Details of the Drug

General Information of Drug (ID: DMH6IKO)

• Drug Name: Lusutrombopag
• Synonyms: LUSUTROMBOPAG; mulpleta; UNII-6LL5JFU42F; 6LL5JFU42F; 2-Propenoic acid, Lusutrombopag [USAN:INN]; SCHEMBL3062

Indication

Disease Entry	ICD 11	Status	REF
Thrombocytopenia	3B64	Approved	[1]
Liver disease	DB90-BD99	Phase 2	[2]

• #Ro5 Violations (Lipinski): 3:
  Molecular Weight (mw); 591.5
  Topological Polar Surface Area (xlogp); 7.7
  Rotatable Bond Count (rotbonds); 13
  Hydrogen Bond Donor Count (hbonddonor); 2
  Hydrogen Bond Acceptor Count (hbondacc); 7
• Chemical Identifiers:
  Formula: C29H32Cl2N2O5S
  IUPAC Name: (E)-3-[2,6-dichloro-4-[[4-[3-[(1S)-1-hexoxyethyl]-2-methoxyphenyl]-1,3-thiazol-2-yl]carbamoyl]phenyl]-2-methylprop-2-enoic acid
  Canonical SMILES: CCCCCCO[C@@H](C)C1=CC=CC(=C1OC)C2=CSC(=N2)NC(=O)C3=CC(=C(C(=C3)Cl)/C=C(\\C)/C(=O)O)Cl
  InChI: InChI=1S/C29H32Cl2N2O5S/c1-5-6-7-8-12-38-18(3)20-10-9-11-21(26(20)37-4)25-16-39-29(32-25)33-27(34)19-14-23(30)22(24(31)15-19)13-17(2)28(35)36/h9-11,13-16,18H,5-8,12H2,1-4H3,(H,35,36)(H,32,33,34)/b17-13+/t18-/m0/s1
  InChIKey: NOZIJMHMKORZBA-KJCUYJGMSA-N
• Cross-matching ID:
  PubChem CID: 49843517
  ChEBI ID: CHEBI:136051
  CAS Number: 1110766-97-6
  DrugBank ID: DB13125
  TTD ID: D0TD1R
  ACDINA ID: D01232

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Thrombopoietin receptor (MPL)	TTIHYA4	TPOR_HUMAN	Agonist	[1]

Molecular Expression Atlas of This Drug

• ICD Disease Classification: 03 Disease of the blood or blood-forming organs
• Disease Class: ICD-11: 3B64 Thrombocytopenia
• The Studied Tissue: Whole blood
• The Studied Disease: Thrombocytopenia [ICD-11:3B64]

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Thrombopoietin receptor (MPL)	DTT	MPL	8.96E-01	0.07	0.28

Drug-Drug Interaction (DDI) Information of This Drug

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

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Troleandomycin	DMUZNIG	Moderate	Decreased clearance of Lusutrombopag due to the transporter inhibition by Troleandomycin.	Bacterial infection [1A00-1C4Z]	[9]
Ag-221	DMS0ZBI	Moderate	Decreased clearance of Lusutrombopag due to the transporter inhibition by Ag-221.	BCR-ABL1-negative chronic myeloid leukaemia [2A41]	[10]
Berotralstat	DMWA2DZ	Moderate	Decreased clearance of Lusutrombopag due to the transporter inhibition by Berotralstat.	Innate/adaptive immunodeficiency [4A00]	[9]
Tedizolid	DMG2SKR	Moderate	Decreased clearance of Lusutrombopag due to the transporter inhibition by Tedizolid.	Skin and skin-structure infection [1F28-1G0Z]	[9]

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
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Carboxymethylcellulose sodium	E00621	Not Available	Adsorbent; Binding agent; Disintegrant; Emulsifying agent; Suspending agent; Viscosity-controlling agent
Hydroxypropyl cellulose	E00632	Not Available	Binding agent; Coating agent; Emulsifying agent; Film/Membrane-forming agent; Modified-release agent; Suspending agent; Viscosity-controlling agent
Hypromellose	E00634	Not Available	Coating agent
Magnesium oxide	E00232	14792	Anticaking agent; Diluent; Emulsifying agent; Glidant; Tonicity agent
Magnesium stearate	E00208	11177	lubricant
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Triethyl citrate	E00128	6506	Plasticizing agent; Solvent
Haematite red	E00236	14833	Colorant
Cellulose microcrystalline	E00698	Not Available	Adsorbent; Suspending agent; Diluent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Lusutrombopag 3 mg tablet	3 mg	Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] 2018 FDA drug approvals.Nat Rev Drug Discov. 2019 Feb;18(2):85-89.
• [2] ClinicalTrials.gov (NCT01054443) A Study to Investigate the Efficacy and Safety of S-888711 Tablets Administered to Adult Subjects With Immune Thrombocytopenia (ITP). U.S. National Institutes of Health.
• [3] 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
• [4] Emerging drugs for idiopathic thrombocytopenic purpura in adults. Expert Opin Emerg Drugs. 2008 Jun;13(2):237-54.
• [5] Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
• [6] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1722).
• [7] A novel nonpeptidyl human c-Mpl activator stimulates human megakaryopoiesis and thrombopoiesis. Blood. 2006 Jun 1;107(11):4300-7.
• [8] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [9] EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".
• [10] Cerner Multum, Inc. "Australian Product Information.".