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Details

Stereochemistry ABSOLUTE
Molecular Formula C29H32Cl2N2O5S
Molecular Weight 591.546
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of LUSUTROMBOPAG

SMILES

CCCCCCO[C@@H](C)C1=C(OC)C(=CC=C1)C2=CSC(NC(=O)C3=CC(Cl)=C(\C=C(/C)C(O)=O)C(Cl)=C3)=N2

InChI

InChIKey=NOZIJMHMKORZBA-KJCUYJGMSA-N
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

HIDE SMILES / InChI

Molecular Formula C29H32Cl2N2O5S
Molecular Weight 591.546
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry
Defined Stereocenters 1 / 1
E/Z Centers 1
Optical Activity UNSPECIFIED

Description

Lusutrombopag (trade name Mulpleta) is an orally bioavailable, small molecule thrombopoietin (TPO) receptor agonist being developed by Shionogi for chronic liver disease (CLD) patients with thrombocytopenia prior to elective invasive surgery. Lusutrombopag acts selectively on the human TPO receptor and activates signal transduction pathways that promote the proliferation and differentiation of bone marrow cells into megakaryocytes, thereby increasing platelet levels. In September 2015, Lusutrombopag received its first global approval in Japan for the improvement of CLD-associated thrombocytopenia in patients scheduled to undergo elective invasive procedures. Oral Lusutrombopag is rapidly absorbed, with a median time to maximum serum concentration (Tmax) of 3.8–4.0 h in healthy subjects administered single doses of oral Lusutrombopag 1, 2 or 4 mg, and 6 h in CLD patients with thrombocytopenia administered oral Lusutrombopag 3 mg once daily for 7 days. The major metabolic pathway for Lusutrombopag appears to be omega- and beta-oxidation. Lusutrombopag is a substrate of breast cancer resistance protein and P-glycoprotein, according to in vitro data.

Originator

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Mulpleta
PubMed

PubMed

TitleDatePubMed
Lusutrombopag: First Global Approval.
2016 Jan
Population Pharmacokinetic and Pharmacodynamic Modeling of Lusutrombopag, a Newly Developed Oral Thrombopoietin Receptor Agonist, in Healthy Subjects.
2016 Nov
Patents

Patents

Sample Use Guides

In Vivo Use Guide
The recommended dosage of oral lusutrombopag is 3 mg once daily for 7 days. It should be avoided in patients undergoing open-heart surgery, brain surgery with craniotomy organ resection or a laparotomy.
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Mon Oct 21 21:33:17 UTC 2019
Edited
by admin
on Mon Oct 21 21:33:17 UTC 2019
Record UNII
6LL5JFU42F
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
LUSUTROMBOPAG
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
LUSUTROMBOPAG [USAN]
Common Name English
(2E)-3-(2,6-DICHLORO-4-((4-(3-((1S)-1-(HEXYLOXY)ETHYL)-2-METHOXYPHENYL)-1,3-THIAZOL-2-YL)CARBAMOYL)PHENYL)-2-METHYLPROP-2-ENOIC ACID
Systematic Name English
2-PROPENOIC ACID, 3-(2,6-DICHLORO-4-(((4-(3-((1S)-1-(HEXYLOXY)ETHYL)-2-METHOXYPHENYL)-2-THIAZOLYL)AMINO)CARBONYL)PHENYL)-2-METHYL-, (2E)-
Common Name English
LUSUTROMBOPAG [WHO-DD]
Common Name English
LUSUTROMBOPAG [INN]
Common Name English
MULPLETA
Brand Name English
RSC888711
Code English
S-888711
Code English
LUSUTROMBOPAG [JAN]
Common Name English
Classification Tree Code System Code
WHO-ATC B02BX07
Created by admin on Mon Oct 21 21:33:18 UTC 2019 , Edited by admin on Mon Oct 21 21:33:18 UTC 2019
Code System Code Type Description
ChEMBL
CHEMBL2107831
Created by admin on Mon Oct 21 21:33:18 UTC 2019 , Edited by admin on Mon Oct 21 21:33:18 UTC 2019
PRIMARY
JAPANESE REVIEW
MULPLETA
Created by admin on Mon Oct 21 21:33:18 UTC 2019 , Edited by admin on Mon Oct 21 21:33:18 UTC 2019
PRIMARY APPROVED SEPTEMBER 2015
EVMPD
SUB183903
Created by admin on Mon Oct 21 21:33:18 UTC 2019 , Edited by admin on Mon Oct 21 21:33:18 UTC 2019
PRIMARY
PUBCHEM
49843517
Created by admin on Mon Oct 21 21:33:18 UTC 2019 , Edited by admin on Mon Oct 21 21:33:18 UTC 2019
PRIMARY
CAS
1110766-97-6
Created by admin on Mon Oct 21 21:33:18 UTC 2019 , Edited by admin on Mon Oct 21 21:33:18 UTC 2019
PRIMARY
INN
9410
Created by admin on Mon Oct 21 21:33:18 UTC 2019 , Edited by admin on Mon Oct 21 21:33:18 UTC 2019
PRIMARY
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ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC DOSE