials studying the treatment of Unspecified Adult Solid Tumor, Protocol Specific.
DB12832PrednimustinePrednimustine has been used in trials studying the treatment of Lymphoma.
DB12873DianhydrogalactitolDianhydrogalactitol has been used in trials studying the treatment of GBM, Glioma, Glioblastoma, Brain Cancer, and Glioblastoma Multiforme.
DB12902TrofosfamideTrofosfamide has been used in trials studying the treatment of Ependymomas, Medulloblastomas, Sarcoma, Soft Tissue, Supratentorial PNETs, and Recurrent Brain Tumors.
DB12916MitolactolMitolactol has been used in trials studying the treatment of Brain and Central Nervous System Tumors.
DB13304TriaziquoneNot Annotated
DB13339EtoglucidNot Annotated
DB13543MitobronitolNot Annotated
DB13647SemustineNot Annotated
DB13677CarboquoneNot Annotated
DB14031TretamineToxic alkylating agent used in industry; also as antineoplastic and research tool to produce chromosome aberrations and cancers.
DB00428StreptozocinA nitrosourea antineoplastic agent used in the treatment of metastatic pancreatic islet cell carcinoma.
DB15466TallimustineAn alkylating agent previously investigated for it's antitumor activity but was stopped due to severe myelotoxicity.
DrugDrug NameTargetType
DB00236PipobromanDNAtarget
DB00262CarmustineGlutathione reductase, mitochondrialtarget
DB00262CarmustineDNAtarget
DB00262CarmustineRNAtarget
DB00291ChlorambucilDNAtarget
DB00291ChlorambucilGlutathione S-transferase Penzyme
DB00291ChlorambucilSolute carrier organic anion transporter family member 1A2transporter
DB00488AltretamineDNAtarget
DB00531CyclophosphamideDNAtarget
DB00531CyclophosphamideCytochrome P450 2B6enzyme
DB00531CyclophosphamideCytochrome P450 2C9enzyme
DB00531CyclophosphamideCytochrome P450 3A4enzyme
DB00531CyclophosphamideCytochrome P450 2C19enzyme
DB00531CyclophosphamideCytochrome P450 2A6enzyme
DB00531CyclophosphamideCytochrome P450 2C18enzyme
DB00531CyclophosphamideCytochrome P450 2C8enzyme
DB00531CyclophosphamideCytochrome P450 3A5enzyme
DB00531CyclophosphamideNuclear receptor subfamily 1 group I member 2target
DB00791Uracil mustardDNAtarget
DB00851DacarbazineDNA polymerase alpha subunit Btarget
DB00851DacarbazineCytochrome P450 1A1enzyme
DB00851DacarbazineCytochrome P450 1A2enzyme
DB00851DacarbazineCytochrome P450 2E1enzyme
DB00851Dacarbazine6-phosphogluconate dehydrogenase, decarboxylatingtarget
DB00851DacarbazineDNAtarget
DB00853TemozolomideDNAtarget
DB00888MechlorethamineDNAtarget
DB00888MechlorethamineCholinesteraseenzyme
DB01008BusulfanDNAtarget
DB01008BusulfanCytochrome P450 3A4enzyme
DB01008BusulfanGlutathione S-transferase A2enzyme
DB01008BusulfanGlutathione S-transferase A1enzyme
DB01008BusulfanGlutathione S-transferase Mu 1enzyme
DB01008BusulfanGlutathione S-transferase Penzyme
DB01008BusulfanMicrosomal glutathione S-transferase 2enzyme
DB01042MelphalanDNAtarget
DB01042MelphalanSolute carrier family 22 member 3transporter
DB01042MelphalanLarge neutral amino acids transporter small subunit 1transporter
DB01181IfosfamideCytochrome P450 2B6enzyme
DB01181IfosfamideDNAtarget
DB01181IfosfamideCytochrome P450 3A4enzyme
DB01181IfosfamideCytochrome P450 3A5enzyme
DB01181IfosfamideCytochrome P450 2C9enzyme
DB01181IfosfamideCytochrome P450 2C8enzyme
DB01181IfosfamideCytochrome P450 2A6enzyme
DB01181IfosfamideCytochrome P450 2C19enzyme
DB01181IfosfamideCytochrome P450 2C18enzyme
DB01181IfosfamideProstaglandin G/H synthase 1enzyme
DB01181IfosfamideNuclear receptor subfamily 1 group I member 2target
DB01196EstramustineEstrogen receptor betatarget
DB01196EstramustineEstrogen receptor alphatarget
DB01196EstramustineMicrotubule-associated protein 2target
DB01196EstramustineMicrotubule-associated protein 1Atarget
DB01196EstramustineP-glycoprotein 1transporter
DB01196EstramustineCytochrome P450 3A4enzyme
DB01206LomustineDNAtarget
DB01206LomustineCytochrome P450 3A4enzyme
DB01206LomustineCytochrome P450 2D6enzyme
DB01206LomustineStathmin-4target
DB04572ThiotepaCytochrome P450 2B6enzyme
DB04572ThiotepaCytochrome P450 3A4enzyme
DB04572ThiotepaDNAtarget
DB04572ThiotepaCholinesteraseenzyme
DB05109TrabectedinCytochrome P450 3A4enzyme
DB05109TrabectedinCytochrome P450 2C9enzyme
DB05109TrabectedinCytochrome P450 2D6enzyme
DB05109TrabectedinCytochrome P450 2E1enzyme
DB05109TrabectedinCytochrome P450 2C19enzyme
DB05109TrabectedinDNAtarget
DB05109TrabectedinProstaglandin G/H synthase 1enzyme
DB05668PalifosfamideDNA (cytosine-5)-methyltransferase 1target
DB05786IrofulvenFar upstream element-binding protein 1target
DB06769BendamustineCytochrome P450 1A2enzyme
DB14031TretamineCholinesteraseenzyme
DB00428StreptozocinDNAtarget
DB00428StreptozocinP-glycoprotein 1transporter
DB00428StreptozocinSolute carrier family 2, facilitated glucose transporter member 2target
DB00428StreptozocinO-GlcNAcase BT_4395target
DB00428StreptozocinCytochrome P450 1A1enzyme
DB00428StreptozocinCytochrome P450 1A2enzyme
DB00428StreptozocinCytochrome P450 2E1enzyme
DB00428StreptozocinBifunctional protein NCOATtarget
DB15466TallimustineDNAtarget