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 Indication
DB00236PipobromanFor the treatment of polycythaemia vera and refractory chronic myeloid leukaemia.
DB00262CarmustineFor the treatment of brain tumors, multiple myeloma, Hodgkin's disease and Non-Hodgkin's lymphomas.
DB00291ChlorambucilFor treatment of chronic lymphatic (lymphocytic) leukemia, childhood minimal-change nephrotic syndrome, and malignant lymphomas including lymphosarcoma, giant follicular lymphoma, Hodgkin's disease, non-Hodgkin's lymphomas, and Waldenström’s Macroglobulinemia.
DB00488AltretamineFor use as a single agent in the palliative treatment of patients with persistent or recurrent ovarian cancer following first-line therapy with a cisplatin and/or alkylating agent-based combination.
DB00531CyclophosphamideCyclophosphamide is indicated for the treatment of malignant lymphomas, multiple myeloma, leukemias, mycosis fungoides (advanced disease), neuroblastoma (disseminated disease), adenocarcinoma of the ovary, retinoblastoma, and carcinoma of the breast. It is also indicated for the treatment of biopsy-proven minimal change nephrotic syndrome in pediatric patients.
DB00791Uracil mustardUsed for its antineoplastic properties.
DB00851DacarbazineFor the treatment of metastatic malignant melanoma. In addition, dacarbazine is also indicated for Hodgkin's disease as a secondary-line therapy when used in combination with other antineoplastic agents.
DB00853TemozolomideFor the treatment of adult patients diagnosed with anaplastic astrocytoma whose disease has progressed after therapy with nitrosourea and procarbazine, as well as concomitantly with radiation therapy for treatment of newly diagnosed glioblastoma multiforme. Also used as maintenance therapy for glioblastoma multiforme.
DB00888MechlorethamineFor the palliative treatment of Hodgkin's disease (Stages III and IV), lymphosarcoma, chronic myelocytic or chronic lymphocytic leukemia, polycythemia vera, mycosis fungoides, and bronchogenic carcinoma. Also for the palliative treatment of metastatic carcinoma resulting in effusion.
DB01008BusulfanFor use in combination with cyclophosphamide as a conditioning regimen prior to allogeneic hematopoietic progenitor cell transplantation for chronic myelogenous (myeloid, myelocytic, granulocytic) leukemia (FDA has designated busulfan as an orphan drug for this use). It is also used as a component of pretransplant conditioning regimens in patients undergoing bone marrow transplantation for acute myeloid leukemia and nonmalignant diseases.
DB01042MelphalanFor the palliative treatment of multiple myeloma and for the palliation of non-resectable epithelial carcinoma of the ovary. Has also been used alone or as part of various chemotherapeutic regimens as an adjunct to surgery in the treatment of breast cancer, alone or in combination regimens for palliative treatment of locally recurrent or unresectable in-transit metastatic melanoma of the extremities, as well as for the treatment of amyloidosis with prednisone.
DB01181IfosfamideUsed as a component of various chemotherapeutic regimens as third-line therapy for recurrent or refractory germ cell testicular cancer. Also used as a component of various chemotherapeutic regimens for the treatment of cervical cancer, as well as in conjunction with surgery and/or radiation therapy in the treatment of various soft tissue sarcomas. Other indications include treatment of osteosarcoma, bladder cancer, ovarian cancer. small cell lung cancer, and non-Hodgkin's lymphoma.
DB01196EstramustineFor the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate
DB01206LomustineFor the treatment of primary and metastatic brain tumors as a component of combination chemotherapy in addition to appropriate surgical and/or radiotherapeutic procedures. Also used in combination with other agents as secondary therapy for the treatment of refractory or relapsed Hodgkin's disease.
DB04572ThiotepaThioTEPA is used a as conditioning treatment prior to allogeneic or autologous haematopoietic progenitor cell transplantation (HPCT) in haematological diseases in adult and paediatric patients. Also, when high dose chemotherapy with HPCT support it is appropriate for the treatment of solid tumours in adult and paediatric patients.
DB05109TrabectedinIndicated for treatment of advanced soft tissue sarcoma in patients refractory to or unsuitable to receive anthracycline or ifosfamide chemotherapy in Europe, Russia and South Korea. Approved for orphan drug status by the U.S. FDA for treatment of soft tissue sarcomas and ovarian cancer. Investigated for use/treatment in cancer/tumors (unspecified), gastric cancer, ovarian cancer, pediatric indications, sarcoma, and solid tumors.
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.
DB06769BendamustineBendamustine is indicated for use in the treatment of chronic lymphocytic leukemia (CLL) and indolent B-cell non-Hodgkin lymphoma (NHL) that has progressed during or within six months of treatment with rituximab or a rituximab-containing regimen.
DB11678TreosulfanNot Available
DB12025TriptolideNot Available
DB12352BizelesinNot Available
DB12832PrednimustineNot Available
DB12873DianhydrogalactitolNot Available
DB12902TrofosfamideNot Available
DB12916MitolactolNot Available
DB13304TriaziquoneNot Available
DB13339EtoglucidNot Available
DB13543MitobronitolNot Available
DB13647SemustineNot Available
DB13677CarboquoneNot Available
DB14031TretamineNot Available
DB00428StreptozocinFor the treatment of malignant neoplasms of pancreas (metastatic islet cell carcinoma).
DrugDrug NameTargetType
DB00262CarmustineGlutathione reductase, mitochondrialtarget
DB00262CarmustineCytochrome P450 1A2enzyme
DB00291ChlorambucilGlutathione S-transferase Penzyme
DB00291ChlorambucilSolute carrier organic anion transporter family member 1A2transporter
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
DB00853TemozolomideCytochrome P450 3A4enzyme
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
DB01042MelphalanSolute carrier family 22 member 3transporter
DB01042MelphalanLarge neutral amino acids transporter small subunit 1transporter
DB01181IfosfamideCytochrome P450 2B6enzyme
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
DB01196EstramustineMultidrug resistance protein 1transporter
DB01196EstramustineCytochrome P450 3A4enzyme
DB01206LomustineCytochrome P450 3A4enzyme
DB01206LomustineCytochrome P450 2D6enzyme
DB04572ThiotepaCytochrome P450 2B6enzyme
DB04572ThiotepaCytochrome P450 3A4enzyme
DB05109TrabectedinCytochrome P450 3A4enzyme
DB05109TrabectedinCytochrome P450 2C9enzyme
DB05109TrabectedinCytochrome P450 2D6enzyme
DB05109TrabectedinCytochrome P450 2E1enzyme
DB05109TrabectedinCytochrome P450 2C19enzyme
DB05109TrabectedinProstaglandin G/H synthase 1enzyme
DB05668PalifosfamideDNA (cytosine-5)-methyltransferase 1target
DB05786IrofulvenFar upstream element-binding protein 1target
DB06769BendamustineCytochrome P450 1A2enzyme
DB00428StreptozocinMultidrug resistance protein 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