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
AdozelesinAdozelesin is a small molecule drug. Adozelesin has a monoisotopic molecular weight of 502.16 Da.
AltretamineAn antineoplastic agent used in palliative treatment of persistent or recurrent ovarian cancer.
BendamustineAn antineoplastic nitrogen mustard agent used in the treatment of indolent B-cell non-Hodgkin lymphoma (NHL) that has progressed following rituximab therapy.
BizelesinBizelesin has been used in trials studying the treatment of Unspecified Adult Solid Tumor, Protocol Specific.
BusulfanAn alkylating agent used to treat chronic myelogenous leukemia.
CarboquoneNot Annotated
CarmustineAn alkylating agent used in the treatment of various malignancies, including brain tumours and multiple myeloma, among others.
CarzelesinCarzelesin is a small molecule drug. Carzelesin has a monoisotopic molecular weight of 728.25 Da.
ChlorambucilA chemotherapy agent used in the management of chronic lymphocytic leukemia and malignant lymphomas.
CyclophosphamideA nitrogen mustard used to treat lymphomas, myelomas, leukemia, mycosis fungoides, neuroblastoma, ovarian adenocarcinoma, retinoblastoma, and breast carcinoma.
DacarbazineAn antineoplastic agent used to treat malignant melanoma and Hodgkin's disease.
DianhydrogalactitolDianhydrogalactitol has been used in trials studying the treatment of GBM, Glioma, Glioblastoma, Brain Cancer, and Glioblastoma Multiforme.
EstramustineAn antineoplastic agent used for the management of metastatic and/or progressive prostate cancer in palliative setting.
Estramustine phosphateA nitrogen mustard linked to estradiol, usually as phosphate; used to treat prostatic neoplasms; also has radiation protective properties.
EtoglucidNot Annotated
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.
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.
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.
MannomustineMannomustine is a small molecule drug. The usage of the INN stem '-mustine' in the name indicates that Mannomustine is a antineoplastic, alkylating agent, (β-chloroethyl) amine derivative. Mannomustine has a...
MechlorethamineAn antineoplastic agent used to treat Hodgkin's disease, lymphosarcoma, and chronic myelocytic or lymphocytic leukemia.
MelphalanAn alkylating agent used to treat multiple myeloma, ovarian carcinoma, uveal melanoma with unresectable hepatic metastases, and for high-dose conditioning before hematopoietic stem cell transplant in patients.
Melphalan flufenamideA melphalan prodrug used to treat relapsed or refractory multiple myeloma.
MinnelideNot Annotated
Minnelide free acidNot Annotated
MitobronitolNot Annotated
MitolactolMitolactol has been used in trials studying the treatment of Brain and Central Nervous System Tumors.
PalifosfamideInvestigated for use/treatment in cancer/tumors (unspecified), lymphoma (unspecified), and sarcoma.
PipobromanFor the treatment of polycythaemia vera and refractory chronic myeloid leukaemia.
PrednimustinePrednimustine has been used in trials studying the treatment of Lymphoma.
SemustineNot Annotated
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.
TemozolomideAn alkylating agent used to treat glioblastoma multiforme and refractory anaplastic astrocytoma.
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).
TreosulfanA DNA alkylating agent used in the context of myeloablative conditioning prior to allogeneic hemoatopoietic stem cell transplantation.
TretamineToxic alkylating agent used in industry; also as antineoplastic and research tool to produce chromosome aberrations and cancers.
TriaziquoneNot Annotated
TriptolideTriptolide has been used in trials studying the treatment of HIV, Crohn's Disease, Intestinal Diseases, Gastrointestinal Diseases, and Digestive System Diseases, among others.
TrofosfamideTrofosfamide has been used in trials studying the treatment of Ependymomas, Medulloblastomas, Sarcoma, Soft Tissue, Supratentorial PNETs, and Recurrent Brain Tumors.
Uracil mustardUsed for its antineoplastic properties.
