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

Details

Stereochemistry ACHIRAL
Molecular Formula C25H22N4O4
Molecular Weight 442.4675
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of ELTROMBOPAG

SMILES

Cc1ccc(cc1C)N2C(=O)/C(=N\Nc3cccc(-c4cccc(c4)C(=O)O)c3O)/C(=N2)C

InChI

InChIKey=XDXWLKQMMKQXPV-QYQHSDTDSA-N
InChI=1S/C25H22N4O4/c1-14-10-11-19(12-15(14)2)29-24(31)22(16(3)28-29)27-26-21-9-5-8-20(23(21)30)17-6-4-7-18(13-17)25(32)33/h4-13,26,30H,1-3H3,(H,32,33)/b27-22-

HIDE SMILES / InChI

Molecular Formula C25H22N4O4
Molecular Weight 442.4675
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Eltrombopag is a thrombopoietin (TPO) nonpeptide mimetic administered orally that activates the TPO receptor by binding to the transmembrane domain and initiates signaling cascades that induce proliferation and differentiation of megakaryocytes from bone marrow progenitor cells. Eltrombopag under brand name promacta is approved for the treatment of the low blood platelet counts in adults with chronic immune (idiopathic) thrombocytopenia (ITP), when certain other medicines, or surgery to remove the spleen, have not worked well enough. ITP is a condition that may cause unusual bruising or bleeding due to an abnormally low number of platelets in the blood. Eltrombopag has also been approved for the treatment of thrombocytopenia (low blood platelet counts) in patients with chronic hepatitis C to allow them to initiate and maintain interferon-based therapy and to treat patients with severe aplastic anemia who have had an insufficient response to immunosuppressive therapy.

CNS Activity

Curator's Comment:: Known to be CNS penetrant in mouse; bovine. Human data not available

Approval Year

Targets

Targets

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
PROMACTA

Approved Use

PROMACTA is indicated for the treatment of thrombocytopenia in adult and pediatric patients 1 year and older with chronic immune (idiopathic) thrombocytopenia (ITP) who have had an insufficient response to corticosteroids, immunoglobulins, or splenectomy. Limitations of Use: PROMACTA should be used only in patients with ITP whose degree of thrombocytopenia and clinical condition increase the risk for bleeding. PROMACTA is indicated for the treatment of thrombocytopenia in patients with chronic hepatitis C to allow the initiation and maintenance of interferon-based therapy. Limitations of Use: PROMACTA should be used only in patients with chronic hepatitis C whose degree of thrombocytopenia prevents the initiation of interferon-based therapy or limits the ability to maintain interferon-based therapy. Safety and efficacy have not been established in combination with direct-acting antiviral agents used without interferon for treatment of chronic hepatitis C infection. Treatment of Severe Aplastic Anemia PROMACTA is indicated for the treatment of patients with severe aplastic anemia who have had an insufficient response to immunosuppressive therapy.

Launch Date

1227139200000
Primary
PROMACTA

Approved Use

PROMACTA is indicated for the treatment of thrombocytopenia in adult and pediatric patients 1 year and older with chronic immune (idiopathic) thrombocytopenia (ITP) who have had an insufficient response to corticosteroids, immunoglobulins, or splenectomy. Limitations of Use: PROMACTA should be used only in patients with ITP whose degree of thrombocytopenia and clinical condition increase the risk for bleeding. PROMACTA is indicated for the treatment of thrombocytopenia in patients with chronic hepatitis C to allow the initiation and maintenance of interferon-based therapy. Limitations of Use: PROMACTA should be used only in patients with chronic hepatitis C whose degree of thrombocytopenia prevents the initiation of interferon-based therapy or limits the ability to maintain interferon-based therapy. Safety and efficacy have not been established in combination with direct-acting antiviral agents used without interferon for treatment of chronic hepatitis C infection. Treatment of Severe Aplastic Anemia PROMACTA is indicated for the treatment of patients with severe aplastic anemia who have had an insufficient response to immunosuppressive therapy.

Launch Date

1227139200000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
7.03 μg/mL
50 mg 1 times / day steady-state, oral
dose: 50 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ELTROMBOPAG plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
101 μg × h/mL
50 mg 1 times / day steady-state, oral
dose: 50 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ELTROMBOPAG plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
21 h
50 mg 1 times / day steady-state, oral
dose: 50 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ELTROMBOPAG plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
1%
50 mg 1 times / day steady-state, oral
dose: 50 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
ELTROMBOPAG plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
300 mg 1 times / day multiple, oral
Highest studied dose
Dose: 300 mg, 1 times / day
Route: oral
Route: multiple
Dose: 300 mg, 1 times / day
Sources:
unhealthy, 52
Health Status: unhealthy
Age Group: 52
Sex: M+F
Sources:
75 mg 1 times / day multiple, oral
Recommended
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
unhealthy
Disc. AE: Hepatic decompensation, Hepatotoxicity...
AEs leading to
discontinuation/dose reduction:
Hepatic decompensation
Hepatotoxicity
Portal vein thrombosis
Sources:
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Other AEs: Hemorrhage, Ataxia...
Other AEs:
Hemorrhage (serious, 3 patients)
Ataxia (serious, 1 patient)
Dyspnea (serious, 3 patients)
Colitis (serious, 1 patient)
Diarrhea (serious, 1 patient)
Graft versus host disease (serious, 1 patient)
Rash (serious, 1 patient)
Seizure (serious, 1 patient)
Cellulitis (serious, 1 patient)
Hypoxia (serious, 1 patient)
Infection (serious, 5 patients)
Nausea (below serious, 12 patients)
Abdominal pain (below serious, 1 patient)
Ascites (below serious, 1 patient)
Headache (below serious, 2 patients)
Bilirubin increased (below serious, 10 patients)
Sources:
AEs

