Delving into the Latest Updates on JBPOS-0101 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

mGluRs

Action

antagonists

Mechanism

mGluRs antagonists(Metabotropic glutamate receptor antagonists)

Therapeutic Areas

Nervous System DiseasesEndocrinology and Metabolic DiseaseUrogenital Diseases+ [1]

Active Indication

Alzheimer DiseaseStatus EpilepticusDepression, Postpartum+ [2]

Inactive Indication

Spasms, Infantile

Originator Organization

Bio-Pharm Solutions Co. Ltd.

Active Organization

Bio-Pharm Solutions Co. Ltd.

Zhejiang Jingxin Pharmaceutical Co., Ltd.

Inactive Organization

BioPharm Solutions, Inc.

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC10H12ClNO3

InChIKeyTZOWVYPYWJLZTK-IMTBSYHQSA-N

CAS Registry1353949-71-9

AbstractJBPOS0101 is a new antiepileptic drug and is a substrate of UDP‐glucuronosyltransferases (UGTs) in in vitro test. In vitro experiments showed different results regarding whether JBPOS0101 induces (EC50 136 μM) or inhibits (IC50 95.4–386.5 μM) cytochrome P450 (CYP) 3A4. As co‐medication of JBPOS0101 and carbamazepine (CBZ) is expected in clinical settings, drug–drug interactions (DDIs) between them should be determined. This study aimed to investigate pharmacokinetic (PK) interactions of JBPOS0101 influenced by CYP3A4 and UGTs using midazolam (MDZ) and CBZ. A two‐cohort, open‐label, fixed‐sequence study was conducted in healthy Koreans. In cohort A, subjects received MDZ IV alone, and then JBPOS0101 were co‐administered with MDZ after oral doses of JBPOS0101 for 7 days. In cohort B, multiple doses of JBPOS0101 and CBZ were administered respectively, and subjects received both together for 7 days. Serial blood samples were collected for PK analysis. When MDZ and JBPOS0101 were co‐administered, the systemic exposure of MDZ decreased by 30%. Meanwhile, JBPOS0101 did not significantly changed the PK of CBZ. CBZ decreased the systemic exposure of JBPOS0101 at steady state by 40%, respectively. With IV administration of MDZ, JBPOS0101 acted as a weak inducer of hepatic CYP3A4 and decreased systemic exposure of MDZ. The ability of JBPOS0101 to similarly modulate gut CYP3A4 activity will require further evaluation. Co‐administration of multiple doses of JBPOS0101 and CBZ did not significantly alter CBZ pharmacokinetics, but the clinical impact of decreased systemic exposure of JBPOS0101 by CBZ should be further considered.

03 Jul 2019·NeuroReportQ4 · MEDICINE

JBPOS0101 attenuates amyloid-β accumulation and memory loss in a mouse model of Alzheimer’s disease

Q4 · MEDICINE

Article

Author: Park, Hyung Joon ; Choi, Won-Seok ; Jang, Ju Kyong ; Choi, Yong Moon

Alzheimer's disease (AD) is a major neurodegenerative disorder characterized by the accumulation of amyloid-β (Aβ) in the brain. Defects in Aβ clearance or the interference of Aβ homeostasis could result in Aβ aggregation. JBPOS0101 has been studied for its antiepileptic activity. It showed a neuroprotective effect and prevented memory deficits in lithium-pilocarpine-induced status epilepticus rats. In this study, we tested the effect of JBPOS0101 in an AD model. We showed that JBPOS0101 attenuated the accumulation of Aβ in 5XFAD mouse brains. Moreover, the treatment of JBPOS0101 rescued the deficits in learning and memory in 5XFAD mice. These data suggest that JBPOS0101 could be a potential therapeutic drug candidate for AD.

PLOS ONEQ3 · CROSS-FIELD

JBPOS0101 regulates amyloid beta, tau, and glial cells in an Alzheimer’s disease model

Q3 · CROSS-FIELD

ArticleOA

Author: Choi, Won-Seok ; Jeong, Jihoon ; Mun, Bo-Ram ; Jang, Ju Kyong ; Park, Hyung Joon ; Choi, Yong Moon

Alzheimer's disease (AD) is the most prevalent neurodegenerative disease characterized by cognitive dysfunction and memory loss as the main symptoms. The deposition of amyloid beta (Aβ) and tau hyperphosphorylation are hallmarks of AD and are major therapeutic targets. However, the exact etiology has not yet been fully elucidated; thus, no drug that cures the disease has been approved. JBPOS0101 is a phenyl carbamate compound that has been tested as a drug for epileptic diseases. In our previous study, we showed that JBPOS0101 attenuated the accumulation of Aβ as well as the deficits in learning and memory in the 5xFAD mouse model. Here, we tested the dose effect (70 or 35 mg/kg) of JBPOS0101 on the memory defect and pathological markers and further investigated the underlying mechanisms in 5xFAD mice. In the behavior tests, JBPOS0101 treatment ameliorated deficits in learning and memory. Moreover, JBPOS0101 attenuated Aβ accumulation and tau phosphorylation. The elevated phosphorylation levels of the active GSK3β form (GSK3β-y216) in 5xFAD, which are responsible for tau phosphorylation, decreased in the JBPOS0101-treated groups. Furthermore, the elevation of reactive astrocytes and microglia in 5xFAD mice was attenuated in JBPOS0101-treated groups. These data suggest that JBPOS0101 may be a new drug candidate to lessen amyloid- and tau-related pathology by regulating glial cells.

100 Deals associated with JBPOS-0101

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB16034

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Alzheimer Disease	Phase 2	South Korea	Bio-Pharm Solutions Co. Ltd.	30 Jan 2022
Status Epilepticus	Phase 2	South Korea	Bio-Pharm Solutions Co. Ltd.	30 Jan 2022
Depression, Postpartum	Phase 1	South Korea	Bio-Pharm Solutions Co. Ltd.	30 Jan 2022
Parkinson Disease	Phase 1	South Korea	Bio-Pharm Solutions Co. Ltd.	30 Jan 2022
Epilepsy	IND Approval	China	Zhejiang Jingxin Pharmaceutical Co., Ltd.	08 Sep 2022
Spasms, Infantile	Discovery	United States	BioPharm Solutions, Inc.	15 Apr 2020
Spasms, Infantile	Discovery	South Korea	BioPharm Solutions, Inc.	15 Apr 2020

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03976076 (CTgov)	Phase 2	Spasms, Infantile	16	JBPOS0101	inewhwzmwk(tojhioakfz) = vcmljplelj ampfkyzfmd (kanrwnrdsb, jsgplbjkee - pbarpqyftl) View more	-	16 Feb 2023