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Identification
NameDactinomycin
Accession NumberDB00970  (APRD00124)
TypeSmall Molecule
GroupsApproved
DescriptionA compound composed of a two cyclic peptides attached to a phenoxazine that is derived from streptomyces parvullus. It binds to DNA and inhibits RNA synthesis (transcription), with chain elongation more sensitive than initiation, termination, or release. As a result of impaired mRNA production, protein synthesis also declines after dactinomycin therapy. (From AMA Drug Evaluations Annual, 1993, p2015)
Structure
Thumb
Synonyms
2-amino-N,N'-bis(hexadecahydro-2,5,9-trimethyl-6,13-bis(1-methylethyl)-1,4,7,11,14-pentaoxo-1H-pyrrolo(2,1-I)(1,4,7,10,13)oxatetra-azacyclohexadecin-10-yl)-4,6-dimethyl-3-oxo-3H-phenoxazine-1,9-dicarboxamide
ActD
Actinomycin C1
Actinomycin D
Actinomycin iv
Dactinomicina
Dactinomycin
Dactinomycine
Dactinomycinum
Meractinomycin
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CosmegenInjection, powder, lyophilized, for solution.5 mg/mLIntravenousRECORDATI RARE DISEASES, INC.1964-12-10Not applicableUs
CosmegenPowder, for solution0.5 mgIntravenousRecordati Rare Diseases Inc1963-12-31Not applicableCanada
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
Lyovac CosmegenLundbeck
Brand mixturesNot Available
SaltsNot Available
Categories
UNII1CC1JFE158
CAS number50-76-0
WeightAverage: 1255.417
Monoisotopic: 1254.628474764
Chemical FormulaC62H86N12O16
InChI KeyRJURFGZVJUQBHK-IIXSONLDSA-N
InChI
InChI=1S/C62H86N12O16/c1-27(2)42-59(84)73-23-17-19-36(73)57(82)69(13)25-38(75)71(15)48(29(5)6)61(86)88-33(11)44(55(80)65-42)67-53(78)35-22-21-31(9)51-46(35)64-47-40(41(63)50(77)32(10)52(47)90-51)54(79)68-45-34(12)89-62(87)49(30(7)8)72(16)39(76)26-70(14)58(83)37-20-18-24-74(37)60(85)43(28(3)4)66-56(45)81/h21-22,27-30,33-34,36-37,42-45,48-49H,17-20,23-26,63H2,1-16H3,(H,65,80)(H,66,81)(H,67,78)(H,68,79)/t33-,34-,36+,37+,42-,43-,44+,45+,48+,49+/m1/s1
IUPAC Name
N1,N9-bis[(6S,9R,10S,13R,18aS)-2,5,9-trimethyl-1,4,7,11,14-pentaoxo-6,13-bis(propan-2-yl)-hexadecahydro-1H-pyrrolo[2,1-i]1-oxa-4,7,10,13-tetraazacyclohexadecan-10-yl]-2-amino-4,6-dimethyl-3-oxo-3H-phenoxazine-1,9-dicarboxamide
SMILES
[H][C@@]12CCCN1C(=O)[[email protected]](NC(=O)[C@@H](NC(=O)C1=C3N=C4C(OC3=C(C)C=C1)=C(C)C(=O)C(N)=C4C(=O)N[[email protected]]1[C@@H](C)OC(=O)[[email protected]](C(C)C)N(C)C(=O)CN(C)C(=O)[C@]3([H])CCCN3C(=O)[[email protected]](NC1=O)C(C)C)[C@@H](C)OC(=O)[[email protected]](C(C)C)N(C)C(=O)CN(C)C2=O)C(C)C
Pharmacology
IndicationFor the treatment of Wilms' tumor, childhood rhabdomyosarcoma, Ewing's sarcoma and metastatic, nonseminomatous testicular cancer as part of a combination chemotherapy and/or multi-modality treatment regimen
Structured Indications
PharmacodynamicsGenerally, the actinomycins exert an inhibitory effect on gram-positive and gram-negative bacteria and on some fungi. However, the toxic properties of the actinomycins (including dactinomycin) in relation to antibacterial activity are such as to preclude their use as antibiotics in the treatment of infectious diseases. Because the actinomycins are cytotoxic, they have an antineoplastic effect which has been demonstrated in experimental animals with various types of tumor implant. This cytotoxic action is the basis for their use in the treatment of certain types of cancer. Dactinomycin is believed to produce its cytotoxic effects by binding DNA and inhibiting RNA synthesis.