AEs

AESignificanceDosePopulation
Hepatic decompensation Disc. AE
75 mg 1 times / day multiple, oral
Recommended
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
unhealthy
Hepatotoxicity Disc. AE
75 mg 1 times / day multiple, oral
Recommended
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
unhealthy
Portal vein thrombosis Disc. AE
75 mg 1 times / day multiple, oral
Recommended
Dose: 75 mg, 1 times / day
Route: oral
Route: multiple
Dose: 75 mg, 1 times / day
Sources:
unhealthy
Abdominal pain below serious, 1 patient
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Ascites below serious, 1 patient
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Bilirubin increased below serious, 10 patients
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Nausea below serious, 12 patients
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Headache below serious, 2 patients
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Ataxia serious, 1 patient
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Cellulitis serious, 1 patient
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Colitis serious, 1 patient
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Diarrhea serious, 1 patient
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Graft versus host disease serious, 1 patient
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Hypoxia serious, 1 patient
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Rash serious, 1 patient
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Seizure serious, 1 patient
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Dyspnea serious, 3 patients
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Hemorrhage serious, 3 patients
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
Infection serious, 5 patients
50 mg 1 times / day steady, oral
Dose: 50 mg, 1 times / day
Route: oral
Route: steady
Dose: 50 mg, 1 times / day
Sources:
unhealthy
Health Status: unhealthy
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
weak
yes [IC50 2.7 uM]
yes (co-administration study)
Comment: concurrent eltrombopag and rosuvastatin treatment resulted in increased rosuvastatin Cmax by 2.03-fold and AUC by 55%
Page: 30, 76
yes [IC50 24.8 uM]
yes [IC50 3.5 uM]
yes [IC50 9.3 uM]
yes
yes
yes
yes
yes
yes
yes
yes
Drug as victimTox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
UDP-glucuronosyltransferases and clinical drug-drug interactions.
2005 Apr
Eltrombopag: Is this "24 karat gold platelet" treatment for thrombocytopenia in cirrhosis associated with hepatitis C?
2008 Apr
Eltrombopag: an effective remedy for thrombocytopaenia?
2008 Jun
Metabolism and disposition of eltrombopag, an oral, nonpeptide thrombopoietin receptor agonist, in healthy human subjects.
2011 Sep
The biology of thrombopoietin and thrombopoietin receptor agonists.
2013 Jul
Patents

