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

Details

Stereochemistry ACHIRAL
Molecular Formula C17H11F6N7O
Molecular Weight 443.306
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of SELINEXOR

SMILES

FC(F)(F)C1=CC(=CC(=C1)C2=NN(C=N2)\C=C/C(=O)NNC3=NC=CN=C3)C(F)(F)F

InChI

InChIKey=DEVSOMFAQLZNKR-RJRFIUFISA-N
InChI=1S/C17H11F6N7O/c18-16(19,20)11-5-10(6-12(7-11)17(21,22)23)15-26-9-30(29-15)4-1-14(31)28-27-13-8-24-2-3-25-13/h1-9H,(H,25,27)(H,28,31)/b4-1-

HIDE SMILES / InChI
Molecular Formula C17H11F6N7O
Molecular Weight 443.306
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 1
Optical Activity NONE

Description

Selinexor (KPT-330) functions by binding with and inhibiting the nuclear export protein XPO1 (also called CRM1), leading to the accumulation of tumor suppressor proteins in the cell nucleus, which subsequently reinitiates and amplifies their tumor suppressor function. This is believed to lead to the selective induction of apoptosis in cancer cells, while largely sparing normal cells. Selinexor has been used in trials studying the treatment of acute myeloid leukaemia; chronic lymphocytic leukaemia, glioma, liposarcoma, among others.

CNS Activity

CNS Penetrant
2523
Curator's Comment: In clinical trials, the dose-limiting side effects of selinexor are central nervous system (CNS)-mediated anorexia with weight loss and malaise, as well as thrombocytopenia.

Originator

Approval Year

2019
339
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8228
Blocker
534
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase III
663
Unknown

Approved Use

Unknown
Primary
Phase III
663
Unknown

Approved Use

Unknown
Primary
Phase I
424
Unknown

Approved Use

Unknown
Primary
Phase III
663
Unknown

Approved Use

Unknown
Primary
Phase II
1144
Unknown

Approved Use

Unknown
Primary
Phase II
1144
Unknown

Approved Use

Unknown
Primary
Phase II
1144
Unknown

Approved Use

Unknown
Primary
Phase II
1144
Unknown

Approved Use

Unknown
Primary
Phase II
1144
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
680 ng/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212306s000lbl.pdf
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELINEXOR plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
5386 ng × h/mL
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212306s000lbl.pdf
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELINEXOR plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
7 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212306s000lbl.pdf
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELINEXOR plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
5%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/212306s000lbl.pdf
80 mg single, oral
dose: 80 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
SELINEXOR plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Other AEs: Thrombocytopenia, Thrombocytopenia...
Other AEs:
Thrombocytopenia (grade 4, 1%)
Thrombocytopenia (grade 3, 23%)
Thrombocytopenia (grade 1-2, 22%)
Hyponatremia (grade 4, 1%)
Hyponatremia (grade 3, 8%)
Hyponatremia (grade 1-2, 3%)
Nausea (grade 3, 12%)
Nausea (grade 1-2, 60%)
Fatigue (grade 3, 14%)
Fatigue (grade 1-2, 52%)
Decreased appetite (grade 3, 5%)
Decreased appetite (grade 1-2, 49%)
Vomiting (grade 3, 7%)
Vomiting (grade 1-2, 49%)
Weight loss (grade 1-2, 55%)
Anemia (grade 3, 11%)
Anemia (grade 1-2, 29%)
Dysgeusia (grade 1-2, 30%)
Blurred vision (grade 3, 1%)
Blurred vision (grade 1-2, 21%)
Diarrhea (grade 3, 1%)
Diarrhea (grade 1-2, 19%)
Constipation (grade 1-2, 8%)
Dizziness (grade 1-2, 14%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
60 mg 2 times / week multiple, oral
Dose: 60 mg, 2 times / week
Route: oral
Route: multiple
Dose: 60 mg, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
unhealthy, 67 years (range: 35–87 years)
n = 127
Health Status: unhealthy
Age Group: 67 years (range: 35–87 years)
Sex: M+F
Population Size: 127
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
Disc. AE: Diarrhea, Pyrexia...
Other AEs: Thrombocytopenia, Neutropenia...
AEs leading to
discontinuation/dose reduction:
Diarrhea (grade 3, 3%)
Pyrexia (grade 3, 4%)
Other AEs:
Thrombocytopenia (grade 4, 15%)
Neutropenia (grade 4, 9%)
Anaemia (grade 4, 1%)
Fatigue (grade 3, 11%)
Hyponatraemia (grade 3, 8%)
Nausea (grade 3, 6%)
Dyspnoea (grade 4, 1%)
Acute respiratory distress syndrome (grade 5, 1 patient)
Cerebrovascular accident (grade 5, 1 patient)
Sepsis (grade 5, 3 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
100 mg 2 times / week multiple, oral
Highest studied dose
Dose: 100 mg, 2 times / week
Route: oral
Route: multiple
Dose: 100 mg, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
unhealthy
n = 92
Health Status: unhealthy
Population Size: 92
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
AEs

