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

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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23