Drugs & Drug Targets
DrugTargetType
AltretamineDNAtarget
BendamustineDNAtarget
BendamustineCytochrome P450 1A2enzyme
BusulfanDNAtarget
BusulfanGlutathione S-transferase A2enzyme
BusulfanMicrosomal glutathione S-transferase 2enzyme
BusulfanGlutathione S-transferase Penzyme
BusulfanGlutathione S-transferase Mu 1enzyme
BusulfanGlutathione S-transferase A1enzyme
BusulfanCytochrome P450 3A4enzyme
CarmustineDNAtarget
CarmustineRNAtarget
CarmustineGlutathione reductase, mitochondrialtarget
ChlorambucilDNAtarget
ChlorambucilGlutathione S-transferase Penzyme
ChlorambucilSolute carrier organic anion transporter family member 1A2transporter
ChlorambucilGlutathione S-transferases (Cytosolic)enzyme
CyclophosphamideDNAtarget
CyclophosphamideCytochrome P450 2B6enzyme
CyclophosphamideCytochrome P450 2C9enzyme
CyclophosphamideCytochrome P450 3A4enzyme
CyclophosphamideCytochrome P450 2C19enzyme
CyclophosphamideCytochrome P450 2A6enzyme
CyclophosphamideCytochrome P450 2C18enzyme
CyclophosphamideCytochrome P450 3A5enzyme
CyclophosphamideNuclear receptor subfamily 1 group I member 2target
CyclophosphamideCytochrome P450 2C8enzyme
DacarbazineDNA polymerase alpha subunit Btarget
DacarbazineCytochrome P450 1A1enzyme
DacarbazineCytochrome P450 1A2enzyme
DacarbazineCytochrome P450 2E1enzyme
Dacarbazine6-phosphogluconate dehydrogenase, decarboxylatingtarget
DacarbazineDNAtarget
EstramustineMicrotubule-associated protein 1Atarget
EstramustineCytochrome P450 3A4enzyme
EstramustineATP-dependent translocase ABCB1transporter
EstramustineMicrotubule-associated protein 2target
EstramustineEstrogen receptortarget
EstramustineEstrogen receptor betatarget
Estramustine phosphateAndrogen receptortarget
Estramustine phosphateMicrotubule-associated protein 2target
Estramustine phosphateMicrotubule-associated protein tautarget
Estramustine phosphateTyrosine-protein phosphatase non-receptor type 11target
IfosfamideCytochrome P450 2A6enzyme
IfosfamideNuclear receptor subfamily 1 group I member 2target
IfosfamideProstaglandin G/H synthase 1enzyme
IfosfamideCytochrome P450 2B6enzyme
IfosfamideDNAtarget
IfosfamideCytochrome P450 3A4enzyme
IfosfamideCytochrome P450 3A5enzyme
IfosfamideCytochrome P450 2C9enzyme
IfosfamideCytochrome P450 2C8enzyme
IfosfamideCytochrome P450 2C18enzyme
IfosfamideCytochrome P450 2C19enzyme
IrofulvenFar upstream element-binding protein 1target
IrofulvenSerine/threonine-protein kinase Chk2target
LomustineDNAtarget
LomustineCytochrome P450 3A4enzyme
LomustineCytochrome P450 2D6enzyme
LomustineStathmin-4target
MechlorethamineCholinesteraseenzyme
MechlorethamineDNAtarget
MelphalanAsc-type amino acid transporter 1transporter
MelphalanAlpha-1-acid glycoprotein 1carrier
MelphalanAlbumincarrier
MelphalanLarge neutral amino acids transporter small subunit 1transporter
MelphalanSolute carrier family 22 member 3transporter
MelphalanDNAtarget
Melphalan flufenamideDNAtarget
Melphalan flufenamideAminopeptidase Nenzyme
MinnelideHeat shock 70 kDa protein 1Btarget
MinnelideHeat shock 70 kDa protein 1Atarget
PalifosfamideDNA (cytosine-5)-methyltransferase 1target
PipobromanDNAtarget
PrednimustineHuman Carboxylesterasesenzyme
SemustineCytochrome P450 1A2enzyme
SemustineCytochrome P450 1A1enzyme
SemustineCytochrome P450 2B1enzyme
SemustineCytochrome P450 2A1enzyme
StreptozocinProtein O-GlcNAcasetarget
StreptozocinCytochrome P450 2E1enzyme
StreptozocinCytochrome P450 1A2enzyme
StreptozocinCytochrome P450 1A1enzyme
StreptozocinO-GlcNAcase BT_4395target
StreptozocinSolute carrier family 2, facilitated glucose transporter member 2target
StreptozocinATP-dependent translocase ABCB1transporter
StreptozocinDNAtarget
TallimustineC-X-C chemokine receptor type 2target
TallimustineDNAtarget
TemozolomideDNAtarget
TemozolomideAlbumincarrier
TemozolomideAlpha-1-acid glycoprotein 1carrier
TemozolomideATP-dependent translocase ABCB1transporter
TemozolomideBroad substrate specificity ATP-binding cassette transporter ABCG2transporter
ThiotepaDNAtarget
ThiotepaCytochrome P450 3A4enzyme
ThiotepaCytochrome P450 2B6enzyme
ThiotepaCholinesteraseenzyme
TrabectedinCytochrome P450 3A4enzyme
TrabectedinProstaglandin G/H synthase 1enzyme
TrabectedinDNAtarget
TrabectedinCytochrome P450 2C19enzyme
TrabectedinCytochrome P450 2E1enzyme
TrabectedinCytochrome P450 2D6enzyme
TrabectedinCytochrome P450 2C9enzyme
TreosulfanCytochrome P450 3A4enzyme
TreosulfanCytochrome P450 2C19enzyme
TreosulfanCytochrome P450 2C8enzyme
TreosulfanCytochrome P450 2D6enzyme
TreosulfanDNAtarget
TretamineCholinesteraseenzyme
TriptolidePeroxiredoxin-5, mitochondrialtarget
TriptolideTranscription factor RelBtarget
TriptolideProto-oncogene c-Reltarget
TriptolideTranscription factor p65target
TriptolideNuclear factor NF-kappa-B p100 subunittarget
TriptolideNuclear factor NF-kappa-B p105 subunittarget
TrofosfamideCytochrome P450enzyme
TrofosfamideCytochrome P450 3A4enzyme
TrofosfamideCytochrome P450 2B6enzyme
Uracil mustardDNAtarget