AEs

AESignificanceDosePopulation
Dizziness grade 1-2, 14%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Diarrhea grade 1-2, 19%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Blurred vision grade 1-2, 21%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Thrombocytopenia grade 1-2, 22%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Anemia grade 1-2, 29%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Hyponatremia grade 1-2, 3%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Dysgeusia grade 1-2, 30%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Decreased appetite grade 1-2, 49%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Vomiting grade 1-2, 49%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Fatigue grade 1-2, 52%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Weight loss grade 1-2, 55%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Nausea grade 1-2, 60%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Constipation grade 1-2, 8%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Blurred vision grade 3, 1%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Diarrhea grade 3, 1%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Anemia grade 3, 11%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Nausea grade 3, 12%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Fatigue grade 3, 14%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Thrombocytopenia grade 3, 23%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Decreased appetite grade 3, 5%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Vomiting grade 3, 7%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Hyponatremia grade 3, 8%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Hyponatremia grade 4, 1%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Thrombocytopenia grade 4, 1%
50 mg/m2 2 times / week multiple, oral
Dose: 50 mg/m2, 2 times / week
Route: oral
Route: multiple
Dose: 50 mg/m2, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
unhealthy, 63 years (range: 31-80 years)
n = 73
Health Status: unhealthy
Age Group: 63 years (range: 31-80 years)
Sex: M+F
Population Size: 73
Sources:
https://pubmed.ncbi.nlm.nih.gov/31822399
Fatigue grade 3, 11%
60 mg 2 times / week multiple, oral
Dose: 60 mg, 2 times / week
Route: oral
Route: multiple
Dose: 60 mg, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
unhealthy, 67 years (range: 35–87 years)
n = 127
Health Status: unhealthy
Age Group: 67 years (range: 35–87 years)
Sex: M+F
Population Size: 127
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
Diarrhea grade 3, 3%
Disc. AE
60 mg 2 times / week multiple, oral
Dose: 60 mg, 2 times / week
Route: oral
Route: multiple
Dose: 60 mg, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
unhealthy, 67 years (range: 35–87 years)
n = 127
Health Status: unhealthy
Age Group: 67 years (range: 35–87 years)
Sex: M+F
Population Size: 127
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
Pyrexia grade 3, 4%
Disc. AE
60 mg 2 times / week multiple, oral
Dose: 60 mg, 2 times / week
Route: oral
Route: multiple
Dose: 60 mg, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
unhealthy, 67 years (range: 35–87 years)
n = 127
Health Status: unhealthy
Age Group: 67 years (range: 35–87 years)
Sex: M+F
Population Size: 127
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
Nausea grade 3, 6%
60 mg 2 times / week multiple, oral
Dose: 60 mg, 2 times / week
Route: oral
Route: multiple
Dose: 60 mg, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
unhealthy, 67 years (range: 35–87 years)
n = 127
Health Status: unhealthy
Age Group: 67 years (range: 35–87 years)
Sex: M+F
Population Size: 127
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
Hyponatraemia grade 3, 8%
60 mg 2 times / week multiple, oral
Dose: 60 mg, 2 times / week
Route: oral
Route: multiple
Dose: 60 mg, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
unhealthy, 67 years (range: 35–87 years)
n = 127
Health Status: unhealthy
Age Group: 67 years (range: 35–87 years)
Sex: M+F
Population Size: 127
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
Anaemia grade 4, 1%
60 mg 2 times / week multiple, oral
Dose: 60 mg, 2 times / week
Route: oral
Route: multiple
Dose: 60 mg, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
unhealthy, 67 years (range: 35–87 years)
n = 127
Health Status: unhealthy
Age Group: 67 years (range: 35–87 years)
Sex: M+F
Population Size: 127
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
Dyspnoea grade 4, 1%
60 mg 2 times / week multiple, oral
Dose: 60 mg, 2 times / week
Route: oral
Route: multiple
Dose: 60 mg, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
unhealthy, 67 years (range: 35–87 years)
n = 127
Health Status: unhealthy
Age Group: 67 years (range: 35–87 years)
Sex: M+F
Population Size: 127
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
Thrombocytopenia grade 4, 15%
60 mg 2 times / week multiple, oral
Dose: 60 mg, 2 times / week
Route: oral
Route: multiple
Dose: 60 mg, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
unhealthy, 67 years (range: 35–87 years)
n = 127
Health Status: unhealthy
Age Group: 67 years (range: 35–87 years)
Sex: M+F
Population Size: 127
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
Neutropenia grade 4, 9%
60 mg 2 times / week multiple, oral
Dose: 60 mg, 2 times / week
Route: oral
Route: multiple
Dose: 60 mg, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
unhealthy, 67 years (range: 35–87 years)
n = 127
Health Status: unhealthy
Age Group: 67 years (range: 35–87 years)
Sex: M+F
Population Size: 127
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
Acute respiratory distress syndrome grade 5, 1 patient
60 mg 2 times / week multiple, oral
Dose: 60 mg, 2 times / week
Route: oral
Route: multiple
Dose: 60 mg, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
unhealthy, 67 years (range: 35–87 years)
n = 127
Health Status: unhealthy
Age Group: 67 years (range: 35–87 years)
Sex: M+F
Population Size: 127
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
Cerebrovascular accident grade 5, 1 patient
60 mg 2 times / week multiple, oral
Dose: 60 mg, 2 times / week
Route: oral
Route: multiple
Dose: 60 mg, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
unhealthy, 67 years (range: 35–87 years)
n = 127
Health Status: unhealthy
Age Group: 67 years (range: 35–87 years)
Sex: M+F
Population Size: 127
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
Sepsis grade 5, 3 patients
60 mg 2 times / week multiple, oral
Dose: 60 mg, 2 times / week
Route: oral
Route: multiple
Dose: 60 mg, 2 times / week
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
unhealthy, 67 years (range: 35–87 years)
n = 127
Health Status: unhealthy
Age Group: 67 years (range: 35–87 years)
Sex: M+F
Population Size: 127
Sources:
https://pubmed.ncbi.nlm.nih.gov/32589977
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
substrate
1709

