KPT-330, (E)-

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 Search

SMILES

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

InChI

InChIKey=DEVSOMFAQLZNKR-DAFODLJHSA-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
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26956669 | https://www.karyopharm.com/pipeline/oral-selinexor-kpt-330/ | https://www.ncbi.nlm.nih.gov/pubmed/27893412http://karyopharm.com/pipeline/oral-selinexor-kpt-330/

Selinexor (KPT-330) is a first in class XPO1 antagonist being evaluated in multiple later stage clinical trials in patients with relapsed and/or refractory hematological and solid tumor malignancies.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Exportin-1 7 Target ID: CHEMBL5661 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26956669	Inhibitor 8504
Exportin-1 7 Target ID: CHEMBL5661 Sources: http://www.ncbi.nlm.nih.gov/pubmed/22847027	Blocker 555

Conditions

Condition	Modality	Highest Phase	Product
Liposarcoma 4 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27893412	Primary	Phase III 665	Unknown Approved Use Unknown
Multiple myeloma 159 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28604120	Primary	Phase III 665	Unknown Approved Use Unknown
Acute myeloid leukemia 141 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28336527	Primary	Phase I 438	Unknown Approved Use Unknown
Dedifferentiated liposarcoma 2 Sources: https://clinicaltrials.gov/show/NCT02606461	Primary	Phase III 665	Unknown Approved Use Unknown
Acute myeloid leukemia (relapsed/refractory) 2 Sources: https://clinicaltrials.gov/show/NCT02249091	Primary	Phase II 1147	Unknown Approved Use Unknown
Breast cancer 432 Sources: https://clinicaltrials.gov/show/NCT02025985	Primary	Phase II 1147	Unknown Approved Use Unknown
Ovarian cancer 160 Sources: https://clinicaltrials.gov/show/NCT02025985	Primary	Phase II 1147	Unknown Approved Use Unknown
Endometrial cancer 44 Sources: https://clinicaltrials.gov/show/NCT02025985	Primary	Phase II 1147	Unknown Approved Use Unknown
Cervical cancer 40 Sources: https://clinicaltrials.gov/show/NCT02025985	Primary	Phase II 1147	Unknown Approved Use Unknown

C_max

Value	Dose	Co-administered	Analyte	Population
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

Value	Dose	Co-administered	Analyte	Population
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

T_1/2

Value	Dose	Co-administered	Analyte	Population
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

F_unbound

Value	Dose	Co-administered	Analyte	Population
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

Dose	Population	Adverse 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 67 years (range: 35–87 years) Sex: M+F 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 Health Status: unhealthy Sources: https://pubmed.ncbi.nlm.nih.gov/32589977	Sources: https://pubmed.ncbi.nlm.nih.gov/32589977

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inducer 1087	inhibitor 2438		inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2B6 926 CYP2C8 1057 CYP2C19 2057 CYP3A4/5 296 OATP1B3 961	CYP3A 220 P-gp 2052 BCRP 697 OATP1B1 503 OATP1B3 435 OAT1 395 OAT3 391 OCT1 393 OCT2 434 MATE1 182 MATE2 98	CYP1A2 832 CYP2B6 669

Drug as perpetrator

Target	Modality	Activity
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=49 Page: 49.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=49 Page: 49.0	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=49 Page: 49.0	no
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=49 Page: 49.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=49 Page: 49.0	no
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=49 Page: 49.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=49 Page: 49.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=49 Page: 49.0	no
CYP3A4/5 357	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=49 Page: 49.0	no
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=49 Page: 49.0	yes [IC50 6.2 uM]

Drug as victim

Target	Modality	Activity
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=48 Page: 48.0	no
MATE1 182	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=48 Page: 48.0	no
MATE2 98	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=48 Page: 48.0	no
OAT1 395	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=48 Page: 48.0	no
OAT3 391	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=48 Page: 48.0	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=48 Page: 48.0	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=48 Page: 48.0	no
OCT1 393	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=48 Page: 48.0	no
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=48 Page: 48.0	no
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=48 Page: 48.0	no
CYP3A 220	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=55 Page: 55.0	yes
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=49 Page: 49.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/212306Orig1s000MultidisciplineR.pdf#page=33 Page: 33.0

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA001APV	https://www.aablocks.com/goods/Goods/detail?id=AA001APV
Aaron Chemicals	AR001BHN	http://www.aaronchem.com/1393477-72-9
abcr GmbH	AB479559	http://www.abcr.com/shop/en/AB479559
Achemtek	0102-028691	http://www.achemtek.com/1393477-72-9
Adooq BioScience	A12582	https://www.adooq.com/kpt-330.html
AK Scientific, Inc. (AKSCI)	2500AH	http://www.aksci.com/item_detail.php?cat=2500AH
ApexBio Technology	B1464	http://www.apexbt.com/kpt-330.html
AvaChem Scientific	6779	https://www.avachem.com/productSearch.asp?6779
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
BLD Pharm	BD00799126	http://www.bldpharm.com/products/1621865-82-4.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
eNovation Chemicals	D571663	https://www.enovationchem.com/ProductDetails.asp?ProductID=D571663
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

