U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ABSOLUTE
Molecular Formula C29H32Cl2N2O5S
Molecular Weight 591.5478
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of LUSUTROMBOPAG

SMILES

CCCCCCO[C@@]([H])(C)c1cccc(-c2csc(n2)N=C(c3cc(c(/C(/[H])=C(\C)/C(=O)O)c(c3)Cl)Cl)O)c1OC

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 591.5478
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 1
Optical Activity UNSPECIFIED

Description
Curator's Comment:: http://www.pmda.go.jp/PmdaSearch/iyakuDetail/ResultDataSetPDF/340018_3399010F1022_1_02#page=4 | https://www.ncbi.nlm.nih.gov/pubmed/28324272 | https://www.ncbi.nlm.nih.gov/pubmed/27209291

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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Mulpleta

Launch Date

1442275200000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
181 ng/mL
3 mg 1 times / day steady-state, oral
dose: 3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LUSUTROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
170 ng/mL
3 mg 1 times / day steady-state, oral
dose: 3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LUSUTROMBOPAG plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
191 ng/mL
3 mg 1 times / day steady-state, oral
dose: 3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LUSUTROMBOPAG plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
217 ng/mL
3 mg 1 times / day steady-state, oral
dose: 3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LUSUTROMBOPAG plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
3381 ng × h/mL
3 mg 1 times / day steady-state, oral
dose: 3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LUSUTROMBOPAG plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
3678 ng × h/mL
3 mg 1 times / day steady-state, oral
dose: 3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LUSUTROMBOPAG plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
4187 ng × h/mL
3 mg 1 times / day steady-state, oral
dose: 3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LUSUTROMBOPAG plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
4808 ng × h/mL
3 mg 1 times / day steady-state, oral
dose: 3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
LUSUTROMBOPAG plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Other AEs: Headache, Portal vein thrombosis...
Other AEs:
Headache (5%)
Portal vein thrombosis (serious, 5%)
Sources:
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Other AEs: Vomiting, Anemia...
Other AEs:
Vomiting (1.17%)
Anemia (2.34%)
Splenomegaly (1.17%)
Atrial fibrillation (1.17%)
Cardiac arrest (0.58%)
Cardiac ventricular thrombosis (0.58%)
Ascites (5.85%)
Abdominal distension (1.17%)
Constipation (6.43%)
Diarrhea (4.09%)
Hemorrhagic erosive gastritis (0.58%)
Mesenteric vein thrombosis (0.58%)
Nausea (1.75%)
Rectal hemorrhage (0.58%)
Upper gastrointestinal hemorrhage (0.58%)
Acute hepatic failure (0.58%)
Hepatic function abnormal (1.17%)
Portal hypertension (0.58%)
Nasopharyngitis (5.26%)
Bronchitis (0.58%)
Aspartate aminotransferase increased (24%)
Alanine aminotransferase increased (16.4%)
Fibrin D dimer increased (7.01%)
Fibrin degradation products increased (5.85%)
Blood bilirubin increased (7.6%)
Oxygen saturation decreased (10.5%)
Fatigue (3.51%)
Peripheral edema (0.58%)
Pyrexia (4.68%)
Cough (1.17%)
Pruritis (2.92%)
Rash (2.34%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Headache 5%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Portal vein thrombosis serious, 5%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Acute hepatic failure 0.58%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Bronchitis 0.58%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Cardiac arrest 0.58%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Cardiac ventricular thrombosis 0.58%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Hemorrhagic erosive gastritis 0.58%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Mesenteric vein thrombosis 0.58%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Peripheral edema 0.58%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Portal hypertension 0.58%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Rectal hemorrhage 0.58%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Upper gastrointestinal hemorrhage 0.58%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Abdominal distension 1.17%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Atrial fibrillation 1.17%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Cough 1.17%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Hepatic function abnormal 1.17%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Splenomegaly 1.17%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Vomiting 1.17%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Nausea 1.75%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Oxygen saturation decreased 10.5%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Alanine aminotransferase increased 16.4%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Anemia 2.34%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Rash 2.34%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Pruritis 2.92%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Aspartate aminotransferase increased 24%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Fatigue 3.51%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Diarrhea 4.09%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Pyrexia 4.68%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Nasopharyngitis 5.26%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Ascites 5.85%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Fibrin degradation products increased 5.85%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Constipation 6.43%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Fibrin D dimer increased 7.01%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
Blood bilirubin increased 7.6%
3 mg 1 times / day steady, oral
Recommended
Dose: 3 mg, 1 times / day
Route: oral
Route: steady
Dose: 3 mg, 1 times / day
Sources:
unhealthy
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no
Drug as victim
PubMed

PubMed

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

Patents

Sample Use Guides

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 Sat Jun 26 07:13:55 UTC 2021
Edited
by admin
on Sat Jun 26 07:13:55 UTC 2021
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
LUSUTROMBOPAG [ORANGE BOOK]
Common 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
LUSUTROMBOPAG [MI]
Common Name English
Classification Tree Code System Code
WHO-ATC B02BX07
Created by admin on Sat Jun 26 07:13:55 UTC 2021 , Edited by admin on Sat Jun 26 07:13:55 UTC 2021
Code System Code Type Description
DRUG CENTRAL
5059
Created by admin on Sat Jun 26 07:13:55 UTC 2021 , Edited by admin on Sat Jun 26 07:13:55 UTC 2021
PRIMARY
ChEMBL
CHEMBL2107831
Created by admin on Sat Jun 26 07:13:55 UTC 2021 , Edited by admin on Sat Jun 26 07:13:55 UTC 2021
PRIMARY
JAPANESE REVIEW
MULPLETA
Created by admin on Sat Jun 26 07:13:55 UTC 2021 , Edited by admin on Sat Jun 26 07:13:55 UTC 2021
PRIMARY APPROVED SEPTEMBER 2015
EVMPD
SUB183903
Created by admin on Sat Jun 26 07:13:55 UTC 2021 , Edited by admin on Sat Jun 26 07:13:55 UTC 2021
PRIMARY
PUBCHEM
49843517
Created by admin on Sat Jun 26 07:13:55 UTC 2021 , Edited by admin on Sat Jun 26 07:13:55 UTC 2021
PRIMARY
DRUG BANK
DB13125
Created by admin on Sat Jun 26 07:13:55 UTC 2021 , Edited by admin on Sat Jun 26 07:13:55 UTC 2021
PRIMARY
RXCUI
2054984
Created by admin on Sat Jun 26 07:13:55 UTC 2021 , Edited by admin on Sat Jun 26 07:13:55 UTC 2021
PRIMARY
CAS
1110766-97-6
Created by admin on Sat Jun 26 07:13:55 UTC 2021 , Edited by admin on Sat Jun 26 07:13:55 UTC 2021
PRIMARY
NCI_THESAURUS
C166948
Created by admin on Sat Jun 26 07:13:55 UTC 2021 , Edited by admin on Sat Jun 26 07:13:55 UTC 2021
PRIMARY
MERCK INDEX
M12103
Created by admin on Sat Jun 26 07:13:55 UTC 2021 , Edited by admin on Sat Jun 26 07:13:55 UTC 2021
PRIMARY
FDA UNII
6LL5JFU42F
Created by admin on Sat Jun 26 07:13:55 UTC 2021 , Edited by admin on Sat Jun 26 07:13:55 UTC 2021
PRIMARY
INN
9410
Created by admin on Sat Jun 26 07:13:55 UTC 2021 , Edited by admin on Sat Jun 26 07:13:55 UTC 2021
PRIMARY
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Name Property Type Amount Referenced Substance Defining Parameters References
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