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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

Description
Curator's Comment:: description was created based on several sources, including 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

Approved Use

Unknown

Launch Date

1.44227526E12
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
n = 171
Health Status: unhealthy
Condition: thrombocytopeni
Population Size: 171
Sources:
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
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

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
In Vitro Use Guide
Unknown
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