PubMed

Title	Date	PubMed
Selinexor (KPT-330) has antitumor activity against anaplastic thyroid carcinoma in vitro and in vivo and enhances sensitivity to doxorubicin.	2017-08-29	28852098
Selinexor Overcomes Hypoxia-Induced Drug Resistance in Multiple Myeloma.	2017-08	28668761
Inhibition of exportin-1 function results in rapid cell cycle-associated DNA damage in cancer cells.	2017-06-13	28467801
Molecular mechanism and therapeutic implications of selinexor (KPT-330) in liposarcoma.	2017-01-31	27893412
Mitochondrial pyruvate carrier regulates autophagy, inflammation, and neurodegeneration in experimental models of Parkinson's disease.	2016-12-07	27928028
CRM1 Inhibition Promotes Cytotoxicity in Ewing Sarcoma Cells by Repressing EWS-FLI1-Dependent IGF-1 Signaling.	2016-05-01	26956669
CRM1 inhibition induces tumor cell cytotoxicity and impairs osteoclastogenesis in multiple myeloma: molecular mechanisms and therapeutic implications.	2014-01	23588715
KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia.	2013-04	23373539
Antileukemic activity of nuclear export inhibitors that spare normal hematopoietic cells.	2013-01	22847027

Patents

Sample Use Guides

In Vivo Use Guide

60 mg (∼35 mg/m2) given twice weekly in a 4-week cycle based on the totality of safety and efficacy data.

Route of Administration: Oral

In Vitro Use Guide

To determine whether inhibition of cell growth was due to an alteration in the cell cycle, we analyzed cell cycle distribution of Anaplastic thyroid carcinoma (ATC) cells either exposed to various concentrations (0–1000 nM, 48 h) of selinexor or XPO1 was silenced by transfection with XPO1 shRNA. XPO1 inhibition significantly increased G1 phase and decreased the S and G2/M phases in ATC cells. Of note, selinexor treatment resulted in cell cycle arrest in a dose-dependent manner. Further, was observed that selinexor altered the expression of its known cargo proteins (e.g., p53, p27 and p21), as well as indirect targets including cyclin B1, cyclin D1 in the ATC cell lines. Selinexor treatment (1000 nM, 24 h) also increased cleaved PARP, cleaved caspase-9 and cleaved caspase-3 in ATC cells. Cleavage of PARP [poly (ADP-ribose) polymerase is one of the hallmarks of apoptosis and caspase activation. This was associated with a decrease in the protein levels of anti-apoptotic proteins such as MCL1 and C-Myc. Moreover, was evaluated the dose-dependent effect of selinexor on the protein expression of a few important genes in CAL62 cells

Substance Class	Chemical Created by `admin` on `Mon Mar 31 23:00:21 GMT 2025` Edited by `admin` on `Mon Mar 31 23:00:21 GMT 2025`
Record UNII	MVY2AE6R24
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

2-PROPENOIC ACID, 3-(3-(3,5-BIS(TRIFLUOROMETHYL)PHENYL)-1H-1,2,4-TRIAZOL-1-YL)-, 2-(2-PYRAZINYL)HYDRAZIDE, (2E)-

Preferred Name

English

KPT-330, (E)-

Common Name

English

SELINEXOR, TRANS

Common Name

English

TRANS-SELINEXOR

Common Name

English

Code System Code Type Description

PUBCHEM

71493320

Created by admin on Mon Mar 31 23:00:21 GMT 2025 , Edited by admin on Mon Mar 31 23:00:21 GMT 2025

PRIMARY

CAS

1421923-86-5

Created by admin on Mon Mar 31 23:00:21 GMT 2025 , Edited by admin on Mon Mar 31 23:00:21 GMT 2025

PRIMARY

FDA UNII

MVY2AE6R24

Created by admin on Mon Mar 31 23:00:21 GMT 2025 , Edited by admin on Mon Mar 31 23:00:21 GMT 2025

PRIMARY

Related Record Type Details


					31TZ62FO8F

SELINEXOR

PARENT -> METABOLITE LESS ACTIVE

Comments:

HAS ABOUT 10% OF ACTIVITY OF Selinexor

Interaction Type:

MAJOR

Qualification:

PLASMA

AE	Significance	Dose	Population
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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 63 years (range: 31-80 years) Sex: M+F 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) Health Status: unhealthy Age Group: 67 years (range: 35–87 years) Sex: M+F 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) Health Status: unhealthy Age Group: 67 years (range: 35–87 years) Sex: M+F 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) Health Status: unhealthy Age Group: 67 years (range: 35–87 years) Sex: M+F 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) Health Status: unhealthy Age Group: 67 years (range: 35–87 years) Sex: M+F 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) Health Status: unhealthy Age Group: 67 years (range: 35–87 years) Sex: M+F 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) Health Status: unhealthy Age Group: 67 years (range: 35–87 years) Sex: M+F 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) Health Status: unhealthy Age Group: 67 years (range: 35–87 years) Sex: M+F 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) Health Status: unhealthy Age Group: 67 years (range: 35–87 years) Sex: M+F 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) Health Status: unhealthy Age Group: 67 years (range: 35–87 years) Sex: M+F 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) Health Status: unhealthy Age Group: 67 years (range: 35–87 years) Sex: M+F 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) Health Status: unhealthy Age Group: 67 years (range: 35–87 years) Sex: M+F 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) Health Status: unhealthy Age Group: 67 years (range: 35–87 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/32589977

Details

SMILES

InChI

DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/26956669 | https://www.karyopharm.com/pipeline/oral-selinexor-kpt-330/ | https://www.ncbi.nlm.nih.gov/pubmed/27893412http://karyopharm.com/pipeline/oral-selinexor-kpt-330/

CNS Activity

Originator

Approval Year

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Conditions

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Approved Use

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Cmax

AUC

T1/2

Funbound

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

Sourcing

PubMed

Patents

Sample Use Guides

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26956669 | https://www.karyopharm.com/pipeline/oral-selinexor-kpt-330/ | https://www.ncbi.nlm.nih.gov/pubmed/27893412http://karyopharm.com/pipeline/oral-selinexor-kpt-330/

C_max

T_1/2

F_unbound

Drug as perpetrator