Mechanism of actionGood evidence exists that this drug bind strongly, but reversibly, to DNA, interfering with synthesis of RNA (prevention of RNA polymerase elongation) and, consequently, with protein synthesis.
TargetKindPharmacological actionActionsOrganismUniProt ID
DNANucleotideyes
adduct
Humannot applicabledetails
DNA topoisomerase 2Protein groupunknownNot AvailableHomo sapiensnot applicabledetails
Related Articles
Absorptionpoorly absorbed from gastrointestinal tract
Volume of distributionNot Available
Protein binding5%
Metabolism

hepatic

Route of eliminationNot Available
Half life36 hours
ClearanceNot Available
Toxicityhepatoxicity
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Dactinomycin.Approved
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Dactinomycin.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Dactinomycin.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Dactinomycin.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Dactinomycin.Approved
AlbendazoleThe serum concentration of Dactinomycin can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Dactinomycin can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Dactinomycin can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Dactinomycin can be increased when it is combined with Alfentanil.Approved, Illicit
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Dactinomycin.Approved, Investigational
ALT-110The risk or severity of adverse effects can be increased when Dactinomycin is combined with ALT-110.Investigational
AmantadineThe serum concentration of Dactinomycin can be increased when it is combined with Amantadine.Approved
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Dactinomycin.Approved, Investigational
Aminohippuric acidThe serum concentration of Dactinomycin can be increased when it is combined with Aminohippuric acid.Approved
AmiodaroneThe serum concentration of Dactinomycin can be decreased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Dactinomycin.Approved
AmlodipineThe serum concentration of Dactinomycin can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Dactinomycin can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Dactinomycin can be increased when it is combined with Amsacrine.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Dactinomycin.Investigational
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Dactinomycin.Approved
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Dactinomycin.Approved, Investigational
AstemizoleThe serum concentration of Dactinomycin can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe serum concentration of Atazanavir can be increased when it is combined with Dactinomycin.Approved, Investigational
AtenololThe serum concentration of Atenolol can be increased when it is combined with Dactinomycin.Approved
AtorvastatinThe serum concentration of Dactinomycin can be increased when it is combined with Atorvastatin.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Dactinomycin.Approved, Investigational
AzelastineThe serum concentration of Dactinomycin can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Dactinomycin can be increased when it is combined with Azithromycin.Approved
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Dactinomycin.Investigational
BenzocaineThe serum concentration of Dactinomycin can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Dactinomycin can be increased when it is combined with Bepridil.Approved, Withdrawn
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Dactinomycin.Approved, Vet Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Dactinomycin.Approved, Investigational
BiperidenThe serum concentration of Dactinomycin can be increased when it is combined with Biperiden.Approved
BoceprevirThe serum concentration of Boceprevir can be increased when it is combined with Dactinomycin.Approved
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Dactinomycin.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Dactinomycin.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Dactinomycin.Approved, Investigational
BuprenorphineThe serum concentration of Dactinomycin can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe serum concentration of Dactinomycin can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Dactinomycin.Approved
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Dactinomycin.Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Dactinomycin.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Dactinomycin.Approved
CandesartanThe serum concentration of Dactinomycin can be increased when it is combined with Candesartan.Approved
CaptoprilThe serum concentration of Dactinomycin can be increased when it is combined with Captopril.Approved
CarbamazepineThe serum concentration of Dactinomycin can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Dactinomycin.Approved
CarvedilolThe serum concentration of Dactinomycin can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Dactinomycin can be increased when it is combined with Caspofungin.Approved
CDX-110The risk or severity of adverse effects can be increased when Dactinomycin is combined with CDX-110.Investigational
CeritinibThe serum concentration of Ceritinib can be increased when it is combined with Dactinomycin.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Dactinomycin.Withdrawn
ChloroquineThe serum concentration of Dactinomycin can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe serum concentration of Dactinomycin can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Dactinomycin can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Dactinomycin can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholesterolThe serum concentration of Dactinomycin can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Dactinomycin can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Dactinomycin can be increased when it is combined with Cilazapril.Approved
CimetidineThe serum concentration of Dactinomycin can be decreased when it is combined with Cimetidine.Approved
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Dactinomycin.Approved, Investigational
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Dactinomycin.Approved
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Dactinomycin.Approved
ClarithromycinThe serum concentration of Dactinomycin can be increased when it is combined with Clarithromycin.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Dactinomycin.Approved, Illicit
