Antineoplastic Agents, Alkylating

Name
Antineoplastic Agents, Alkylating
Accession Number
DBCAT000592
Description

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)

Drugs
DrugDrug Description
PipobromanFor the treatment of polycythaemia vera and refractory chronic myeloid leukaemia.
CarmustineAn alkylating agent used in the treatment of various malignancies, including brain tumours and multiple myeloma, among others.
ChlorambucilA chemotherapy agent used in the management of chronic lymphocytic leukemia and malignant lymphomas.
AltretamineAn antineoplastic agent used in palliative treatment of persistent or recurrent ovarian cancer.
CyclophosphamideA nitrogen mustard used to treat lymphomas, myelomas, leukemia, mycosis fungoides, neuroblastoma, ovarian adenocarcinoma, retinoblastoma, and breast carcinoma.
Uracil mustardUsed for its antineoplastic properties.
DacarbazineAn antineoplastic agent used to treat malignant melanoma and Hodgkin's disease.
TemozolomideAn alkylating agent used to treat glioblastoma multiforme and refractory anaplastic astrocytoma.
MechlorethamineAn antineoplastic agent used to treat Hodgkin's disease, lymphosarcoma, and chronic myelocytic or lymphocytic leukemia.
BusulfanAn alkylating agent used to treat chronic myelogenous leukemia.
MelphalanAn alkylating antineoplastic agent used for high-dose conditioning prior to hematopoietic stem cell transplant in patients with multiple myeloma.
IfosfamideAn 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.
EstramustineAn antineoplastic agent used for the management of metastatic and/or progressive prostate cancer in palliative setting.
LomustineAn 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.
ThiotepaAn 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.
TrabectedinAn alkylating agent approved for the treatment of unresectable or metastatic soft tissue sarcoma (liposarcoma or leiomyosarcoma).
PalifosfamideInvestigated for use/treatment in cancer/tumors (unspecified), lymphoma (unspecified), and sarcoma.
IrofulvenInvestigated for use/treatment in brain cancer, breast cancer, endometrial cancer, liver cancer, lung cancer, ovarian cancer, pancreatic cancer, pediatric indications, prostate cancer, and sarcoma.
BendamustineAn 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.
TreosulfanTreosulfan is under investigation in Allogeneic Haematopoietic Stem Cell Transplantation. Treosulfan has been investigated for the treatment of Lymphoblastic Leukemia, Acute, Childhood.
TriptolideTriptolide has been used in trials studying the treatment of HIV, Crohn's Disease, Intestinal Diseases, Gastrointestinal Diseases, and Digestive System Diseases, among others.
PrednimustinePrednimustine has been used in trials studying the treatment of Lymphoma.
DianhydrogalactitolDianhydrogalactitol has been used in trials studying the treatment of GBM, Glioma, Glioblastoma, Brain Cancer, and Glioblastoma Multiforme.
TrofosfamideTrofosfamide has been used in trials studying the treatment of Ependymomas, Medulloblastomas, Sarcoma, Soft Tissue, Supratentorial PNETs, and Recurrent Brain Tumors.
MitolactolMitolactol has been used in trials studying the treatment of Brain and Central Nervous System Tumors.
TriaziquoneNot Annotated
EtoglucidNot Annotated
MitobronitolNot Annotated
SemustineNot Annotated
CarboquoneNot Annotated
TretamineToxic alkylating agent used in industry; also as antineoplastic and research tool to produce chromosome aberrations and cancers.
StreptozocinA nitrosourea antineoplastic agent used in the treatment of metastatic pancreatic islet cell carcinoma.
TallimustineAn alkylating agent previously investigated for it's antitumor activity but was stopped due to severe myelotoxicity.
Melphalan flufenamideA melphalan prodrug used to treat relapsed or refractory multiple myeloma.
