Details of the Drug

General Information of Drug (ID: DM2YGNW)

• Drug Name: Dactinomycin
• Synonyms: Cosmegen; Dactinomicina; Dactinomycine; Dactinomycinum; Meractinomycin; ACT D; ACTINOMYCIN D AMP; Actactinomycin A IV; Actinomycin A IV; Actinomycin Aiv; Actinomycin I; Actinomycin IV; Actinomycin cl; Actinomycin x i; Antibiotic from Streptomyces parvullus; Chounghwamycin B; D Actinomycin; Dactinomycin D; Dactinomyein d; Dilactone actin omycindioic D acid; Dilactone actinomycin D acid; Dilactone actinomycindioic D acid; Lyovac cosmegen; Oncostatin K; Actinomycin 11 cosmegen; Actinomycin 7; Actinomycin C1; Actinomycin I1; Actinomycin X 1; Actinomycin X1; HBF 386; HBF 386 meractinomycin; X 97; AD (VAN); Actinomycin C (sub1); Actinomycin C(sub1); Actinomycin D (JP15); Actinomycin D, sodium deoxyribonucleic acid complex; Actinomycin I (sub1); Actinomycin I(sub 1); Actinomycin I(sub1); Actinomycin-IV; Actinomycindioic D acid, dilactone; Acto-D; COSMEGEN (TN); Dactinomicina [INN-Spanish]; Dactinomycin (USP); Dactinomycin [USAN:BAN]; Dactinomycine [INN-French]; Dactinomycinum [INN-Latin]; NP-005932; Actinomycin D deriv. of 3H-phenoxaocardazine; GNF-PF-1977; Actinomycin-[threo-val-pro-sar-meval]; Actinomyein-theo-val-pro-sar-meval; Actinomycin-(threo-val-pro-sar-meval); O)-(1-oxo-1,2-ethanediyl)]bis(N-methyl)L-valine; PXZ-THR-DVA-PRO-SAR-MVA-THR-DVA-PRO-SAR-MVA; DVA-DPR-SAR-MVA-(c1)DTH-PXZ-(c11)DTH-DVA-DPR-SAR-MVA; 1H-Pyrrolo(2,1-1)-(1,4,7,10,13)oxatetraazacyclohexadecine; 4,6-dimethyl-3-oxo-3H-phenoxazine-1,9-dicarboxamide

Indication

Disease Entry	ICD 11	Status	REF
Solid tumour/cancer	2A00-2F9Z	Approved	[1]

• Therapeutic Class: Anticancer Agents
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 2:
  Molecular Weight (mw); 1255.4
  Topological Polar Surface Area (xlogp); 3.8
  Rotatable Bond Count (rotbonds); 8
  Hydrogen Bond Donor Count (hbonddonor); 5
  Hydrogen Bond Acceptor Count (hbondacc); 18
• ADMET Property:
  Absorption: The drug is poorly absorbed from gastrointestinal tract [2]
  BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [3]
  Elimination: 10% of drug is excreted from urine in the unchanged form [3]
  Half-life: The concentration or amount of drug in body reduced by one-half in 36 hours [4]
  Metabolism: The drug is metabolized via the hepatic [2]
  MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 0.01195 micromolar/kg/day [5]
  Water Solubility: The ability of drug to dissolve in water is measured as 0.5 mg/mL [3]
• Chemical Identifiers:
  Formula: C62H86N12O16
  IUPAC Name: 2-amino-4,6-dimethyl-3-oxo-1-N,9-N-bis[(3R,6S,7R,10S,16S)-7,11,14-trimethyl-2,5,9,12,15-pentaoxo-3,10-di(propan-2-yl)-8-oxa-1,4,11,14-tetrazabicyclo[14.3.0]nonadecan-6-yl]phenoxazine-1,9-dicarboxamide
  Canonical SMILES: C[C@@H]1[C@@H](C(=O)N[C@@H](C(=O)N2CCC[C@H]2C(=O)N(CC(=O)N([C@H](C(=O)O1)C(C)C)C)C)C(C)C)NC(=O)C3=C4C(=C(C=C3)C)OC5=C(C(=O)C(=C(C5=N4)C(=O)N[C@H]6[C@H](OC(=O)[C@@H](N(C(=O)CN(C(=O)[C@@H]7CCCN7C(=O)[C@H](NC6=O)C(C)C)C)C)C(C)C)C)N)C
  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
  InChIKey: RJURFGZVJUQBHK-IIXSONLDSA-N
• Cross-matching ID:
  PubChem CID: 457193
  ChEBI ID: CHEBI:27666
  CAS Number: 50-76-0
  DrugBank ID: DB00970
  TTD ID: D0P8IV
  VARIDT ID: DR01203
  ACDINA ID: D00983

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Human Deoxyribonucleic acid (hDNA)	TTUTN1I	NOUNIPROTAC	Breaker	[6]

Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	MOA	REF
Multidrug resistance-associated protein 1 (ABCC1)	DTSYQGK	MRP1_HUMAN	Substrate	[7]
Breast cancer resistance protein (ABCG2)	DTI7UX6	ABCG2_HUMAN	Substrate	[8]
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Substrate	[9]