ClofazimineThe serum concentration of Dactinomycin can be increased when it is combined with Clofazimine.Approved, Investigational
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Dactinomycin.Approved, Investigational
ClomipramineThe serum concentration of Dactinomycin can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Dactinomycin.Approved
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Dactinomycin.Approved, Nutraceutical
ClotrimazoleThe serum concentration of Dactinomycin can be decreased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Dactinomycin is combined with Clozapine.Approved
CobicistatThe serum concentration of Dactinomycin can be increased when it is combined with Cobicistat.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Dactinomycin.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Dactinomycin.Approved
ColforsinThe serum concentration of Dactinomycin can be increased when it is combined with Colforsin.Experimental
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Dactinomycin.Approved
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Dactinomycin.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Dactinomycin.Approved, Investigational
CyclosporineThe serum concentration of Dactinomycin can be decreased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Dactinomycin.Approved
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Dactinomycin.Approved
DaclatasvirThe serum concentration of Dactinomycin can be increased when it is combined with Daclatasvir.Approved
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Dactinomycin.Approved
DasatinibThe serum concentration of Dasatinib can be increased when it is combined with Dactinomycin.Approved, Investigational
DaunorubicinThe serum concentration of Dactinomycin can be decreased when it is combined with Daunorubicin.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Dactinomycin.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Dactinomycin.Approved
DesipramineThe serum concentration of Dactinomycin can be increased when it is combined with Desipramine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Dactinomycin.Approved
DesloratadineThe serum concentration of Dactinomycin can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Dactinomycin can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Dactinomycin can be increased when it is combined with Dextromethorphan.Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Dactinomycin.Approved, Illicit, Vet Approved
DiclofenacThe serum concentration of Dactinomycin can be increased when it is combined with Diclofenac.Approved, Vet Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Dactinomycin.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Dactinomycin.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Dactinomycin.Approved
DihydroergotamineThe serum concentration of Dactinomycin can be increased when it is combined with Dihydroergotamine.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Dactinomycin.Illicit
DiltiazemThe serum concentration of Dactinomycin can be increased when it is combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Dactinomycin can be increased when it is combined with Dipyridamole.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Dactinomycin.Approved, Investigational
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Dactinomycin.Approved, Investigational, Vet Approved
DoxazosinThe serum concentration of Dactinomycin can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Dactinomycin can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Dactinomycin.Approved, Investigational
DoxorubicinThe serum concentration of Dactinomycin can be decreased when it is combined with Doxorubicin.Approved, Investigational
DronabinolThe serum concentration of Dactinomycin can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe serum concentration of Dactinomycin can be increased when it is combined with Dronedarone.Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Dactinomycin.Approved
ElbasvirThe serum concentration of Dactinomycin can be increased when it is combined with Elbasvir.Approved
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Dactinomycin.Approved, Investigational
EltrombopagThe serum concentration of Dactinomycin can be increased when it is combined with Eltrombopag.Approved
EnalaprilThe serum concentration of Dactinomycin can be increased when it is combined with Enalapril.Approved, Vet Approved
EnzalutamideThe serum concentration of Dactinomycin can be increased when it is combined with Enzalutamide.Approved
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Dactinomycin.Approved, Investigational
ErgonovineThe serum concentration of Dactinomycin can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Dactinomycin can be increased when it is combined with Ergotamine.Approved
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Dactinomycin.Approved, Investigational
ErythromycinThe serum concentration of Dactinomycin can be decreased when it is combined with Erythromycin.Approved, Vet Approved
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Dactinomycin.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Dactinomycin can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Dactinomycin can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Dactinomycin can be decreased when it is combined with Estrone.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Dactinomycin.Approved
EtoposideThe serum concentration of Dactinomycin can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Dactinomycin can be increased when it is combined with Etravirine.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Dactinomycin.Approved
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Dactinomycin.Approved
FelodipineThe serum concentration of Dactinomycin can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Dactinomycin can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Dactinomycin.Approved
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Dactinomycin.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Dactinomycin.Approved
FingolimodDactinomycin may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FluconazoleThe serum concentration of Dactinomycin can be increased when it is combined with Fluconazole.Approved
FluoxetineThe serum concentration of Dactinomycin can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Dactinomycin can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Dactinomycin can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Dactinomycin can be increased when it is combined with Flurazepam.Approved, Illicit
