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Details

Stereochemistry ABSOLUTE
Molecular Formula C9H15N3O5
Molecular Weight 245.2325
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of LX-2931

SMILES

C\C(=N/O)C1=NC=C(N1)[C@@H](O)[C@H](O)[C@H](O)CO

InChI

InChIKey=AMXVYJYMZLDINS-RSWLNLDNSA-N
InChI=1S/C9H15N3O5/c1-4(12-17)9-10-2-5(11-9)7(15)8(16)6(14)3-13/h2,6-8,13-17H,3H2,1H3,(H,10,11)/b12-4+/t6-,7-,8-/m1/s1

HIDE SMILES / InChI

Description

LX 2931 (LX 3305) is an inhibitor of sphingosine 1-phosphate (S1P) lyase. S1P lyase is an enzyme identified as a promising new target on a pathway associated with regulation of the immune system. Lexicon Pharmaceuticals, Inc. was developing LX 2931 for the treatment of rheumatoid arthritis. LX 2931 has disappeared from the pipeline of Lexicon Pharmaceuticals, Inc. In preclinical studies LX 2931 was effective against experimental cerebral malaria, lung inflammation in a F508del CFTR murine cystic fibrosis model and osteoporosis.

Originator

Approval Year

PubMed

Sample Use Guides

In Vivo Use Guide
Phase I clinical trials indicated that LX 2931, the first clinically studied inhibitor of S1PL, produced a dose-dependent and reversible reduction of circulating lymphocytes and was well tolerated at dose levels of up to 180 mg daily. Lexicon Pharmaceuticals, Inc. was planning the Phase 2 clinical trial is designed as a 12-week, randomized, double-blind, placebo-controlled study to evaluate the safety and tolerability of LX2931 and its effects on symptoms associated with rheumatoid arthritis. Three dose levels will be evaluated: a 70 mg dose, a 110 mg dose and a 150 mg dose, each administered once daily.
Route of Administration: Oral