ELTANEXOR

Details

Stereochemistry	ACHIRAL
Molecular Formula	C17H10F6N6O
Molecular Weight	428.2913
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

NC(=O)C(=C\N1C=NC(=N1)C2=CC(=CC(=C2)C(F)(F)F)C(F)(F)F)\C3=CN=CN=C3

InChI

InChIKey=JFBAVWVBLRIWHM-AWNIVKPZSA-N

InChI=1S/C17H10F6N6O/c18-16(19,20)11-1-9(2-12(3-11)17(21,22)23)15-27-8-29(28-15)6-13(14(24)30)10-4-25-7-26-5-10/h1-8H,(H2,24,30)/b13-6+

HIDE SMILES / InChI

Molecular Formula	C17H10F6N6O
Molecular Weight	428.2913
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	1
Optical Activity	NONE

Description
Sources: https://www.karyopharm.com/pipeline/oral-eltanexor/ | https://adisinsight.springer.com/drugs/800044323

Eltanexor (KPT-8602) is an investigational second-generation Selective Inhibitor of Nuclear Export (SINE) compound that is designed to selectively block the nuclear export protein XPO1. Most of the key tumor suppressor proteins (TSPs), are cargos of XPO1 and inhibition of XPO1 by eltanexor is believed to sequester TSPs in the nucleus where they can carry out their normal functions. Karyopharm Therapeutics is developing eltanexor for the treatment of relapsed/refractory cancers.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Exportin-1 8 Target ID: CHEMBL5661 Sources: https://worldwide.espacenet.com/publicationDetails/biblio?DB=EPODOC&II=0&ND=3&adjacent=true&locale=en_EP&FT=D&date=20141224&CC=WO&NR=2014205389A1&KC=A1	Inhibitor 8297

PubMed

Title	Date	PubMed
KPT-8602, a second-generation inhibitor of XPO1-mediated nuclear export, is well tolerated and highly active against AML blasts and leukemia-initiating cells.	2017 Jan	27211268
Down-regulation of AR splice variants through XPO1 suppression contributes to the inhibition of prostate cancer progression.	2018 Oct 19	30450161
Nuclear-Cytoplasmic Transport Is a Therapeutic Target in Myelofibrosis.	2019 Apr 1	30563936

Sample Use Guides

In Vivo Use Guide

In Phase 1/2 study in patients with refractory multiple myeloma, using a 3+3 dose escalation design, eltanexor is dosed orally (QDx5 or QoDx3 weekly) for a 28-day cycle with a starting dose of 5 mg.

Route of Administration: Oral

Substance Class	Chemical Created by `admin` on `Sat Dec 16 19:28:08 GMT 2023` Edited by `admin` on `Sat Dec 16 19:28:08 GMT 2023`
Record UNII	Q59IQJ9NTK
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ELTANEXOR

Official Name

English

KPT-8602

Code

English

5-PYRIMIDINEACETAMIDE, .ALPHA.-((3-(3,5-BIS(TRIFLUOROMETHYL)PHENYL)-1H-1,2,4-TRIAZOL-1-YL)METHYLENE)-, (.ALPHA.E)-

Systematic Name

English

ELTANEXOR [USAN]

Common Name

English

Eltanexor [WHO-DD]

Common Name

English

(2E)-3-{3-[3,5-Bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl}-2-(pyrimidin-5-yl)prop-2-enamide

Systematic Name

English

(E)-3-(3-(3,5-BIS(TRIFLUOROMETHYL)PHENYL)-1H-1,2,4-TRIAZOL-1-YL)-2-(PYRIMIDIN-5-YL)ACRYLAMIDE

Systematic Name

English

eltanexor [INN]

Common Name

English

Classification Tree Code System Code

FDA ORPHAN DRUG

857421