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Dactinomycin.Approved
FluvoxamineThe serum concentration of Dactinomycin can be increased when it is combined with Fluvoxamine.Approved, Investigational
G17DTThe risk or severity of adverse effects can be increased when Dactinomycin is combined with G17DT.Investigational
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Dactinomycin.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Dactinomycin.Approved
GenisteinThe serum concentration of Dactinomycin can be increased when it is combined with Genistein.Investigational
GI-5005The risk or severity of adverse effects can be increased when Dactinomycin is combined with GI-5005.Investigational
GlyburideThe serum concentration of Dactinomycin can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Dactinomycin can be increased when it is combined with Glycerol.Experimental
Gramicidin DThe serum concentration of Dactinomycin can be increased when it is combined with Gramicidin D.Approved
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Dactinomycin.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Dactinomycin.Withdrawn
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Dactinomycin.Approved
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Dactinomycin.Approved, Vet Approved
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Dactinomycin.Approved
IdelalisibThe serum concentration of Idelalisib can be increased when it is combined with Dactinomycin.Approved
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Dactinomycin.Approved
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Dactinomycin.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Dactinomycin.Approved
IndinavirThe serum concentration of Dactinomycin can be decreased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Dactinomycin.Approved, Investigational
INGN 201The risk or severity of adverse effects can be increased when Dactinomycin is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Dactinomycin is combined with INGN 225.Investigational
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Dactinomycin.Approved, Investigational
IsavuconazoniumThe serum concentration of Dactinomycin can be increased when it is combined with Isavuconazonium.Approved, Investigational
ItraconazoleThe serum concentration of Dactinomycin can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Dactinomycin can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Dactinomycin.Approved, Vet Approved
KetamineThe serum concentration of Dactinomycin can be increased when it is combined with Ketamine.Approved, Vet Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Dactinomycin.Approved
KetoconazoleThe serum concentration of Dactinomycin can be increased when it is combined with Ketoconazole.Approved, Investigational
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Dactinomycin.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Dactinomycin.Approved, Investigational
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Dactinomycin.Approved, Investigational
LapatinibThe serum concentration of Dactinomycin can be increased when it is combined with Lapatinib.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Dactinomycin.Approved
LeflunomideThe risk or severity of adverse effects can be increased when Dactinomycin is combined with Leflunomide.Approved, Investigational
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Dactinomycin.Approved
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Dactinomycin.Approved
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Dactinomycin.Approved, Investigational
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Dactinomycin.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Dactinomycin.Approved
LevothyroxineThe serum concentration of Dactinomycin can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Dactinomycin can be increased when it is combined with Lidocaine.Approved, Vet Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Dactinomycin.Approved
LiothyronineThe serum concentration of Dactinomycin can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Dactinomycin can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Dactinomycin can be increased when it is combined with Lisinopril.Approved, Investigational
LomitapideThe serum concentration of Dactinomycin can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Dactinomycin.Approved
LopinavirThe serum concentration of Dactinomycin can be increased when it is combined with Lopinavir.Approved
LoratadineThe serum concentration of Dactinomycin can be increased when it is combined with Loratadine.Approved
LosartanThe serum concentration of Losartan can be increased when it is combined with Dactinomycin.Approved
LovastatinThe serum concentration of Dactinomycin can be increased when it is combined with Lovastatin.Approved, Investigational
LumacaftorThe serum concentration of Dactinomycin can be decreased when it is combined with Lumacaftor.Approved
MannitolThe serum concentration of Mannitol can be increased when it is combined with Dactinomycin.Approved, Investigational
MaprotilineThe serum concentration of Dactinomycin can be increased when it is combined with Maprotiline.Approved
MebendazoleThe serum concentration of Dactinomycin can be increased when it is combined with Mebendazole.Approved, Vet Approved
MefloquineThe serum concentration of Dactinomycin can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Dactinomycin can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Dactinomycin can be increased when it is combined with Meprobamate.Approved, Illicit
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Dactinomycin.Withdrawn
MethadoneThe serum concentration of Dactinomycin can be increased when it is combined with Methadone.Approved
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Dactinomycin.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Dactinomycin.Approved, Vet Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Dactinomycin.Approved, Investigational
MibefradilThe serum concentration of Dactinomycin can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Dactinomycin can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Dactinomycin can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Dactinomycin can be decreased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Dactinomycin.Approved