inducer
768
inhibitor
1752
inhibitor
1599

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1509

CYP2B6
799

CYP2C8
901

CYP2C19
1463

CYP3A4/5
273

OATP1B3
700
CYP3A
189

P-gp
1527

BCRP
555

OATP1B1
403

OATP1B3
347

OAT1
320

OAT3
333

OCT1
322

OCT2
348

MATE1
132

MATE2
94
CYP1A2
689

CYP2B6
538
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
CYP1A2
1673
 no
CYP1A2
1673
 no
CYP2B6
985
 no
CYP2B6
985
 no
CYP2C19
1537
 no
CYP2C8
955
 no
CYP2C9
1803
 no
CYP3A4
1909
 no
CYP3A4/5
330
 no
OATP1B3
709
 yes [IC50 6.2 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
BCRP
555
 no
MATE1
132
 no
MATE2
94
 no
OAT1
320
 no
OAT3
333
 no
OATP1B1
403
 no
OATP1B3
347
 no
OCT1
322
 no
OCT2
348
 no
P-gp
1527
 no
CYP3A
189
 yes
CYP3A4
1709
 yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1632
Sourcing

Sourcing

Vendor/AggregatorIDURL
AA Blocks
AA001APV
https://www.aablocks.com/goods/Goods/detail?id=AA001APV
AK Scientific, Inc. (AKSCI)
2500AH
http://www.aksci.com/item_detail.php?cat=2500AH
Aaron Chemicals
AR001BHN
http://www.aaronchem.com/1393477-72-9
Achemtek
0102-028691
http://www.achemtek.com/1393477-72-9
Adooq BioScience
A12582
https://www.adooq.com/kpt-330.html
ApexBio Technology
B1464
http://www.apexbt.com/kpt-330.html
AvaChem Scientific
6779
https://www.avachem.com/productSearch.asp?6779
BLD Pharm
BD00799126
http://www.bldpharm.com/products/1621865-82-4.html
BioCrick
BCC4446
http://www.biocrick.com/KPT-330-BCC4446.html
BioSynth
J-690156
https://www.biosynth.com/en/products/all-products/products/J-690177.html
ChemShuttle
141891
http://www.chemshuttle.com/catalogsearch/result/?q=1393477-72-9&cat=
Chemspace
CSSB00025704619
https://chem-space.com/CSSB00025704619
DC Chemicals
DC7067
http://www.dcchemicals.com/product_show-KPT_330_Selinexor_.html
Excenen
EX-A870
http://www.excenen.com/searchresultlist.php?id=1393477-72-9
Lab Network
LN01288396
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01288396
Smolecule
S542946
http://www.smolecule.com/products/s542946
Smolecule
S542947
http://www.smolecule.com/products/s542947
THE BioTek
bt-282530
https://www.thebiotek.com/product/inhibitors/bt-282530
THE BioTek
bt-282531
https://www.thebiotek.com/product/inhibitors/bt-282531
TubePharm
Tube706
http://www.tubepharm.com/product/1393477-72-9-en.html
Yuhao Chemical
YH65264
http://www.chemyuhao.com/1393477-72-9.html
abcr GmbH
AB479559
http://www.abcr.com/shop/en/AB479559
eNovation Chemicals
D571663
https://www.enovationchem.com/ProductDetails.asp?ProductID=D571663
PubMed