Sample Use Guides

Chronic Immune (Idiopathic) Thrombocytopenia: use the lowest dose of PROMACTA (eltrombopag) to achieve and maintain a platelet count greater than or equal to 50 x 109 /L as necessary to reduce the risk for bleeding. Dose adjustments are based upon the platelet count response. Initial Dose Regimen: Adult and Pediatric Patients 6 Years and Older with ITP: Initiate PROMACTA at a dose of 50 mg once daily, except in patients who are of East Asian ancestry (such as Chinese, Japanese, Taiwanese, or Korean) or who have mild to severe hepatic impairment (Child-Pugh Class A, B, C). For patients of East Asian ancestry with ITP, initiate PROMACTA at a reduced dose of 25 mg once daily. For patients with ITP and mild, moderate, or severe hepatic impairment (Child-Pugh Class A, B, C), initiate PROMACTA at a reduced d ose of 25 mg once daily. For patients of East Asian ancestry with ITP and hepatic impairment (Child-Pugh Class A, B, C), consider initiating PROMACTA at a reduced dose of 12.5 mg once daily. Pediatric Patients with ITP Aged 1 to 5 Years: Initiate PROMACTA at a dose of 25 mg once daily. Monitoring and Dose Adjustment: After initiating PROMACTA, adjust the dose to achieve and maintain a platelet count greater than or equal to 50 x 109 /L as necessary to reduce the risk for bleeding. Do not exceed a dose of 75 mg daily. Monitor clinical hematology and liver tests regularly throughout therapy with PROMACTA and modify the dosage regimen of PROMACTA based on platelet counts as outlined in Table 1. During therapy with PROMACTA, assess CBCs with differentials, including platelet counts, weekly until a stable platelet count has been achieved. Obtain CBCs with differentials, including platelet counts, monthly thereafter. When switching between
Route of Administration: Oral
It was investigated eltrombopag's effects on human UCB hematopoietic stem cell (HSC) and hematopoietic progenitor cell (HPC) expansion, and its effects on hematopoiesis in vivo. Eltrombopag selectively augmented the expansion of human CD45+, CD34+, and CD41+ cells in bone marrow compartment without effects on mouse bone marrow cells in the NOD/SCID mice xenotrans plant model. Eltrombopag increased peripheral human platelets and white blood cells. Both eltrombopag and recombinant human TPO (rhTPO) induced phosphorylation of STAT5 of CD34+ CD41-, CD34- CD41+, and CD34- CD41- cells. For this purpose the cells were treated with 100ng/ml rhTPO or 3μg/ml eltrombopag for 10 to 60 minutes at 37°C. rhTPO preferentially induced pSTAT3, pAKT, and more pSTAT5 in CD34- C41+ cells, while eltrombopag had no effects on pSTAT3. Eltrombopag differed somewhat from rhTPO in the signal transduction pathways by favoring earlier HSC/HPC populations.
Substance Class Chemical
Created
by admin
on Sat Jun 26 00:17:20 UTC 2021
Edited
by admin
on Sat Jun 26 00:17:20 UTC 2021
Record UNII
S56D65XJ9G
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ELTROMBOPAG
DASH   EMA EPAR   INN   MART.   MI   VANDF   WHO-DD  
INN  
Official Name English
SB497115
Code English
ELTROMBOPAG [INN]
Common Name English
ELTROMBOPAG [EMA EPAR]
Common Name English
(1,1'-BIPHENYL)-3-CARBOXYLIC ACID, 3'-((2Z)-(1-(3,4-DIMETHYLPHENYL)-1,5-DIHYDRO-3-METHYL-5-OXO-4H-PYRAZOL-4-YLIDENE)HYDRAZINO)-2'-HYDROXY-
Common Name English
3'-((2Z)-2-(1-(3,4-DIMETHYLPHENYL)-3-METHYL-5-OXO-1,5-DIHYDRO-4H-PYRAZOL-4-YLIDENE)DIAZANYL)-2'-HYDROXYBIPHENYL-3-CARBOXYLIC ACID
Systematic Name English
(1,1'-BIPHENYL)-3-CARBOXYLIC ACID, 3'-(2-(1-(3,4-DIMETHYLPHENYL)-4,5-DIHYDRO-3-METHYL-5-OXO-1H-PYRAZOL-4-YL)DIAZENYL)-2'-HYDROXY-
Systematic Name English
ELTROMBOPAG [MART.]
Common Name English
ELTROMBOPAG [MI]
Common Name English
ELTROMBOPAG [WHO-DD]
Common Name English
ELTROMBOPAG [VANDF]
Common Name English
Classification Tree Code System Code
NDF-RT N0000175969
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
NCI_THESAURUS C78275
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
NDF-RT N0000175968
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
LIVERTOX 344
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
FDA ORPHAN DRUG 251907
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
WHO-VATC QB02BX05
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
FDA ORPHAN DRUG 410213
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
NDF-RT N0000175973
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
NDF-RT N0000175970
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
WHO-ATC B02BX05
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
NDF-RT N0000178368
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
NDF-RT N0000175967
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
Code System Code Type Description
ChEMBL
CHEMBL461101
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY
INN
8655
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY
NCI_THESAURUS
C71634
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY
MESH
C520809
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY
IUPHAR
6961
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY
RXCUI
711942
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY RxNorm
MERCK INDEX
M4879
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY Merck Index
NDF-RT
N0000191277
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY UGT1A6 Inhibitors [MoA]
CAS
496775-61-2
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY
NDF-RT
N0000191274
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY UGT2B15 Inhibitors [MoA]
CAS
376591-99-0
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
NON-SPECIFIC STEREOCHEMISTRY
FDA UNII
S56D65XJ9G
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY
NDF-RT
N0000191272
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY UGT1A1 Inhibitors [MoA]
EPA CompTox
496775-61-2
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY
EVMPD
SUB30140
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY
HSDB
8212
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY
DRUG CENTRAL
4399
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY
DRUG BANK
DB06210
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY
CAS
2097678-09-4
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
ALTERNATIVE
NDF-RT
N0000191278
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY UGT1A9 Inhibitors [MoA]
WIKIPEDIA
ELTROMBOPAG
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY
NDF-RT
N0000191276
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY UGT1A4 Inhibitors [MoA]
NDF-RT
N0000191275
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY UGT1A3 Inhibitors [MoA]
NDF-RT
N0000190113
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY Breast Cancer Resistance Protein Inhibitors [MoA]
NDF-RT
N0000190107
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY Organic Anion Transporting Polypeptide 1B1 Inhibitors [MoA]
NDF-RT
N0000191273
Created by admin on Sat Jun 26 00:17:21 UTC 2021 , Edited by admin on Sat Jun 26 00:17:21 UTC 2021
PRIMARY UGT2B7 Inhibitors [MoA]
Related Record Type Details
METABOLIC ENZYME -> SUBSTRATE
EXCRETED UNCHANGED
AMOUNT EXCRETED
URINE
SALT/SOLVATE -> PARENT
BINDER->LIGAND
BINDING
EXCRETED UNCHANGED
AMOUNT EXCRETED
FECAL
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC in healthy subjects