MitomycinThe serum concentration of Dactinomycin can be increased when it is combined with Mitomycin.Approved
MitoxantroneThe serum concentration of Dactinomycin can be decreased when it is combined with Mitoxantrone.Approved, Investigational
MorphineThe serum concentration of Morphine can be increased when it is combined with Dactinomycin.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Dactinomycin.Approved, Investigational
NadololThe serum concentration of Nadolol can be increased when it is combined with Dactinomycin.Approved
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Dactinomycin.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Dactinomycin.Approved, Vet Approved
NaltrexoneThe serum concentration of Dactinomycin can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Dactinomycin can be increased when it is combined with Naringenin.Experimental
NatalizumabThe risk or severity of adverse effects can be increased when Dactinomycin is combined with Natalizumab.Approved, Investigational
NefazodoneThe serum concentration of Dactinomycin can be decreased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Dactinomycin can be decreased when it is combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Dactinomycin can be increased when it is combined with Neostigmine.Approved, Vet Approved
NicardipineThe serum concentration of Dactinomycin can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Dactinomycin can be decreased when it is combined with Nifedipine.Approved
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Dactinomycin.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Dactinomycin.Approved
NisoldipineThe serum concentration of Dactinomycin can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Dactinomycin can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Dactinomycin can be increased when it is combined with Nitrendipine.Approved
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Dactinomycin.Approved
NorethisteroneThe serum concentration of Dactinomycin can be decreased when it is combined with Norethisterone.Approved
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Dactinomycin.Approved, Investigational
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Dactinomycin.Approved
OmeprazoleThe serum concentration of Dactinomycin can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Osimertinib can be increased when it is combined with Dactinomycin.Approved
OuabainOuabain may decrease the cardiotoxic activities of Dactinomycin.Approved
P-NitrophenolThe serum concentration of Dactinomycin can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Dactinomycin.Approved, Vet Approved
Palmitic AcidThe serum concentration of Dactinomycin can be increased when it is combined with Palmitic Acid.Experimental
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Dactinomycin.Approved, Investigational
PantoprazoleThe serum concentration of Dactinomycin can be increased when it is combined with Pantoprazole.Approved
ParoxetineThe serum concentration of Dactinomycin can be increased when it is combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Dactinomycin.Approved
PerindoprilThe serum concentration of Dactinomycin can be increased when it is combined with Perindopril.Approved
PhenobarbitalThe serum concentration of Dactinomycin can be decreased when it is combined with Phenobarbital.Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Dactinomycin.Approved, Vet Approved
Picosulfuric acidThe therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Dactinomycin.Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Dactinomycin.Approved, Investigational
PimozideThe serum concentration of Dactinomycin can be increased when it is combined with Pimozide.Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Dactinomycin.Approved
Platelet Activating FactorThe serum concentration of Dactinomycin can be decreased when it is combined with Platelet Activating Factor.Experimental
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Dactinomycin.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Dactinomycin.Approved
PosaconazoleThe serum concentration of Dactinomycin can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Dactinomycin.Approved
PrazosinThe serum concentration of Dactinomycin can be increased when it is combined with Prazosin.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Dactinomycin.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Dactinomycin.Approved, Vet Approved
ProbenecidThe serum concentration of Dactinomycin can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Dactinomycin can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromethazineThe serum concentration of Dactinomycin can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Dactinomycin can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Propranolol can be increased when it is combined with Dactinomycin.Approved, Investigational
ProtriptylineThe serum concentration of Dactinomycin can be increased when it is combined with Protriptyline.Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Dactinomycin.Approved
QuercetinThe serum concentration of Dactinomycin can be increased when it is combined with Quercetin.Experimental
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Dactinomycin.Approved
QuinacrineThe serum concentration of Dactinomycin can be increased when it is combined with Quinacrine.Approved
QuinidineThe serum concentration of Dactinomycin can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Quinine can be increased when it is combined with Dactinomycin.Approved
Rabies vaccineThe risk or severity of adverse effects can be increased when Dactinomycin is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Dactinomycin.Approved
RanitidineThe serum concentration of Dactinomycin can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Dactinomycin.Approved, Investigational
ReboxetineThe serum concentration of Dactinomycin can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Dactinomycin can be increased when it is combined with Regorafenib.Approved
ReserpineThe serum concentration of Dactinomycin can be decreased when it is combined with Reserpine.Approved
RifampicinThe serum concentration of Dactinomycin can be decreased when it is combined with Rifampicin.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Dactinomycin.Approved, Investigational
RilpivirineThe serum concentration of Dactinomycin can be increased when it is combined with Rilpivirine.Approved
