SAMIDORPHAN L-MALATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C21H26N2O4.C4H6O5
Molecular Weight	504.5296
Optical Activity	UNSPECIFIED
Defined Stereocenters	4 / 4
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O[C@@H](CC(O)=O)C(O)=O.NC(=O)C1=CC=C2C[C@H]3N(CC4CC4)CC[C@@]5(CC(=O)CC[C@@]35O)C2=C1O

InChI

InChIKey=RARHXUAUPNYAJF-QSYGGRRVSA-N

InChI=1S/C21H26N2O4.C4H6O5/c22-19(26)15-4-3-13-9-16-21(27)6-5-14(24)10-20(21,17(13)18(15)25)7-8-23(16)11-12-1-2-12;5-2(4(8)9)1-3(6)7/h3-4,12,16,25,27H,1-2,5-11H2,(H2,22,26);2,5H,1H2,(H,6,7)(H,8,9)/t16-,20-,21-;2-/m10/s1

HIDE SMILES / InChI

Description
Sources: https://clinicaltrials.gov/ct2/show/NCT01903837 | https://www.ncbi.nlm.nih.gov/pubmed/30188587 | https://www.ncbi.nlm.nih.gov/pubmed/30859977

Samidorphan was developed as a sublingually bioavailable µ-opioid receptor antagonist. This drug participated in clinical trials for the treatment of Schizophrenia, Alcohol Dependence, and Binge Eating Disorder. The oral dose pharmacokinetics, safety, and tolerability of samidorphan were evaluated in phase II double blind, placebo-controlled, randomized studies in healthy adults. In addition, the combination of samidorphan (SAM) with buprenorphine (BUP) was studied in phase III clinical trial in patients with major depressive disorder (MDM). It was shown that the long-term treatment did not reveal any new safety findings and confirmed that the risk of abuse and dependence with BUP/SAM was low.

Approval Year

PubMed

Title	Date	PubMed
Evaluation of samidorphan, a μ-opioid antagonist, in a drug discrimination assay in rats.	2018 Aug	30188587

Patents

Sample Use Guides

In Vivo Use Guide

Samidorphan (Low Dose). Tablets taken once daily

Route of Administration: Oral

Name

Type

Language

SAMIDORPHAN L-MALATE

Official Name

English

SAMIDORPHAN MALATE

Common Name

English

Samidorphan l-malate [WHO-DD]

Common Name

English

LYBALVI COMPONENT SAMIDORPHAN L-MALATE

Brand Name

English

SAMIDORPHAN L-MALATE [ORANGE BOOK]

Common Name

English

SAMIDORPHAN L-MALATE [USAN]

Common Name

English

MORPHINAN-3-CARBOXAMIDE, 17-(CYCLOPROPYLMETHYL)-4,14-DIHYDROXY-6-OXO-, (2S)-2-HYDROXYBUTANEDIOATE (1:1)

Common Name

English

SAMIDORPHAN L-MALATE COMPONENT OF LYBALVI

Brand Name

English

RDC-0313-02

Code

English

17-(CYCLOPROPYLMETHYL)-4,14-DIHYDROXY-6-OXOMORPHINAN-3-CARBOXAMIDE HYDROGEN (2S)-2-HYDROXYBUTANEDIOATE SALT

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C681