Estramustine phosphateA nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.
BizelesinBizelesin has been used in trials studying the treatment of Unspecified Adult Solid Tumor, Protocol Specific.
Drugs & Drug Targets
DrugTargetType
PipobromanDNAtarget
CarmustineGlutathione reductase, mitochondrialtarget
CarmustineDNAtarget
CarmustineRNAtarget
ChlorambucilDNAtarget
ChlorambucilGlutathione S-transferase Penzyme
ChlorambucilSolute carrier organic anion transporter family member 1A2transporter
ChlorambucilGlutathione S-transferases (Cytosolic)enzyme
AltretamineDNAtarget
CyclophosphamideDNAtarget
CyclophosphamideCytochrome P450 2B6enzyme
CyclophosphamideCytochrome P450 2C9enzyme
CyclophosphamideCytochrome P450 3A4enzyme
CyclophosphamideCytochrome P450 2C19enzyme
CyclophosphamideCytochrome P450 2A6enzyme
CyclophosphamideCytochrome P450 2C18enzyme
CyclophosphamideCytochrome P450 2C8enzyme
CyclophosphamideCytochrome P450 3A5enzyme
CyclophosphamideNuclear receptor subfamily 1 group I member 2target
Uracil mustardDNAtarget
DacarbazineDNA polymerase alpha subunit Btarget
DacarbazineCytochrome P450 1A1enzyme
DacarbazineCytochrome P450 1A2enzyme
DacarbazineCytochrome P450 2E1enzyme
Dacarbazine6-phosphogluconate dehydrogenase, decarboxylatingtarget
DacarbazineDNAtarget
TemozolomideDNAtarget
TemozolomideSerum albumincarrier
TemozolomideAlpha-1-acid glycoprotein 1carrier
TemozolomideP-glycoprotein 1transporter
TemozolomideATP-binding cassette sub-family G member 2transporter
MechlorethamineDNAtarget
MechlorethamineCholinesteraseenzyme
BusulfanDNAtarget
BusulfanCytochrome P450 3A4enzyme
BusulfanGlutathione S-transferase A2enzyme
BusulfanGlutathione S-transferase A1enzyme
BusulfanGlutathione S-transferase Mu 1enzyme
BusulfanGlutathione S-transferase Penzyme
BusulfanMicrosomal glutathione S-transferase 2enzyme
MelphalanDNAtarget
MelphalanSolute carrier family 22 member 3transporter
MelphalanLarge neutral amino acids transporter small subunit 1transporter
IfosfamideCytochrome P450 2B6enzyme
IfosfamideDNAtarget
IfosfamideCytochrome P450 3A4enzyme
IfosfamideCytochrome P450 3A5enzyme
IfosfamideCytochrome P450 2C9enzyme
IfosfamideCytochrome P450 2C8enzyme
IfosfamideCytochrome P450 2A6enzyme
IfosfamideCytochrome P450 2C19enzyme
IfosfamideCytochrome P450 2C18enzyme
IfosfamideProstaglandin G/H synthase 1enzyme
IfosfamideNuclear receptor subfamily 1 group I member 2target
EstramustineEstrogen receptor betatarget
EstramustineEstrogen receptor alphatarget
EstramustineMicrotubule-associated protein 2target
EstramustineMicrotubule-associated protein 1Atarget
EstramustineP-glycoprotein 1transporter
EstramustineCytochrome P450 3A4enzyme
LomustineDNAtarget
LomustineCytochrome P450 3A4enzyme
LomustineCytochrome P450 2D6enzyme
LomustineStathmin-4target
ThiotepaCytochrome P450 2B6enzyme
ThiotepaCytochrome P450 3A4enzyme
ThiotepaDNAtarget
ThiotepaCholinesteraseenzyme
TrabectedinCytochrome P450 3A4enzyme
TrabectedinCytochrome P450 2C9enzyme
TrabectedinCytochrome P450 2D6enzyme
TrabectedinCytochrome P450 2E1enzyme
TrabectedinCytochrome P450 2C19enzyme
TrabectedinDNAtarget
TrabectedinProstaglandin G/H synthase 1enzyme
PalifosfamideDNA (cytosine-5)-methyltransferase 1target
IrofulvenFar upstream element-binding protein 1target
BendamustineCytochrome P450 1A2enzyme
TretamineCholinesteraseenzyme
StreptozocinDNAtarget
StreptozocinP-glycoprotein 1transporter
StreptozocinSolute carrier family 2, facilitated glucose transporter member 2target
StreptozocinO-GlcNAcase BT_4395target
StreptozocinCytochrome P450 1A1enzyme
StreptozocinCytochrome P450 1A2enzyme
StreptozocinCytochrome P450 2E1enzyme
StreptozocinBifunctional protein NCOATtarget
TallimustineDNAtarget
Melphalan flufenamideAminopeptidase Nenzyme
Melphalan flufenamideDNAtarget