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Dactinomycin.Approved, Investigational
RitonavirThe serum concentration of Dactinomycin can be decreased when it is combined with Ritonavir.Approved, Investigational
RivaroxabanThe serum concentration of Rivaroxaban can be increased when it is combined with Dactinomycin.Approved
RoflumilastRoflumilast may increase the immunosuppressive activities of Dactinomycin.Approved
RolapitantThe serum concentration of Dactinomycin can be increased when it is combined with Rolapitant.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Dactinomycin.Approved, Investigational
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Dactinomycin.Approved, Vet Approved
SaquinavirThe serum concentration of Dactinomycin can be decreased when it is combined with Saquinavir.Approved, Investigational
ScopolamineThe serum concentration of Dactinomycin can be increased when it is combined with Scopolamine.Approved
SelegilineThe serum concentration of Dactinomycin can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Dactinomycin.Approved
SertralineThe serum concentration of Dactinomycin can be increased when it is combined with Sertraline.Approved
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Dactinomycin.Approved
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Dactinomycin.Approved
SimvastatinThe serum concentration of Dactinomycin can be increased when it is combined with Simvastatin.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Dactinomycin.Approved
SirolimusThe serum concentration of Dactinomycin can be decreased when it is combined with Sirolimus.Approved, Investigational
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Dactinomycin.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Dactinomycin.Approved
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Dactinomycin.Approved, Investigational
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Dactinomycin.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Dactinomycin.Experimental
SpironolactoneThe serum concentration of Dactinomycin can be increased when it is combined with Spironolactone.Approved
SRP 299The risk or severity of adverse effects can be increased when Dactinomycin is combined with SRP 299.Investigational
St. John's WortThe serum concentration of Dactinomycin can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Dactinomycin can be increased when it is combined with Staurosporine.Experimental
StreptozocinThe serum concentration of Dactinomycin can be decreased when it is combined with Streptozocin.Approved
SulfinpyrazoneThe serum concentration of Dactinomycin can be increased when it is combined with Sulfinpyrazone.Approved
SumatriptanThe serum concentration of Dactinomycin can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Dactinomycin can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Dactinomycin can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Dactinomycin.Approved, Investigational
TacrolimusThe serum concentration of Dactinomycin can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Dactinomycin can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Dactinomycin.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Dactinomycin.Approved
TelaprevirThe serum concentration of Telaprevir can be increased when it is combined with Dactinomycin.Approved
TelmisartanThe serum concentration of Dactinomycin can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Dactinomycin.Approved
TerazosinThe serum concentration of Dactinomycin can be increased when it is combined with Terazosin.Approved
TerfenadineThe serum concentration of Dactinomycin can be increased when it is combined with Terfenadine.Withdrawn
TeriflunomideThe serum concentration of Dactinomycin can be increased when it is combined with Teriflunomide.Approved
TesmilifeneThe serum concentration of Dactinomycin can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Dactinomycin can be increased when it is combined with Testosterone.Approved, Investigational
TG4010The risk or severity of adverse effects can be increased when Dactinomycin is combined with TG4010.Investigational
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Dactinomycin.Approved
TimololThe serum concentration of Timolol can be increased when it is combined with Dactinomycin.Approved
TofacitinibDactinomycin may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Dactinomycin.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Dactinomycin.Approved, Investigational
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Dactinomycin.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Dactinomycin.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Dactinomycin.Approved
TrazodoneThe serum concentration of Dactinomycin can be decreased when it is combined with Trazodone.Approved, Investigational
TrifluoperazineThe serum concentration of Dactinomycin can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Dactinomycin can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Dactinomycin can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Dactinomycin can be increased when it is combined with Trimipramine.Approved
TroleandomycinThe serum concentration of Dactinomycin can be increased when it is combined with Troleandomycin.Approved
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Dactinomycin.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Dactinomycin.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Dactinomycin.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Dactinomycin.Approved
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Dactinomycin.Approved
VerapamilThe serum concentration of Dactinomycin can be decreased when it is combined with Verapamil.Approved
VinblastineThe serum concentration of Dactinomycin can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Dactinomycin.Approved, Investigational
VincristineThe serum concentration of Dactinomycin can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Dactinomycin can be increased when it is combined with Vinorelbine.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Dactinomycin.Approved
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Dactinomycin.Approved
ZimelidineThe serum concentration of Dactinomycin can be increased when it is combined with Zimelidine.Withdrawn
Food InteractionsNot Available
References
Synthesis Reference

Waksman, S.A. and Woodruff, H.B.; US. Patent 2,378,876; June 19,1945; assigned to
Merck & Co., Inc.