PubMed

TitleDatePubMed
Antileukemic activity of nuclear export inhibitors that spare normal hematopoietic cells.
2013 Jan
Selinexor (KPT-330) has antitumor activity against anaplastic thyroid carcinoma in vitro and in vivo and enhances sensitivity to doxorubicin.
2017 Aug 29
Molecular mechanism and therapeutic implications of selinexor (KPT-330) in liposarcoma.
2017 Jan 31
Inhibition of exportin-1 function results in rapid cell cycle-associated DNA damage in cancer cells.
2017 Jun 13
Patents

Patents

20140235653
4
20140364408
4
20150274698
4
8999996
4
9079865
4
9206158
4
WO2013019548A1
4
WO2013019561A1
4
WO2014144772A1
4

Sample Use Guides

In Vivo Use Guide
Ovarian, endometrial, or cervical carcinoma treatment: 50 mg/m2 twice weekly. Breast cancer oral 60 mg twice weekly.
Route of Administration: Oral
In Vitro Use Guide
Growth of 14 T-ALL lines, which harbour different genetic aberrations, was dramatically reduced in response to treatment with KPT-330, with 50% inhibitory concentration (IC50) values of 34–203 nM after 72 h of exposure
Substance Class Chemical
Created
by admin
on Thu Jul 06 16:19:47 UTC 2023
Edited
by admin
on Thu Jul 06 16:19:47 UTC 2023
Record UNII
31TZ62FO8F
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
SELINEXOR
INN   USAN   WHO-DD  
INN   USAN  
Official Name English
SELINEXOR [USAN]
Common Name English
(Z)-3-(3-(3,5-BIS(TRIFLUOROMETHYL)PHENYL)-1H-1,2,4-TRIAZOL-1-YL)-N'-(PYRAZIN-2-YL)ACRYLOHYDRAZIDE
Systematic Name English
selinexor [INN]
Common Name English
KPT-330
Code English
2-PROPENOIC ACID, 3-(3-(3,5-BIS(TRIFLUOROMETHYL)PHENYL)-1H-1,2,4-TRIAZOL-1-YL)-, 2-(2-PYRAZINYL)HYDRAZIDE, (2Z)-
Systematic Name English
SELINEXOR [MI]
Common Name English
Selinexor [WHO-DD]
Common Name English
XPOVIO
Brand Name English
SELINEXOR [ORANGE BOOK]
Common Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 880222
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
FDA ORPHAN DRUG 825721
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
NCI_THESAURUS C274
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
FDA ORPHAN DRUG 459014
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
FDA ORPHAN DRUG 527816
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
FDA ORPHAN DRUG 436414
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
EU-Orphan Drug EU/3/14/1355
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
FDA ORPHAN DRUG 432414
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
Code System Code Type Description
FDA UNII
31TZ62FO8F
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
EVMPD
SUB177942
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
CAS
1393477-72-9
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
SMS_ID
100000163576
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
DRUG BANK
DB11942
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
DAILYMED
31TZ62FO8F
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
PUBCHEM
71481097
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
EPA CompTox
DTXSID801026013
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
NCI_THESAURUS
C102546
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
LACTMED
Selinexor
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
DRUG CENTRAL
5330
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
MERCK INDEX
M12226
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
RXCUI
2178390
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
USAN
CD-85
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
WIKIPEDIA
Selinexor
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
INN
9872
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
ChEMBL
CHEMBL3545185
Created by admin on Thu Jul 06 16:19:48 UTC 2023 , Edited by admin on Thu Jul 06 16:19:48 UTC 2023
PRIMARY
Related Record Type Details
EXPORTIN-1
TARGET -> INHIBITOR
In cell-based assays, selinexor inhibits XPO1-mediated nuclear export with an IC50≈20 nM.
IC50
CYTOCHROME P450 3A4
METABOLIC ENZYME -> SUBSTRATE
MAJOR
OATP-8
TRANSPORTER -> INHIBITOR
In vitro, selinexor inhibits OATP1B3 with an IC50 value of 6.20 μM.
IC50
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
Related Record Type Details
Structure of KPT-330, (E)-
METABOLITE LESS ACTIVE -> PARENT
HAS ABOUT 10% OF ACTIVITY OF Selinexor
MAJOR
PLASMA
Related Record Type Details
Structure of SELINEXOR
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Tmax PHARMACOKINETIC ORAL ADMINISTRATION

Biological Half-life PHARMACOKINETIC
Blood-to-plasma ratio PHARMACOKINETIC
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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