Alkylating Drugs

Name
Alkylating Drugs
Accession Number
DBCAT003311  (DBCAT000591)
Description

Highly reactive chemicals that introduce alkyl radicals into biologically active molecules and thereby prevent their proper functioning. Many are used as antineoplastic agents, but most are very toxic, with carcinogenic, mutagenic, teratogenic, and immunosuppressant actions. They have also been used as components in poison gases.

ATC Classification
Drugs
DrugDrug Description
PipobromanFor the treatment of polycythaemia vera and refractory chronic myeloid leukaemia.
PrednimustinePrednimustine has been used in trials studying the treatment of Lymphoma.
TrofosfamideTrofosfamide has been used in trials studying the treatment of Ependymomas, Medulloblastomas, Sarcoma, Soft Tissue, Supratentorial PNETs, and Recurrent Brain Tumors.
TreosulfanTreosulfan is under investigation in Allogeneic Haematopoietic Stem Cell Transplantation. Treosulfan has been investigated for the treatment of Lymphoblastic Leukemia, Acute, Childhood.
TriaziquoneNot Annotated
EtoglucidNot Annotated
MitobronitolNot Annotated
SemustineNot Annotated
CarboquoneNot Annotated
Uracil mustardUsed for its antineoplastic properties.
TinidazoleA nitroimidazole used to treat trichomoniasis, giardiasis, amebiasis, and bacterial vaginosis.
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.
TriptolideTriptolide has been used in trials studying the treatment of HIV, Crohn's Disease, Intestinal Diseases, Gastrointestinal Diseases, and Digestive System Diseases, among others.
BizelesinBizelesin has been used in trials studying the treatment of Unspecified Adult Solid Tumor, Protocol Specific.
DianhydrogalactitolDianhydrogalactitol has been used in trials studying the treatment of GBM, Glioma, Glioblastoma, Brain Cancer, and Glioblastoma Multiforme.
MitolactolMitolactol has been used in trials studying the treatment of Brain and Central Nervous System Tumors.
TretamineToxic alkylating agent used in industry; also as antineoplastic and research tool to produce chromosome aberrations and cancers.
FotemustineNot Available
NimustineNimustine has been used in trials studying the treatment of Glioblastoma.
MannosulfanNot Annotated
RanimustineNot Annotated
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.
MitomycinAn antimetabolite used as an adjunct to ab externo (outside approach) eye surgeries for the treatment of glaucoma and used as a chemotherapeutic agent for various malignancies.
StreptozocinA nitrosourea antineoplastic agent used in the treatment of metastatic pancreatic islet cell carcinoma.
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.
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 to treat multiple myeloma and ovarian carcinoma.
ProcarbazineAn antineoplastic agent indicated for the treatment of stage III and stage IV Hodgkin's disease in combination with other chemotherapeutic agents.
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).
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.
TallimustineAn alkylating agent previously investigated for it's antitumor activity but was stopped due to severe myelotoxicity.
Drugs & Drug Targets
DrugTargetType
PipobromanDNAtarget
Uracil mustardDNAtarget
TinidazoleCytochrome P450 3A4enzyme
TinidazoleDNAtarget
TinidazoleBile salt export pumptransporter
PalifosfamideDNA (cytosine-5)-methyltransferase 1target
IrofulvenFar upstream element-binding protein 1target
TretamineCholinesteraseenzyme
FotemustineThioredoxin reductase 1, cytoplasmictarget
CarmustineGlutathione reductase, mitochondrialtarget
CarmustineDNAtarget
CarmustineRNAtarget
ChlorambucilDNAtarget
ChlorambucilGlutathione S-transferase Penzyme
ChlorambucilSolute carrier organic anion transporter family member 1A2transporter
MitomycinDNAtarget
MitomycinNADPH--cytochrome P450 reductaseenzyme
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
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
DacarbazineDNA polymerase alpha subunit Btarget
DacarbazineCytochrome P450 1A1enzyme
DacarbazineCytochrome P450 1A2enzyme
DacarbazineCytochrome P450 2E1enzyme
Dacarbazine6-phosphogluconate dehydrogenase, decarboxylatingtarget
DacarbazineDNAtarget
TemozolomideDNAtarget
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
ProcarbazineDNAtarget
ProcarbazineXanthine dehydrogenase/oxidaseenzyme
ProcarbazineMonoamine oxidasetarget
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
BendamustineCytochrome P450 1A2enzyme
TallimustineDNAtarget