General References
  1. Sobell HM: Actinomycin and DNA transcription. Proc Natl Acad Sci U S A. 1985 Aug;82(16):5328-31. [PubMed:2410919 ]
  2. Turan T, Karacay O, Tulunay G, Boran N, Koc S, Bozok S, Kose MF: Results with EMA/CO (etoposide, methotrexate, actinomycin D, cyclophosphamide, vincristine) chemotherapy in gestational trophoblastic neoplasia. Int J Gynecol Cancer. 2006 May-Jun;16(3):1432-8. [PubMed:16803542 ]
  3. Abd El-Aal HH, Habib EE, Mishrif MM: Wilms' tumor: the experience of the pediatric unit of Kasr El-Aini center of radiation oncology and nuclear medicine (NEMROCK). J Egypt Natl Canc Inst. 2005 Dec;17(4):308-14. [PubMed:17102824 ]
  4. Khatua S, Nair CN, Ghosh K: Immune-mediated thrombocytopenia following dactinomycin therapy in a child with alveolar rhabdomyosarcoma: the unresolved issues. J Pediatr Hematol Oncol. 2004 Nov;26(11):777-9. [PubMed:15543019 ]
External Links
ATC CodesL01DA01
AHFS Codes
  • 10:00.00
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.7619
Blood Brain Barrier-0.9659
Caco-2 permeable-0.6568
P-glycoprotein substrateSubstrate0.8368
P-glycoprotein inhibitor INon-inhibitor0.6482
P-glycoprotein inhibitor IINon-inhibitor0.8638
Renal organic cation transporterNon-inhibitor0.8178
CYP450 2C9 substrateNon-substrate0.8589
CYP450 2D6 substrateNon-substrate0.8535
CYP450 3A4 substrateSubstrate0.759
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.923
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8614
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8681
Ames testNon AMES toxic0.9133
CarcinogenicityNon-carcinogens0.9019
BiodegradationNot ready biodegradable0.983
Rat acute toxicity4.3767 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9208
hERG inhibition (predictor II)Non-inhibitor0.5171
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Lundbeck inc
  • Bedford laboratories div ben venue laboratories inc
Packagers
Dosage forms
FormRouteStrength
Injection, powder, lyophilized, for solutionIntravenous.5 mg/mL
Powder, for solutionIntravenous0.5 mg
Prices
Unit descriptionCostUnit
Cosmegen 0.5 mg vial684.36USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point241.5-243 °CNot Available
water solubilitySoluble at 10 °CNot Available
logP1.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.02 mg/mLALOGPS
logP2.76ALOGPS
logP-0.097ChemAxon
logS-4.8ALOGPS
pKa (Strongest Acidic)10.52ChemAxon
pKa (Strongest Basic)-0.13ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count16ChemAxon
Hydrogen Donor Count5ChemAxon
Polar Surface Area355.54 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity326.17 m3·mol-1ChemAxon
Polarizability129.2 Å3ChemAxon
Number of Rings7ChemAxon
Bioavailability0ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as cyclic depsipeptides. These are natural or synthetic compounds having sequences of amino and hydroxy carboxylic acid residues (usually α-amino and α-hydroxy acids) connected in a ring. The residues are commonly but not necessarily regularly alternating.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentCyclic depsipeptides
Alternative Parents
Substituents
  • Cyclic depsipeptide
  • Phenoxazine
  • Macrolide lactam
  • N-acyl-alpha amino acid or derivatives
  • Macrolactam
  • Alpha-amino acid ester
  • 2-aminobenzamide
  • Aminobenzoic acid or derivatives
  • Benzamide
  • Aminobenzamide
  • Benzoyl
  • Benzenoid
  • Primary aromatic amine
  • Dicarboxylic acid or derivatives
  • Heteroaromatic compound
  • Vinylogous amide
  • Tertiary carboxylic acid amide
  • Pyrrolidine
  • Cyclic ketone
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Lactone
  • Lactam
  • Carboxylic acid ester
  • Carboxamide group
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

1. DNA
Kind
Nucleotide
Organism
Human
Pharmacological action
yes
Actions
adduct
General Function:
Used for biological information storage.
Specific Function:
DNA contains the instructions needed for an organism to develop, survive and reproduce.