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Dactinomycin (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Roflumilast	DMPGHY8	Moderate	Additive immunosuppressive effects by the combination of Dactinomycin and Roflumilast.	Asthma [CA23]	[45]
Ofloxacin	DM0VQN3	Minor	Decreased absorption of Dactinomycin due to intestinal mucosa variation caused by Ofloxacin.	Bacterial infection [1A00-1C4Z]	[46]
Sparfloxacin	DMB4HCT	Minor	Decreased absorption of Dactinomycin due to intestinal mucosa variation caused by Sparfloxacin.	Bacterial infection [1A00-1C4Z]	[46]
Gemifloxacin	DMHT34O	Minor	Decreased absorption of Dactinomycin due to intestinal mucosa variation caused by Gemifloxacin.	Bacterial infection [1A00-1C4Z]	[46]
Norfloxacin	DMIZ6W2	Minor	Decreased absorption of Dactinomycin due to intestinal mucosa variation caused by Norfloxacin.	Bacterial infection [1A00-1C4Z]	[46]
ABT-492	DMJFD2I	Minor	Decreased absorption of Dactinomycin due to intestinal mucosa variation caused by ABT-492.	Bacterial infection [1A00-1C4Z]	[46]
Levofloxacin	DMS60RB	Minor	Decreased absorption of Dactinomycin due to intestinal mucosa variation caused by Levofloxacin.	Bacterial infection [1A00-1C4Z]	[46]
Lomefloxacin	DMVRH9C	Minor	Decreased absorption of Dactinomycin due to intestinal mucosa variation caused by Lomefloxacin.	Bacterial infection [1A00-1C4Z]	[46]
Teriflunomide	DMQ2FKJ	Major	Additive immunosuppressive effects by the combination of Dactinomycin and Teriflunomide.	Hyper-lipoproteinaemia [5C80]	[47]
Denosumab	DMNI0KO	Moderate	Additive myelosuppressive effects by the combination of Dactinomycin and Denosumab.	Low bone mass disorder [FB83]	[48]
Thalidomide	DM70BU5	Major	Additive thrombogenic effects by the combination of Dactinomycin and Thalidomide.	Multiple myeloma [2A83]	[49]
Tecfidera	DM2OVDT	Moderate	Additive immunosuppressive effects by the combination of Dactinomycin and Tecfidera.	Multiple sclerosis [8A40]	[50]
Siponimod	DM2R86O	Major	Additive immunosuppressive effects by the combination of Dactinomycin and Siponimod.	Multiple sclerosis [8A40]	[51]
Fingolimod	DM5JVAN	Major	Additive immunosuppressive effects by the combination of Dactinomycin and Fingolimod.	Multiple sclerosis [8A40]	[52]
Ocrelizumab	DMEZ2KH	Moderate	Additive immunosuppressive effects by the combination of Dactinomycin and Ocrelizumab.	Multiple sclerosis [8A40]	[53]
Ozanimod	DMT6AM2	Major	Additive immunosuppressive effects by the combination of Dactinomycin and Ozanimod.	Multiple sclerosis [8A40]	[45]
Omacetaxine mepesuccinate	DMPU2WX	Moderate	Additive immunosuppressive effects by the combination of Dactinomycin and Omacetaxine mepesuccinate.	Myeloproliferative neoplasm [2A20]	[54]
Gatifloxacin	DMSL679	Minor	Decreased absorption of Dactinomycin due to intestinal mucosa variation caused by Gatifloxacin.	Respiratory infection [CA07-CA4Z]	[46]
Canakinumab	DM8HLO5	Moderate	Additive immunosuppressive effects by the combination of Dactinomycin and Canakinumab.	Rheumatoid arthritis [FA20]	[55]
Rilonacept	DMGLUQS	Moderate	Additive immunosuppressive effects by the combination of Dactinomycin and Rilonacept.	Rheumatoid arthritis [FA20]	[55]
Golimumab	DMHZV7X	Major	Additive immunosuppressive effects by the combination of Dactinomycin and Golimumab.	Rheumatoid arthritis [FA20]	[56]
Leflunomide	DMR8ONJ	Major	Additive immunosuppressive effects by the combination of Dactinomycin and Leflunomide.	Rheumatoid arthritis [FA20]	[47]
Anthrax vaccine	DM9GSWY	Moderate	Antagonize the effect of Dactinomycin when combined with Anthrax vaccine.	Sepsis [1G40-1G41]	[57]
Fostamatinib	DM6AUHV	Moderate	Decreased clearance of Dactinomycin due to the transporter inhibition by Fostamatinib.	Thrombocytopenia [3B64]	[58]
Azathioprine	DMMZSXQ	Moderate	Additive myelosuppressive effects by the combination of Dactinomycin and Azathioprine.	Transplant rejection [NE84]	[51]
Ganciclovir	DM1MBYQ	Moderate	Additive myelosuppressive effects by the combination of Dactinomycin and Ganciclovir.	Virus infection [1A24-1D9Z]	[51]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Mannitol	E00103	6251	Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Water	E00035	962	Solvent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Dactinomycin 0.5mg/1ml lyophilized powder	0.5mg/1ml	Lyophilized Powder	Intravenous

Jump to Detail Pharmaceutical Formulation Page of This Drug

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