Molecular Weight:
2.15 x 1012 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284 ]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423 ]
  3. Yang XL, Wang AH: Structural studies of atom-specific anticancer drugs acting on DNA. Pharmacol Ther. 1999 Sep;83(3):181-215. [PubMed:10576292 ]
  4. Sobell HM: Actinomycin and DNA transcription. Proc Natl Acad Sci U S A. 1985 Aug;82(16):5328-31. [PubMed:2410919 ]
  5. Hudson JS, Brooks SC, Graves DE: Interactions of actinomycin D with human telomeric G-quadruplex DNA. Biochemistry. 2009 Jun 2;48(21):4440-7. doi: 10.1021/bi900203z. [PubMed:19348506 ]
Kind
Protein group
Organism
Homo sapiens
Pharmacological action
unknown
General Function:
Ubiquitin binding
Specific Function:
Control of topological states of DNA by transient breakage and subsequent rejoining of DNA strands. Topoisomerase II makes double-strand breaks. Essential during mitosis and meiosis for proper segregation of daughter chromosomes. May play a role in regulating the period length of ARNTL/BMAL1 transcriptional oscillation (By similarity).
Components:
NameUniProt IDDetails
DNA topoisomerase 2-alphaP11388 Details
DNA topoisomerase 2-betaQ02880 Details
References
  1. Felix CA, Hosler MR, Winick NJ, Masterson M, Wilson AE, Lange BJ: ALL-1 gene rearrangements in DNA topoisomerase II inhibitor-related leukemia in children. Blood. 1995 Jun 1;85(11):3250-6. [PubMed:7756657 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Symporter activity
Specific Function:
Sodium-ion dependent, high affinity carnitine transporter. Involved in the active cellular uptake of carnitine. Transports one sodium ion with one molecule of carnitine. Also transports organic cations such as tetraethylammonium (TEA) without the involvement of sodium. Also relative uptake activity ratio of carnitine to TEA is 11.3.
Gene Name:
SLC22A5
Uniprot ID:
O76082
Molecular Weight:
62751.08 Da
References
  1. Ohashi R, Tamai I, Yabuuchi H, Nezu JI, Oku A, Sai Y, Shimane M, Tsuji A: Na(+)-dependent carnitine transport by organic cation transporter (OCTN2): its pharmacological and toxicological relevance. J Pharmacol Exp Ther. 1999 Nov;291(2):778-84. [PubMed:10525100 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. [PubMed:11602674 ]
  2. Nagy H, Goda K, Fenyvesi F, Bacso Z, Szilasi M, Kappelmayer J, Lustyik G, Cianfriglia M, Szabo G Jr: Distinct groups of multidrug resistance modulating agents are distinguished by competition of P-glycoprotein-specific antibodies. Biochem Biophys Res Commun. 2004 Mar 19;315(4):942-9. [PubMed:14985103 ]
  3. Ambudkar SV, Lelong IH, Zhang J, Cardarelli CO, Gottesman MM, Pastan I: Partial purification and reconstitution of the human multidrug-resistance pump: characterization of the drug-stimulatable ATP hydrolysis. Proc Natl Acad Sci U S A. 1992 Sep 15;89(18):8472-6. [PubMed:1356264 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Transporter activity
Specific Function:
Isoform 1: May participate directly in the active transport of drugs into subcellular organelles or influence drug distribution indirectly. Transports glutathione conjugates as leukotriene-c4 (LTC4) and N-ethylmaleimide S-glutathione (NEM-GS).Isoform 2: Inhibits TNF-alpha-mediated apoptosis through blocking one or more caspases.
Gene Name:
ABCC6
Uniprot ID:
O95255
Molecular Weight:
164904.81 Da
References
  1. Belinsky MG, Chen ZS, Shchaveleva I, Zeng H, Kruh GD: Characterization of the drug resistance and transport properties of multidrug resistance protein 6 (MRP6, ABCC6). Cancer Res. 2002 Nov 1;62(21):6172-7. [PubMed:12414644 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Breuninger LM, Paul S, Gaughan K, Miki T, Chan A, Aaronson SA, Kruh GD: Expression of multidrug resistance-associated protein in NIH/3T3 cells confers multidrug resistance associated with increased drug efflux and altered intracellular drug distribution. Cancer Res. 1995 Nov 15;55(22):5342-7. [PubMed:7585598 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Wang X, Furukawa T, Nitanda T, Okamoto M, Sugimoto Y, Akiyama S, Baba M: Breast cancer resistance protein (BCRP/ABCG2) induces cellular resistance to HIV-1 nucleoside reverse transcriptase inhibitors. Mol Pharmacol. 2003 Jan;63(1):65-72. [PubMed:12488537 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23